Novel Drug Delivery System

(13PH0704)

Unit 5 (Part B)
Intrauterine Device
(IUDs)

Presented by:
Ms. Suman R. Borsadiya
Assistant Professor
FOP, MU
IUD-Intra Uterine Devices
 Introduction
❖ The intrauterine device (IUD) is a small T-shaped device that is used as a method of
birth control designed for insertion through the cervix and placed in the uterus to
prevent pregnancy.
❖ IUDs also have been referred to as ''intrauterine contraception" (IUC).
❖ An IUD is a type of long-acting reversible contraception. IUDs have been shown to be
over 99% effective in preventing pregnancy.
❖ Contraceptives are devices or methods for preventing pregnancy, either by
preventing the fertilization of the female egg by the male sperm or by preventing
implantation of the fertilized egg.
 Introduction
Historical background
❖ The modem era of the IUD started in 1909 when Richard Richter in Germany used a ring from
silkworm gut as an intrauterine device. This device was, the first genuine IUD.
❖ Ernst Grafenberg described in 1929 a device consisting of a core of silkworm gut encircled by
an alloy of copper, nickel, and zinc that was highly effective in preventing pregnancy; results of
his experiments started a strong controversy on the problem of the induction of PIO
(pelvic inflammatory disease) and European practitioners rejected the idea.

❖ Fortunately, in Japan in 1934, Tenrey Ota presented the results of his studies on the use of
elastic metallic rings as IUDs. The idea was accepted and the IUDs rapidly started to be used.
❖ Second-generation copper-T IUDs were also introduced in the 1970s.

❖ These devices had higher surface areas of copper, and for the first time consistently achieved
effectiveness rates of greater than 99%
 Introduction
Anatomy of the Uterus
The uterus is a pear shaped; thick walled, muscular organ suspended in the anterior wall of
pelvic cavity. Fallopian tubes enter its upper portion, one on each side and the lower portion
of the uterus projects into the vagina. The uterine cavity is normally triangular in shape and
flattened anterior- posteriorly.
 Introduction
Anatomy of the Uterus
The wall of the uterus consists of three layers:
Endometrium: It represents the mucous membrane which forms the inner coat of the uterine
wall. It consists of an epithelial lining and connective tissue with two types of arteries
supplying blood to the endometrium
Myometrium: It is a thick muscular middle layer made up of bundles of smooth muscles
embedded in connective tissue.
Peritoneum: It covers the uterus and is anchored to both sides of the pelvic cavity by broad
ligament
 Intrauterine Devices (IUD's)
Intrauterine Devices (IUD's)

❖ It is the small object that is inserted through the cervix

and placed in the uterus to prevent pregnancy.
❖ A small string hangs down from the IUD into the upper
part of the vagina.
❖ IUD's show pharmacological efficacy for about 1-10
years. They work by changing the lining of the uterus
and fallopian tubes affecting the movements of eggs
and sperm and so that fertilization does not occur.
 Intrauterine Devices (IUD's)

Development of IUD's

❖ These devices cause more endometrial compression and myometrium distention, leading
to uterine cramps, bleeding and expulsion of IUDs.

❖ Researchers developed IUDs in past 30 years with the aim to add antifertility agents to
more tolerated, smaller devices, such as T-shaped device, to enhance effectiveness; or
antifibrinolytic agents, such as e-amino-caproic acid and tranexamic acid to larger IUDs to
minimize the bleeding and pain.
 Intrauterine Devices (IUD's)
Development of IUD's

❖ Tatum developed a T-shaped device that would work better with the shape of the uterus,
which forms a T when contracted. This reduced side effects significantly.
❖ Zipper 1968 added contraceptive metals (Cu) and Doyle and Clewe developed Progestin
releasing IUD.
❖ This development initiated a new era of R and D for long term JU contraception,
leading to generation of recent IUDs-medicated IUDs.
❖ Copper bearing IUDs such as Cu-7 and Progesterone releasing IUDs such as Progestasert
(approved by FDA in 1976) thus evolved.
 Intrauterine Devices (IUD's)
Types of IUDs
1. Non-medicated IUDs
2. Medicated IUDs

1. Non-medicated IUDs: These exert their contraceptive action by producing a sterile

inflammatory response in the Endometrium by its mechanical interaction. These do not
contain any therapeutic effect. For e.g. Ring-Shaped IUDs of Stainless Steel, Plastic IUDs, Lippes
Loop, Dalkon Shield, Saf- T-Coil.
 Intrauterine Devices (IUD's)
2. Medicated IUDs: These are capable of
delivering pharmacologically active
antifertility agents. For e.g. Copper bearing
IUDs, Progesterone releasing IUD.
❖ There are two types of medicated IUDs:
1. Copper bearing IUDs.
2. Hormone releasing IUDs:
There are two types (H-IUD):
(a)Progesterone releasing IUD -
Progestasert.
(b)Levonorgesterone IUD - Levonorgestrel
releasing device - [MIRENA].
 Advantages of IUD's
Advantages of IUD's
❖ The IUD is one of the most popular contraceptive methods, especially for long-term eversible
contraception, as it can be easily fitted and removed.
✓ It is highly effective, with a 98-99% success rate over five years of IUD use.
✓ It can be used by almost any woman including nulliparous.
✓ Its action lasts for ten years if it is not removed in between.
✓ The onset of action is immediate.
✓ It is suitable for lactating women.
✓ Fertility returns promptly on discontinuation.
✓ It can be used by women who are on any type of medication.
✓ It is not associated with cancer of any organ unlike hormonal contraception.
✓ It is cost effective.
 Disadvantages of IUD's
Disadvantages of IUD's
❖ Sometimes users feel pain, cramps or dizziness when the IUD is put in or taken out of uterus.
❖ There is a small risk of infection (about 1 %) when an IUD is put in uterus.
❖ There is a very small risk of damage to the uterus (about 1in1000 people).
❖ A copper IUD might give you more bleeding and cramping during period, but this usually gets
better over time.
❖ The copper IUD can cause an allergic reaction, but this is very rare
❖ The hormonal IUD might give you irregular or light bleeding
❖ The risk of pelvic infection may be increased around the time of insertion of IUD, but routine
screening before insertion is generally not recommended.
❖ The IUD can sometimes come out by itself (about 5% of all IUDs). You can check the strings are still
in the right place at any time.
Classification of IUD’s
Classification of IUD’s

