Preparation of emulsions-filled sodium alginate hydrogel beads to enhance the anti-cancer activity of fangchinoline in vivo and in vitro

文献类型： 外文期刊

第一作者： Liu, Chao

作者： Liu, Chao;Wang, Mu-Xuan;Lyu, Xu-Tao;Guo, Xu;Sun, Jin-Yue;Lu, Chao-Xia;Li, Ning-Yang;Zhang, Kai;Prieto, M. A.

作者机构：

关键词： Fangchinoline; Emulsions; Hydrogel beads; Anti-cancer; Molecular mechanism

期刊名称：EUROPEAN POLYMER JOURNAL （ 影响因子：6.0； 五年影响因子：5.1 ）

ISSN： 0014-3057

年卷期： 2024 年 202 卷

页码：

收录情况： SCI

摘要： Fangchinoline (Fan) is a natural alkaloids compound with a series of remarkable bioactivity, but the poor aqueous solubility limits the clinical application. Emulsions (EM) systems are commonly used to encapsulate and deliver hydrophobic active compound to enhance the bioavailability. Hydrogel beads (HGB) are threedimensional hydrophilic polymer networks, which are able to immobilize colloidal delivery systems, resulting to the enhanced stability and controlled release in the gastrointestinal tract. In order to give full play to the bilateral advantages of emulsion and hydrogel, Fan loaded EM-filled sodium alginate HGB (Fan@EM-HGB) were designed and prepared in this paper. The average size of Fan@EM was 121.6 +/- 2.7 nm and the zeta potential was -17.7 +/- 0.3 mV. Physicochemical characterization demonstrated that Fan was successfully encapsulated in HGB with entrapment efficiency of 93.98 % and drug loading of 5.18 mg/g. The released behavior of Fan@EM-HGB followed a pH-controlled mechanism that was consistent with the first-order model. In vitro activity research shown that Fan@EM-HGB could significantly promote the apoptosis of A549 cells, with IC50 value more than 2.37 times higher than that of Fan. The in vivo results indicated that Fan@EM-HGB had an obvious anti- cancer effect, and molecular mechanism shown that Fan@EM-HGB could promote tumor cell apoptosis by inhibiting the activation of the PI3K/Akt/mTOR signaling pathway. The above research results suggest that nanoemulsionsfilled hydrogel beads have potential application in delivery system for hydrophobic composition.

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