TY - GEN
T1 - Thermosensitive vaginal gel containing PLGA-NRTI conjugated nanoparticles for HIV prophylaxis
AU - Rajca, Andrzej
AU - Li, Qingsheng
AU - Date, Abhijit
AU - Belshan, Michael
AU - Destache, Chris
PY - 2013/8/9
Y1 - 2013/8/9
N2 - Nucleoside reverse transcriptase inhibitors (NRTIs) have shown efficacy as pre-exposure prophylaxis (PrEP). The research goal is conjugating NRTIs to biodegradable polymer poly (lactic-co-glycolic acid; PLGA) by an amide bond. NRTIs-PLGA conjugates were chemically activated and conjugated to free amine group of emtricitabine (FTC) and lamivudine (3TC). The conjugates were made into nanoparticles (NPs) and incorporated into a thermosensitive gel for vaginal PrEP. PLGA-FTC and PLGA-3TC NPs were <200nm and zeta potential of-13.7 and -14.1 mV, respectively. The conjugated NPs were not toxic to HeLa cells up to 100 mcg/ml. Thermosensitive gel containing fluorescent NPs fabricated similarly and administered vaginally, were seen in submucosa for up to 5 days. FTC-NPs showed similar EC50 compared to FTC solution. This thermosensitive gel would be a novel vaginal sustained-release PrEP option.
AB - Nucleoside reverse transcriptase inhibitors (NRTIs) have shown efficacy as pre-exposure prophylaxis (PrEP). The research goal is conjugating NRTIs to biodegradable polymer poly (lactic-co-glycolic acid; PLGA) by an amide bond. NRTIs-PLGA conjugates were chemically activated and conjugated to free amine group of emtricitabine (FTC) and lamivudine (3TC). The conjugates were made into nanoparticles (NPs) and incorporated into a thermosensitive gel for vaginal PrEP. PLGA-FTC and PLGA-3TC NPs were <200nm and zeta potential of-13.7 and -14.1 mV, respectively. The conjugated NPs were not toxic to HeLa cells up to 100 mcg/ml. Thermosensitive gel containing fluorescent NPs fabricated similarly and administered vaginally, were seen in submucosa for up to 5 days. FTC-NPs showed similar EC50 compared to FTC solution. This thermosensitive gel would be a novel vaginal sustained-release PrEP option.
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M3 - Conference contribution
AN - SCOPUS:84881112694
SN - 9781482205862
T3 - Technical Proceedings of the 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013
SP - 293
EP - 296
BT - Technical Proceedings of the 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013
T2 - Nanotechnology 2013: Bio Sensors, Instruments, Medical, Environment and Energy - 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013
Y2 - 12 May 2013 through 16 May 2013
ER -