Thermosensitive Gel Containing Cellulose Acetate Phthalate-Efavirenz Combination Nanoparticles for Prevention of HIV-1 Infection

被引：31

作者：

Date, Abhijit A. ^{[1
]}

Shibata, Annemarie ^{[2
]}

McMullen, Emily ^{[2
]}

La Bruzzo, Krista ^{[2
]}

Bruck, Patrick ^{[2
]}

Belshan, Michael ^{[3
]}

Zhou, You ^{[4
]}

Destache, Christopher J. ^{[1
]}

机构：

[1] Creighton Univ, Sch Pharm & Hlth Profess, Omaha, NE 68178 USA

[2] Creighton Univ, Dept Biol, Omaha, NE 68178 USA

[3] Creighton Univ, Dept Med Microbiol & Immunol, Sch Med, Omaha, NE 68178 USA

[4] Univ Nebraska, Ctr Biotechnol, Lincoln, NE 68588 USA

来源：

JOURNAL OF BIOMEDICAL NANOTECHNOLOGY | 2015年 / 11卷 / 03期

关键词：

Cellulose Acetate Phthalate; Nanoparticles; Efavirenz; HIV Prophylaxis; Pluronic; Thermosensitive Gel; HUMAN-IMMUNODEFICIENCY-VIRUS; PRECLINICAL INTERVENTIONS; CANDIDATE MICROBICIDES; ANTI-HIV-1; ACTIVITY; PROPHYLAXIS; EXPOSURES; STRATEGY;

D O I：

10.1166/jbn.2015.1942

中图分类号：

TB3 [工程材料学];

学科分类号：

0805 ; 080502 ;

摘要：

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.

引用

页码：416 / 427

页数：12

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