0% found this document useful (0 votes)
46 views84 pages

Chemistry Proj

This document discusses an acknowledgment for a project. It thanks Mrs. Sanchita Banerjee for providing guidance and support that helped complete the project. It also thanks the teaching staff of the Chemistry Department for their encouragement.
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
0% found this document useful (0 votes)
46 views84 pages

Chemistry Proj

This document discusses an acknowledgment for a project. It thanks Mrs. Sanchita Banerjee for providing guidance and support that helped complete the project. It also thanks the teaching staff of the Chemistry Department for their encouragement.
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
Available Formats
Download as DOCX, PDF, TXT or read online on Scribd
You are on page 1/ 84

1|Page

Acknowledgment

The success and final outcome of this


project required a lot of guidance and
assistance from many people and I am
extremely privileged to have got this all
along the completion of my project. All
that I have done is only due to such
supervision and assistance and I would not
forget to thank them.

I respect and thank Mrs. Sanchita Banerjee,


for providing me an opportunity to do the
project work and giving us all support and
guidance which made me complete the
project duly. I am extremely thankful to her
for providing such a nice support and
1
2|Page

guidance, although he had busy schedule


managing the corporate affairs.

I am thankful to our respected ma’am Mrs


Sanchita Banerjee and fortunate enough to
get constant encouragement, support and
guidance from all Teaching staffs of
Chemistry Department which helped us in
successfully completing our project work.
Also, I would like to extend our sincere
esteems to all staff in laboratory for their
timely support.

2
3|Page

INTRODUCTION

Polymer means large molecules whose


structure is composed of multiple repeating
units, from which originates a
characteristic of high relative molecular
mass and attendant properties. The small
units by which a polymer is made up of is
called monomer. So, a large number of
monomers combine together to form a
polymer. These polymers are formed either
by the process of addition polymerization
or condensation polymerization.

3
4|Page

NEED OF HERBAL
POLYMERS

1. Biodegradable – Naturally occurring


polymers produced by all living
organisms. They show no adverse effects
on the environment or human being.
2. Biocompatible and non-toxic –
Chemically, nearly all of these plant
materials are carbohydrates in nature and
composed of repeating monosaccharide
units. Hence they are non-toxic.
3. Economic – They are cheaper and their
production cost is less than synthetic
material.

4
5|Page

4. Safe and devoid of side effects – They


are from a natural source and hence, safe
and without side effects.
5. Easy availability – In many countries,
they are produced due to their application
in many industries.

DISADVANTAGES OF HERBAL
POLYMERS

1. Microbial contamination – During


production, they are exposed to external
environment and hence, there are
chances of microbial contamination.
2. Batch to batch variation –
Synthetic manufacturing is controlled
procedure with fixed quantities of
ingredients while production of natural
5
6|Page

polymers is dependent on environment


and various physical factors.
3. The uncontrolled rate of hydration

Due to differences in the collection of
natural
materials at different times, as well as
differences in region, species, and
climate conditions the percentage of
chemical constituents present in a given
material may vary.
4. Slow Process – As the production
rate is depends upon the environment
and many other factors, it can’t be
changed. So natural polymers have a
slow rate of production.
5. Heavy metal contamination –
There are chances of Heavy metal

6
7|Page

contamination often associated with


herbal excipients.
Polymers are of two types: naturally
occurring and synthetic or man-made.

NATURAL POLYMER

Natural polymers occur in nature and can


be extracted. They are often water based.
Our body too is made up of many natural
polymers like nucleic acids, proteins, etc.
The Cellulose is another natural polymer
which is a main structural component of
7
8|Page

the plants. Most of the natural polymers are


formed from the condensation polymers
and this formation from the monomers,
water is obtained as a by-product.

Some Natural polymers also include DNA


and RNA, these polymers are very much
important in all the life processes of all the
living organisms. This messenger RNA is
the one that makes possible peptides,
proteins, and enzymes in a living body.
Enzymes inside the living organisms help
the reactions to happen and the peptides
makes up the structural components of
hair, skin, and also the horns of a rhino.
The other natural polymers are
polysaccharides or called as sugar
polymers and polypeptides such as keratin,
8
9|Page

silk, and the hair. Natural rubber is also a


natural polymer which is made of
hydrogen and carbon.

Plant origin – Cellulose, Hemicellulose,


Glucomannan, Agar, Starch, Pectin, Inulin,
Rosin, Guar gum, Locust bean Gum, Gum
Acacia, Karaya gum, Gum Tragacanth,
Aloe Vera gel.
Animal origin – Chitin, Alginates,
Carageenans, Psyllium, Xanthum gum.

Examples of Natural Polymers

9
10 | P a g e

There are about many examples of natural


polymers which occur in nature. A brief
description on some of them are listed
below-

Proteins and Polypeptides


Proteins are the basic type of natural
polymers which constitutes in almost all
the living organisms. Proteins are said to
be most versatile in nature. They can also
be as catalysts. Some proteins are called as
enzymes. These enzymes are responsible
for various chemical reactions occurring in
our body and it happens about a million
times faster even without these enzymes.
One type of protein in our blood called as
haemoglobin carries the oxygen from lungs
to the cells of a human body.
10
11 | P a g e

Collagen
Collagen is one of the natural polymers
and is a protein. It makes up the connective
tissue present in the skin of human beings.
This Collagen-polymer is also a fiber that
creates an elastic layer below the skin and
thus helps in keeping it supple and smooth.

Latex
Latex is known to be a kind of rubber, and
rubber is a natural polymer. This latex
occurs in both the forms either synthetic or
natural. The natural form of latex is mainly
collected from the rubber trees and it is
also found in variety of plants which
includes the milkweed. It can also be
prepared artificially by the process of

11
12 | P a g e

building up long chains of molecules of


styrene.

