Thermosensitive and mucoadhesive pluronic-hydroxypropylmethylcellulose hydrogel containing the mini-CD4 M48U1 is a promising efficient barrier against HIV diffusion through macaque cervicovaginal mucus.
Antimicrob Agents Chemother
; 59(4): 2215-22, 2015 Apr.
Article
em En
| MEDLINE
| ID: mdl-25645853
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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Polietilenoglicóis
/
Propilenoglicóis
/
Antígenos CD4
/
Muco do Colo Uterino
/
HIV-1
/
Fármacos Anti-HIV
/
Poloxâmero
/
Hidrogéis
/
Inibidores da Fusão de HIV
/
Derivados da Hipromelose
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Revista:
Antimicrob Agents Chemother
Ano de publicação:
2015
Tipo de documento:
Article
País de afiliação:
França