Thermo-sensitive micelles based on amphiphilic poly(butylene 2-methylsuccinate)-poly(ethylene glycol) multi-block copolyesters as the pesticide carriers
Thermo-sensitive micelles based on amphiphilic poly(butylene 2-methylsuccinate)-poly(ethylene glycol) multi-block copolyesters as the pesticide carriers
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基于两亲性聚(2-甲基丁二酸丁二醇酯)-聚乙二醇多嵌段共聚酯作为农药载体的热敏胶束
DOI：
10.1016/j.colsurfa.2019.04.057
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发表时间：
2019-08-20
影响因子：
5.2
通讯作者：
Guo, Baohua
中科院分区：
文献类型：
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作者：
Han, Jiarui;Weng, Yunxuan;Guo, Baohua
以1，4-丁二醇（BDO）、2-甲基丁二酸（MSA）和聚乙二醇（PEG）为原料，钛酸四丁酯为催化剂，通过直接酯化和缩聚反应合成了一种新型生物基可生物降解脂肪族多嵌段共聚物-聚丁二酸丁二醇酯-聚乙二醇（PBMS-PEG）。采用透析法将两亲性嵌段共聚酯在水溶液中自组装成温度敏感的PBMS-PEG胶束。这些具有不同PEG含量的胶束具有从74.3nm至138.3nm的尺寸变化，并且在水中稳定超过200天而没有任何沉淀。疏水性农药阿维菌素，通过相同的透析方法包封在胶束中。这种PBMS-PEG胶束可以用作温度响应性药物载体，因为它们的受控的低临界溶解温度（LCST）可以通过改变PEG比例来精确调节。LCST从27.0 ℃增加到40.0 ℃，同时将PEG比例从30%增加到60%。通过HPLC测定，结果表明，当载药量达到20%时，载药率仍接近100%。这些两亲性胶束的性质表明，释放系统具有很好的潜力，可进一步开发一个高效的和可生物降解的疏水农药释放制剂。
A novel bio-based and biodegradable aliphatic multi-block copolyester, poly(butylene 2-methylsuccinate)-poly (ethylene glycol) (PBMS-PEG), was synthesized from 1,4-butanediol (BDO), 2-methylsuccinate acid (MSA) and poly(ethylene glycol) (PEG) via direct esterification and polycondensation process with tetrabutyl titanate as catalyst. Thermo-sensitive PBMS-PEG micelles were obtained by self-assembly of amphiphilic block copolyesters in aqueous medium by dialysis method. These micelles with different PEG contents have sizes varying from 74.3 nm to 138.3 nm and are stable in water over 200 days without any precipitation. A hydrophobic pesticide, Avermectin, was encapsulated in micelles by the same dialysis method. Such PBMS-PEG micelles can be used as thermo-responsive drug carrier owing to their controlled lower critical solution temperature (LCST) which can be accurately adjusted by varying the PEG proportion. The LCST increases from 27.0 degrees C to 40.0 degrees C while increasing the PEG proportion from 30% to 60%. By using the HPLC measurements, the results show when the drug loading is up to 20%, the loading efficiency is still nearly 100%. The properties of these amphiphilic micelles show that the delivery system has a promising potential to be further explored for developing a highly effective and biodegradable hydrophobic-pesticide-release formulation.