VAGINAL DRUG DELIVERY SYSTEM

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VAGINAL DRUG DELIVERY SYSTEM : 

VAGINAL DRUG DELIVERY SYSTEM PRESENTED BY:- GURPREET ARORA M.PHARMACY (PHARMACEUTICS) 1ST SEMESTER M090400003

Contents : 

Contents Introduction Anatomy and Physiology of vagina Advantages Disadvantages Factors affecting absorption of drugs Vaginal and uterine route for sustained release Vaginal dosage form Different delivery systems Recent developments Applications Conclusion References

Introduction : 

Introduction Vagina is route for administration for contraceptives , antifungals, antimicrobials. It is used for the achievement of local or for systemic absorption. The vaginal wall is very well suited for the absorption of drugs for systemic use. As it contains a vast network of blood vessels

Anatomy & Physiology of Vagina : 

Anatomy & Physiology of Vagina The vagina in the adult premenopausal female is approximately 7-8 cm in length and 2 cm wide, shrinking in the postmenopausal female to approximately 4.5-6 cm in length and 1-1.5 cm in width. Normal pH of the vagina in premenopausal women ranges from 4 to 5, and rises to almost 7 in the post menopausal female. The vagina is characterized by an exceptional elasticity and the surface area of the vagina is increased by numerous folds by microridges covering the epithelium cell surface.

Slide 5: 

A layer of relatively thick connective tissue is located between the anterior vaginal wall and the urinary canal as well as between the posterior vaginal wall and the intestinal tract. The vaginal wall itself consists of three layers:- The epithelial layer, The tunica adventitia, The muscular coat. The epithelial layer is made up of an epithelial lamina and a lamina propria. It consists of noncornified, stratified squamous epithelial cells, which changes with age.

Slide 6: 

In the subepithelial layer rests a network of elastic fibers around the lamina propria and collagenous fibers around the tunica adventitia, creating a connection to the muscular coat. The muscular coat of the vagina is composed of smooth muscle and elastic fibers. A spiral arrangement of these fibers provides support to withstand stretching without rupturing the vagina The tunica adventitia is formed of loose connective tissue that is attached to the muscular coat. The vagina is encompassed by a vascular supply of arteries, veins and lymph capillaries, as well as sensory and autonomous nerves

Slide 7: 

Because the vaginal epithelium is affected by ovarian hormones, a cyclic variation occurs. Age related changes associated with menopause cause reduction in vaginal size, loss of elasticity, decrease in vascularity and a thinning of the mucosa. This thinning of the vaginal epithelium leads to a substantial increase in permeability of this tissue. The structural changes would influence vaginal absorption, and must be taken into account as a significant factor in vaginal application of drugs. It was found that the vaginal absorption of insulin was varied by changes in the thickness of the vaginal epithelium.

Slide 8: 

Female reproductive system and related structures: vagina (1), cervix (2), uterus (3), ovary (4), fallopian tube (5), urinary bladder (6), urethra (7), anus (8), rectum (9), colon (10), vestibule (11), and pubic symphysis (12). (Courtesy of Lu í s Paup é rio.)

Advantages : 

Advantages Prolonged release. Minimal systemic side effects. An increase in bioavailability. Use of less total drug than an oral dose. First-pass metabolism can be avoided. Self medication is possible.

Disadvantages : 

Disadvantages Patient incompliance. Only a few drugs are administered by this route. Variability in drug absorption related with menstrual cycle, menopause and pregnancy, can also limit vaginal drug delivery route usage. Influence with sexual intercourse. Gender specificity.

Factors affecting absorption of drugs : 

Factors affecting absorption of drugs Physicochemical properties of the drug as lipophilicity, ionization, chemical structure and interaction with vaginal secretions and tissues. The thickness of vaginal wall. The ovarian cycle or by pregnancy. Changes in the vaginal epithelium and pH with menopause.

Improvement of vaginal absorption : 

Improvement of vaginal absorption Use of penetration enhancers e.g. PEG. By increasing the contact time between the dosage form and the vaginal membrane by using mucoadhesive polymers e.g. Carbopol. By increasing vaginal blood flow, thereby raising the concentration gradient across the vaginal mucosa. By the use of pro-drugs enhances drug permeability through modification of the hydrophilicity or lipophilicity of the drug.

