Fabrication of doxorubicin and heparin co-loaded microcapsules for synergistic cancer therapy.
Fabrication of doxorubicin and heparin co-loaded microcapsules for synergistic cancer therapy.
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DOI：
10.1016/j.ijbiomac.2014.06.016
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发表时间：
2014-08
影响因子：
8.2
通讯作者：
Jingxiao Chen;Yan Liang;Wen Liu;Jin Huang;Jinghua Chen
中科院分区：
文献类型：
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作者：
Jingxiao Chen;Yan Liang;Wen Liu;Jin Huang;Jinghua Chen
在本研究中，通过交替沉积肝素(HEP)和壳聚糖(CHI)到载多柔比星(DOX)的CaCO3模板上，制备了包埋了盐酸阿霉素(DOX)的层层组装(HEP/CHI)5微囊。微胶囊结构稳定，在水介质中具有良好的分散性。荧光观察表明，DOX在微囊壁和囊腔中均有分布，而HEP在囊壁中有分布。与碱性pH相比，DOX在酸性pH条件下的释药速率较高，说明药物释放行为具有pH响应性。外层带有正电荷CHI的微囊可以保护HEP免受肝素酶的降解，实现DOX和HEP的细胞内共给药。因此，DOX微囊可以通过结合DOX和HEP的药理作用来提高对A549细胞的抑制活性。
In this study, a layer-by-layer (LbL) assembly (HEP/CHI)5microcapsule with doxorubicin hydrochloride (DOX) encapsulating inside was fabricatedviaalternatively depositing heparin (HEP) and chitosan (CHI) onto DOX-loaded CaCO3templates. The microcapsules were of stable architecture and had good dispersity in aqueous medium. Fluorescence observation showed that DOX distributed both in the wall and in the cavity of microcapsules, while HEP presented in the capsule wall. The release rate of DOX increased at acidic pH as compared with that at basic pH, suggesting a pH-responsive drug release behavior. The microcapsules with positively charged CHI lying on the outer layer could protect HEP from heparanase degradation and achieve intracellular co-delivery of both DOX and HEP. Thus, the DOX-loaded microcapsules could have improved inhibition activity against A549 cells by combining pharmacological actions of DOX and HEP.