Thermosensitive gel containing cellulose acetate phthalate-efavirenz combination nanoparticles for prevention of HIV-1 infection

Abhijit A. Date, Annemarie Shibata, Emily McMullen, Krista La Bruzzo, Patrick Bruck, Michael Belshan, You Zhou, Christopher J. Destache

Research output: Contribution to journalArticle

23 Scopus citations

Abstract

The objective of this investigation was to develop and evaluate a nano-microbicide containing a combination of cellulose acetate phthalate (HIV-1 entry inhibitor) and efavirenz (anti-HIV agent) for HIV prophylaxis. Cellulose acetate phthalateefavirenz combination nanoparticles (CAP-EFV-NPs) were fabricated by the nanoprecipitation method and were characterized for particle size, zeta potential and encapsulation efficiency of efavirenz. CAP-EFV-NPs were incorporated into a thermosensitive gel (CAP-EFV-NP-Gel). CAP-EFV-NPs, CAP-EFV-NP-Gel and efavirenz solution were evaluated for cytotoxicity to HeLa cells and for in vitro short-term (1-day) and long-term (3-day) prophylaxis against HIV-1 infection in TZM-bl cells. CAP-EFV-NPs had size <100 nm, negative surface charge and encapsulation efficiency of efavirenz was >98%. CAP-EFV-NPs and CAP-EFV-NP-Gel were significantly less toxic (P < 0.01) to HeLa cells as compared to efavirenz solution. CAP-EFV-NPs showed significantly higher prophylactic activity (P <0.01) against HIV-1 infection to TZM-bl cells as compared to efavirenz solution and blank CAP nanoparticles. CAP-EFV-NP-Gel can be a promising nano-microbicide for long-term HIV prophylaxis.

Original languageEnglish (US)
Pages (from-to)416-427
Number of pages12
JournalJournal of Biomedical Nanotechnology
Volume11
Issue number3
DOIs
StatePublished - Mar 1 2015

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Keywords

  • Cellulose acetate phthalate
  • Efavirenz
  • HIV prophylaxis
  • Nanoparticles
  • Pluronic
  • Thermosensitive gel

ASJC Scopus subject areas

  • Bioengineering
  • Medicine (miscellaneous)
  • Biomedical Engineering
  • Materials Science(all)
  • Pharmaceutical Science

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