Vaginal and Uterine route for sustained/controlled-release drug delivery : 

Vaginal and Uterine route for sustained/controlled-release drug delivery Sustained and controlled-release devices for drug delivery in the vaginal and uterine areas are most often for the delivery of contraceptive steroid hormones. One such application is the medicated vaginal ring. Medicated vaginal rings fabricated from silastic 382 medical grade elastomer. These are of ‘doughnut-shaped’. Also known as intravaginal rings or V-Rings

Slide 14: 

Vaginal rings, provide a means of delivering a drug to the systemic circulation at a controlled release rate.

Slide 15: 

Several vaginal ring products are currently available, including:- Estring - a low-dose estradiol-releasing ring, manufactured from silicone elastomer, for the treatment of vaginal atrophy. Femring - a low-dose estradiol-acetate releasing ring, manufactured from silicone elastomer, for the relief of hot flashes and vaginal atrophy associated with menopause. NuvaRing - a low-dose contraceptive vaginal ring, manufactured from poly(ethylene-co-vinyl acetate), and releasing etonogestrel (a progesterone) ethinylestradiol (an estrogen).

Slide 16: 

NuvaRing - NuvaRing is inserted into the vagina and left in place for three weeks, after which it is removed for a 'ring-free' week to allow menstruation to occur.

Slide 17: 

A more common contraceptive device is the intrauterine device (IUD). Two types of medicated IUD are generally used; contraceptive metals and steroid hormones. The metal device is exemplified by the CU-7, a polypropylene plastic device in shape of number 7. Copper is released by a combination of ionization and chelation from a copper wire wrapped around the vertical limb. This is effective for up to 40 m. Application of prostaglandin containing vaginal rings for induction of labor or pregnancy termination. Antifungals have been important drug candidates for the treatment of gynecological conditions.

Slide 18: 

The vaginal delivery of azole antigungals as clotrimazole, miconazole, econazole, itraconazole and sertaconazole is effective in the topical treatment of vaginal candidiasis.

Ideality of intra-vaginal drug delivery system : 

Ideality of intra-vaginal drug delivery system Component should melt at vaginal temperature i.e. at 36 °C. Intra-vaginal drug delivery device should be non-toxic and non irritating. It should not have any meta-stable form. The preparation should have high water number. The preparation should have wetting and emulsifying properties.

Slide 20: 

The preparation should be non-sensitized on vaginal pH (i.e. 3.5-4.9). It should be stable on storage. The preparation should have small interval between melting and solidification point. The preparation should have proper viscosity, so avoid the leakage of preparation from vagina (in case of semisolid dosage form). The preparation should have proper bio-adhesive/mucoadhesive properties, so increase the contact time between the membrane and Preparation.

Vaginal dosage forms : 

Vaginal dosage forms In the development of vaginal dosage forms, several considerations should be addressed as:- Maintenance of an optimal pH for vaginal epithelium. Ease of application. Even distribution of the drug. Retention time in the vagina. Compatibility with co-administered medicines.

Slide 22: 

Many different types of formulations have been applied vaginally as, tablets, vaginal suppositories or pessaries, foams, douches, sprays, gels, creams and vaginal rings. Creams, gels, sprays and foams are used as vehicles for drugs such as anti-infective or contraceptive agents. Douches are aqueous solutions that are administered into the vagina for cleansing purpose. Vaginal suppositories, also called pessaries, are usually globular, oviform or cone-shaped, and weighing about 5 g each.

Slide 23: 

Plastic insertion devices are usually used to hold the vaginal suppository during insertion for proper placement within the vagina. Vaginal suppositories intended for localized effects are employed mainly as contraceptives, antiseptics and antifungals. Design of a liposome delivery system for vaginal administration of acyclovir was investigated, to provide sustained release and improve bioavailability of the encapsulated drug for the local treatment of genital herpes.

Different Systems for Delivery : 

Different Systems for Delivery Solid Systems-include tablets, capsules and vaginal suppositories. Semisolid Systems-creams,gels,ointments. Liquid Systems-Vaginal douching with liquids containing antimicrobial drugs like povidine-iodine. Vaginal Foams-It is new vaginal drug delivery systems. In fact, foams containing antimicrobials, local anesthetics, and hormones have the potential to gradually substitute several currently available dosage forms, namely creams and ovules.most foam bases are nonirritating.

