以生物相容性好且可生物降解的海藻酸钠(Sodium Alginate,Alg)、几丁聚糖(Chitosan,Chi)为壁材,采用静电液滴装置制备了球形度好、表面光洁、分散性好、平均粒径为210μm的海藻酸钙(Calcium Alginate,Ca-Alg)胶珠,并以卡培他滨(CAP)为模型药物,采用一步法和两步法制备了栓塞型载CAP Ca-Alg/Chi微胶囊,并考察了CAP浓度对微胶囊载药量和药物释放的影响。结果表明:随着CAP浓度的增大,载药量增大,包封率却随之减小;微胶囊在0.5 h内的累积释放量不到20%,无突释效应;微胶囊有一定的缓释性能,有望成为一种栓塞型抗肿瘤药物新剂型。
The Ca-Alg(Sodium Alginate) beads with smooth surface,good sphericity and dispersivity,and average size of 210 μm were prepared by the electronic droplet generator,and Alg and chitosan(Chi) were used as wall materials.Then embolic Ca-Alg/Chi microcapsules loading CAP(Capecitabine) were prepared by one-step method and two-step method.Effect of CAP concentrations on drug-loading and drug-release of the microcapsules were investigated.The results show that the drug-loading increases with the CAP concentrations,but the encapsulation efficiency decreases.The cumulative amount of CAP released from the microcapsules is lower than 20% in 0.5 h,which indicate that there is no initial burst release.The embolic microcapsules are likely to be a new dosage form of embolic anti-tumor drugs.
参考文献
[1] | 刘德忠, 张石革. 分子和抗体靶向抗肿瘤药的研究进展[J]. 中国药房, 2007, 18(26): 2067-2068. |
[2] | Park J H, Saravanakumar G, Kim K, et al. Targeted delivery of low molecular drugs using chitosan and its derivatives [J].Advanced Drug Delivery Reviews, 2010, 62(1): 28-41. |
[3] | 安富荣, 戈升荣, 祝德秋. 卡培他滨的药理特性及临床应用进展[J]. 中国新药与临床杂志, 2002, 21(8): 503-507. |
[4] | Lee P B, Bidard F C, Pierga J Y. Contemporary issues and the potential uses of capecitabine in metastatic breast cancer[J]. Cancer Treatment Reviews, 2009, 35(7): 582-589. |
[5] | Kosuri K V, Wu X, Wang L, et al. An epigenetic mechanism for capecitabine resistance in mesothelioma [J]. Biochemical and Biophysical Research Communications, 2010, 391(3): 1465-1470. |
[6] | Wang J, Fan Y, Xu B.Ixabepilone plus capecitabine for Chinese patients with metastatic breast cancer progressing after anthracycline and taxane treatment [J]. Cancer Chemotherapy and Pharmacology, 2010, 66(3): 597-603. |
[7] | 蓝琪, 陈宝剑, 王士斌, 等. 聚氨基酸复合微胶囊对Hb的控制释放[J]. 复合材料学报, 2008, 25(6): 33-38. |
[8] | 蓝琪. 几丁聚糖-海藻酸钙微囊及聚精氨酸-海藻酸钙微囊的生物相容性研究[D]. 厦门: 华侨大学, 2008. |
[9] | Wang S B, Xu F H, He H S, et al. Novel alginate-poly (L-histidine) microcapsules as drug carriers: In vitro protein release and short term stability [J]. Journal of Macromolecular Bioscience, 2005, 5(5): 408-414. |
[10] | 国家药典委员会. 中华人民共和国药典第二部 [M]. 北京: 化学工业出版社, 2010: 附录203-204. |
[11] | 薛伟明, 于炜婷, 刘袖洞, 等. 载细胞海藻酸钠/壳聚糖微胶囊的化学破囊方法研究[J]. 高等学校化学学报, 2004, 25(7): 1342-1346. |
[12] | Wang S B, Chen A Z, Weng L J, et al. Effect of drug-loading methods on drug load, encapsulation efficiency and release properties of alginate/poly-L-arginine/chitosan ternary complex microcapsules [J]. Macromolecular Bioscience, 2004, 4(1): 27-30. |
[13] | 陈爱政.海藻酸钠/聚精氨酸-几丁聚糖复合微胶囊的制备[D]. 泉州: 华侨大学, 2004. |
[14] | 王春, 杨连生, 扶雄. 水溶性壳聚糖纳米粒子的制备及其BSA载药性能[J]. 化工进展, 2006, 25(12): 1431-1435. |
[15] | 姚文彬. 岩藻聚糖微球的制备及其性能表征[D]. 厦门: 华侨大学, 2010. |
[16] | Gupta K C, Kumar M N V Ravi. Drug release behavior of beads and microgranules of chitosan [J]. Biomaterials, 2000, 21(11): 1115-1119. |
[17] | 姚文彬, 郑琪瑶, 王士斌, 等. 岩藻聚糖控释微粒的制备及其性能表征[C]/ /第十二届全国生物材料学术会议论文集.广州: 中国生物医学工程学会生物材料分会, 2009: 114. |
[18] | Sikorski P, Mo F, Skj k-Braek G, et al. Evidence for egg-box-compatible interactions in calcium-alginate gels from fiber X-ray diffraction [J]. Biomacromolecules, 2007, 8(7): 2098-2103. |
[19] | Kang Jichao, Schwendeman S P. Pore closing and opening in biodegradable polymers and their effect on the controlled release of proteins [J]. Molecular Pharmaceutics, 2007, 4(1): 104-118. |
[20] | 刘丽萍, 黄黎明, 马小涛, 等. 吸附和包埋法制备洛美沙星淀粉微球及其体外释放比较研究[J]. 中国现代应用药学, 2010, 27(6): 523-527. |
- 下载量()
- 访问量()
- 您的评分:
-
10%
-
20%
-
30%
-
40%
-
50%