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

doi:10.1166/jbn.2015.1942

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

Veterinary and Biomedical Sciences

Research output: Contribution to journal › Article › peer-review

36 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 language	English (US)
Pages (from-to)	416-427
Number of pages	12
Journal	Journal of Biomedical Nanotechnology
Volume	11
Issue number	3
DOIs	https://doi.org/10.1166/jbn.2015.1942
State	Published - Mar 1 2015

Keywords

Cellulose acetate phthalate
Efavirenz
HIV prophylaxis
Nanoparticles
Pluronic
Thermosensitive gel

ASJC Scopus subject areas

General Medicine

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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 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.",

keywords = "Cellulose acetate phthalate, Efavirenz, HIV prophylaxis, Nanoparticles, Pluronic, Thermosensitive gel",

author = "Date, {Abhijit A.} and Annemarie Shibata and Emily McMullen and {La Bruzzo}, Krista and Patrick Bruck and Michael Belshan and You Zhou and Destache, {Christopher J.}",

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doi = "10.1166/jbn.2015.1942",

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T1 - Thermosensitive gel containing cellulose acetate phthalate-efavirenz combination nanoparticles for prevention of HIV-1 infection

AU - Date, Abhijit A.

AU - Shibata, Annemarie

AU - McMullen, Emily

AU - La Bruzzo, Krista

AU - Bruck, Patrick

AU - Belshan, Michael

AU - Zhou, You

AU - Destache, Christopher J.

PY - 2015/3/1

Y1 - 2015/3/1

N2 - 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.

AB - 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.

KW - Cellulose acetate phthalate

KW - Efavirenz

KW - HIV prophylaxis

KW - Nanoparticles

KW - Pluronic

KW - Thermosensitive gel

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ER -

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

Abstract

Keywords

ASJC Scopus subject areas

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