Cellulose
Cellulose is one of the most abundant
organic compounds found on the Earth and
moreover the purest form of natural
cellulose is the cotton. The paper
manufactured from the woods of trees and
also the supporting materials in leaves and
plants mainly comprise cellulose. Like the
amylose, it is also a polymer which is
made from the monomers of glucose.
Cellulose was discovered in 1838 by the
French chemist Anselme Payen, who
isolated it from plant matter and
determined its chemical formula. Cellulose
is an organic polysaccharide with the
12
13 | P a g e

formula (C6H10O5)n, consisting of a


linear chain of several hundred to over ten
thousand β(1→4) linked D-glucose units.
The polysaccharides of the plant cell wall
consist mainly of cellulose, hemicelluloses
and pectin.11 Cellulose is an essential
structural component of cell walls in higher
plants and is the most abundant organic
polymer on earth. Many parallel cellulose
molecules form crystalline microfibrils that
are mechanically strong and highly
resistant to enzymatic attack. These are
aligned with each other to provide structure
to the cell wall. Cellulose is insoluble in
water and indigestible by the human body.
Microcrystalline cellulose is mainly used
in the pharmaceutical industry as a
diluent/binder in tablets for both the
13
14 | P a g e

granulation and direct compression


processes.
Controlled release applications for
cellulose derivatives include the
formulation of membrane

controlled drug release systems or


monolithic matrix systems. Film coating
techniques for the manufacture of
membrane controlled release systems
include enteric coated dosage forms and
the use of semi- permeable membranes in
osmotic pump delivery systems.

Hydroxypropylmethylcellulose is a partly
O- methylated and O-(2-
hydroxypropylated) cellulose ether

14
15 | P a g e

derivative that has been extensively


investigated as an excipient in controlled
release drug delivery systems due to its gel
forming ability. In a study where two
cellulose ethers;
hydroxypropylmethylcellulose and
carboxymethylcellulose were employed as
polymeric carrier materials in matrix
tablets for controlling the release of a
soluble drug, diltiazem, it was found that
each polymer on its own could sustain drug
release over an extended period of time in
these systems.
More importantly, a mixture of the two
cellulose ethers in the matrix type tablets
enabled zero order drug release kinetics at
both pH 4.5 and 6.8.
Hydroxypropylmethylcellulose
15
16 | P a g e

monolithic matrix systems showed


similar dissolution profiles as a
commercial osmotic pump system for
glipizide, a drug with low solubility. It was
further found that the
hydroxypropylmethylcellulose matrix
systems have a stronger gel
structure than those
made of polyethylene oxide, which may
provide superior in vivo performance in
terms of matrix resistance to the
destructive forces within the
gastrointestinal tract.

Hemicellulose
A hemicellulose is a heteropolymer (matrix
polysaccharides), such as arabinoxylans,
present along with cellulose in almost all

16
17 | P a g e

plant cell walls. While cellulose is


crystalline, strong, and resistant to
hydrolysis, hemicellulose has a random,
amorphous structure with little strength.

Unlike cellulose, hemicellulose (also a


polysaccharide) consists of shorter chains –
500-3,000 sugar units. In addition,
hemicellulose is a branched polymer, while
cellulose is unbranched.
Hemicellulose polysaccharides consist of
xyloglucans, xylans and mannans that can
be extracted from the plant cell wall with a
strong alkali. They have backbones made
up of β-1,4-linked D- glycans. Xyloglucan
has a similar backbone as cellulose, but
contains xylose branches on 3 out of every
4 glucose monomers. The β-1,4-linked D-
17
18 | P a g e

Xylan backbone of arabinoxylan contains


arabinose branches polymer,while
cellulose is unbranched.
Glucomannan
Glucomannan is a hydrocolloidal
polysaccharide of the mannan family
consisting of β-1,4 linked D- mannose and
D-glucose monomers (with acetyl side
branches on some of the backbone units),
but the mannose:glucose ratio may differ
depending on the source. The acetyl groups
contribute to its solubility and swelling
capacity and assist in making it a soluble
natural polysaccharide with the highest
viscosity and water-holding capacity. It is
very abundant in Nature and this
polysaccharide is specifically derived from
softwoods, roots, tubers and plant bulbs.
18
19 | P a g e

The most commonly used type of


Glucomannan is referred to as konjac
Glucomannan, which is extracted from the
tubers of Amorphophallus konjac and is a
very promising polysaccharide for
incorporation into drug delivery systems.
Since konjac Glucomannan by itself forms
very weak gels, it has been investigated as
an effective exponent in controlled release
drug delivery devices in combination with
other polymers or by modifying its
chemical structure.17, 18

It was shown that konjac Glucomannan gel


systems were able to maintain the integrity
and control the
release of theophylline and diltiazem for 8
hours. This was, however, dependent on
19
20 | P a g e

the country of origin (i.e. Japan, Europe or


America) due to differences in the degree
of acetylation of the konjac
Glucomannan.Matrix tablets prepared from
konjac glucomannan alone showed the
ability to sustain the release of cimetidine
in the physiological environments of the
stomach and small intestines but the
presence of β-mannanase (colon)
accelerated the drug release substantially.
Mixtures of konjac Glucomannan and
xanthan gum in matrix type tablets showed
high potential to sustain and control the
release of the drug due to stabilization of
the gel phase of the tablets by a network of
intermolecular hydrogen bonds between
the two polymers to effectively retard drug
diffusion. Konjac Glucomannan was used

20
21 | P a g e

to form hydrophilic cylinders and particles


for controlled release of DNA. Konjac
Glucomannan cross-linked with trisodium
trimetaphosphate formed hydrogel systems
that could sustain hydrocortisone release
dependent on cross- linking density and
enzymatic degradation.

Agar
Agar or agar-agar is the dried gelatinous
substance obtained from Gelidium amansii
(Gelidaceae) and several other species of
red algae like, grailaria (Gracilariaceae)
and Pterocladia (Gelidaceae).

