NDLI: Preformulation and Vaginal Film Formulation Development of Microbicide Drug Candidate CSIC for HIV Prevention

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Preformulation and Vaginal Film Formulation Development of Microbicide Drug Candidate CSIC for HIV Prevention

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Journal of Pharmaceutical Innovation : Volume 12, Issue 1, March 2017

Journal of Pharmaceutical Innovation : Volume 11

Journal of Pharmaceutical Innovation : Volume 10

Journal of Pharmaceutical Innovation : Volume 9

Journal of Pharmaceutical Innovation : Volume 8

Journal of Pharmaceutical Innovation : Volume 7

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Journal of Pharmaceutical Innovation : Volume 3

Journal of Pharmaceutical Innovation : Volume 2

Journal of Pharmaceutical Innovation : Volume 1

Preformulation and Vaginal Film Formulation Development of Microbicide Drug Candidate CSIC for HIV Prevention

Content Provider	Springer Nature Link
Author	Gong, Tiantian Zhang, Wei Parniak, Michael A. Graebing, Phillip W. Moncla, Bernard Gupta, Phalguni Empey, Kerry M. Rohan, Lisa C.
Copyright Year	2017
Abstract	5-Chloro-3-[phenylsulfonyl] indole-2-carboxamide (CSIC) is a highly potent non-nucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 which has been shown to have a more desirable resistance profile than other NNRTIs in the development as HIV prevention strategies. This work involves generation of preformulation data for CSIC and systematic development of a cosolvent system to effectively solubilize this hydrophobic drug candidate. This system was then applied to produce a polymeric thin film solid dosage form for vaginal administration of CSIC for use in prevention of sexual acquisition of HIV.Extensive preformulation, formulation development, and film characterization studies were conducted. An HPLC method was developed for CSIC quantification. Preformulation tests included solubility, crystal properties, stability, and drug-excipient compatibility. Cytotoxicity was evaluated using both human epithelial and mouse macrophage cell lines. Ternary phase diagram methodology was used to identify a cosolvent system for CSIC solubility enhancement. Following preformulation evaluation, a CSIC film formulation was developed and manufactured using solvent casting technique. The developed film product was assessed for physicochemical properties, anti-HIV bioactivity, and Lactobacillus biocompatibility during 12-month stability testing period.Preformulation studies showed CSIC to be very stable. Due to its hydrophobicity, a cosolvent system consisting of polyethylene glycol 400, propylene glycol, and glycerin (5:2:1, w/w/w) was developed, which provided a uniform dispersion of CSIC in the film formulation. The final film product met target specifications established for vaginal microbicide application.The hydrophobic drug candidate CSIC was successfully formulated with high loading capacity in a vaginal film by means of a cosolvent system. The developed cosolvent strategy is applicable for incorporation of other hydrophobic drug candidates in the film platform.
Starting Page	142
Ending Page	154
Page Count	13
File Format	PDF
ISSN	18725120
Journal	Journal of Pharmaceutical Innovation
Volume Number	12
Issue Number	2
e-ISSN	19398042
Language	English
Publisher	Springer US
Publisher Date	2017-03-03
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Microbicide Ternary phase diagram Drug-excipient compatibility Solvent cast Vaginal drug delivery Pharmacology/Toxicology Industrial and Production Engineering Biotechnology Biochemical Engineering
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Pharmaceutical Science

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