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一种新型壳聚糖-柠檬酸交联的β-环糊精纳米载体用于难溶性药物传递。

A novel chitosan-citric acid crosslinked beta-cyclodextrin nanocarriers for insoluble drug delivery.

机构信息

Department of Chemistry, Faculty of Science, Kasetsart University, 50 Ngamwongwan Rd., Chatuchak, Bangkok, 10900, Thailand.

Department of Chemistry, Faculty of Science, Kasetsart University, 50 Ngamwongwan Rd., Chatuchak, Bangkok, 10900, Thailand.

出版信息

Carbohydr Res. 2020 Dec;498:108184. doi: 10.1016/j.carres.2020.108184. Epub 2020 Oct 28.

Abstract

In this work a new system nanocarrier consisting of chitosan (CS) and beta-cyclodextrin crosslinked citric acid (pbCD) was prepared. Curcumin (cur), which is well-known for having a wide range of biological properties suitable for the treatment of several diseases, was selected as a model for forming the inclusion complex in pbCD and then encapsulated into CS nanoparticles (CSpbCD-cur). The effects of both the concentration of pbCD-cur and the pH were investigated. The CSpbCD-cur nanoparticles were characterised by SEM, FT-IR, DLS, drug loading and in vitro release. The results showed that the size of CSpbCD nanoparticles were unstable at higher pH values (pH ≥ 6) and pbCD concentrations. Moreover, the loading efficiency of the inclusion complex of curcumin with pbCD (pbCD-cur) entrapped into the CS nanoparticles (CSpbCD-cur), increased when the pbCD-cur concentration was increased. The size and size distritution (PDI) of nanoparticles showed the best at the concentration of pbCD-cur 20 mL/mg (with 1.5 mg/mL of CS) at pH 4. The release profile showed that CSpbCD-cur had a slower release than free curcumin resulting in that the cytotoxicity of CSpbCD-cur was less than that of pbCD-cur, and free curcumin, respectively.

摘要

在这项工作中,制备了一种由壳聚糖(CS)和交联柠檬酸的β-环糊精(pbCD)组成的新型纳米载体系统。姜黄素(cur)具有广泛的生物特性,适用于治疗多种疾病,被选为形成 pbCD 包合物的模型,然后封装到 CS 纳米颗粒(CSpbCD-cur)中。研究了 pbCD-cur 的浓度和 pH 值的影响。通过 SEM、FT-IR、DLS、药物载药量和体外释放对 CSpbCD-cur 纳米颗粒进行了表征。结果表明,在较高 pH 值(pH≥6)和 pbCD 浓度下,CSpbCD 纳米颗粒的尺寸不稳定。此外,当 pbCD-cur 浓度增加时,pbCD-cur 包封到 CS 纳米颗粒(CSpbCD-cur)中的姜黄素包合物(pbCD-cur)的负载效率增加。纳米颗粒的粒径和粒径分布(PDI)在 pbCD-cur 浓度为 20 mL/mg(CS 为 1.5 mg/mL)、pH 值为 4 时最佳。释放曲线表明,CSpbCD-cur 的释放速度比游离姜黄素慢,导致 CSpbCD-cur 的细胞毒性小于 pbCD-cur 和游离姜黄素。

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