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具有低胶凝温度的环糊精功能化琼脂糖凝胶用于控制药物传递系统。

Cyclodextrin functionalized agarose gel with low gelling temperature for controlled drug delivery systems.

机构信息

Department of Bioscience and Biotechnology, Microbial Carbohydrate Resource Bank (MCRB), Konkuk University, 120 Neungdong-ro, Gwangjin-gu, Seoul, 05029, South Korea.

Department of Bioscience and Biotechnology, Microbial Carbohydrate Resource Bank (MCRB), Konkuk University, 120 Neungdong-ro, Gwangjin-gu, Seoul, 05029, South Korea; Institute for Ubiquitous Information Technology and Applications (UBITA), Center for Biotechnology Research in UBITA (CBRU), Konkuk University, Seoul, 05029, South Korea.

出版信息

Carbohydr Polym. 2019 Oct 15;222:115011. doi: 10.1016/j.carbpol.2019.115011. Epub 2019 Jun 20.

DOI:10.1016/j.carbpol.2019.115011
PMID:31320040
Abstract

Conventional agaroses with high gelling temperature are limited to apply to the field of drug delivery. In this study, β-cyclodextrin (βCD) functionalized agarose (CFA) with low gelling temperature was successfully prepared from ethylenediamine-functionalized agarose using mono-succinyl βCD. The gelling temperature of CFA dramatically decreased to 26.7 °C from 65 °C and the melting temperature declined from 95 °C to 66.1 °C. Upon drug loading, CFA can be used at 30 °C because of its low gelling temperature compared to agarose. CFA gel could be used both for bovine serum albumin as a full release, and for the doxorubicin (DOX) for sustained release, via inclusion complexation of βCD. Furthermore, cytotoxicity tests revealed that CFA was noncytotoxic. DOX in the CFA gel could retain the anti-cancer activity. Newly synthesized CFA with low gelling temperature offer a new means for the development of hydrogel-based delivery systems for a variety of therapeutic drugs.

摘要

传统的琼脂糖凝胶化温度较高,限制了其在药物输送领域的应用。本研究通过乙二胺功能化琼脂糖与单琥珀酰-β-环糊精反应,成功制备了低凝胶化温度的β-环糊精(βCD)功能化琼脂糖(CFA)。CFA 的凝胶化温度从 65°C 急剧降低至 26.7°C,熔融温度从 95°C 降低至 66.1°C。由于 CFA 的凝胶化温度较低,在载药后,其可以在 30°C 下使用。CFA 凝胶可以通过 βCD 的包合作用,作为牛血清白蛋白的完全释放载体,也可以作为阿霉素(DOX)的持续释放载体。此外,细胞毒性试验表明 CFA 无细胞毒性。CFA 凝胶中的 DOX 保留了抗癌活性。这种具有低凝胶化温度的新型 CFA 为各种治疗药物的水凝胶给药系统的开发提供了新的手段。

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