TRANSPORT AND ACTIVITY OF MICROBICIDES FORMULATIONS

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The broad long-term goals of this project are to better understand the kinetics of transport of active and excipient microbicide agents through vaginal/cervical tissue, to evaluate the effects of excipients on components of the genital tract as well as STD pathogens including HIV, and to incorporate knowledge of these factors into formulation strategies for octyl glycerol with or without peptides. Remedies have been developed which show promise as active agents against STDs as microbicides. However, very little basic information has been generated regarding the transport kinetics in vaginal and cervical tissues for active and excipient agents which may be used in topical microbicide formulations. Therefore, the specific aims of this project are to: 1) define the transport kinetics of hydrophilic and lipophilic low molecular weight compounds through vaginal and cervical tissue using a Franz cell diffusion model, 2) assess the impact of formulation excipients on transport of active microbicide agents through vaginal and cervical tissue, 3) evaluate the in vitro activity of formulation components on Neisseria gonorrhoeae, Chlamydia trachomatis, Lactobacillus crispatus, Trichomonas vaginalis and other competents of the genital tract in collaboration with the Cores 4) develop a formulation for octyl glycerol in collaboration with Dr. Isaacs as proposed in the second Project, 5) assess the physical and chemical properties of the developed octyl glycerol formulation using traditional pharmaceutical dosage form evaluation techniques and 6) evaluate the effectiveness of individual formulation components and formulated products against HIV in a tissue model system in collaboration with the third project and against Chlamydia trachomatis in the pig-tailed macaque in collaboration with the first Project.