Agar consists of a mixture of agarose and


agaropectin. The predominant component,
21
22 | P a g e

agarose, is a linear polymer, made up of


the repeating monomeric unit of
agarobiose. Agarobiose is a disaccharide
made up of D-galactose and 3,6- anhydro-
L-galactopyranose. Agaropectin is a
heterogeneous mixture of smaller acidic
molecules that gel poorly. Its great gelling
power in an aqueous environment allows it
to form gels which are more resistant
(stronger) than those of any other gel-
forming agent, assuming the use of equal
concentrations. It can be used over a wide
range of pH, from 5 to 8, and in some cases
beyond these limits. It withstands thermal
treatments very well, even above 100°C
which allows good sterilization. A 1.5%
aqueous solution gels between 32°C-43°C
and does not melt below 85°C. This is a

22
23 | P a g e

unique property of agar, compared to other


gelling agents. Agar gives gels without
flavour and does not need the additions of
cations with strong flavours (potassium or
calcium) it can be used without problems
to gel food products with soft flavours. Its
gel has an excellent reversibility allowing
it to be repeatedly gelled and melted
without losing any of the original
properties. Agar is used as Suspending
agent, emulsifying agent, gelling agent in
suppositories, surgical lubricant, tablet
disintegrants, medium for bacterial culture,
laxative.

Starch
Starch is the derivative of condensation
polymerization and consists of glucose

23
24 | P a g e

monomers, which further split into water


molecules when combined chemically.
Starch is also a member of basic food
groups called the carbohydrates and it is
found in the grains, cereal and potatoes.
Starch is a polymer of monosaccharide
glucose. The molecules of starch consist of
2 kinds of glucose polymers namely
amylopectin and amylose which are the
main component of starch in most of the
plants.

Starch or amylum is a carbohydrate


consisting of a large number of glucose
units joined together by glycosidic bonds.
This polysaccharide is produced by all
green plants as an energy store. It is the
24
25 | P a g e

principal form of carbohydrate reserve in


green plants and especially present in seeds
and underground organs. Starch occurs in
the form of granules (starch grains). A
number of starches are recognized for

pharmaceutical use. These include maize


(Zea mays), rice (Oryza sativa), wheat
(Triticum aestivum), and potato (Solanum
tuberosum).

It is comprised of two polymers, namely


amylose (a non-branching helical polymer
consisting of α-1, 4 linked D-glucose
monomers) and amylopectin (a highly

25
26 | P a g e

branched polymer consisting of both α-1,4


and α-1,6 linked D-glucose monomers).

Modified Starch
It was tested for general applicability of a
new pregelatinized starch product in
directly compressible controlled-release
matrix systems.

It was prepared by enzymatic degradation


of potato starch followed by precipitation
(retrogradation), filtration and washing
with ethanol. The advantages of the
material include ease of tablet preparation,
the potential of a constant release rate
(zero-order) for an extended period of time
and its ability to incorporate high
26
27 | P a g e

percentages of drugs with different


physicochemical properties. Release rates
from retrograded pregelatinized starch
tablets can be enhanced or decreased to the
desired profile by different parameters like
geometries of the tablet, compaction force
and the incorporation of additional
excipients.

Native Starch
It may not be suitable in controlled release
drug delivery systems due to substantial
swelling and rapid enzymatic degradation
resulting in too fast release of many drugs.
This has led to the use of derivatives of
starch that are more resistant to enzymatic
degradation as well as crosslinking and
formation of co-polymers. Starch acetate

27
28 | P a g e

prepared by acetyl esterification has shown


retarded enzymatic degradation with the
potential to be used as a colon- targeted
drug delivery carrier. High amylase
carboxymethyl starch produced by spray
drying showed a high loading capacity for
the soluble drug, acetaminophen, in
controlled release direct compressible
matrix systems.

To deliver proteins or peptide drugs orally,


microcapsules containing a protein and a
proteinase inhibitor were prepared.
Starch/bovine serum albumin mixed-
walled microcapsules were prepared using
interfacial cross-linking with terephthaloyl
chloride. The microcapsules were loaded
28
29 | P a g e

with native or amino-protected aprotinin


by incorporating protease inhibitors in the
aqueous phase during the cross-linking
process. The protective effect of
microcapsules with aprotinin for bovine
serum albumin was revealed in vitro.

Pectin
Pectin is the purified carbohydrate product
obtained by acid hydrolysis from the inner
portion of the rind of citrus peels i.e. Citrus
Simon or Citrus Aurantium, (Rutaceae).
The main component of pectin is a linear
polysaccharide composed of α-1,4-linked
D- galacturonic acid residues interrupted
by 1,2- linked L-rhamnose residues with a
few hundred to about one thousand
building blocks per molecule,

29
30 | P a g e

corresponding to an average molecular


weight of about 50,000 to about 1,80,000.
The galacturonic acid polysaccharides are
rich in neutral sugars such as rhamnose,
arabinose, galactose, xylose and glucose.
The composition of pectin can vary based
on the botanical source, for example pectin
from citrus contains less neutral sugars and
has a smaller molecular size as compared
to pectin obtained from apples.

Pectin has been investigated as an


excipient in many different types of dosage
forms such as film coating of colon-
specific drug delivery systems when mixed
with ethyl cellulose, microparticulate
delivery systems for ophthalmic
30
31 | P a g e

preparations and matrix type transdermal


patches. It has high potential as a
hydrophilic polymeric material for
controlled release matrix drug delivery
systems, but its aqueous solubility
contributes to the premature and fast
release of the drug from these matrices.

It was investigated that the suitability of


amidated pectin as a matrix patch for
transdermal chloroquine delivery in an
effort to mask the bitter taste when orally
administered. The results suggest that the
pectin-chloroquine patch matrix
preparation has potential applications for
the transdermal delivery of chloroquine
and perhaps in the management of malaria.
31
32 | P a g e

Calcium pectinate nanoparticles to deliver


insulin were prepared as a potential colonic
delivery system by ionotropic gelation.

