透明质酸功能化白蛋白纳米粒的构建及眼刺激性评价  

Preparation and Ocular Irritation Evaluation of Albumin Nanoparticles Functionalized by Hyaluronic Acid

作　　者：任河 李春玲 宋璇 秦迎丹 孙玉琦 REN He;LI Chun-ling;SONG Xuan;QIN Ying-dan;SUN Yu-qi(College of Pharmacy,Jinzhou Medical University,Jinzhou 121001,China)

机构地区：[1]锦州医科大学药学院,辽宁锦州121001

出　　处：《中国药学杂志》2022年第14期1173-1178,共6页Chinese Pharmaceutical Journal

基　　金：辽宁省自然科学基金项目资助(2019-ZD-0825)。

摘　　要：目的制备性质稳定,眼刺激性小的透明质酸功能化白蛋白纳米粒。方法以香豆素6为荧光探针,采用乳化-沉降法制备白蛋白纳米粒,碳二亚胺法将透明质酸偶联到纳米粒表面,荧光胺衍生化法测定氨基的减少量计算取代度,考察纳米粒的制剂学性质和对家兔眼刺激性。结果修饰后透明质酸对白蛋白纳米粒表面氨基的取代度为25.06%,纳米粒呈球形,包封率为86.94%,载药量为2.97%,48 h累计释放率接近70%,Draize实验结果表明功能化纳米粒对家兔眼部无明显刺激。结论该方法成功制得透明质酸功能化的白蛋白纳米粒,所得纳米粒刺激性小,有望作为眼后部给药的药物载体。OBJECTIVE To prepare the hyaluronic acid functionalized albumin nanoparticles with stable properties and low ocular irritation.METHODS Using coumarin 6 as fluorescent probe,the albumin nanoparticles were prepared by emulsification-sedimentation method,and hyaluronic acid was coupled to the surface of the nanoparticles in carbodiimide method.The substitution degree of hyaluronic acid was calculated with the reduction of amino groups which was determined by fluorescamine-derivatization method.The pharmaceutical properties and their ocular irritation to rabbits of nanoparticles were furtherly studied.RESULTS The degree of substitution of hyaluronic acid was 25.06%when functionlized by hyaluronic acid.The nanoparticles were spherical.The encapsulation rate is 86.94%,drug loading is 2.97%,and the cumulative release ratio was close to 70%in 48 h.Draize testing showed that the functionalized nanoparticles have no obvious irritation to rabbit eyes.CONCLUSION The hyaluronic acid functionalized albumin nanoparticles are successfully prepared.The degree of substitution of hyaluronic acid also can be measured.The obtained nanoparticles are less irritation.It is expected to use the nanoparticles as carriers to delivery drug to the back of the ocular.

关 键 词：透明质酸 白蛋白 纳米粒 眼部给药系统 刺激性 取代度 

分 类 号：R944[医药卫生—药剂学]