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INTRAUTERINE AND INTRAVAGINAL
DRUG DELIVERY SYSTEM
By
Gaurav Shriram Patil.
Final Year B.Bharm.
Kvps, Institute of Pharmaceutical Education, Boradi.
Gaurav Patil
1
Contents
 Introduction
 Anatomy and Physiology of female reproductive system
 Advantages
 Disadvantages
 Classification of Intrauterine devices
 Intrauterine and Intravaginal drug delivery System
 References
Gaurav Patil
2
Introduction
 Vagina and Uterus are the route for administration of contraceptives , antifungals
and antimicrobials.
 These are used for local or systemic absorption.
 Because of vast network of blood vessels, vaginal wall is suitable for drug
absorption.
 The rate and extent of drug absorption may vary depends upon:
1) Formulation factors
2) Physiology
3) Age of patient
4) Menstrual cycle
Gaurav Patil
3
 An Intra Uterine Device(IUD) is a small plastic contraceptive
device that is gently inserted into the uterus (womb) by the
physician or nurse practitioner.
 IUDs are about 98-98% effective in preventing pregnancy and one
type of IUDs can stay in place for up to 10 years before needing to
be replaced.
 The IUD is most effective choice for the women who had her
children and now want long term , but not permanent contraception.
 The IUD may also a good choice for women who cannot take birth
control pills.
Gaurav Patil
4
Anatomy and Physiology of Female Reproductive System
Female Reproductive System
Gaurav Patil
5
The Female Reproductive system mainly consist of Following organs:
1. Vagina- Muscular canal about 3 inches long. Muscular canal about 3 inches long. Vaginal
wall surface is covered with epithelium cells. Size: in premenopausal female 7.8 cm in
length & 2 cm wide, in postmenopausal female 4.5 cm in length & 1-1.5 cm in width.
2. Uterus- Non pregnant uterus is around 7.5cm long, 5cm wide and 2.5cm thick.
Endometrium is highly vascular made up of simple columnar epithelium and highly
sensitive to hormonal secretions of ovary. During complete cycle endometrium goes
thickening with hormonal impact
3. Fallopian Tubes- Also called as Oviducts or Uterine tubes around cm long. The internal
surface is of ciliated columnar epithelium cells.
4. Ovaries- Two in number each on either side of uterus. These having shape and size like
of unehllled almond. Ovaries produced hormone called Progesterone, Estrogen.
5. Vulva- Its has basic five parts namely Labia Majora , Labia Minora, Vestibules, Cliotoris,
Mons Pubis
Gaurav Patil
6
Advantages
 Reversible
 Highly effective contraceptive method
 Method is private
 Less expensive over a time
 It can be use by a women who is breastfeed
 Avoid first pass effect
 Minimal side effects compare to others
 Increase bioavailabity.
Gaurav Patil
7
Disadvantages
 Possible irregular bleeding or increased cramping
 Possible expulsion of device
 Does not protect against STDs or HIV
 Patient Incompliance
 Only few drugs can be administered
 Influence with sexual intercourse.
 Gender specificity.
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8
Classification of IUDs
IUD
Medicated
2nd Generation
(Eg. Copper IUD.)
3rd Generation
(Eg. Hormonal IUD )
Non-Medicated
1st Generation
(Eg. Lippe’s loop)
Gaurav Patil
9
Classification of Intravaginal DDS
Vaginal
Drug
Delivery
System
Vaginal
Rings
Onitment
Supposito
ries
Vaginal
Capsules
and
Tablets
Gels and
Creams
Powders
Gaurav Patil
10
Intrauterine Drug Delivery System
Definition : The IUDs are the small objects that are inserted through the cervix
and placed in the uterus to prevent the pregnancy.
Types of IUDs for controlled drug delivery:-
1) Non-hormonal IUDs. (Ex. copper-T, copper-7)
2) Hormonal IUDs. ( Ex. Progestasert)
1) Non-hormonal IUDs/ copper medicated IUDs.
• It is consists of polyethylene or polypropylene plastic support of number-7 or
letter-T with certain amount of pure electrolytic copper wire wound around them.
• Copper is cytotoxic and enhance spermicidal & spermatodepressive action of
IUD.
Gaurav Patil
11
• The Non-hormonal IUDs does not contain any therapeutic agent.