Micro particulate polymeric delivery


systems have been suggested as a possible
approach to improve the low
bioavailability characteristics shown by
standard ophthalmic vehicles (collyria). In
this context pectin microspheres of
piroxicam were prepared by the spray
drying technique. In vivo tests in rabbits
with dispersions of piroxicam-loaded
microspheres also indicated a significant
improvement of piroxicam bioavailability
in the aqueous humour (2.5-fold) when
compared with commercial piroxicam eye
drops.
32
33 | P a g e

Depending on the type and structure of the


pectin molecule, pectins can gel in various
ways. Gelling can be induced by acid or
cross-linking with calcium ion or by
reaction with alginate. When a pectin
solution is titrated with acid, the ionization
of carboxylate groups on pectins is
repressed causing pectin molecules to no
longer repel each other over their entire
chains. The pectins can thus associate over
a portion of their chains to form acid-
pectin gels. Gel forming systems have been
investigated widely for sustained drug
delivery. A mixture of xyloglucan with
pectin resulted in an in situ gel forming
system with sustained paracetamol drug
delivery in rats.
33
34 | P a g e

In relation to cosmetics, using citronella as


a model compound, pectin gel formulations
were evaluated for controlled fragrance
release by kinetic and static methods.
These formulations showed a prolonged
duration of fragrance release and limitation
of fragrance adsorption to the receptor skin
layers. The increase in pectin
concentrations suppressed the fragrance
release by a diffusion mechanism, thereby
proving that pectin/calcium microparticles
are promising materials for controlled
fragrance release.

In relation to the food industry, folic acid


incorporated microcapsules were prepared
using alginate and combinations of alginate
34
35 | P a g e

and pectin polymers so as to improve


stability of folic acid. Folic acid stability
was evaluated with reference to
encapsulation efficiency, gelling and
hardening of capsules, capsular retention
during drying and storage. The blended
alginate and pectin polymer matrix
increased the folic acid encapsulation
efficiency and reduced leakage from the
capsules as compared to those made with
alginate alone, they showed higher folic
acid retention after freeze drying and
storage.

Inulin
It is a polysaccharide from the bulbs of
Dehlia, Inula Helenium (Compositae),
roots of Dendelion, Taraxacum officinale

35
36 | P a g e

(Compositae). Burdock root, Saussurea


lappa (Compositae) or chicory roots,
Cichonium intybus (Compositae).

Inulin consists of a mixture of oligomers


and polymers that belong to the group of
gluco-fructans and occur in plants such as
garlic, onion, artichoke and chicory. The
inulin molecules contain from two to more
than 60 fructose molecules linked by β-
2,1- bonds. Inulin is resistant to digestion
in the upper gastrointestinal tract, but is
degraded by colonic microflora.

Inulin with a high degree of polymerization


was used to prepare biodegradable colon-
specific films in combination with

36
37 | P a g e

Eudragit® RS that could withstand break


down by the gastric and intestinal fluids. It
was shown in another study where
different Eudragits® were formulated into
films with inulin that when a combination
of Eudragit® RS and Eudragit® RL was
mixed with inulin it exhibited better
swelling and permeation properties in
colonic medium rather than other
gastrointestinal media. Methylated inulin
hydrogels were developed as colon-
specific drug delivery systems and
investigated for water uptake and swelling.
The hydrogels exhibited a relatively high
rate of water uptake and anomalous
dynamic swelling behaviour.

37
38 | P a g e

Inulin derivatised with methacrylic


anhydride and succinic anhydride produced
a pH sensitive hydrogel by UV irradiation
that exhibited a reduced swelling and low
chemical degradation in acidic medium,
but it had a good swelling and degradation
in simulated intestinal fluid in the presence
of its specific enzyme, inulinase.

Rosin
Rosin, also called colophony or Greek
pitch (Pix græca), is a solid form of resin
obtained from pines and some other plants,
mostly conifers, produced by heating fresh
liquid resin to vaporize the volatile liquid
terpene components. Rosin is a natural
polymer with a low molecular weight of
38
39 | P a g e

400 Da obtained from the oleoresin of pine


trees, with the principle sources being
Pinus soxburghui, Pinus longifolium and
Pinus toed a. Rosin is primarily composed
of abietic and pimaric acids and has
excellent film-forming properties. Rosin
and its derivatives are biopolymers that are
increasingly used for their pharmaceutical
applications. In the pharmaceutical context
it has been investigated for
Microencapsulation, film-forming and
coating properties, matrix materials in the
tablets for sustained and controlled release.

Derivatives of rosin synthesized by a


reaction with polyethylene glycol 200 and
maleic anhydride proofed suitable for
39
40 | P a g e

sustaining the drug release from matrix


tablets and pellets. Polymerized rosin films
containing hydrophobic plasticizers
showed excellent potential as coating
materials for the preparation of sustained
release dosage forms. Different studies on
the film forming and coating properties of
rosin and the glycerol ester of maleic rosin
demonstrated their potential to be used as
coating materials for pharmaceutical
products as well as in sustained- release
drug delivery systems. It was shown that
hydrocortisone loaded nanoparticles
prepared from rosin could slowly release
this model drug, which was dependent on
the rosin content. This in vitro study
demonstrated the potential of rosin for the

40
41 | P a g e

production of effective nanoparticulate


drug delivery system.

Guar Gum
Guar gum is the powder of the endosperm
of the seeds of Cyamopsis
tetragonolobus Linn.
(Leguminosae). Guar gum is also called
guaran, clusterbean, Calcutta lucern,
Gum cyamposis, Cyamopsis gum,
Guarina, Glucotard and Guyarem. It is a
galactomannans which is a linear
polysaccharide consisting of (1→4)-
diequatorially linked β-D- mannose
monomers, some of which are linked to
single sugar side-chains of α-D-galactose
attached. Guar gum has a backbone
composed of β-1,4 linked- D-
41
42 | P a g e

mannopyranoses to which, on average,


every alternate mannose an α-D-galactose
is linked 1→6. The FDA has affirmed guar
gum as generally safe. Guar gum has
recently been highlighted as an
inexpensive and flexible carrier for oral
extended release drug delivery. Guar gum
is particularly useful for colon delivery
because it can be degraded by specific
enzymes in this region of the
gastrointestinal tract. The gum protects the
drug while in the stomach and small
intestine environment and delivers the drug
to the colon where it undergoes
assimilation by specific microorganisms or
degraded by the enzymes excreted by these
microorganisms. Guar gum on its own
showed high potential to serve as a carrier

42
43 | P a g e

for oral controlled release matrix systems.


