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Advanced Drug Delivery and Targeting

This document discusses various mechanisms for controlling drug release from delivery systems, including diffusion, dissolution, osmosis, mechanical processes, and bio-responsive mechanisms. It provides examples of each type, such as reservoir and matrix devices for diffusion-controlled release and how osmotic pumps can achieve zero-order drug release. The document also discusses drug targeting systems and various dosage forms that can be used for advanced drug delivery and targeting, including molecular carriers, nanoparticles, microparticles, and macrodevices.

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hafiz patah
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42 views

Advanced Drug Delivery and Targeting

This document discusses various mechanisms for controlling drug release from delivery systems, including diffusion, dissolution, osmosis, mechanical processes, and bio-responsive mechanisms. It provides examples of each type, such as reservoir and matrix devices for diffusion-controlled release and how osmotic pumps can achieve zero-order drug release. The document also discusses drug targeting systems and various dosage forms that can be used for advanced drug delivery and targeting, including molecular carriers, nanoparticles, microparticles, and macrodevices.

Uploaded by

hafiz patah
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PPTX, PDF, TXT or read online on Scribd
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RATE-CONTROLLED

RELEASE IN DRUG
DELIVERY AND TARGETING
RATE-CONTROLLED RELEASE IN
DRUG DELIVERY AND TARGETING
Drug release from a delivery system can be zero-order, variable or
bioresponsive. Although there are literally hundreds of commercial products
based on controlling drug release rate from delivery systems, there are in fact
only a small number of mechanisms by which drug release rate is controlled:
• Diffusion-controlled release mechanisms
• Dissolution-controlled release mechanisms
• Osmosis-controlled release mechanisms
• Mechanical-controlled release mechanisms
• Bio-responsive controlled release mechanisms
Diffusion-controlled and dissolution-controlled release
In this case, the drug must diffuse
through either a polymeric
membrane or polymeric or lipid
matrix, in order to be released.
Diffusion-controlled devices can
be divided into :
• reservoir devices: in which the
drug is surrounded by a
polymeric membrane which
retains the drug. After a certain
period of time the polymeric
membrane dissolves, thereby
releasing the drug;
• matrix devices: in which the
drug is distributed throughout a
polymeric matrix, which
dissolves with time, thereby
releasing the drug.
Dissolution-controlled release -reservoir devices

• Since the dissolution of polymeric materials is the key to this


mechanism, the polymers used must be water soluble and/or
degradable in water.
• The choice of a particular polymer for a particular controlled release
dosage form depends on various factors such as the dissolution
mechanism, delivery period, delivery route, the drug etc.
• In general, synthetic water-soluble polymers tend to be widely used
for oral-controlled release dosage forms.
• Biodegradable polymers tend to be used for injectable, or
implantable, drug delivery systems.
Dissolution-controlled release -matrix devices
• In this case, drug release is controlled by dissolution of the matrix.
• Since the size of the matrix decreases as the dissolution process
continues, the amount of drug released also decreases with time.
• The decrease in drug release can be compensated in part by
constructing a non-linear concentration profile in the polymer matrix
 This strategy is used in the oral dosage form, Adalat, where the
core of the dissolution matrix contains more drug than the outer
layer.
• Matrix dissolution devices are widely used in parenteral therapy 
Zoladex subcutaneous implant
Dissolution-controlled release -matrix devices
• oral dosage form, Adalat : the core of the dissolution matrix contains
more drug than the outer layer.
• Matrix dissolution devices are widely used in parenteral therapy 
Zoladex subcutaneous implant
Osmosis-controlled drug release
• Osmosis is defined as the movement of water through a semi-permeable membrane into a
solution.
• The movement of water results in an increase in pressure in the solution and the excess
pressure is known as the osmotic pressure.
• Osmotic pressure can used to pump out a drug at a constant rate from the delivery system.
Osmosis-controlled drug release
• Device and formulation
parameters can be
controlled so that drug
release is zero-order.

