Thermosensitive vaginal gel containing PLGA-NRTI conjugated nanoparticles for HIV prophylaxis

Andrzej Rajca, Qingsheng Li, Abhijit Date, Michael Belshan, Chris Destache

Research output: Chapter in Book/Report/Conference proceedingConference contribution

2 Scopus citations

Abstract

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.

Original languageEnglish (US)
Title of host publicationTechnical Proceedings of the 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013
Pages293-296
Number of pages4
StatePublished - 2013
EventNanotechnology 2013: Bio Sensors, Instruments, Medical, Environment and Energy - 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013 - Washington, DC, United States
Duration: May 12 2013May 16 2013

Publication series

NameTechnical Proceedings of the 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013
Volume3

Conference

ConferenceNanotechnology 2013: Bio Sensors, Instruments, Medical, Environment and Energy - 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013
CountryUnited States
CityWashington, DC
Period5/12/135/16/13

Keywords

  • Conjugated NRTIs
  • HIV
  • Nanoparticles
  • Pre-exposure prophylaxis
  • Sustained vaginal delivery

ASJC Scopus subject areas

  • Biotechnology

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  • Cite this

    Rajca, A., Li, Q., Date, A., Belshan, M., & Destache, C. (2013). Thermosensitive vaginal gel containing PLGA-NRTI conjugated nanoparticles for HIV prophylaxis. In Technical Proceedings of the 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013 (pp. 293-296). (Technical Proceedings of the 2013 NSTI Nanotechnology Conference and Expo, NSTI-Nanotech 2013; Vol. 3).