和厚朴酚泊洛沙姆F-127胶束的制备及其体外抗肿瘤研究

Honokiol/Pluronic F-127 Micelles: Preparation and Its in Vitro Anti-tumor Study

关键词:  泊洛沙姆  胶束  和厚朴酚  体外抗肿瘤

Key words:  泊洛沙姆  胶束  和厚朴酚  体外抗肿瘤

摘要:

目的 以泊洛沙姆F-127为载体制备一种新型的和厚朴酚胶束制剂，以提高其抗肿瘤效果。方法 选用泊洛沙姆F-127为药物载体，采用自组装法制备和厚朴酚胶束制剂，通过透射电镜观察和厚朴酚胶束的形貌，采用紫外分光光度法测定载药量、药物包封率以及体外药物释放行为。采用MTT法检测和厚朴酚及其和厚朴酚胶束制剂对BGC-823人胃癌细胞的抑制作用。结果 本研究所制备的和厚朴酚胶束纳米制剂，具有壳-核的球型结构。纳米粒子分布较窄，平均粒径为28.7 nm。和厚朴酚与泊洛沙姆F-127的投料比影响胶束制剂载药量，随着和厚朴酚与泊洛沙姆F-127的投料比从1∶10增加到1∶2.5，载药胶束的载药量从(8.4±1.6)%增加到(25.7±2.7)%，而包封率维持在97%左右。体外释放结果显示和厚朴酚可以缓慢地从泊洛沙姆F-127胶束中释放出来。体外抗肿瘤实验结果显示：相比于溶液剂型的和厚朴酚，和厚朴酚/泊洛沙姆F-127胶束具有更好的体外抗BGC-823人胃癌细胞效果。结论 和厚朴酚/泊洛沙姆F-127胶束是一种新型的和厚朴酚纳米制剂，能有效提高体外抗BGC-823人胃癌细胞效果。

Abstract:

OBJECTIVE To develop a novel honokiol loaded pluronic F-127 micelles formulation to improve its anti-tumor capacity. METHODS Honokiol loaded pluronic F-127 micelles was developed by a self-assemble method. The developed honokiol micelles was characterized by TEM and DLS. Drug loading capacity and encapsulation effciency were measured by UV-IS spectroscopy. In vitro release of honokiol from pluronic F-127 micelles was performed in PBS solution at 37 ℃. In vitro cytotoxicity of honokiol micelles against BGC-823 cell lines was detected by MTT assay. RESULTS The developed honokiol loaded pluronic F-127 micelles with core-shell structure had mean diameter of 20-30 nm. With the increase of honokiol/pluronic F-127 feed ratio from 1∶10 to 1∶2.5, the drug loading capacity increased from (8.4±1.6)% to (25.7±2.7)% accordingly, while drug encapsulation efficiency reached nearly 97%. In vitro cytotoxicity test indicated that the developed honokiol micelles showed higher cytotoxicity against BGC-823 cells with respect to honokiol solution. CONCLUSION The developed honokiol loaded pluronic F-127 micelles is a novel honokiol nano-formualtion, that can effciently improve its anti-tumor capacity.