• This kind of IUDs are available in the forms of rings. Eg. Lippe’s
loop, Copper-.
• The exposed surface area of copper is 380 mm².
• This kind of IUDs having no hormonal side effects.
• They are easy to insert.
• Types- Cu T-200--------200 mm².
Cu T-30---------30 mm².
Copper-T
Gaurav Patil
12
2) Hormonal IUDs/ Medicated IUDs
• These are the T-shaped devices made up of polyethylene frame measures 32mm both
vertical and horizontal directions
• There is a silicone reservoir containing either progesterone or levonogestral on a vertical
stem and further enclosed in a sleeve of rate controlling membrane of ethylenevinyl-
copolymer.
• It prevents the pregnancy up to 5 years by steadily realizing small amount of Progesterone
directly into the uterus.
• For some womens it may also prevent the ovulation from occurring.
• The hormonal IUD is available in Australia and USA under a brand name Mirena.
• This kind of IUD is also used in a condition of Breast cancer.
• Example: Mirena IUD.
Gaurav Patil
13
Intravaginal Drug Delivery System
Ideality of Intravaginal DDS
1) Component should melt at vaginal temperature i.e. at 37oC.
2) Device should be nontoxic and nonirritating.
3) Formulation should be nonsensitive on vaginal pH.
4) Formulation should have wetting and emulsifying properties.
5) It should be stable on storage.
6) Formulation should have proper viscosity to avoid leakage of drug
from vagina.
Gaurav Patil
14
Classification of Intravaginal drug delivery system
 A. Localized :
1) Barrier contraception
(Diaphragm, Cervical cap, Sponge)
2) Prevention/Treatment of infection
( Gels, Cream, Ointment)
 B. Systemic :
A. Suppositories or pessaries.
B. Bio(muco)adhesive semisolids.
• These are emulsion bases formulation to deliver antifungal agents such asimidazole. Give
controlled delivery for 3 or more hrs.
Gaurav Patil
15
 C. Solid polymeric carriers.
a. Solid hydrogels:
Having swelling property which enables the drug to diffuse out of the macromolecular
network. eg. Nu-gel ( Johnson & Johnson)
b. Elastomeric intravaginal rings( IVR):
1) Matrix (homogeneous dispersion)
2) Reservoir (core)
3) Sandwich (shell)
Elastomer exert slight tension on vaginal wall, more suitable for hydrophobic drugs.
Normally designed to contain steroidal hormones.
Gaurav Patil
16
Other novel approaches :
1) Medicated Vaginal Tampons- A medicated vaginal tampon, approved as a medical
device by the Food and Drug Administration (FDA) .
• This bifunctional tampon contains a polymeric delivery system (strips) that absorb menstrual
fluid while gradually releasing lactic acid and citric acid.
• eg. Brilliant pH tampons.
Gaurav Patil
17
2) Vaginal Films-
• Vaginal films are polymeric drug delivery systems shaped as thin sheets, usually ranging
from 220 to 240 μ m in thickness.
• These systems are often square (approximately 5cm × 5cm), colorless, and soft, presenting
a homogenous surface.
• Vaginal films are produced with polymers such as polyacrylates, polyethylene glycol,
polyvinyl alcohol, and cellulose derivatives.
• Eg.VCF (vaginal contraceptive films)
Gaurav Patil
18
# ADVANTAGES
• Minimal side effects
• Rapid drug absorption
• Avoid first pass effect
• Increases the bioavailability.
# DISADVANTAGES
• Only few drugs are administered
• Patient Incomplianace
• Gender Specificity
• Some drugs are sensitive at
vaginal pH. May causes irritation.
Gaurav Patil
19
References
1. Chatterjee Arkendu & Kumar Lalit (2009), On overview of Intra-vaginal Drug
deliverysystem, Journal of Pharmacy research, 2 (4) 698-700.
2. Chien Y. W. (2007), Novel Drug Delivery Systems, Revised and Expanded, Marcel
Dekker, Inc., New York, Second Indian Reprint , Vol.-50, p. 529-629.
3. Baviskar D.T & Jain D.K , Novel Drug Delivery Systems, Nirali Prakashan,
p. 10.1-10.8
4. Brahmankar D. M. & Jaiswal S. B. (2009), Biopharmaceutics and
PharmacokineticsA Treatise, 2nd edition, Vallabh Prakashan, p. 502-508.
