Coprecipitation of nonoxynol-9 with polyvinylpyrrolidone to decrease vaginal irritation potential while maintaining spermicidal potency.
The aim of this study was to test the hypothesis that polyvinylpyrrolidone (PVP) would increase the critical micelle concentration (CMC) of nonoxynol-9 (N-9), providing a reduction in its irritation potential, while maintaining essential spermicidal activity. Solid coprecipitates of N-9 with PVP were manufactured with the use of a modified lyophilization process. The irritation potential of N-9 was estimated by an in vitro assay, monitoring the extent of hemolysis of red blood cells. CMCs of N-9 were measured in the presence of various concentrations of PVP. A modified Sander-Cramer assay was implemented to measure the spermicidal activity of N-9 and the N-9/PVP coprecipitates. With the use of the lyophilization process and more suitable solvents, solid coprecipitates of N-9/PVP were manufactured with no residual organic solvents. The irritation potential of N-9 was reduced when in the presence of PVP-50% hemolysis values increased from 0.054 mM to more than 0.2mM. N-9 CMC values increased in the presence of PVP from 0.085 mM (0% PVP) to 0.110 mM (3.5% PVP) and 0.16 6mM (10% PVP). However, spermicidal activities ranged from 0.213 mM to 0.238 mM, N-9 remaining steady regardless of the amount of PVP. By use of N-9/PVP coprecipitates, the self-association properties and irritation potentials of N-9 were altered. This result suggests a process to produce a spermicidal product that reduces the detrimental implications to the vaginal epithelium while maintaining the essential spermicidal activity.
Fowler
Philip T
PT
Division of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, KY, USA.
Doncel
Gustavo F
GF
Bummer
Paul M
PM
Digenis
George A
GA
D000818:Animals; D001681:Biological Assay; D011232:Chemical Precipitation; D004285:Dogs; D004912:Erythrocytes / Q000187:drug effects; D005260:Female; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D007509:Irritants / Q000008:administration & dosage / Q000009:adverse effects / Q000037:antagonists & inhibitors; D008297:Male; D008823:Micelles; D017137:Nonoxynol / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry*; D010592:Pharmaceutic Aids / Q000737:chemistry / Q000627:therapeutic use; D011205:Povidone / Q000737:chemistry* / Q000627:therapeutic use; D013089:Spermatocidal Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000737:chemistry; D013094:Spermatozoa / Q000378:metabolism; D014627:Vaginitis / Q000209:etiology / Q000517:prevention & control
D007509:Irritants; D008823:Micelles; D010592:Pharmaceutic Aids; D013089:Spermatocidal Agents; D017137:Nonoxynol; D011205:Povidone