Vagina is an important site for the delivery of drugs, particularly contraceptives for ages. As the advacement in pharmaceutical technology, the new delivery systems are taking the place of the traditional delivery sytems such as suppositories, tablets, creams and gels. The consideration of women’s opinions on vaginal products is also important for the development of acceptable dosage forms and better compliance.
Mucoadhesive systems have a unique place among the different new delivery systems. Mucoadhesive polymers have been successfully applied for systemic and local vaginal drug delivery. Acrylic acid polymers (Carbomer or polycarbophil) and cellulose derivatives, such as hydroxyethylcellulose,
Hydroxypropylcellulose and hydroxypropyl methylcellulose have been widely used as mucoadhesive polymers for the preparation of mucoadhesive vaginal drug delivery systems. There are a number of patents based on both group of polymers. In particular it can be said that polyacryclic acid polymers are excellent multipurpose vehicles for vaginal drug delivery. The current systems are used for vaginal lubrication, contraception, vaginal infections, labour inducement and infertility. Among the possible topical compositions, gels present notable advantages in comparison with other types of pharmaceutical products, such as good compliance in administration by the patient and ease of distribution of the pharmaceutical product on the surface of the vaginal mucosa. Gels in particular, on account of the high water content in their structure, present the further advantage of a hydrating and lubricating action, which is particularly useful in pathological
situations characterised by dryness of the vaginal mucosa.
Despite the numerous vaginal gel formulations patented, relatively few gel preparation are commercially available. Most of them are used for contraception and moisturazition of vagina. Up to our knowledge, there is no commercially available mucoadhesive vaginal tablet formulations present.
When present patents checked for mucoadhesive vaginal drug delivery systems it can be noticed that there are many patents available having these key words. Moreover, as it is a general complain, these patents claim several different things. For instance, some of them have many active and inactive ingredients with broad range of quantity or one patent have a claim of even different dosage forms in the same application such as gel, ointment, tablet, film or suppository etc. for vaginal application. This claims obviously written just to increase the coverage of the patents to make breaking attempts of patent impossible. It is really difficult to find precise patents and precise claims. All claims were found to be exaggerated much. It is therefore difficult to focus on precise aim. It may be just normal for applicant to increase the border of their patent coverage but, it also makes new applications difficult and many times impossible. Although there are limited numbers of commercially available mucoadhesive vaginal drug delivery systems, in the near future mucoadhesive vaginal drug delivery systems will gain more significance due to the increase in sexually transmitted diseases such as HIV.
180 Table 3:- Marketed mucoadhesive vaginal gels
References:
1. Acartürk, F. "Effect of the spermicide, nonoxynol 9, on vaginal permeability in normal and ovariectomized rabbits." Pharma Res., 1996: 950-951.
2. al, das Neves et. "Gels as vaginal drug delivery systems." International Journal of Pharmaceutics, 2006: 1-14.
3. al, Waugh Anne et. "Anatomy and Physiology in Health and Illness." In Anatomy and Physiology in Health and Illness, by Waugh Anne et al, 423-424.
Hong Kong: Churchill Livingstone, Longman, 1996.
4. C, Valenta. "Development and in vitro evaluation of a mucoadhesive vaginal delivery system for progesterone." J Control Release, 2001: 323-332.
5. C., Valenta. "The use of mucoadhesive polymers in vaginal delivery." Advanced Drug Delivery Rev, 2005: 1692-1712.
6. Deim, T. et al. "Development of controlled release sildenafil formulations for vaginal administration."
Drug Delivery, 2008: 259-265.
7. Deshpande, A. A. "Intravaginal drug delivery."
Drug Development and Industrial Pharmacy, 1992:
1225-1279.
8. Guler, E. et al. "Studies on vaginal bioadhesive tablets of acyclovir." Pharmazie, 2000: 297-299.
9. Hussain, A.et al. "The vagina as a route for systemic drug delivery." Journal of Controlled Release, 2005: 301-313.
10. Hussain, A.et al. "The vagina as a route for systemic drug delivery." Journal of Control Release, 2005: 301-313.
11. Jain, N.K. "Controlled and Novel Drug Delivery."
In Controlled and Novel Drug Delivery, by N.K.
Jain, 353-377. New Delhi: CBS Publishers and Distributors, 1997.
12. Karasulu, H.Y. et al. "Güneri T. Efficacy of a new ketoconazole bioadhesive vaginal tablet on Candida albicans." Farmaco, 2004: 163-167.
13. Knuth, K. et al. "Hydrogel delivery systems for vaginal and oral applications. Formulation and biological considerations." Advanced Drug Delivery Rev, 1993: 137-167.
14. Mauck, C.K.et al. "Vaginal distribution of Replens and K-Y Jelly using three imaging techniques." Contraception, 2008: 195-204.
15. Ozer, O. et al. "W/O/W multiple emulsion containing nitroimidazole derivatives for vaginal delivery." Drug Delivery, 2007: 139-145.
Brand name Gelling agent Active substance Usage
Acid jelly® Tragacanth, acacia gum Oxyquinoline sulphate, Ricinoleic acid, Acetic acid
Maintainence of the vaginal acidity
Gynol 11® Sodium carboxy methyl
cellulose
Nonoxynol-9 Contraceptive
Prostin E2® Colloidal silicon dioxide Dinoprostone Labour inducer
Replens® Polycarbophil and
Carbopol®974P
- Vaginal mosturizer
Metrogel vaginal® Carbopol®974P Metronidazole Bacterial vaginosis
181 16. Perioli, L. et al. "FG90 chitosan as a new polymer for metronidazole mucoadhesive tablets for vaginal administration." Int J Pharm, 2009.
17. R., Friend David. "Advances in vaginal drug delivery." Drug Deliv. and Transl. Res., 2011: 183–
184.
18. Richardson, J.L. "Routes of Delivery:case studies." Adv. Drug Del. Rev., 1992: 341-366.
19. Robinson, J.R.et al. "Gels as vaginal drug delivery systems." International journal of pharmacy, 2006: 1-14.
20. Washington, N et al. "Physiological pharmaceutics: barriers to drug absorption." In Physiological pharmaceutics: barriers to drug absorption, by N et al Washington. London: Taylor &
Francis, 2001.
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