In vitro permeation study of a mucoadhesive drug delivery system for controlled delivery of nonoxynol-9.
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 vaginal mucosa.
Lee
C H
CH
College of Pharmacy, Rutgers-State University, Piscataway, New Jersey 08854, USA.
Chien
Y W
YW
D000269:Adhesives / Q000737:chemistry*; D002118:Calcium / Q000737:chemistry; D002614:Chelating Agents / Q000737:chemistry; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D016503:Drug Delivery Systems; D004492:Edetic Acid / Q000737:chemistry; D005260:Female; D006801:Humans; D008954:Models, Biological; D009092:Mucous Membrane / Q000378:metabolism; D017137:Nonoxynol / Q000737:chemistry*; D010539:Permeability; D019999:Pharmaceutical Solutions; D013089:Spermatocidal Agents / Q000737:chemistry*; D014621:Vagina / Q000378:metabolism
D000269:Adhesives; D002614:Chelating Agents; D019999:Pharmaceutical Solutions; D013089:Spermatocidal Agents; D017137:Nonoxynol; D004492:Edetic Acid; D002118:Calcium