title: Thermosensitive Gel Containing Cellulose Acetate Phthalate-Efavirenz Combination Nanoparticles for Prevention of HIV-1 Infection.
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 phthalate-efavirenz 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.
authors: Abhijit A
authors: AA
authors: Date
authors: Annemaria
authors: A
authors: Shibata
authors: Emily
authors: E
authors: McMullen
authors: Krista
authors: K
authors: La Bruzzo
authors: Patrick
authors: P
authors: Bruck
authors: Michael
authors: M
authors: Belshan
authors: You
authors: Y
authors: Zhou
authors: Christopher J
authors: CJ
authors: Destache
mesh_terms: D000480:Alkynes; D000998:Antiviral Agents / Q000008:administration & dosage / Q000737:chemistry; D048588:Benzoxazines / Q000008:administration & dosage* / Q000737:chemistry; D049109:Cell Proliferation / Q000187:drug effects; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D003521:Cyclopropanes; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000138:chemical synthesis*; D004058:Diffusion; D005782:Gels / Q000737:chemistry; D015658:HIV Infections / Q000517:prevention & control*; D015497:HIV-1 / Q000187:drug effects* / Q000502:physiology; D006367:HeLa Cells; D006801:Humans; D053769:Nanocapsules / Q000008:administration & dosage / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D013696:Temperature
chemical_list: D000480:Alkynes; D000998:Antiviral Agents; D048588:Benzoxazines; D003521:Cyclopropanes; D003692:Delayed-Action Preparations; D005782:Gels; D053769:Nanocapsules; D002482:Cellulose; C011708:cellulose acetate phthalate; C098320:efavirenz