Development and characterization of bioadhesive vaginal films of sodium polystyrene sulfonate (PSS), a novel contraceptive antimicrobial agent.
OBJECTIVE
Polystyrene sulfonate (PSS) is a novel noncytotoxic antimicrobial contraceptive agent. A gel formulation of PSS was found safe for vaginal administration in phase I clinical trials. The purpose of the current study was to develop and evaluate novel bioadhesive vaginal film formulations of PSS.


METHODS
PSS films were prepared by solvent evaporation and optimized for various physical, mechanical, and aesthetic properties. Further, films were evaluated for various biological activities and safety.


RESULTS
Vaginal films containing 300 mg PSS per unit have been developed, using generally regarded as safe (GRAS) listed excipients. The films are colorless, transparent, thin, soft, and tough, dissolve rapidly in physiologic fluid to form a smooth, viscous and bioadhesive solution that could be retained in the vagina for prolonged intervals. Sperm function inhibition (hyaluronidase and cervical mucus penetration) and antimicrobial activities against human immunodeficiency virus (HIV) and herpes simplex virus (HSV) by PSS films were found comparable to PSS. Also, films did not inhibit normal vaginal microflora (Lactobacillus) and were noncytotoxic as indicated by negligible sperm immobilization and cytotoxicity to host cell assays.


CONCLUSIONS
Rapidly dissolving bioadhesive vaginal film formulation of PSS with desired physical, mechanical, aesthetic, and biological properties is a suitable candidate vaginal microbicide for prevention of sexually transmitted disease (STDs) and is ready for toxicological and clinical evaluation.
Garg
Sanjay
S
Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, SAS Nagar, Punjab 160062, India. s.sarg@auckland.ac.nz
Vermani
Kavita
K
Garg
Alka
A
Anderson
Robert A
RA
Rencher
William B
WB
Zaneveld
Lourens J D
LJ
D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage* / Q000494:pharmacology; D002460:Cell Line; D002582:Cervix Mucus / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D003270:Contraceptive Agents / Q000008:administration & dosage / Q000494:pharmacology; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry; D015497:HIV-1 / Q000187:drug effects* / Q000472:pathogenicity; D018258:Herpesvirus 2, Human / Q000187:drug effects* / Q000472:pathogenicity; D006801:Humans; D006821:Hyaluronoglucosaminidase / Q000037:antagonists & inhibitors; D020100:Hydrogels / Q000737:chemistry; D066298:In Vitro Techniques; D010968:Plasticizers / Q000737:chemistry; D011137:Polystyrenes / Q000008:administration & dosage* / Q000494:pharmacology; D011142:Polyvinyl Alcohol; D013012:Sorbitol; D013081:Sperm Motility / Q000187:drug effects; D014622:Vaginal Creams, Foams, and Jellies / Q000737:chemistry
D000890:Anti-Infective Agents; D003270:Contraceptive Agents; D005079:Excipients; D020100:Hydrogels; D010968:Plasticizers; D011137:Polystyrenes; D014622:Vaginal Creams, Foams, and Jellies; C062364:polyvinyl alcohol hydrogel; D013012:Sorbitol; C003321:polystyrene sulfonic acid; D011142:Polyvinyl Alcohol; D006821:Hyaluronoglucosaminidase