Danafar H, Rostamizadeh K, Davaran S, Hamidi M
Faculty of Pharmacy, Tabriz University of Medical Sciences , Tabriz , Iran .
Drug Dev Ind Pharm. 2014 Oct;40(10):1411-20. doi: 10.3109/03639045.2013.828223. Epub 2013 Aug 14.
Tri-block poly(lactide)-poly(ethylene glycol)-poly(lactide) (PLA-PEG-PLA) copolymers were synthesized and used to prepare polymersomes loaded separately by the hydrophobic and hydrophilic model drugs, atorvastatin and lisinopril, respectively. The resulting nanostructures were characterized by various techniques such as FTIR, DSC, PCS and AFM. The polymersomes exhibited high encapsulation efficiencies of almost 78% and 70.8% for atorvastatin and lisinopril, respectively. Investigation on FTIR and DSC results revealed that such a high encapsulation efficiency is due to strong interaction between atorvastatin and the copolymer. The impact of drug/copolymer ratio and copolymer composition on drug-loading efficiency and drug release behavior were also studied. The results showed that in case of lisinopril, polymersomes exhibited a triphasic drug release, while for atorvastatin a biphasic release profile was obtained. Overall, the results indicated that PLA-PEG-PLA polymersomes can be considered as a promising carrier for both hydrophilic and hydrophobic drugs.
合成了三嵌段聚（丙交酯）-聚（乙二醇）-聚（丙交酯）（PLA-PEG-PLA）共聚物，并分别用于制备由疏水和亲水模型药物阿托伐他汀和赖诺普利单独负载的聚合物囊泡。通过傅里叶变换红外光谱（FTIR）、差示扫描量热法（DSC）、动态光散射（PCS）和原子力显微镜（AFM）等多种技术对所得纳米结构进行了表征。聚合物囊泡对阿托伐他汀和赖诺普利的包封效率分别高达78%和70.8%。对FTIR和DSC结果的研究表明，如此高的包封效率是由于阿托伐他汀与共聚物之间的强相互作用。还研究了药物/共聚物比例和共聚物组成对载药效率和药物释放行为的影响。结果表明，对于赖诺普利，聚合物囊泡呈现三相药物释放，而对于阿托伐他汀则获得双相释放曲线。总体而言，结果表明PLA-PEG-PLA聚合物囊泡可被视为亲水性和疏水性药物的有前途的载体。
