PMID- 17154368 OWN - NLM STAT- MEDLINE DCOM- 20070501 LR - 20101118 IS - 0022-3549 (Print) IS - 0022-3549 (Linking) VI - 96 IP - 3 DP - 2007 Mar TI - Temperature and pH sensitive hydrogels: an approach towards smart semen-triggered vaginal microbicidal vehicles. PG - 670-81 AB - Microbicides are drug delivery systems (DDSs) for the prevention of sexual transmission of HIV and other STDs. A topically applied vaginal microbicidal gel should provide uniform coating of vaginal tissue, retention of this gel layer prior to intercourse, and controlled release kinetics of antivirals to inactivate the viral load potentially introduced during sexual activity. Here, we describe the microbicide-oriented characterization of a DDS made with a dual pH sensitive and thermosensitive smart polymer gel composed of a random terpolymer of N-isopropyl acrylamide, butyl methacrylate, and acrylic acid. The system was engineered to coat vaginal tissue with a stable gel layer and to release entrapped model agents in a burst release profile in response to the presence of the infecting agent: semen. The gel rheology, layer erosion properties, model drug release kinetics, and cytocompatibility of the terpolymer system were studied. Negligible erosion of the gel in the presence of vaginal fluid simulant suggests prolonged retention. Burst release of molecular and macromolecular model compounds was observed when the system's pH changed from the vaginal pH to the pH of semen, and cytotoxicity studies showed that the terpolymer is equally cytocompatible as a commonly used polymeric vaginal carrier. CI - 2006 Wiley-Liss, Inc. and the American Pharmacists Association FAU - Gupta, Kavita M AU - Gupta KM AD - Department of Bioengineering, University of Utah, Biopolymers Research Building, 20 S. 2030 E. Salt Lake City, Utah 84112, USA. FAU - Barnes, Scott R AU - Barnes SR FAU - Tangaro, Rachel A AU - Tangaro RA FAU - Roberts, Meredith C AU - Roberts MC FAU - Owen, Derek H AU - Owen DH FAU - Katz, David F AU - Katz DF FAU - Kiser, Patrick F AU - Kiser PF LA - eng GR - R01-AI48103/AI/NIAID NIH HHS/United States GR - R21-AI062445/AI/NIAID NIH HHS/United States PT - Journal Article PT - Research Support, N.I.H., Extramural PL - United States TA - J Pharm Sci JT - Journal of pharmaceutical sciences JID - 2985195R RN - 0 (Anti-Infective Agents, Local) RN - 0 (Hydrogels) RN - 0 (Pharmaceutical Vehicles) SB - IM EIN - J Pharm Sci. 2009 Mar;98(3):1198 MH - Administration, Intravaginal MH - Anti-Infective Agents, Local/*administration & dosage/chemistry/pharmacology MH - Chemistry, Pharmaceutical MH - *Drug Delivery Systems MH - Female MH - HIV Infections/*prevention & control/transmission MH - Humans MH - Hydrogels MH - Hydrogen-Ion Concentration MH - Male MH - Pharmaceutical Vehicles MH - Semen/*metabolism MH - Solubility MH - Temperature MH - Vagina/*metabolism MH - Viscosity EDAT- 2006/12/13 09:00 MHDA- 2007/05/02 09:00 CRDT- 2006/12/13 09:00 PHST- 2006/12/13 09:00 [pubmed] PHST- 2007/05/02 09:00 [medline] PHST- 2006/12/13 09:00 [entrez] AID - S0022-3549(16)32201-8 [pii] AID - 10.1002/jps.20752 [doi] PST - ppublish SO - J Pharm Sci. 2007 Mar;96(3):670-81. doi: 10.1002/jps.20752.