Gaurav Patil
20

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Intrauterine and Intravaginal drug delivery system

  • 1. INTRAUTERINE AND INTRAVAGINAL DRUG DELIVERY SYSTEM By Gaurav Shriram Patil. Final Year B.Bharm. Kvps, Institute of Pharmaceutical Education, Boradi. Gaurav Patil 1
  • 2. Contents  Introduction  Anatomy and Physiology of female reproductive system  Advantages  Disadvantages  Classification of Intrauterine devices  Intrauterine and Intravaginal drug delivery System  References Gaurav Patil 2
  • 3. Introduction  Vagina and Uterus are the route for administration of contraceptives , antifungals and antimicrobials.  These are used for local or systemic absorption.  Because of vast network of blood vessels, vaginal wall is suitable for drug absorption.  The rate and extent of drug absorption may vary depends upon: 1) Formulation factors 2) Physiology 3) Age of patient 4) Menstrual cycle Gaurav Patil 3
  • 4.  An Intra Uterine Device(IUD) is a small plastic contraceptive device that is gently inserted into the uterus (womb) by the physician or nurse practitioner.  IUDs are about 98-98% effective in preventing pregnancy and one type of IUDs can stay in place for up to 10 years before needing to be replaced.  The IUD is most effective choice for the women who had her children and now want long term , but not permanent contraception.  The IUD may also a good choice for women who cannot take birth control pills. Gaurav Patil 4
  • 5. Anatomy and Physiology of Female Reproductive System Female Reproductive System Gaurav Patil 5
  • 6. The Female Reproductive system mainly consist of Following organs: 1. Vagina- Muscular canal about 3 inches long. Muscular canal about 3 inches long. Vaginal wall surface is covered with epithelium cells. Size: in premenopausal female 7.8 cm in length & 2 cm wide, in postmenopausal female 4.5 cm in length & 1-1.5 cm in width. 2. Uterus- Non pregnant uterus is around 7.5cm long, 5cm wide and 2.5cm thick. Endometrium is highly vascular made up of simple columnar epithelium and highly sensitive to hormonal secretions of ovary. During complete cycle endometrium goes thickening with hormonal impact 3. Fallopian Tubes- Also called as Oviducts or Uterine tubes around cm long. The internal surface is of ciliated columnar epithelium cells. 4. Ovaries- Two in number each on either side of uterus. These having shape and size like of unehllled almond. Ovaries produced hormone called Progesterone, Estrogen. 5. Vulva- Its has basic five parts namely Labia Majora , Labia Minora, Vestibules, Cliotoris, Mons Pubis Gaurav Patil 6
  • 7. Advantages  Reversible  Highly effective contraceptive method  Method is private  Less expensive over a time  It can be use by a women who is breastfeed  Avoid first pass effect  Minimal side effects compare to others  Increase bioavailabity. Gaurav Patil 7
  • 8. Disadvantages  Possible irregular bleeding or increased cramping  Possible expulsion of device  Does not protect against STDs or HIV  Patient Incompliance  Only few drugs can be administered  Influence with sexual intercourse.  Gender specificity. Gaurav Patil 8
  • 9. Classification of IUDs IUD Medicated 2nd Generation (Eg. Copper IUD.) 3rd Generation (Eg. Hormonal IUD ) Non-Medicated 1st Generation (Eg. Lippe’s loop) Gaurav Patil 9
  • 10. Classification of Intravaginal DDS Vaginal Drug Delivery System Vaginal Rings Onitment Supposito ries Vaginal Capsules and Tablets Gels and Creams Powders Gaurav Patil 10
  • 11. Intrauterine Drug Delivery System Definition : The IUDs are the small objects that are inserted through the cervix and placed in the uterus to prevent the pregnancy. Types of IUDs for controlled drug delivery:- 1) Non-hormonal IUDs. (Ex. copper-T, copper-7) 2) Hormonal IUDs. ( Ex. Progestasert) 1) Non-hormonal IUDs/ copper medicated IUDs. • It is consists of polyethylene or polypropylene plastic support of number-7 or letter-T with certain amount of pure electrolytic copper wire wound around them. • Copper is cytotoxic and enhance spermicidal & spermatodepressive action of IUD. Gaurav Patil 11
