An Evaluation of Polycaprolactone Matrices for Vaginal Delivery of the Antiviral, Tenofovir, in Preventing Heterosexual Transmission of HIV

Investigation of Polycaprolactone Matrices for Intravaginal Delivery of Doxycycline

“…PCL is synthetic polyester that has been studied extensively for controlled drug delivery and tissue engineering applications in a wide variety of forms including films, fibers, microparticles, and nanoparticles . Microporous matrices of PCL have been investigated previously for vaginal delivery of the antivirals nevirapine and tenofovir, the antibacterial gentamicin and metronidazole (MTZ), and the antifungal miconazole, for prevention and treatment of STIs. The aim of this study was to explore the potential of PCL matrices for vaginal delivery of doxycycline through investigations of the preparation, morphology, thermal and compressive properties, and in vitro drug release of doxycycline from PCL matrices.…”

Evaluation of Polycaprolactone Matrices for Sustained Vaginal Delivery of Nevirapine in the Prevention of Heterosexual HIV Transmission

“…Anti‐HIV activity of NVP released from PCL matrices were assayed using luciferase‐expressing, VSV‐G pseudo‐typed HIV‐1 as previously described . Briefly, HeLa cells (ATCC number CCL‐2) were cultured in RPMI 1640 (Invitrogen Corporation, Melbourne, Australia) supplemented with 10% fetal bovine serum (Life Technologies Australia Pty Ltd., Victoria, Australia), 100 mg/mL streptomycin and 100 U/mL penicillin at 37°C and 5% CO 2 .…”

“…Anti-HIV activity of NVP released from PCL matrices were assayed using luciferase-expressing, VSV-G pseudo-typed HIV-1 as previously described. 14 Briefly, HeLa cells (ATCC number CCL-2) were cultured in RPMI 1640 (Invitrogen Corporation, Melbourne, Australia) supplemented with 10% fetal bovine serum (Life Technologies Australia Pty Ltd., Victoria, Australia), 100 mg/mL streptomycin and 100 U/mL penicillin at 37 • C and 5% CO 2 . HeLa cells (10 5 cells/mL) were seeded in 24well plates to achieve confluence above 80% after 24 h. Aliquots (100 :L) of the SVF release medium collected at day 1, 7, 14 and 23 which had contained drug-free matrices or NVP-loaded matrices were filtered through a 0.22-:m membrane and fivefold dilutions were added to each well.…”

“…We have previously shown the potential utility of micro‐porous polycaprolactone (PCL) matrices for vaginal delivery of hydrophilic antibacterial (ciprofloxacin) and hydrophobic anti‐fungal agents (miconazole) in the treatment of gonorrhea and candida . More recently, we incorporated the hydrophilic NRTI, tenofovir, in PCL matrices and achieved gradual release over 30 days in simulated vaginal fluid (SVF) with over 70% retention of anti‐viral activity against pseudo‐typed HIV‐1 viruses . In this study, we describe the development of PCL matrices incorporating a hydrophobic NNRTI, nevirapine (NVP), as part of an on‐going evaluation of the materials for prevention and treatment of sexually transmitted infections.…”

“…13 More recently, we incorporated the hydrophilic NRTI, tenofovir, in PCL matrices and achieved gradual release over 30 days in simulated vaginal fluid (SVF) with over 70% retention of anti-viral activity against pseudo-typed HIV-1 viruses. 14 In this study, we describe the development of PCL matrices incorporating a hydrophobic NNRTI, nevirapine (NVP), as part of an on-going evaluation of the materials for prevention and treatment of sexually transmitted infections. NVP is an attractive option as an anti-retroviral drug because it is inexpensive and is widely used in resource-poor areas for treating both HIV and preventing mother-to-child transmission.…”