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INTRAUTERINE
DRUG DELIVERY SYSTEM




           Prepared by:
           Murari Pavan
           M.Pharm(Pharmaceutics)
• What is an Intrauterine Contraceptive Devices (IUD)?
  IUD’s are medicated or non-medicated devices which exerts
  it’s contraceptive action in the uterine cavity continuously for a
  prolonged period of time without requiring patients motivation.

• How Does an IUD Work?
  An IUD prevents sperm from meeting an egg.
  An IUD may stop a fertilized egg from growing inside the
  uterus.
Types of IUD’s:
1. Non-medicated IUD’s:
    Contraceptive action by producing sterile inflammatory
    response in Endometrium. These are available in ring shaped
    IUD’s made up of s.s and plastic fabricated form
    polyethylene, polypropylene.

2. Medicated IUD’s:
    - Copper IUD’s
    - Progesterone releasing IUD’s
Copper bearing IUD’s:
A) 7-Shaped IUD:
- Further development of the concept of intra-uterine
  contraception by metallic copper has resulted in copper barring
  IUD, which contains 89mg copper wire, wound around the
  vertical limb of a 7-shaped polypropylene device, to give an
  effective surface of approximately 200mm2 used for 3years as
  intra-uterine contraceptive treatment.
• This device release copper ion at a mean daily dose of
  9.87µg/day continuously in the uterine cavity for up to
  40months.
• The Cu-7 appears to be substantially smaller then other.
• It can be easily inserted because of it’s special 7-configuration
  in addition to its small size.
• Insertion can usually be accomplished without the need for
  cervical dilation and further more removal is generally
  painless.
B) T-Shaped IUD’s:
• T-shaped IUD containing 200mm2 contraceptive copper wire
    winding around the vertical leg of a T-shaped polyethylene
    device in the manner as copper-7 device.
• It is used for 3years of contraceptive treatment.
• This T-shaped device has a volume of 0.16cm3,which is
    almost twice as large as the 7-shaped device.
C) New development of copper bearing IUD’s:
  The Cu-T-380A with 2 collars of copper positioned on the
  transverse arms of the letter T. Each collar provides an
  additional surface area of 30mm2. It has relatively small
  surface area of copper but effective than Cu-T-200.
 Another new version of copper bearing IUD:
  The combined multi load copper IUD (MLCU-250) was also
  introduced.
  It is a compromise between Cu-T IUD, but without the central
  plastic membrane and has a surface area of 250mm2 copper
  wire.
  The blunt apex of the device fits into the vault of the uterine
  cavity without penetrating the endometrial walls and its two
  arms studded side arms fully adapt to the contours of the
  uterine cavity.
IUD Inserting method:
Potential development
1) Membrane controlled reservoir-type drug delivery system:
    These drug delivery devices consist of a polymeric membrane
    that both encapsulates and controls the release of
    contraceptive agent
a)Single component system:
    In this system the contraceptive agent is encapsulated in its
    pure solid form in a capsule fabricated form bio-compatible
    polymeric materials (silicon elastomers and polyethylene-
    polymers)
    The release of contraceptive agent such as progesterone
    follows essentially zero-order kinetics.
b)Multi component system:
  In this system a constant drug release profile is maintained by encapsulating
  a liquid medium saturated with excess drug profiles in a rate-controlling
  polymeric membrane.


2)Polymer matrix diffusion controlled drug delivery devices:
  This drug delivery device is prepared by homogenously dispersing the drug
  particles in a crossed linked polymeric matrix.
a)Retrievable matrix device:
  This drug delivery system is designed for feasibility of retrieval at
  termination of treatment. It can be easily fabricated from silicone elastomers
  by premixing a drug in powder form with a semisolid silicone elastomers
  before vulcanization at room or low temperature or from polyethylene by
  dry mixing. The rate of drug release is not constant but time dependent.
b)Bio-degradable matrix device:
  This drug delivery system is designed to eliminate the need for
  retrieving at the end of treatment it can be prepared by
  dissolving such a poly lactic acid, in a common organic solvent
  to dryness, to produce drug dispersing biodegradable matrix
  devices of varying shapes and sizes,
  The rate of drug-release from this type of drug delivery system
  is a combination of polymer hydrolysis and drug diffusion.
MECHANISM OF ANTIFERTILITY ACTION OF COPPER:
• Copper is known to be cytotoxic in high concentration it
    enhances the spermatocidal and spermato depressive
    action of an IUD.
•   The copper concentration in endometrial epithelium and
    superficial stromata inhibits the binding of steroids of
    their receptors.
•   Cupric ion inhibits the binding of 17-β- estradiol to human
    endometrial cytosol.
•   Cupric ions shows only little effect on sperm motility.
•   Copper wire was also “Blastocystocidal”.
• A copper bearing IUD was reported to produce significant
  effects like:
   • Increased alkaline phosphate activity in uterine fluids and
     endometrium tissue.
   • No change of acid phosphate activity in uterine fluid but its
     concentration in endometrium tissue increases.
Advantages of the IUD:
 Provides long-term birth control.
 Cost effective.
 Can be removed when a woman would like to become
  pregnant.
 Convenient - a woman does not need to remember it daily
  or weekly.
Disadvantages of an IUD:
 Between 2 and 10% fall out, most commonly in the first
  year of use.
 Increased risk of miscarriage if an IUD is left in the uterus
  during pregnancy.
 In rare cases, the IUD may attach to or perforate the wall
  of the uterus.
 With the copper IUD, a woman may experience heavier
  bleeding and cramping with periods.
Thank you

