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 fluorescent-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 slowed-down by pluronic® hydrogels in comparison with Cynomolgus macaque cervico-vaginal mucus and hydroxyethylcellulose hydrogel (HEC 1.5 wt%) used as negative controls. Formulation of the peptide mini CD4 M48U1 used as 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 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%) can be used to create efficient barrier against particle diffusion in comparison to conventional HEC hydrogels.
Thermosensitive and mucoadhesive pluronic®/hydroxypropylmethylcellulose hydrogel containing the mini CD4 M48U1 is a promising efficient barrier against HIV diffusion through macaque cervico-vaginal mucus
GIBELLINI, Davide;
2015-01-01
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 fluorescent-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 slowed-down by pluronic® hydrogels in comparison with Cynomolgus macaque cervico-vaginal mucus and hydroxyethylcellulose hydrogel (HEC 1.5 wt%) used as negative controls. Formulation of the peptide mini CD4 M48U1 used as 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 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%) can be used to create efficient barrier against particle diffusion in comparison to conventional HEC hydrogels.
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