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含吲哚美辛的甲氧基聚(乙二醇)/ε-己内酯两亲性嵌段共聚物胶束。I. 制备与表征。

Methoxy poly(ethylene glycol)/epsilon-caprolactone amphiphilic block copolymeric micelle containing indomethacin. I. Preparation and characterization.

作者信息

Shin I G, Kim S Y, Lee Y M, Cho C S, Sung Y K

机构信息

Department of Industrial Chemistry, College of Engineering, Hanyang University, Seoul, Korea.

出版信息

J Control Release. 1998 Jan 23;51(1):1-11. doi: 10.1016/s0168-3659(97)00164-8.

DOI:10.1016/s0168-3659(97)00164-8
PMID:9685899
Abstract

Amphiphilic diblock copolymers composed of methoxy polyethylene glycol (MePEG) and epsilon-caprolactone (epsilon-CL) were prepared for the formation of micelles. The copolymer was formed by ring opening mechanism of epsilon-CL in the presence of MePEG containing hydroxyl functional groups at one end of the chain. To estimate their feasibility as vehicles for drugs, MePEG/epsilon-CL block copolymeric micelles were prepared by dialysis against water. Indomethacin was incorporated into the hydrophobic inner core of these micelles as a typical model drug for non-steroidal anti-inflammatory drugs. From the dynamic light scattering measurements, the size of micelle formed was less than 200 mm, and their size increases with the amount of indomethacin encapsulated into the inner core of MePEG/epsilon-CL block copolymers. The selected solvents used to prepare micelles by dialysis in water affect the size of polymeric micelles. As the hydrophobic components of copolymer increase, the critical micelle concentration values and hydrophilic-lipophilic balance decreased. An increase of molecular weight and hydrophobic components of diblock copolymer produced larger micelles.

摘要

制备了由甲氧基聚乙二醇(MePEG)和ε-己内酯(ε-CL)组成的两亲性二嵌段共聚物以形成胶束。该共聚物是通过ε-CL在链一端含有羟基官能团的MePEG存在下的开环机理形成的。为了评估它们作为药物载体的可行性,通过对水透析制备了MePEG/ε-CL嵌段共聚物胶束。吲哚美辛作为非甾体抗炎药的典型模型药物被包封到这些胶束的疏水内核中。通过动态光散射测量,形成的胶束尺寸小于200nm,并且其尺寸随着包封到MePEG/ε-CL嵌段共聚物内核中的吲哚美辛量的增加而增大。用于在水中通过透析制备胶束的所选溶剂会影响聚合物胶束的尺寸。随着共聚物疏水成分的增加,临界胶束浓度值和亲水亲油平衡降低。二嵌段共聚物分子量和疏水成分的增加产生了更大的胶束。

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