生物粘附
化学
色谱法
角膜上皮
渗透
生物利用度
剂型
药物输送
微球
角膜
毒品携带者
药理学
眼科
生物化学
医学
化学工程
膜
有机化学
工程类
作者
Libero Italo Giannola,Viviana De,Giulia Giandalia,Maria Gabriella Siragusa,Lorenzo Cordone
出处
期刊:Journal of Ocular Pharmacology and Therapeutics
[Mary Ann Liebert]
日期:2008-03-16
卷期号:24 (2): 186-196
被引量:18
标识
DOI:10.1089/jop.2007.0113
摘要
The model drug norfloxacin (NOR) was encapsulated into trehalose (TRH) and hydroxyethylcellulose (NAT) microspheres to obtain a novel gelling ophthalmic delivery system for prolonged release on corneal tissue.We assessed NOR release from microspheres, prepared by the emulsion-solvent evaporation method. A new in vitro tear turnover model, including inserts containing reconstituted human corneal epithelium (RHC), was designed to evaluate the TRH/NAT microspheres' precorneal retention time. Bioadhesive properties of TRH/NAT microspheres were validated by using drug-loaded microspheres prepared with gelatine (GLT) commonly used as reference material in adhesion studies.In vitro drug release showed a typical trend of swelling systems. Precorneal retention tests showed that TRH/NAT microspheres maintained fluorescence in tear fluid for 81.7 min, whereas TRH/GLT microspheres and water solution maintained fluorescence for 51.8 and 22.3 min, respectively. NOR released from microspheres permeated throughout RHC slower (J(s) = 23.08 microg/cm(2)h) than NOR from commercial eye drops (J(s) = 42.77 microg/cm(2)h) used as the control.Adequate drug concentrations in aqueous humor could be prolonged after the administration of TRH/NAT/NOR microspheres. Good bioadhesive properties of the system and slow drug release on corneal surface might increase ocular NOR bioavailability.
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