In vitro permeation study of a mucoadhesive drug delivery system for controlled delivery of nonoxynol-9

Pharmaceutical Development and Technology
C H Lee, Y W Chien

Abstract

A carbopol 934P-based drug delivery system (AmDDS) was developed to achieve the dual-controlled delivery of Nonoxynol-9 (N-9), a spermicidal agent, and EDTA, a potentiator of spermicidal activity. This gel-type system made intimate contact with vaginal mucosa and maintained an effective drug concentration within the vagina for a prolonged period of time. An existing mathematical model, based on a unilayer diffusion membrane, was applied for describing permeation of N-9 through vaginal mucosa. Vaginal permeation of N-9 from AmDDS was negligible over the initial 5 hr, then increased in a Q versus t pattern, but remained low. A relationship was observed between the permeation rate (Js) of drug through vaginal mucosa and the release flux (Q/t1/2) from AmDDS, which showed that the permeation rate (Js) increased with increased square of the release flux [(Q/t1/2)2] in a hyperbolic manner. This result indicated that release of N-9 from AmDDS is still the rate-limiting step at doses within the tested range. EDTA, at concentration of up to 0.32%, did not change the permeation rate of N-9 through vaginal mucosa. It is thus concluded that the developed AmDDS can control the intravaginal delivery of N-9 as well as its permeation through va...Continue Reading

References

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Citations

Aug 28, 2014·The European Journal of Contraception & Reproductive Health Care : the Official Journal of the European Society of Contraception·Li RongxiuTian Huiyan
Jul 6, 2004·Journal of Pharmaceutical Sciences·Alexandra B SassiLisa Cencia Rohan
Feb 18, 2015·Advanced Drug Delivery Reviews·Rita Monteiro MachadoRita Palmeira-de-Oliveira
Oct 18, 2005·International Journal of Pharmaceutics·Armorél D van Eyk, Pieter van der Bijl
Mar 23, 2001·Journal of Biomaterials Science. Polymer Edition·B S Lele, A S Hoffman
Dec 12, 2012·International Urogynecology Journal·Sushma Srikrishna, Linda Cardozo

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