Self Assembly of Amphiphilic (PEG)3-PLA Copolymer as Polymersomes: Preparation, Characterization, and Their Evaluation As Drug Carrier
Self Assembly of Amphiphilic (PEG)3-PLA Copolymer as Polymersomes: Preparation, Characterization, and Their Evaluation As Drug Carrier
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DOI：
10.1021/bm1000026
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发表时间：
2010-04-01
影响因子：
6.2
通讯作者：
Kumar, Neeraj
中科院分区：
文献类型：
--
作者：
Jain, Jay Prakash;Kumar, Neeraj
（PEG）（3）-PLA共聚物已被探索用于形成聚合物囊泡。为此，通过酯化将甲氧基-PEG（1100）的三个链直接连接到柠檬酸。然后通过开环聚合使（甲氧基-PEG（1100））（3）-柠檬酸盐在其羟基末端与不同摩尔数的D，L-丙交酯反应，以获得具有范围为10：90至90：10的五种不同PEG与PLA比率的聚合物。采用GPC、FUR、H-1 NMR和DSC对聚合物进行了表征，用接触角表征了膜的亲水性，用SEM和AFM观察了膜的表面形貌。评价所有五种聚合物的聚合物囊泡形成。其中，PEG含量为10-30%的聚合物能够自组装成聚合物囊泡。为了确认它们的自排列和药物载体性质，亲水性和疏水性染料同时封装在这些结构中。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，即亲水性核和疏水性壁。疏水性染料，荧光素从聚合物囊泡的壁释放相对较快，而亲水性染料，碘化丙啶，以受控的方式释放长达18天。预期这些系统可用作同时或单独递送具有不同物理化学性质的药物分子的合适载体。
(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, FUR, H-1 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.