苦参碱聚乳酸微球的缓释性和玻璃体腔注射的安全性研究  被引量:14

Sustained release ability and safety of matrine polyactic acid microsphere intravitreal injection

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作  者:刘丹岩[1] 马景学[1] 曹德英[2] 王建欣[2] 刘建宗[1] 吕兰存[1] 

机构地区:[1]河北医科大学第二医院眼科,石家庄050000 [2]河北医科大学药剂学教研室,石家庄050000

出  处:《眼科研究》2010年第1期34-38,共5页Chinese Ophthalmic Research

基  金:河北省自然科学基金资助(303638)

摘  要:目的研究苦参碱聚乳酸微球(MAT-PLA-MS)的缓释性和玻璃体腔注射的安全性。方法透射电镜观察MAT-PLA-MS的形态,紫外分光光度法观测其体外释放情况。玻璃体腔彩色照相记录其分解过程,裂隙灯显微镜、间接检眼镜、视网膜电图(ERG)、光学显微镜和透射电镜观察不同剂量组的苦参碱游离药物和MAT-PLA-MS在注药后不同时间点对眼组织的影响。结果MAT-PLA-MS的平均粒径为2.28μm,载药量为6.17%。体外释放672 h,累积释放百分率为87.93%,缓释作用明显。MAT-PLA-MS在玻璃体腔内随时间延长表现为逐渐降解的过程。游离药物各剂量组和载药微球各剂量组在玻璃体腔注射后各时间点裂隙灯显微镜和间接检眼镜检查均未见异常。游离药物4 mg组注药后1 d ERG b波振幅下降。组织病理学检查表明,游离药物4 mg组在注药后1 d开始出现视网膜毒性反应,载药微球6 mg组在注药7 d后出现轻微的视网膜毒性反应。结论MAT-PLA-MS具有明显的缓释效果,安全剂量较游离药物大,有望成为一种理想的防治增生性玻璃体视网膜病变的给药系统。Background The anti-proliferative effect of matrine has been demonstrated and its relevance to prevention and treatment of proliferative retinovitreopathy is concerned. However,the intravitreous injection of free-matrine reiteratively may raise the risk of ocular infection. Objective The goal of the present study is to investigate the sustained releasing ability and safety of matrine polyactic acid microsphere(MAT-PLA-MS) intravitreal injection. Methods MAT-PLA-MS was prepared by Hebei Medical University and examined under the transmission electron microscope. The release of MAT-PLA-MS was monitored by ultraviolet spectrophotometry. Free-matrine with the dose of 1,2,4 mg was intravitreally injected respectively in 12 eyes of New Zealand albino rabbits in free-matrine group, and M AT-PLA-MS with matrine (2,4,6 mg respectively)was administered in 16 eyes separately in matrine microsphere group. The blank microsphere was injected in 6 right eyes as blank control group and normal saline solution was injected in 6 fellow eyes as control group. The retinal function change was evaluated by electroretinogram (ERG) ,and the morphological and histological change of retina following drug injection were assessed under the slit lamp biomicroscope,indirect ophthalmoscope,light microscope and transmission electron microscope. The decomposed process of MAT- PLA-MS in vitreous was recorded with ocular anterior segment and fundus color camera. Results MAT-PLA-MS containing matrine showed the spherical shape with the mean diameter of 2.28 - 0.47 μm under the transmission electron microscope and the drug-loading rate 6. 17% and drug-release rate 87.93% in vitro for 672 hours, presenting the controllable release characteristics. After implantation into the vitreous,the MAT-PLA-MS containing matrine decomposed gradually with the prolong of time. The b amplitudes of ERG maximum response were significantly declined in 4 mg free-matrine injection group in comparison with before injection in various time points( P 〈 0.01

关 键 词:苦参碱 聚乳酸 微球 玻璃体 

分 类 号:R285.5[医药卫生—中药学]

 

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