Coaxially electrospun fiber-based microbicides facilitate broadly tunable release of maraviroc

Citation

Ball, C.; Chou, S. F.; Jiang, Y.; & Woodrow, K. A. (2016). Coaxially electrospun fiber-based microbicides facilitate broadly tunable release of maraviroc. Mater Sci Eng C Mater Biol Appl, 63, 117-124. PMCID: 5283717

Abstract

Electrospun fibers show potential as a topical delivery system for vaginal microbicides. Previous reports have demonstrated delivery of anti-HIV and anti-STI (sexually transmitted infection) agents from fibers formulated using hydrophilic, hydrophobic, or pH-responsive polymers that result in rapid, prolonged, or stimuli-responsive release, respectively. However, coaxial electrospun fibers have yet to be evaluated as a highly tunable microbicide delivery vehicle. In this research, we explored the opportunities and limitations of a model coaxial electrospun fiber system to provide broad and tunable release rates for the HIV entry inhibitor maraviroc. Specifically, we prepared ethyl cellulose (EC)-shell and polyvinylpyrrolidone (PVP)-core fibers that were capable of releasing actives over a range of hours to several days. We further demonstrated simple and effective methods for combining core-shell fibers with rapid-release formulations to provide combined instantaneous and sustained maraviroc release. In addition, we investigated the effect of varying release media on maraviroc release from core-shell fibers, and found that release was strongly influenced by media surface tension and drug ionization. Finally, in vitro cell culture studies show that our fiber formulations were not cytotoxic and that electrospun maraviroc maintained similar antiviral activity compared to neat maraviroc.

Keyword(s)

Anti-HIV Agents/chemistry/metabolism/toxicity
Anti-Infective Agents/*chemistry/metabolism/toxicity
Cell Line
Cell Survival/drug effects
Cellulose/analogs & derivatives/chemistry
Cyclohexanes/*chemistry/metabolism/toxicity
Drug Carriers/*chemistry
Drug Liberation
Humans
Hydrogen-Ion Concentration
Hydrophobic and Hydrophilic Interactions
Microscopy, Electron, Scanning
Photoelectron Spectroscopy
Povidone/chemistry
Surface Properties
Triazoles/*chemistry/metabolism/toxicity

Notes

Ball, Cameron
Chou, Shih-Feng
Jiang, Yonghou
Woodrow, Kim A
R21 AI098648/AI/NIAID NIH HHS/
P41 EB-002027/EB/NIBIB NIH HHS/
AI112002/AI/NIAID NIH HHS/
A1098648/PHS HHS/
P41 EB002027/EB/NIBIB NIH HHS/
R01 AI112002/AI/NIAID NIH HHS/
Netherlands
Mater Sci Eng C Mater Biol Appl. 2016 Jun;63:117-24. doi: 10.1016/j.msec.2016.02.018. Epub 2016 Feb 4.

Reference Type

Journal Article

Secondary Title

Mater Sci Eng C Mater Biol Appl

Author(s)

Ball, C.
Chou, S. F.
Jiang, Y.
Woodrow, K. A.

Year Published

2016

Date Published

1464739200

Volume Number

Pages

117-124

ISSN/ISBN

1873-0191 (Electronic)
0928-4931 (Linking)

DOI

10.1016/j.msec.2016.02.018

PMCID

5283717