眼用小檗碱白蛋白纳米粒温敏原位凝胶的制备及性质研究  

Preparation and characterization of thermosensitive in situ gel containing berberine bovine serum albumin nanoparticles for ophthalmic drug delivery

作　　者：娄杰[1] 贾运涛[2] 田睿[3] 周燕萍[1] 谷萌辉[1] 张良珂[1] 

机构地区：[1]重庆医科大学药学院,重庆400016 [2]重庆医科大学附属儿童医院药剂科,重庆400010 [3]重庆医科大学实验教学中心,重庆400016

出　　处：《中草药》2013年第3期277-281,共5页Chinese Traditional and Herbal Drugs

基　　金：重庆市教育委员会科学技术研究项目(KJ110323);重庆市卫生局课题资助项目(2010-2-202);重庆市渝中区科委科技三费资助项目(20100203);重庆医科大学大学生科研与创新实验项目(201244;201229;201217)

摘　　要：目的制备眼用温敏型小檗碱白蛋白纳米粒原位凝胶(Ber-BSA-NPs-Gel),并对其理化性质进行初步研究。方法以泊洛沙姆407(F127)和泊洛沙姆188(F68)为凝胶基质,以凝胶胶凝温度为考察指标对处方进行优化;去溶剂化法制备小檗碱白蛋白纳米粒(Ber-BSA-NPs),冷溶法制备Ber-BSA-NPs-Gel;使用NDJ—1型黏度计测定凝胶黏度;以模拟泪液为释放介质、UV法考察凝胶的体外释放特性。结果经过处方优化,确定原位凝胶基质的处方为26%F127和4%F68,优化处方在30.9℃为自由流动的液体,经泪液稀释后在34.2℃能够发生相变形成凝胶。体外释放结果表明Ber-BSA-NPs-Gel具有较好的缓释作用。结论制备得到的眼用温敏凝胶符合眼部应用要求,具有良好的应用前景。Objective To prepare a thermosensitive in situ gel containing berberine bovine serum albumin nanoparticles （Ber-BSA- NPs-Gel） for ophthalmic drug delivery and preliminarily investigate its physicochemical properties. Methods Poloxamer 407 （F127） and Poloxamer 188 （F68） were used as gel matrix, and gelatinization temperature was applied as a target to optimize the prescription. The Ber-BSA-NPs were prepared by desolvation method, and the in situ gel system of Ber-BSA-NPs-Gel was obtained by cold-dissolving method. NDJ--1 Viscometer was used to determine the viscosity of the system, simulated tear fluid （STF） was applied as release medium, and ultraviolet spectrophotometry was employed as the assay method to inspect its in vitro release characteristics. Results After optimization, the gel prescription was finally confirmed as 26% F127 and 4% F68. The optimized formulation was freely flowing liquid at 30.9 ℃ and converted to a firm gel at 34.2 ℃ after STF diluted. The in vitro study indicated that Ber-BSA-NPs-Gel possessed a superior sustained-release effect. Conclusion The in situ thermosensitve gel system meets the requirements for ophthalmic application and shows the great potential in ocular application.

关 键 词：小檗碱 白蛋白纳米粒 温敏原位凝胶 眼部给药 泊洛沙姆 

分 类 号：R283.6[医药卫生—中药学]