包载盐酸小檗碱的磷脂/壳聚糖自组装纳米粒构建及表征  

Preparation and evaluation of self-assembled lecithin/chitosan nanoparticles for berberine hydrochloride delivery

作　　者：张世彩 陈坤 刘黎瑶 ZHANG Shi-cai;CHEN Kun;LIU Li-yao(College of Basic Science,Tianjin Agricultural University,Tianjin 300384,China;Institute of Materia Medica,Peking Union Medical College&Tsinghua University,Beijing 100050,China)

机构地区：[1]天津农学院基础科学学院,天津300384 [2]北京协和医学院药物研究所,清华大学医学部,北京100050

出　　处：《天津农学院学报》2018年第1期59-63,共5页Journal of Tianjin Agricultural University

基　　金：中央高校基本科研业务费专项资金资助-协和青年基金资助(3332015044);国家自然科学基金面上项目(31170442)

摘　　要：磷脂/壳聚糖自组装纳米粒(lecithin/chitosan nanoparticles,L/CS NPs)是通过磷脂与壳聚糖的静电作用而自组装形成的一种特殊聚电解质复合物,可作为药物载体,有利于提高难溶性药物的口服利用度。本研究中,以难溶性药物盐酸小檗碱为目标递送药物,构建了包载盐酸小檗碱的磷脂/壳聚糖自组装纳米粒,并建立了包封率测定方法。通过正交设计,以包封率为指标,筛选出制备载药自组装纳米粒的最优处方,其中水相pH值为8.0、V_(乙醇)∶V_水=8∶92、m_(磷脂)∶m_(壳聚糖)=20∶1。在优选处方下,制备的载药自组装纳米粒的平均粒径为(214.8±9.3)nm、Zeta电位为(24.3±3.1)mV、包封率为(82.4±5.2)%,4℃下可稳定存放3个月。该研究为后期实际应用奠定了基础。With the development of nano-medicine,a novel kind of self-assembled nanoparticle was fabricated through electrostatic crosslink method using negative-charged lecithin and positive-charged chitosan.This kind of self-assembled nano-carrier could be used to improve oral bioavailability of drugs with poor solubility.In this study,we utilized this nano-carrier to facilitate the drug delivery of berberine hydrochloride,whose water solubility is low to 1:200(g:mL).At the same time,the method for entrapment efficiency(EE)measurement was established.Afterwards,orthogonal screening was used to determine the optimal formulation of drug-loaded self-assembled nanoparticle,in which entrapment efficiency(EE)was set as evaluation indicator.In the selected formulation,pH value of water phase was 8.0,volume ratio of ethanol phase/water phase was 8∶92,and mass ratio of lecithin/chitosan was 20∶1.Three batches self-assembled nanoparticle were prepared under the selected formulation,and evaluation results showed that the average particle size,Zeta potential and entrapment efficiency was(214.8±9.3)nm,(24.3±3.1)mV and(82.4±5.2)%,separately.Berberine hydrochloride loaded self-assembled nanoparticle remains high stability under 4℃storage,which provided the basis for practical application.

关 键 词：自组装纳米粒 盐酸小檗碱 药物递送 正交设计 处方筛选 

分 类 号：P641.131[天文地球—地质矿产勘探] S152.72[天文地球—地质学]