In addition, it was found that inclusion of
excipients can be used as a tool to
modulate drug release from these matrix
systems.

Guar gum, in the form of three-layer


matrix tablets, is a potential carrier in the
design of oral controlled drug delivery
systems for highly water-soluble drugs
such as trimetazidine dihydrochloride. The
same study was carried out by using
metoprolol tartrate a model drug with high
solubility. The results indicated that guar
gum, in the form of three-layer matrix
tablets, is a potential carrier in the design
of oral controlled drug delivery systems for
43
44 | P a g e

highly water- soluble drugs such as


metoprolol tartrate.

Another water soluble drug, diltiazem HCl


has given controlled release comparable
with marketed sustained release diltiazem
HCl tablets (D-SR tablets), which are
prepared in the form of matrix tablets with
guar gum using the wet granulation
technique.

Locust Bean Gum


Locust bean gum also known as Carob
bean gum is derived from the seeds of the
leguminous plant Ceratonia siliqua Linn
(Leguminosae). The brown pods or beans
of the locust bean tree are processed by
44
45 | P a g e

milling the endosperms to form locust bean


gum and it is therefore not an extract of the
native plant but flour. Locust bean gum
consists mainly of a neutral galactomannan
polymer made up of 1,4-linked D-
mannopyranosyl units and every fourth or
fifth chain unit is substituted on C6 with a
D-galactopyranosyl unit. Locust bean gum
is a neutral polymer and its viscosity and
solubility are therefore little affected by pH
changes within the range of 3-11.
Locust bean gum was used to produce
matrix tablets with and without the cross-
linker, glutaraldehyde that showed similar
drug release profiles for different model
drugs as guar gum and scleroglucan. In
another study, sustained release of
diclofenac sodium could be obtained for
45
46 | P a g e

minimatrix systems made from locust bean


gum. A commercially available tablet
system (TIMERx®) developed by the
Penwest Pharmaceuticals Company
consisting of locust bean gum and xanthan
gum showed both in vitro and in vivo
controlled release potential.

Gum Arabic
Gum acacia or Gum Arabic is the dried
gummy exudation obtained from the stem
and branches of Acacia Arabica wild,
belonging to (Leguminosae). The gum has
been recognized as an acidic
polysaccharide containing D-galactose, L-
arabinose, L-rhamnose, and D-glucuronic
acid.

46
47 | P a g e

Acacia is mainly used in oral and topical


pharmaceutical formulations as a
suspending and emulsifying agent, often in
combination with tragacanth. It is also used
in the preparation of pastilles and lozenges
and as a tablet binder.

Gum Arabic was successfully used as a


matrix microencapsulating agent for the
enzyme, endoglucanase, which proofed to
give a slow release of the encapsulated
enzyme and in addition increased its
stability.

Gum Arabic was used as an osmotic


suspending and expanding agent to prepare

47
48 | P a g e

a monolithic osmotic tablet system. The


optimum system delivered the water-
insoluble drug, naproxen, at a rate of
approximately zero order for up to 12
hours at a pH of 6.8. Sustained release of
ferrous sulphate was achieved for 7 h by
preparing gum Arabic pellets. The release
was further sustained for more than 12 h by
coating the pellets with polyvinyl acetate
and ethylene vinyl acetate, respectively. An
increase in the amount of gum Arabic in
the pellets decreased the rate of release
due to the gelling property of gum Arabic.
The gel layer acts as a barrier and retards
the rate of diffusion of FeSO4 through the
pellet.

Karaya Gum
48
49 | P a g e

Karaya gum is obtained from Sterculia


urens (Sterculiaceae) is a partially
acetylated polymer of galactose, rhamnose,
and glucuronic acid. Swellable hydrophilic
natural gums like xanthan gum and karaya
gum were used as release-controlling
agents in producing directly compressed
matrices. Caffeine and diclofenac sodium,
which are having different solubilities in
aqueous medium were selected for gum
erosion, hydration and drug release studies
using a dissolution apparatus (basket
method) at two agitation speeds. It was
concluded that drug release from xanthan
and karaya gum matrices depended on
agitation speed, solubility and proportion
of the drug.

49
50 | P a g e

Both xanthan and karaya gums produced


near the zero order drug release with the
erosion mechanism playing a dominant
role, especially in karaya gum matrices. 60
It was shown that mucoadhesive tablets
prepared by karaya gum for buccal
delivery, had superior adhesive properties
as compared to guar gum and was able to
provide zero-order drug release, but
concentrations greater than 50% w/w may
be required to provide suitable sustained
release.

Tragacanth
This gum is obtained from the branches of
Astragalus gummifer (Leguminosae).
Tragacanth contains from 20% to 30% of a
50
51 | P a g e

water-soluble fraction called tragacanthin


(composed of tragacanthic acid and
arabinogalactan). It also contains from
60% to 70% of a water-insoluble fraction
called bassorin. Tragacanthic acid is
composed of D-galacturonic acid, D-
xylose, L-fructose, D-galactose, and other
sugars. Tragacanthin is composed of uronic
acid and arabinose and dissolves in water
to form a viscous colloidal solution (sol),
while bassorin swells to form a thick gel.

