A novel tanshinone IIA/chitosan solid dispersion: Preparation, characterization and cytotoxicity evaluation
A novel tanshinone IIA/chitosan solid dispersion: Preparation, characterization and cytotoxicity evaluation
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新型丹参酮IIA/壳聚糖固体分散体的制备、表征及细胞毒性评价
DOI：
10.1016/j.jddst.2018.11.024
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发表时间：
2019-02-01
影响因子：
5
通讯作者：
Yang, Kai
中科院分区：
文献类型：
--
作者：
Luo, Chao;Wu, Weibin;Yang, Kai
本研究旨在制备丹参酮IIA（TA）/壳聚糖（CS）固体分散体（TA-CS-SD），并对其生物利用度进行评价。利用壳聚糖基质的pH响应性溶出特性，采用pH倒置法制备丹参酮IIA壳聚糖固体分散体。体外溶出实验表明，固体分散体可显著提高TA的溶出速率，且释放机制具有pH响应性。采用X射线衍射（XRD）、差示扫描量热法（DSC）、傅里叶变换红外光谱（FTIR）和扫描电子显微镜（SEM）对固体分散体进行了表征。结果表明，TA在固体分散体中以微晶或超细晶的形式存在，结晶度的降低与CS基体的含量有关。采用CCK-8法对人非小细胞肺癌A549细胞进行体外细胞毒性试验。与结晶药物相比，TA在TA-CS-SD中的抗肿瘤活性得到显著改善。结果表明，与游离TA相比，TA-CS-SD具有更高的溶出速率和生物活性。
The objective of this study was to develop and evaluate a novel tanshinone IIA (TA)/chitosan (CS) solid dispersion (TA-CS-SD) to improve the bioavailability. Solid dispersion of tanshinone IIA with chitosan was prepared by a pH inversion method via the pH-responsive dissolution property of chitosan matrix. The in vitro dissolution study confirmed dramatically elevated dissolution rate of TA by solid dispersion approach, and the release mechanism exhibited pH-responsive performance. The solid dispersion was characterized by x-ray diffractometry (XRD), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). Our results showed that TA existed in the form of microcrystal or superfine crystal in solid dispersion, and the reduction of crystallinity was correlated with the content of CS matrix. In vitro cytotoxicity study was performed in human non-small cell lung cancer A549 cell line by CCK-8 assay. Significant improvement in antitumor activity of TA in TA-CS-SD was achieved compared to the crystalline drug. These results indicated that, compared with free TA, TA-CS-SD demonstrated higher dissolution rate and bioactivity.