Classification of
IUD’s

Second Third generation

First generation
generation IUD’s- IUD’s- Steroid
IUD’s- Plastic Copper bearing medicated
devices devices devices
 Classification of IUD’s
Classification of IUD’s: First generation IUD’s- Plastic devices
❖ IUD technology has come a long way since the first plastic IUDs appeared on the scene. The
first of the so-called "first generation" IUDs, represented by the Margulies spiral was
introduced in 1960.
❖ After many experiments, Dr Jack Lippes invented the double-S Loop (the Lippes Loop) in
1962. It
was made from polyethylene, with barium sulphate added for visibility under X-rays;
and was available in four slzes, from A to D.
❖ This IUD was the first to have a nylon thread attached to the lowest part of the device; this
made it easier to remove, and it was also possible to verify by simple vaginal examination
that the IUD was in the uterine cavity.
 Classification of IUD’s
❖ The Lippes Loop was to become extremely popular and, of all the first-generation IUDs, had the
greatest worldwide impact
❖ Dalkon Shield developed by Dr Hugh Davis, and released in 1971. The Dalkon Shield was a
plastic device which looked like a round bug with one large eye and five legs on each side. It had a
unique tail not a single filament, but many fibers wound together and enclosed in a sheath. Because
the Dalkon Shield's unique shape made it difficult to remove, a multifilament string was used to
provide increased tensile strength during removal.
❖ The multifilament tail string unique to the Dalkon Shield, was most probably responsible for the
facilitated ascent of bacteria from the vagina upward into the uterine cavity, cause pelvic
infections.
 Classification of IUD’s
Second generation IUD’s- Copper bearing devices
❖ The development of the first copper-bearing IUD (Cu-IUD) was announced in 1969 by Dr Jaime
Zipper and Dr Howard Tatum.
❖ Small T-shaped IUD is most appropriate and on account of the "fundal-seeking effect", the T-
shaped device would be less prone to expulsion. A copper filament with a free (ionizable) surface
of 200 mm2 was optimal in terms of contraceptive efficacy.
❖ The first copper-bearing IUD, the TCu200, was produced in 1969. Using a T-carrier, with the addition
of 200 mm2- copper wire, reduced the pregnancy rate from 18 per 100 woman years with the plain T
carriers to 1 per 100 woman years.
 Classification of IUD’s
Second generation IUD’s- Copper bearing devices
❖ The Multiload IUD, invented in 1974 by the Dutch gynecologist Dr Willem Van Os; was very
successful.
❖ The MLCu-250 was the first version, available in three sizes (standard, mini and short), to allow
insertion into different sized uteri, including the nulliparous.
❖ The MLCu-375 followed, with more copper to enhance efficacy and length of use. The lower copper-
load versions are licensed for 3 years' use and the MLCu-375 model for 5 years, although efficacy to 8
years has been demonstrated for the latter device.
❖ Over the years, Dr Tatum himself developed a series of copper bearing T devices. His TCu220C
model is of particular interest, because, in carrying copper collars instead of a copper filament,
metal loss was prevent
 Classification of IUD’s
Second generation IUD’s- Copper bearing devices
 Classification of IUD’s
Third generation IUD’s- Steroid medicated devices

❖ Dr Antonio Scommegna, demonstrated the uterine effects of progesterone in the late 1960s
❖ He developed a hormone releasing device. and showed that it is as effective in preventing
pregnancy as the copper-bearing IUD.
❖ A device is a ‘T-shaped, consisting of a permeable polymer membrane which releases
progesterone at a predictable, controlled rate of 65 mg per 24 h over the period of a year.
❖ The levonorgestrel releasing intrauterine system (LNG-IUS) is a T-shaped polyethylene device
with a steroid reservoir around the vertical stem.
Mechanism of action
 Mechanism of action
❖ The IUD induces an intense local inflammatory response, especially by the copper containing
devices, which in turn leads to lysosomal activation and other inflammatory changes that are
spermicidal. Whenever fertilization occurs, the same inflammatory actions are directed against
the developing embryo.

❖ Inert devices, such as the Lippes-leop, are more effective with increased size and extent of
contact with the endometrium. Certain metals, especially copper, greatly enhance the
contraceptive action of inert devices, probably by inducing a more intense local intrauterine
inflammatory response
❖ The progesterone carrying devices induce atrophic endometrial changes. which make the
endometrium a hostile site for implantation if fertilization and successful tubal transport have
occurred.
 Mechanism of action
❖ It is not possible to demonstrate a single mode of action of the levonorgestrel-releasing IUD.
Scanty cervical mucus and strong suppression of the endometrium is the main factors behind the
contraceptive action of the device

❖ Other. suggested mechanisms to prevent conception are inhibition of sperm motility and function
inside the uterus and in the fallopian tubes, preventing fertilization and endometrial growth.
 Applications of IUD's
❖ Applications of IUD's
• It is used as a contraceptive to prevent pregnancy.
• It can be suitable for use in Hormone Replacement Therapy.
• It can be safely used in women with heavy bleeding to prevent/control the same.
• In the treatment of fibroids.
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India 360003.
www.marwadiuniversity.ac.in