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KMID : 0369820140440050329
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Jorunal of Korean Pharmaceutical Sciences
2014 Volume.44 No. 5 p.329 ~ p.337
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Effects of surfactant type and cholesterol level on niosomes physical properties and in vivo ocular performance using timolol maleate as a model drug
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Abdelkader Hamdy
Farghaly Usama
Moharram Hossam
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Abstract
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This study aimed at investigating the roles of both Span® surfactant type (having a gel/liquid transition temperature range from <10 to 55 °C), and cholesterol level on in vitro characteristics and in vivo performance of timolol maleate niosomes. Span 20, Span 40 and Span 60 niosomes were prepared using the thin film hydration method. Span:cholesterol levels employed were 7:3 mol/mol (a minimum concentration for stable niosomes) and 1:1 mol/mol (a maximum concentration accommodated by niosomes). Niosomes were characterized for size, percentage entrapment efficiency, morphology, in vitro release and intra-ocular pressure (IOP) lowering activity in rabbits. The order of the area under IOP-time curve (AUC) was ranked as follows: Span 40 > Span 20 > Span 60. The AUC and IOPmax values for Span 40:cholesterol (7:3) niosomes were superior due to having a good compromise between thermo-responsiveness and efficient capacity for loading a significant drug cargo, compared with Span 20 and Span 60.
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KEYWORD
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Niosomes, Intraocular pressure, Timolol maleate, Ocular delivery, Span® surfactants
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