Slide 25: 

Medicated Vaginal Tampons-A medicated vaginal tampon, approved as a medical device by the Food and Drug Administration (FDA), is available (Ela Tampon, Rostam, Israel). This bifunctional tampon contains a polymeric delivery system (strips) that absorb menstrual fluid while gradually releasing lactic acid and citric acid. Vaginal Sponges-A vaginal sponge made of soft polyurethane foam (diameter of 5.5 cm and 2.5 cm thick) and saturated with 1 g of nonoxynol - 9 authorized as a spermicide.

Slide 26: 

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 5 cm × 5 cm), colorless, and soft, presenting a homogenous surface. Vaginal fi lms are produced with polymers such as polyacrylates, polyethylene glycol, polyvinyl alcohol, and cellulose derivatives. Vaginal Rings-Nuva ring of estradiol

Novel concepts in vaginal drug delivery : 

Novel concepts in vaginal drug delivery NVDDS are designed with desirable distribution, bioadhesion, retention and release characteristics. The conventional VDFs, such as suppositories, gels, creams and foams can meet some but not all of these requirements. Achieved by the use of bioadhesive and other novel delivery systems.

Bioadhesive delivery systems : 

Bioadhesive delivery systems Bioadhesive vaginal formulations that are capable of delivering the active agent for an extended period at a predictable rate. Bioadhesive formulations have been found to reduce the conventional treatment time of fungal infections by at least 25%. A bioadhesive formulation might not necessarily contain a therapeutic agent and can be used as a moisturizer for the treatment of dry vagina.

Other novel delivery systems : 

Other novel delivery systems Phase change polymers such as poloxamers exhibit sol–gel transition in response to body temperature, pH and specific ions and they prolong the residence time of the dosage form in the vagina. Formulations based on a thermoplastic graft copolymer have been developed to provide the prolonged release of active ingredients such as nonoxynol-9, progestins, estrogens, peptides and proteins in a vaginal environment

In vitro and in vivo evaluation of vaginal formulations : 

In vitro and in vivo evaluation of vaginal formulations In vitro studies include the determination of release and bioadhesive characteristics in addition to various physical and chemical properties of formulations. In vivo studies are carried out for the assessment of efficacy, distribution, spreading and retention of formulations in the vagina.

Recent developments : 

Recent developments Recently, effervescent vaginal tablets of nystatin were formulated, their antifungal and therapeutic effect was found higher than that of conventional one. Also,the antifungal activity of effervescent vaginal tablets containing clotrimazole was improved as compared to the conventional one. Moreover, bioadhesive effervescent ketoconazole tablets for vaginal delivery was studied. Therefore, effervescent vaginal tablets can consider as one of vaginal medication dosage forms.

List of vaginal preparations recently developed or under development : 

List of vaginal preparations recently developed or under development

Applications of intra-vaginal drug delivery system : 

Applications of intra-vaginal drug delivery system This route of drug administration is useful for vaginal immunization. Multi-cycle administration of vaginal contraceptive rings. Effective route for the treatment of HIV infection. Effective route for the treatment of local fungal infection. Effective for the delivery of hormones.

Conclusions : 

Conclusions The vaginal route has been traditionally used for the local application of drugs, but is now gaining importance as a possible site for systemic delivery. For the prevention of STDs, AIDS and conception, the use of vaginal products might provide a better alternative to behavioural modifications and the use of condoms. Novel developments such as bioadhesive systems and liposomes overcome some of the major limitations of conventional vaginal products

References : 

References ‘Chein.w.yie’, “Novel Drug Delivery System” 2nd edition,p 529-584. ‘Gad cox shayne’, “Pharmaceutical Manufacturing Handbook”, vaginal drug delivery, p 809-857. Arkendu Chatterjee et al. / Journal of Pharmacy Research 2009, 2(4),698-700. Kavita Vermani and Sanjay Garg, PSTT Vol. 3, No. 10 October 2000 “The scope and potential of vaginal drug delivery”.

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