Tragacanth when used as the carrier in the


formulation of 1- and 3-layer matrices
produced satisfactory release prolongation
either alone or in combination with other
polymers.
51
52 | P a g e

As with other water-soluble gums, there is


some preliminary evidence that
concomitant ingestion of tragacanth with a
high sugar load can moderate the blood
sugar levels in patients with diabetes,64
although this effect has not been
demonstrated consistently and requires
much more detailed investigation.
Although gum tragacanth swells to
increase stool weight and decrease the GI
transit time, it appears to have no effect on
serum cholesterol, triglyceride or
phospholipid levels after a 21-day
supplementation period as do other soluble
fibers.Tragacanth has been used since

52
53 | P a g e

ancient times as an emulsifier, thickening


agent, and suspending agent.

Aloe Gel
The inner part of the leaves of Aloe Vera
(L.) Baum. f. (Aloe barbadensis Miller)
consists of the parenchyma tissue that
contains the mucilaginous gel.

After extraction of the A. Vera gel from the


leaves and a filtration step, the acetone
precipitate was directly compressed in
matrix systems with diclofenac sodium as a
model drug. The mucilage produced direct
compressible matrix tablets that showed
good swelling and sustained release of the
model drug.

53
54 | P a g e

Many of the health benefits associated with


Aloe Vera have been attributed to the
polysaccharides contained in the gel of the
leaves. These biological activities include
promotion of wound healing, antifungal
activity, hypoglycemic or antidiabetic
effects antiinflammatory, anticancer,
immunomodulatory and gastroprotective
properties. These effects include the
potential of whole leaf or inner fillet gel
liquid preparations of A. Vera to enhance
the intestinal absorption and bioavailability
of co-administered compounds as well as
enhancement of skin permeation. In
addition, important pharmaceutical
applications such as the use of the dried A.
Vera gel powder as an excipient in
54
55 | P a g e

sustained release pharmaceutical dosage


forms.

Chitin
Chitin is the polysaccharide derivative
containing amino and acetyl groups and are
the most abundant organic constituent in
the skeletal material of the invertebrates. It
is found in mollusks, annelids, arthropods
and also as a constituent of the mycelia and
spores of many fungi. It may be regarded
as a derivative of cellulose, in which the
hydroxyl groups of the second carbon of
each glucose unit have been replaced with
acetamido (-NH(C=O)CH3) group.

55
56 | P a g e

The new polyelectrolyte complex gel beads


based on Phosphorylated Chitosan (PCS)
were developed for controlled release of
ibuprofen in oral administration. The PCS
gel beads were readily prepared from
soluble phosphorylated chitosan by using
an ionotropic gelation with counter
polyanion, tripolyphosphate (TPP), at pH
4.0. Ibuprofen was highly loaded, around
90%, in the PCS gel beads. The release
percents of ibuprofen from PCS gel beads
were found to be increased as the pH of
dissolution medium increased. Chitosan
and their derivatives (N-trimethyl chitosan,
mono-N-carboxymethyl chitosan) are
effective and safe absorption enhancers to
improve mucosal (nasal, peroral) delivery
56
57 | P a g e

of hydrophylic macromolecules such as


peptide and protein drugs and heparins.
This absorption enhancing effect of
chitosan is caused by the opening of the
intercellular tight junctions, thereby
favouring the paracellular transport of
macromolecular drugs. Chitosan nano- and
microparticles are also suitable for
controlled drug release. Association of
vaccines to some of these particulate
systems has shown to enhance the antigen
uptake by mucosal lymphoid tissues,
thereby inducing strong systematic and
mucosal immune responses against the
antigens. The aspecific adjuvant activity of
chitosans seems to be dependent on the
degree of deacetylation and the type of
formulation. From the studies reviewed it

57
58 | P a g e

is concluded that chitosan and chitosan


derivatives are promising polymeric
excipients for mucosal drug and vaccine
delivery.

Alginates
Alginates or alginic acids is an anionic
polysaccharide are linear, unbranched
polysaccharides found in brown seaweed
and marine algae such as Laminaria
hyperborea, Ascophyllum nodosum and
Macrocystis pyrifera.

Alginic acid can be converted into its salts,


of which sodium alginate is the major form
currently used. These polymers consist of
two different monomers in varying
58
59 | P a g e

proportions, namely β-D-mannuronic acid


and α-L-guluronic acid linked in α- or β-
1,4 glycosidic bonds as blocks of only β-
D-mannuronic acid or α-L-guluronic acid
in homopolymers or alternating the two in
heteropolymeric blocks. Alginates have
high molecular weights of 20 to 600 kDa.

Alginates have been used and investigated


as stabilizers in emulsions, suspending
agents, tablet binders and tablet
disintegrants.

The in vivo delivery of anti-tuberculosis


drugs were investigated in mice for
alginate nanoparticles prepared by cation
induced gelation. A single oral dose

59
60 | P a g e

achieved therapeutic drug concentrations in


the blood plasma for 7-11 days and in
organs such as the lungs, liver and spleen
for a total of 15 days. The drugs
encapsulated in these nanoparticles
resulted in significantly higher
bioavailability compared to the

free drug. Furthermore, in M. Tuberculosis


infected mice only three oral doses of the
nanoparticles that were spaced 15 days
apart resulted in complete bacterial
clearance from specific organs, which is
comparable to 45 conventional doses of the
free drug.

Bioadhesive sodium alginate microspheres


of metoprolol tartrate for intranasal
60
61 | P a g e

systemic delivery were prepared to avoid


the first-pass effect, as an alternative
therapy for injection, and to obtain
improved therapeutic efficacy in the
treatment of hypertension and angina
pectoris. The microspheres were prepared
using emulsification-cross linking method.
In vivo studies indicated significantly
improved therapeutic efficacy of
metoprolol from microspheres, with
sustained and controlled inhibition of
isoprenaline-induced tachycardia as
compared with oral and nasal
administration of drug solution.

In a comparative study, alginate


formulation appeared to be better than the
polylactide-co- glycolide (PLG)
61
62 | P a g e

formulation in improving the


bioavailability of two clinically important
antifungal drugs-clotrimazole and
econazole. The nanoparticles were
prepared by the emulsion-solvent-
evaporation technique in case of PLG and
by the cation-induced controlled
gelification in case of alginate.

