普朗尼克胶束用于抗癌药物阿霉素的负载和释放

Pluronic Micelles Used to Load and Release of the Anticancer Drug Doxorubicin

为了研究阿霉素胶束中药物的存在形式及其与胶束释药行为的关系,以不同类型的普朗尼克胶束为载体材料制备了3种阿霉素胶束。普朗尼克载药胶束首先由阿霉素盐酸盐和脱氧胆酸钠通过静电相互作用形成复合物,然后通过亲疏水性作用封装到普朗尼克胶束的疏水段形成。以载药量和包封率为评价指标,动态光散射法测定其粒径大小及其分布、透析法测定载药胶束的体外释放行为。结果表明,制备的普朗尼克F127,F128,F68胶束的载药量分别为(0.15±0.11)%,(0.16±0.07)%和(0.17±0.1)%,包封率分别为(3.03±0.24)%,(3.11±0.15)%和(3.36±0.02)%。载药胶束的粒径分布均匀。在690 min内累计释放率均能达到70%以上,且无显著性差异。本文成功制备了均一、稳定的普朗尼克载药胶束,研究了不同普朗尼克载药胶束的药物释放行为,为药物输送系统提供理论依据和参考。

In order to study the existing form of doxorubicin micelles and its relationship with the release behavior of micelles,three types of Pluronic micelles were used as carrier material to prepare three kinds of doxorubicin F127,F128,F68 and F108 micelles.The Pluronic drug-loaded micelles were first formed by doxorubicin hydrochloride and sodium deoxycholate through electrostatic interactions to form the complexes,and then formed by hydrophilic and hydrophobic encapsulation to the hydrophobic segments of Pluronic micelles.The drug loading capacity and encapsulation rate were used as evaluation indicator.The particle size and distribution were determined by dynamic light scattering method,and the in vitro release behavior of drug-loaded micelle was determined by dialysis method.The results show that the drug loadings of the prepared Pluronic F127,F128 and F68 micelles are(0.15±0.1)%,(0.16±0.07)%and(0.17±0.1)%,encapsulation rates are(3.03±0.24)%,(3.11±0.147)%and(3.36±0.024)%.The particle size distribution of the drug-loaded micelles is uniform.The cumulative release rate can reach more than 70%within 690 min,with no significant difference.This study shows that uniform and stable Plantronics-loaded micelle were been successfully prepared.There is no significant difference in the release behavior of different Plantronics-loaded micelles.