淀粉基荧光微球的制备及其布洛芬包载和释药性能

Preparation and Drug-release Properties of Ibuprofen-loaded and Fluorescein-labeled Starch-based Nanospheres

以淀粉为原料,用乙酸酐酰化后,将异硫氰酸荧光素(FITC)接枝到淀粉醋酸酯大分子链上,以自组装的方法制备出包载布洛芬的淀粉基荧光微球,同时考察了淀粉基荧光纳米微球对布洛芬的控制释放性能。荧光淀粉酯的用量、布洛芬的加入量及丙酮与水的体积比可影响载药微球的包封率和药物释放速度。研究结果表明,当荧光淀粉酯用量为200 mg、布洛芬的量为60 mg、水和丙酮体积分别为50和20 mL时所合成的载药微球包封率最高,为69.5%,其药物体外释放也最快,48 h可释放62.7%。用扫描电子显微镜和激光共聚焦显微镜(CLSM)对包药微球的体外释放过程进行了表征。

Starch was firstly acylated by acetic anhydride,fluorescein isothiocyanate（FITC） was then covalently attached onto the starch acetate.And the fluorescein-labeled starch acetate could self-assemble to form uniform nanospheres encapsulated with ibuprofen.The controlled-release properties of obtained ibuprofen-loaded fluorescein-labeled starch nanospheres were investigated in details.The amounts of drug-loading and release rate could be tuned by changing the amounts of fluorescein-labeled starch acetate,ibuprofen and volume ratio of acetone to water.The results showed that up to 69.5% of the drug could be encapsulated when the amounts of fluorescein-labeled starch acetate and ibuprofen were 200 mg and 60 mg,and the volumes of water and acetone were 50 mL and 20 mL,respectively.The drug release rate in vitro of these nanospheres was 62.7% at 48 h.Moreover,the release process in vitro of the drug-loaded nanospheres was characterized by scanning electron microscope（SEM） and confocal laser scanning microscope（CLSM）.