Sustained release micellar carrier systems for iontophoretic transport of dexamethasone across human sclera

JOURNAL OF CONTROLLED RELEASE

卷:160

Article

Chopra, Poonam¹  Hao, Jinsong¹  Li, S. Kevin¹ 

[1] Univ Cincinnati, Div Pharmaceut Sci, James L Winkle Coll Pharm, Cincinnati, OH 45267 USA

关键词: Human sclera;    Dexamethasone;    Mixed micelles;    Simple micelles;    Transscleral iontophoresis;    Sustained release;   

DOI  :  10.1016/j.jconrel.2012.01.032

来源: Elsevier

【 摘 要 】

A challenge in ocular drug delivery is to maintain the therapeutic concentration of a drug at the site of action in the eye. The objective of the present study was to investigate the feasibility of micellar carrier systems for sustained drug delivery in transscleral iontophoresis in vitro. Simple and mixed micelles prepared using sodium taurocholate (TA) alone or with egg lecithin (LE) were the carrier systems studied. Dexamethasone (DEX), a poorly water soluble corticosteroid, was the model drug. The micellar carrier systems were first characterized for their solubilization and encapsulation of the drug. Passive and 2-mA iontophoretic (both cathodal and anodal) transport experiments were conducted using these micellar carrier systems in side-by-side diffusion cells with excised human sclera in vitro. Drug release studies were performed after the transport experiments. Saturated DEX solution without the micellar carriers was used as a control. It was found that the solubilization capacity of the micellar carrier systems increased as the total lipid concentration of the systems increased. Drug release from the sclera was significantly prolonged with the micellar carrier systems as compared to the control after passive and iontophoretic delivery. Less than similar to 20% of DEX was released from the sclera in approximately 2 h after cathodal iontophoretic delivery of the micellar carrier systems, whereas more than similar to 50% of DEX was released from the control in the same time period under the same condition. Micellar carrier systems can be a suitable transscleral drug delivery system for poorly water soluble drugs by enhancing their aqueous solubilities and providing sustained drug delivery. These micellar carrier systems can be efficiently delivered into and across the sclera by iontophoresis for drug delivery. (C) 2012 Elsevier B. V. All rights reserved.

【 授权许可】

Free