Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Sector 67, SAS Nagar-160062 India.
Biomacromolecules. 2010 Apr 12;11(4):1027-35. doi: 10.1021/bm1000026.
(PEG)(3)-PLA copolymer has been explored for the formation of polymersomes. For this, three chains of methoxy-PEG(1100) were directly attached to citric acid by esterification. (Methoxy-PEG(1100))(3)-citrate was then reacted at its hydroxyl terminal with different moles of d,l-lactide by ring-opening polymerization to obtain polymers with five different PEG-to-PLA ratios ranging from 10:90 to 90:10. Polymers were characterized by GPC, FTIR, (1)H NMR, and DSC, films were characterized for hydrophilicity by contact angle, and surface topography was observed by SEM and AFM. All five polymers were evaluated for the formation of polymersomes. Among these, polymers with PEG content of 10-30% were able to self-assemble into polymersomes. To affirm their self-arrangement and drug carrier properties, hydrophilic and hydrophobic dyes were simultaneously encapsulated in these structures. SEM and TEM analysis of the blank polymersomes confirmed the vesicular nature of the polymersomes, whereas CLSM analysis of dye-loaded polymersomes demonstrated the presence of two separate regions viz. hydrophilic core and hydrophobic wall. Hydrophobic dye, fluorescein was released relatively faster from the wall of polymersomes, whereas hydrophilic dye, propidium iodide, was released in controlled fashion up to 18 days. It is expected that these systems may serve as a suitable carrier for simultaneous or separate delivery of drug molecules with varying physicochemical properties.
(PEG)(3)-PLA 共聚物已被探索用于聚合物囊泡的形成。为此，通过酯化反应将三条甲氧基-PEG(1100)链直接连接到柠檬酸上。然后，(甲氧基-PEG(1100))(3)-柠檬酸在其羟基末端与不同摩尔的 d,l-丙交酯通过开环聚合反应反应，得到具有五种不同 PEG 到 PLA 比例的聚合物，范围从 10:90 到 90:10。聚合物通过 GPC、FTIR、(1)H NMR 和 DSC 进行表征，通过接触角对薄膜进行亲水性能表征，通过 SEM 和 AFM 观察表面形貌。所有五种聚合物都被评估用于聚合物囊泡的形成。在这些聚合物中，PEG 含量为 10-30%的聚合物能够自组装成聚合物囊泡。为了确认它们的自组装和药物载体特性，同时将亲水性和疏水性染料包封在这些结构中。空白聚合物囊泡的 SEM 和 TEM 分析证实了聚合物囊泡的囊泡性质，而负载染料的聚合物囊泡的 CLSM 分析表明存在两个独立的区域，即亲水核和疏水壁。疏水性染料荧光素从聚合物囊泡的壁中释放得相对较快，而亲水性染料碘化丙啶则以受控的方式释放长达 18 天。预计这些系统可以作为同时或分别输送具有不同物理化学性质的药物分子的合适载体。