Carrageenans
Carrageenan is sulphated polysaccharide
extract of the seaweed called carrageen; or
Irish moss, the red algae obtained from
Chondrus Crispus
(Rhodophyceae).Carrageenan extracted
from seaweed is not assimilated by the
human body and provides only bulk but no
62
63 | P a g e

nutrition. There are three basic types of


carrageenan – kappa (κ), iota (ι) and
lambda (λ) respectively.The λ-type
carrageenan results in viscous solutions but
are non-gelling, while the κ- type
carrageenan forms a brittle gel.

The ι-type carrageenan produces elastic


gels. A study where the compaction ability
of two κ- carrageenans (Gelcarin® GP-812
NF and GP-911NF) and one ι-carrageenan
(Gelcarin® GP-379 NF) was investigated
showed that these carrageenans are able to
form strong compacts with a high elastic
recovery. It was finally concluded from the
results that the carrageenans investigated
were suitable tableting excipients for the
manufacturing of controlled-release tablets.
63
64 | P a g e

Hydrogel beads were prepared from a


mixture of cross-linked κ-carrageenan with
potassium and cross- linked alginate with
calcium and they exhibited a smoother
surface morphology than that of the one-
polysaccharide network beads. The
carrageenan parts of the hydrogen
pronouncedly enhanced the thermostability
of the polymeric network. These beads
were introduced as novel carriers for
controlled drug delivery systems.

Psyllium
Psyllium mucilage is obtained from the
seed coat of Plantago ovata by milling the
outer layer of the seeds. It has been
64
65 | P a g e

evaluated for its tablet binding


properties,but also to form hydrogels
through radiation-induced cross-linking for
controlled release of 5-fluorouracil as a
model drug.

Psyllium and methacrylamide based


hydrogels were prepared by using N,N’-
methylenebisacrylamide as a cross-linker,
which were then loaded with insulin.

These cross-linked hydrogels showed


controlled release of the active ingredient
by means of non- Fickian diffusion of the
drug through polymer chain relaxation
during swelling.81 Psyllium husk was used
in combination with other excipients such
as hydroxypropyl methylcellulose to
65
66 | P a g e

prepare a novel sustained release, swellable


and bioadhesive gastroretentive drug
delivery systems for ofloxacin.

Xanthan Gum
Xanthan gum is a high molecular weight
extracellular polysaccharide produced by
the fermentation of the gram-negative
bacterium Xanthomonas campestris. The
primary structure of this naturally
produced cellulose derivative contains a
cellulosic backbone (β-D-glucose residues)
and a trisaccharide side chain of β-D-
mannose-β-D-glucuronicacid-α-D-
mannose attached with alternate glucose
residues of the main chain.

66
67 | P a g e

In one of the trials, xanthan gum showed a


higher ability to retard the drug release
than synthetic
hydroxypropylmethylcellulose. Xanthan
gum and hydroxypropylmethylcellulose
were used as hydrophilic matrixing agents
for preparing modified release tablets of
diltiazem HCl. The amount of
hydroxypropylmethylcellulose and xanthan
gum exhibited significant effect on drug
release from the tablets prepared by direct
compression technique. It was concluded
that by using a suitable blend of
hydroxypropylmethylcellulose and xanthan
gum desired modified drug release could
be achieved.

67
68 | P a g e

By utilizing retention properties of xanthan


gum and releasing properties of
galactomannan, the desired release profile
was achieved in delivering of theophylline.
Hydrophilic galactomannan is obtained
from the seeds of the Brazilian tree
Mimosa scabrella (Leguminosae). The
matrices made alone with xanthan gum (X)
showed higher drug retention for all
concentrations, compared with
galactomannan (G) matrices that released
the drug too fast. The matrices prepared by
a combination of both gums were able to
produce near zero-order drug release. The
XG (conc. 8%) tablets provided the
required release rate (about 90% at the end
of 8 h), with zero-order release kinetics.

68
69 | P a g e

APPLICATIONS
Many of the applications of natural
polymers lost out in the competitive world
to synthetic polymers, in which properties
could be tailored to needs. Petroleum-
based products had properties independent
of the material vagaries associated with
crops, whose component properties can
vary significantly with growin8 site,
agronomic factors including weather, and
other complicated considerations.
69
70 | P a g e

Molecular weight, degree of branching,


and chemical groups in side and main
chain sites can be more readily modified
and controlled for syna« pliers than for
most natural materials. However, in some
cases, chemical modifications of naMal
polymers can lead to materials of
particularly interesting properties; e.g.,
hydrolyzed starch/polyacrylonitrile graft
copolymers with astounding water
absorption and holding characteristics…the
first superabsorbent (i4). In general,
however, these problems caused natuml
polymers to become comparatively
unattractive at the commercial level. As a
result, Morris emphasized that by the
1990’s two thirds of our clothes were
derived from oil, plastics replaced paper

70
71 | P a g e

containers, food dyes came from mineral


oil and so on. These were all changes
indicative of the shift of markets from
natural to synthetic materials.

In recent years, the socio-economic


situation has changed to make natural
polymers once a8ain worth consideration
for many applications. First of all, oil
embargos and higher oil prices and concern
over long-term availability of oil forced
technologists and scientists to consider
alternative, and especially renewable,
sources of materials. Second,
environmental considerations made the use
of many natural materials very attractive
because of their biodegradability, low
toxicity and low disposal costs. Finally,
71
72 | P a g e

properhes aside, the use of natural


materials, such as starch, for fillers in
composite materials was economically
attractive because of the high price of
synthetic polymer matrices and the low
prices of such natural products as starch
and starch granules. These low costs are
related, of course, to the large agricultural
surpluses of recent years and the ability of
farmers to produce more. However,
utilization of natural polymers only
because they are cheap fillers hardly
justifies their inclusion as “advanced
materials.” To classify as advanced
materials, there should be significant new
and sophisticated technical features in their
design, development, or processing. That
is, there must be scientific or engineering

72
73 | P a g e

factors, that go significantly beyond mere


economic advantage, to warrant the
designation “advanced.”