(B) Operation principle of a


single compartment pump.
Constant (zero-order) release
is maintained as long as the
drug solution is saturated.
(C) Operation principle of a
two compartment pump. The
constant (zero-order) release
can be maintained for the
entire period of operation.
Osmosis-controlled drug release
• An important consideration is that osmotic-controlled devices require
only osmotic pressure to be effective, thus such devices operate
essentially independently of the environment.
• Hence, in vitro drug release rate is often consistent with the in vivo
release profile.
• Also, for oral delivery, changes in pH or ionic strength in the
gastrointestinal tract will not affect the drug release rate.
Osmosis-controlled drug release
• In parenteral therapy, the
subcutaneously
implantable, osmotic
mini-pumps developed by
the Alza Corp. are used
widely used for animal.
• The DUROS implant
developed specifically for
the controlled delivery of
peptides and proteins.
• Osmotic mini-pumps,
such as the Oros osmotic
pump via the oral route
Mechanical-controlled drug release
• Mechanically driven pumps are
common tools for the
intravenous administration of
drugs in the hospital setting.
• They allow physicians and
patients to precisely control
the infusion rate of a drug.
• Externally programmable
pumps can facilitate:
• zero-order controlled drug
release;
• intermittent drug release.
• Ideally, a pump should deliver the drug at the
prescribed rate(s) for extended periods of time and
thus should incorporate a wide range of delivery
rates, ensure accurate, precise and stable delivery,
contain reliable pump and electrical components
and finally, provide a simple means to monitor
pump status and performance.
• A pump should also be convenient for the patient
and thus should ideally be reasonably small in size
and inconspicuous, have a long reservoir life and
be easy to program.
• The biocompatibility of the device surface is also
an important issue for consideration. Other safety
concerns include danger of over dosage, drug
leakage and pump blockage.
Bio-responsive controlled drug release
• Bio-responsive controlled drug delivery
systems modulate drug release in response
to changes in the external environment, such
as pH and ionic strength.
• More sophisticated systems incorporate
specific enzymes which causes changes in
localized pH or increases in localized
concentrations of specific substrates such as
glucose.
• The change in pH caused by the
biotransformation of the substrate by the
enzyme thereby causes a change in
permeability of a pH-sensitive polymeric
system in response to the specific
biomolecule.
DRUG TARGETING SYSTEMS
• An important point to remember is that while rate-controlled systems
can deliver the drug at a predetermined rate, they are generally
unable to control the fate of the drug, once it enters the body.
• Drug targeting systems are used to achieve site-specific drug delivery.
• Site-specific drug delivery is desirable in therapeutics, in order to
improve:
• drug safety, as toxic side-effects caused by drug action at non-target sites are
minimized;
• drug efficacy, as the drug is concentrated at the site of action rather than
being dispersed throughout the body;
• patient compliance, as increased safety and efficacy should make therapy
more acceptable and thus improve compliance.
DOSAGE FORMS FOR ADVANCED
DRUG DELIVERY AND TARGETING
Types of dosage forms for drug delivery and targeting systems:
• Molecular carrier -Drugs is attached to water-soluble carriers, such as
monoclonal antibodies, carbohydrates, lectins and immuno-toxins to
achieve site-specific drug delivery. Release of the attached drug molecules at
the target site can be achieved by enzymatic or hydrolytic cleavage.
• Nanoparticle carrier - solid colloidal particles nanoparticles used for
parenteral drug delivery and targeting.
• microparticles carrier – Synthetic/natural polymer (gelatin/starch) polymers
used for microparticulate and biodegradable implantable devices
• Macrodevices - see notes
Properties of an “ideal” dosage form and route of administration

• Patient acceptability and compliance


• Reproducibility
• Ease of termination
• Biocompatibility and absence of adverse effects
• Large effective area of contact
• Prolonged contact time
• Low metabolic activity
• Blood supply
• Accessibility
• Lack of variability
• Permeability

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