College of Pharmacy Faculty Research ​and Publications

Document Type

Article

Publication Title

Acta Scientific Pharmaceutical Sciences

Publication Date

2-2023

Volume

7

Issue

2

First Page

23

Last Page

36

Abstract

Purpose: Topical Microbicides have been used as vaginal microbicides in clinical trials as anti-HIV-1 products. The objectives of this project were to evaluate selected popular topical microbicide drug products for their acute toxicities to colorectal epithelial cells and primary immune cells such as Peripheral Blood Mononuclear Cells (PBMC) and Macrophages and to further determine if these microbicide products could induce genital tract inflammation via extra production of pro-inflammatory cytokines such as TNF-α, IL-1β, IL-6 and IL-8.

Methodology: Toxicities of Nonoxynol-9, KY jelly, CAP, PRO2000 (4%), PRO2000 (0.5%), UC781(1%), UC781(0.1%) and VenaGelTM microbicides were determined by cellular viability of colorectal adenocarcinoma cells (CaCo2 ), the model vaginal epithelial cell and the vaginal tract primary immune cells of peripheral blood mononuclear cells (PBMCs) and Macrophages by culturing them for 24-hours in the presence of serial dilutions of products or placebo. Products and placebo dilutions that gave culture viabilities of ≥60% compared to control cultures were considered as nontoxic

Results: The results indicated safety and low toxicity of these microbicides in terms of cytokine release. Furthermore, it showed that usage of these microbicides as anti-HIV formulation will not trigger cytokine release. However, IL-8 has shown relatively higher levels for all microbicides tested in toxic and nontoxic formulation. This indicated that microbicides induced the release of IL-8 and could trigger the recruitment of HIV-1 susceptible cells and increase HIV-1 replication.

Creative Commons Usage License

All Rights Reserved

Copyright held by

author

Download

Share

COinS