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可修饰天然胶基微凝胶胶囊作为可持续药物传递系统。

Modifiable natural gum based microgel capsules as sustainable drug delivery systems.

机构信息

Faculty of Science & Arts, Chemistry Department, Canakkale Onsekiz Mart University, Terzioglu Campus, 17100 Canakkale, Turkey.

Faculty of Science & Arts, Chemistry Department, Canakkale Onsekiz Mart University, Terzioglu Campus, 17100 Canakkale, Turkey; Nanoscience and Technology Research and Application Center (NANORAC), Canakkale Onsekiz Mart University, Terzioglu Campus, 17100 Canakkale, Turkey.

出版信息

Carbohydr Polym. 2018 Nov 15;200:128-136. doi: 10.1016/j.carbpol.2018.07.085. Epub 2018 Jul 29.

Abstract

Few hundred micrometer size microgel capsules from natural locust bean gum (LBG) was synthesized by means of divinyl sulfone (DVS) crosslinking in a surfactant free cyclohexane medium with 100% yield in 1 h. These LBG microgel capsules were chemically modified with different numbers of linear amine containing modifying agents such as ethylenediamine (EDA), diethylenetriamine (DETA), triethylenetetraamine (TETA) and branched polyethyleneimine (PEI) to induce cationic character for LBG microgels. The biggest change in zeta potential of LBG microgels that is +44.9 mV from -17.67 mV was observed upon the modification of LBG microgels with branched PEI (LBG/PEI). The blood compatibility studies were revealed that bare LBG microgels possess a good blood compatibility with non-hemolytic value, 0.96 ± 0.15%, and high blood clotting index, 87.35 ± 4.10%, whereas the blood compatibility of LBG/PEI microgels was found to be slightly-hemolytic, 4.96 ± 1.03%, and also moderate blood clotting index, 65.98 ± 98%. Additionally, sodium diclofenac (SDC) as a model drug was loaded into the LBG based microgels by directly loading from solution (absorption) and by chemical conjugation methods for in vitro release studies at physiological conditions, pH 7.4 at 37.5 °C A longer, and sustainable drug release profiles were obtained from chemical drug conjugated LBG microgels and the amine modified LBG microgels.

摘要

在无表面活性剂的环己烷介质中,通过二乙烯基砜(DVS)交联,在 1 小时内以 100%的产率合成了尺寸为数百微米的天然刺槐豆胶(LBG)微凝胶胶囊。这些 LBG 微凝胶胶囊用不同数量的线性含胺改性剂(如乙二胺(EDA)、二乙烯三胺(DETA)、三乙烯四胺(TETA)和支化聚乙烯亚胺(PEI))进行化学修饰,以诱导 LBG 微凝胶的阳离子特性。LBG 微凝胶的 ζ 电位从 -17.67 mV 最大变化到+44.9 mV,观察到 LBG 微凝胶用支化 PEI(LBG/PEI)修饰时。血液相容性研究表明,裸 LBG 微凝胶具有良好的血液相容性,非溶血值为 0.96±0.15%,血液凝固指数为 87.35±4.10%,而 LBG/PEI 微凝胶的血液相容性为轻度溶血,4.96±1.03%,血液凝固指数也适中,65.98±98%。此外,将双氯芬酸钠(SDC)作为模型药物通过直接从溶液(吸收)加载和化学接枝方法加载到基于 LBG 的微凝胶中,用于在生理条件下(pH 7.4,37.5°C)进行体外释放研究。通过化学药物接枝 LBG 微凝胶和胺修饰 LBG 微凝胶得到了更长、更可持续的药物释放曲线。

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