New Natural Polymers and Modeling-


Computer based techniques have begun to
be used to design and predict the properties
of polymers, primarily of the synthetic type
(2J). Some pioneering molecular modeling
studies of plant proteins, starch and
cellulose have been carried out recently .
These have just scratched the surface of
what is possible. The potential of emerging
computer based methods to predict
conformation, interactions and properties
of natuml polymers, their chemical
derivatives and blends is immense. This
has become feasible for large molecules
73
74 | P a g e

only recently as computer speed has


increased and molecular dynamics
simulations and new approximate methods
have been developed.

Due to phenomenal advances in molecular


biology, it may well become feasible in the
near future to genetically manipulate plants
(such as corn or soybeans) to produce pipe
maalldefined molecular weight and
branching and even introduce functional
groups, such as acetyl, sulphate, amino and
phosphate moieties. This may be easiest in
the case of proteins, where the amino acid
sequence follows directly from the
sequence of bases in the plant’s DNA. For
example, researchers are now modifying
genes to improve the mechanical properties
74
75 | P a g e

of animal proteins, such as elastin, silk and


various adhesive polymers (i2). For other
types of natural polymers, a« chemical
structure is determined from DNA
indirectly via the activity of a series of
enzymes. Nevertheless, work on
expression of bacterial genes for the
production of poly(hydroxybutyrates) in
plants is progressing and may eventually
yield a polyester of very low cost . New
genetic varieties of com containing
starches of different branch frequency and
length have recently been developed . The
preparation of completely new polymers in
plants may even be possible.

This points to the need for more


understanding of the relationships between
75
76 | P a g e

structure and function in natural polymers


so we will know what kind of polymer we
should make fora given application when
the genetic/synthetic machinery is
developed. Computer modeling may well
become the “screening method” ofchoice
to identify new polymers without having to
go through the long and tedious process of
synthesizing or “growing” every
possibility. Also, it should not be forgotten
that we currently raise only a dozen or so
plant crops in large amounts and that the
hundreds of thousands of other species of
plants (not to menfion millions of species
of microorganisms) represent an
undiscovered source of new polymers and
fiber. Exciting work for the botanical
explorer!

76
77 | P a g e

Water Soluble and Swellnble Natural


Polymers- Most natural polymers are
water swellable. Applications that take
advantage of this property would seem to
be preferred. Since many water-soluble
polymers are discharged directly into
wastewater streams after use, the
biodegradability of natural polymers would
be an asset in preventing the build up or
toxicity in fresh water sources. Water based
polymer systems avoid the use of toxic
organic solvents, the use of which is
becoming more restricted by legislation.
Also, the prices of synthetic, water soluble
synthetic polymers are quite high, usually
over Slflb. Thus, it is no surprise that
starch and cellulose derivatives are widely
77
78 | P a g e

used as water soluble adhesives,


thickeners, binders and coatings (5, 12).
Some emerging applications include
polyaspartic acid and oxidized starches as
metal ion sequestrants in detergents,
mussel proteins as adhesives, cross-linked
anionic starches as superabsorbents in
drapers and modified agricultural residues
as absorbents of organic wastes (43-48).
More research is needed on basic stricture-
property relationships of natural polymers
to understand their behavior in aqueous
systems.

78
79 | P a g e

NATURAL POLYMERS
AND SUSTAINABILITY
In many ways, our current utilization of
natural resources cannot be sustained. Most
of our fuel for power and transportation
comes from fossil fuels, such as oil which
will be depleted in the future. Rising
atmospheric carbon dioxide levels from
combustion of fossil fuels are thought to be
increasing global temperatures which, in
turn, may cause droughts, crop losses,
storm damage, etc. Soil for growing crops
is being lost to erosion from wind and rain
and the expansion of cities. Irrigation
water, particularly in the western U.S., is
gradually being depleted as aquifer wells
are pumped down. The number of species
79
80 | P a g e

of living things in the world, estimated at


>l0 million, are going extinct at a rate of
about 0.3% per year (49). World
population is presently growing at about
1.5% per year, while food production is
increasing at only 0.5% per year [50). If
these trends continue, world population
will approximately double to 11 billion in
50 years.

How can natural polymers contribute


solutions to these problems?
The use of natural polymers as materials
and as sources of fuel, such as ethanol,
lessens our dependence on non-renewable
petroleum. As pointed out by Orts and
Glenn in this Symposium, certain natural
polymer have the potential of acting as
80
81 | P a g e

flocculating agents to control soil loss from


erosion. Clearly, if the properties of a
natural polymer, such as its strength, were
improved, less would be needed for a
specific application. New applications for
agricultural wastes and by products of
processing, as well as recycling of natural
polymers, promise to make more efficient
use of our natural resources. Also,
alternative crops can produce more
biomass per acre of land. Fiber from kenaf
and hemp, rather than slow growing trees,
can be utilized for a number of
applications. This points to the need to
conserve plant germplasm since solutions
to future problems may lie in species as yet
undiscovered.

81
82 | P a g e

CONCLUSION
Polymers play a vital role in the drug
delivery. So, the selection of polymer
plays an important role in drug
manufacturing. But, while selecting
polymers care has to be taken regarding its
toxicity, drug compatibility and
degradation pattern. By this review, we
82
83 | P a g e

can say that natural polymers can be good


substitute for the synthetic polymers and
many of the side effects of the synthetic
polymers can be overcome by using natural
polymers.

83
84 | P a g e

Bibliography

1. https://en.wikipedia.org/wiki/Polymer
2. https://byjus.com/chemistry/natural-
polymers/
3. https://www.researchgate.net/
publication/2362175

84

You might also like