摘要
目的 制备冬凌草甲素/胆固醇甲酰-壳聚糖共聚物（ORI/CF-CS）纳米胶束并研究其体外抗肿瘤活性。方法 采用酰胺化反应合成胆固醇甲酰-壳聚糖共聚物（CF-CS）；以CF-CS为载体材料制备ORI/CF-CS纳米胶束，并测定其载药量、包封率、形态、粒径和ξ电位；MTT法测定其对宫颈癌Hela肿瘤细胞的细胞毒作用。结果 ORI/CF-CS纳米胶束载药量为9.16%，包封率为48.83%，粒径控制在68.10~113.8 nm内，ξ电位为-34.97~-29.19 mV，体外释药缓慢；ORI/CF-CS纳米胶束对Hela肿瘤细胞的细胞毒作用优于冬凌草甲素溶液，且IC50 值比冬凌草甲素溶液低约3倍。结论 CF-CS是冬凌草甲素的优良载体，且可提高其抗Hela肿瘤细胞的活性。
Abstract
OBJECTIVE To prepare oridonin-loaded cholesteryl formate-graft chitosan copolymer （abbreviated as ORI/CF-CS） nano-micelles and study the in vitro anti-tumor activity. METHODS Cholesteryl formate-graft chitosan copolymer （abbreviated as CF-CS） was synthesized via amidation reaction. ORI/CF-CS nano-micelles were prepared by evaporating and characterized by drug loading content，entrapment efficiency，morphology，particle size，and ξ potential. MTT test were applied to assess the cytotoxicity of ORI/CF-CS nano-micelles on Hela cells line. RESULTS The prepared ORI/CF-CS nanomicelles had loading content of 9.16% and entrapment efficiency of 48.83%，small size range of 68.10-113.8 nm，ξ potential range of -34.97--29.19 mV，and slow release in vitro. The cytotoxicity of ORI/CF-CS nanomicelles was stronger than that of oridonin solution. IC50 value of ORI/CF-CS nanomicelles was about 3 times lower，than those of oridonin solution. CONCLUSION CF-CS nano-micelles might be used as potential carriers of oridonin for cancer therapy.
关键词
冬凌草甲素 /
胆固醇甲酰-壳聚糖共聚物 /
纳米胶束 /
体外抗肿瘤作用
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Key words
oridonin /
cholesteryl formate-graft chitosan copolymer /
nano-micelles /
in vitro anti-tumor effect
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赵永星 赵阳 张振中 张雪晓 孙倩.
冬凌草甲素/胆固醇甲酰-壳聚糖共聚物纳米胶束的制备及其体外抗肿瘤作用[J]. 中国药学杂志, 2011, 46(13): 1015-1019
ZHO Yong-xing;ZHO Yng;ZHNG Zhen-zhong;ZHNG Xue-xio;SUN Qin.
Preparation and Anti-Tumor Effect of Oridonin Loaded Cholesteryl Formate-Graft Chitosan Copolymer Nano-micelles[J]. Chinese Pharmaceutical Journal, 2011, 46(13): 1015-1019
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