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Intra Uterine Devices

  • 1. INTRAUTERINE DRUG DELIVERY SYSTEM Prepared by: Murari Pavan M.Pharm(Pharmaceutics)
  • 2. • What is an Intrauterine Contraceptive Devices (IUD)? IUD’s are medicated or non-medicated devices which exerts it’s contraceptive action in the uterine cavity continuously for a prolonged period of time without requiring patients motivation. • How Does an IUD Work? An IUD prevents sperm from meeting an egg. An IUD may stop a fertilized egg from growing inside the uterus.
  • 3. Types of IUD’s: 1. Non-medicated IUD’s: Contraceptive action by producing sterile inflammatory response in Endometrium. These are available in ring shaped IUD’s made up of s.s and plastic fabricated form polyethylene, polypropylene. 2. Medicated IUD’s: - Copper IUD’s - Progesterone releasing IUD’s
  • 4. Copper bearing IUD’s: A) 7-Shaped IUD: - Further development of the concept of intra-uterine contraception by metallic copper has resulted in copper barring IUD, which contains 89mg copper wire, wound around the vertical limb of a 7-shaped polypropylene device, to give an effective surface of approximately 200mm2 used for 3years as intra-uterine contraceptive treatment. • This device release copper ion at a mean daily dose of 9.87µg/day continuously in the uterine cavity for up to 40months. • The Cu-7 appears to be substantially smaller then other.
  • 5. • It can be easily inserted because of it’s special 7-configuration in addition to its small size. • Insertion can usually be accomplished without the need for cervical dilation and further more removal is generally painless. B) T-Shaped IUD’s: • T-shaped IUD containing 200mm2 contraceptive copper wire winding around the vertical leg of a T-shaped polyethylene device in the manner as copper-7 device. • It is used for 3years of contraceptive treatment. • This T-shaped device has a volume of 0.16cm3,which is almost twice as large as the 7-shaped device.
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  • 7. C) New development of copper bearing IUD’s: The Cu-T-380A with 2 collars of copper positioned on the transverse arms of the letter T. Each collar provides an additional surface area of 30mm2. It has relatively small surface area of copper but effective than Cu-T-200.  Another new version of copper bearing IUD: The combined multi load copper IUD (MLCU-250) was also introduced. It is a compromise between Cu-T IUD, but without the central plastic membrane and has a surface area of 250mm2 copper wire. The blunt apex of the device fits into the vault of the uterine cavity without penetrating the endometrial walls and its two arms studded side arms fully adapt to the contours of the uterine cavity.
  • 9. Potential development 1) Membrane controlled reservoir-type drug delivery system: These drug delivery devices consist of a polymeric membrane that both encapsulates and controls the release of contraceptive agent a)Single component system: In this system the contraceptive agent is encapsulated in its pure solid form in a capsule fabricated form bio-compatible polymeric materials (silicon elastomers and polyethylene- polymers) The release of contraceptive agent such as progesterone follows essentially zero-order kinetics.
  • 10. b)Multi component system: In this system a constant drug release profile is maintained by encapsulating a liquid medium saturated with excess drug profiles in a rate-controlling polymeric membrane. 2)Polymer matrix diffusion controlled drug delivery devices: This drug delivery device is prepared by homogenously dispersing the drug particles in a crossed linked polymeric matrix. a)Retrievable matrix device: This drug delivery system is designed for feasibility of retrieval at termination of treatment. It can be easily fabricated from silicone elastomers by premixing a drug in powder form with a semisolid silicone elastomers before vulcanization at room or low temperature or from polyethylene by dry mixing. The rate of drug release is not constant but time dependent.
  • 11. b)Bio-degradable matrix device: This drug delivery system is designed to eliminate the need for retrieving at the end of treatment it can be prepared by dissolving such a poly lactic acid, in a common organic solvent to dryness, to produce drug dispersing biodegradable matrix devices of varying shapes and sizes, The rate of drug-release from this type of drug delivery system is a combination of polymer hydrolysis and drug diffusion.
  • 12. MECHANISM OF ANTIFERTILITY ACTION OF COPPER: • Copper is known to be cytotoxic in high concentration it enhances the spermatocidal and spermato depressive action of an IUD. • The copper concentration in endometrial epithelium and superficial stromata inhibits the binding of steroids of their receptors. • Cupric ion inhibits the binding of 17-β- estradiol to human endometrial cytosol. • Cupric ions shows only little effect on sperm motility. • Copper wire was also “Blastocystocidal”.
  • 13. • A copper bearing IUD was reported to produce significant effects like: • Increased alkaline phosphate activity in uterine fluids and endometrium tissue. • No change of acid phosphate activity in uterine fluid but its concentration in endometrium tissue increases.
  • 14. Advantages of the IUD:  Provides long-term birth control.  Cost effective.  Can be removed when a woman would like to become pregnant.  Convenient - a woman does not need to remember it daily or weekly.
  • 15. Disadvantages of an IUD:  Between 2 and 10% fall out, most commonly in the first year of use.  Increased risk of miscarriage if an IUD is left in the uterus during pregnancy.  In rare cases, the IUD may attach to or perforate the wall of the uterus.  With the copper IUD, a woman may experience heavier bleeding and cramping with periods.