  • 12. • The Non-hormonal IUDs does not contain any therapeutic agent. • This kind of IUDs are available in the forms of rings. Eg. Lippe’s loop, Copper-. • The exposed surface area of copper is 380 mm². • This kind of IUDs having no hormonal side effects. • They are easy to insert. • Types- Cu T-200--------200 mm². Cu T-30---------30 mm². Copper-T Gaurav Patil 12
  • 13. 2) Hormonal IUDs/ Medicated IUDs • These are the T-shaped devices made up of polyethylene frame measures 32mm both vertical and horizontal directions • There is a silicone reservoir containing either progesterone or levonogestral on a vertical stem and further enclosed in a sleeve of rate controlling membrane of ethylenevinyl- copolymer. • It prevents the pregnancy up to 5 years by steadily realizing small amount of Progesterone directly into the uterus. • For some womens it may also prevent the ovulation from occurring. • The hormonal IUD is available in Australia and USA under a brand name Mirena. • This kind of IUD is also used in a condition of Breast cancer. • Example: Mirena IUD. Gaurav Patil 13
  • 14. Intravaginal Drug Delivery System Ideality of Intravaginal DDS 1) Component should melt at vaginal temperature i.e. at 37oC. 2) Device should be nontoxic and nonirritating. 3) Formulation should be nonsensitive on vaginal pH. 4) Formulation should have wetting and emulsifying properties. 5) It should be stable on storage. 6) Formulation should have proper viscosity to avoid leakage of drug from vagina. Gaurav Patil 14
  • 15. Classification of Intravaginal drug delivery system  A. Localized : 1) Barrier contraception (Diaphragm, Cervical cap, Sponge) 2) Prevention/Treatment of infection ( Gels, Cream, Ointment)  B. Systemic : A. Suppositories or pessaries. B. Bio(muco)adhesive semisolids. • These are emulsion bases formulation to deliver antifungal agents such asimidazole. Give controlled delivery for 3 or more hrs. Gaurav Patil 15
  • 16.  C. Solid polymeric carriers. a. Solid hydrogels: Having swelling property which enables the drug to diffuse out of the macromolecular network. eg. Nu-gel ( Johnson & Johnson) b. Elastomeric intravaginal rings( IVR): 1) Matrix (homogeneous dispersion) 2) Reservoir (core) 3) Sandwich (shell) Elastomer exert slight tension on vaginal wall, more suitable for hydrophobic drugs. Normally designed to contain steroidal hormones. Gaurav Patil 16
  • 17. Other novel approaches : 1) Medicated Vaginal Tampons- A medicated vaginal tampon, approved as a medical device by the Food and Drug Administration (FDA) . • This bifunctional tampon contains a polymeric delivery system (strips) that absorb menstrual fluid while gradually releasing lactic acid and citric acid. • eg. Brilliant pH tampons. Gaurav Patil 17
  • 18. 2) Vaginal Films- • Vaginal films are polymeric drug delivery systems shaped as thin sheets, usually ranging from 220 to 240 μ m in thickness. • These systems are often square (approximately 5cm × 5cm), colorless, and soft, presenting a homogenous surface. • Vaginal films are produced with polymers such as polyacrylates, polyethylene glycol, polyvinyl alcohol, and cellulose derivatives. • Eg.VCF (vaginal contraceptive films) Gaurav Patil 18
  • 19. # ADVANTAGES • Minimal side effects • Rapid drug absorption • Avoid first pass effect • Increases the bioavailability. # DISADVANTAGES • Only few drugs are administered • Patient Incomplianace • Gender Specificity • Some drugs are sensitive at vaginal pH. May causes irritation. Gaurav Patil 19
  • 20. References 1. Chatterjee Arkendu & Kumar Lalit (2009), On overview of Intra-vaginal Drug deliverysystem, Journal of Pharmacy research, 2 (4) 698-700. 2. Chien Y. W. (2007), Novel Drug Delivery Systems, Revised and Expanded, Marcel Dekker, Inc., New York, Second Indian Reprint , Vol.-50, p. 529-629. 3. Baviskar D.T & Jain D.K , Novel Drug Delivery Systems, Nirali Prakashan, p. 10.1-10.8 4. Brahmankar D. M. & Jaiswal S. B. (2009), Biopharmaceutics and PharmacokineticsA Treatise, 2nd edition, Vallabh Prakashan, p. 502-508. Gaurav Patil 20