生物利用度
泊洛沙姆407
泊洛沙姆
壳聚糖
化学
色谱法
妥布霉素
药物输送
渗透
药理学
眼药水
毒品携带者
剂型
医学
聚合物
有机化学
生物化学
庆大霉素
抗生素
膜
共聚物
作者
Shagufta Khan,Sonali Warade,Dilesh J. Singhavi
出处
期刊:Journal of Ocular Pharmacology and Therapeutics
[Mary Ann Liebert]
日期:2018-04-01
卷期号:34 (3): 287-297
被引量:19
标识
DOI:10.1089/jop.2017.0079
摘要
Purpose: Conventional topical delivery in hyperacute bacterial conjunctivitis and endophthalmitis is associated with low drug bioavailability due to rapid precorneal clearance. Hence, in the present investigation, an attempt has been made to enhance ocular bioavailability of tobramycin sulfate by formulating drug-loaded microparticles dispersed in thermosensitive in situ gel. Methods: Microparticles prepared by emulsion–ionic gelation technique were characterized for drug loading, entrapment efficiency, particle size, surface morphology, and in vitro drug release. Consequently microparticles (F2 prepared with 1.5%w/v chitosan, 0.2%w/v tripolyphosphate, and drug, 30%w/w of polymer) with high drug loading and encapsulation efficiency were dispersed in thermosensitive in situ gel containing poloxamer 407 and varying percentage of chitosan. In situ gel containing drug-loaded microparticles were evaluated for gelation temperature, rheological behavior, mucoadhesive strength, in vitro drug release, in vitro permeation, ocular irritation, and bioavailability in aqueous humor of rabbits. Results: Formulation containing 17%w/v poloxamer 407 and 0.5%w/v chitosan (P2) gelled at 32°C ± 1.5°C gave pseudoplastic behavior. In vitro permeability of tobramycin from the formulation P2 was found 2-folds greater than eye drops. It also gave significantly higher aqueous humor concentration of tobramycin compared with eye drops with no signs of ocular irritation. Conclusion: Thus, the formulation possesses high potential for treating ocular infections.
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