Abstract |
To be efficient, vaginal microbicide hydrogels should form a barrier against viral infections and prevent virus spreading through mucus. Multiple particle tracking was used to quantify the mobility of 170-nm fluorescently labeled COOH-modified polystyrene particles (COOH-PS) into thermosensitive hydrogels composed of amphiphilic triblock copolymers with block compositions EOn-POm-EOn (where EO refers to ethylene oxide and PO to propylene oxide) containing mucoadhesive hydroxypropylmethylcellulose (HPMC). COOH-PS were used to mimic the size and the surface charge of HIV-1. Analysis of COOH-PS trajectories showed that particle mobility was decreased by Pluronic hydrogels in comparison with cynomolgus macaque cervicovaginal mucus and hydroxyethylcellulose hydrogel (HEC; 1.5% by weight [wt%]) used as negative controls. Formulation of the peptide mini-CD4 M48U1 used as an anti-HIV-1 molecule into a mixture of Pluronic F127 (20 wt%) and HPMC (1 wt%) did not affect its anti-HIV-1 activity in comparison with HEC hydrogel. The 50% inhibitory concentration (IC50) was 0.53 μg/ml (0.17 μM) for M48U1-HEC and 0.58 μg/ml (0.19 μM) for M48U1-F127-HPMC. The present work suggests that hydrogels composed of F127-HPMC (20/1 wt%, respectively) can be used to create an efficient barrier against particle diffusion in comparison to conventional HEC hydrogels.
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Authors | Kawthar Bouchemal, Armelle Aka-Any-Grah, Nathalie Dereuddre-Bosquet, Loïc Martin, Vanessa Lievin-Le-Moal, Roger Le Grand, Valérie Nicolas, Davide Gibellini, David Lembo, Christian Poüs, Armand Koffi, Gilles Ponchel |
Journal | Antimicrobial agents and chemotherapy
(Antimicrob Agents Chemother)
Vol. 59
Issue 4
Pg. 2215-22
(Apr 2015)
ISSN: 1098-6596 [Electronic] United States |
PMID | 25645853
(Publication Type: Journal Article)
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Copyright | Copyright © 2015, American Society for Microbiology. All Rights Reserved. |
Chemical References |
- Anti-HIV Agents
- CD4 Antigens
- Fluorescent Dyes
- HIV Fusion Inhibitors
- Hydrogels
- PEO-PPO-PEO
- Propylene Glycols
- Poloxamer
- Hypromellose Derivatives
- Polyethylene Glycols
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Topics |
- Animals
- Anti-HIV Agents
(chemical synthesis, pharmacology)
- CD4 Antigens
(chemistry, pharmacology)
- Cervix Mucus
(drug effects, virology)
- Diffusion
- Female
- Fluorescent Dyes
- HIV Fusion Inhibitors
(chemical synthesis, pharmacology)
- HIV Infections
(prevention & control, virology)
- HIV-1
(drug effects)
- Humans
- Hydrogels
(chemical synthesis, chemistry, pharmacology)
- Hypromellose Derivatives
(chemical synthesis, chemistry, pharmacology)
- Macaca fascicularis
- Poloxamer
(chemistry, pharmacology)
- Polyethylene Glycols
(chemistry, pharmacology)
- Propylene Glycols
(chemistry, pharmacology)
- Rheology
- Viscosity
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