姜黄素长循环脂质体注射剂的制备和评价.docVIP

姜黄素长循环脂质体注射剂的制备与评价 赵秀丽，宏伟，胡海洋，乔明曦，陈大为*（沈阳药科大学药学院，110016，沈阳） 摘要:目的 制备姜黄素长循环脂质体 方法 采用乙醇注入法制备长循环脂质体，以包封率为指标，对姜黄素脂质体进行单因素考察、正交试验设计，得到姜黄素脂质体的最优处方最优处方磷脂用量为50mg，磷脂与胆固醇的质量比为5:1，药脂比为13:1，选用分子量为2000的PEG-用量为磷脂的5%(mol/mol)，选用pH为6.5的PBS/20 mmmol?L-1。136±18）nm，Zeta电位为-17.7mv，包封率为（88.27±2.16）%，体外释放具有明显缓释特点。 结论 可按照最佳处方组成制备姜黄素长循环脂质体。 关键词: 姜黄素； 长循环脂质体；乙醇注入法；体外释放 Preparation and evaluation of Curcumin long-circulating liposome injection ZHAO Xiu-li, HONG Wei, HU Hai-yang, QIAO Ming-xi， CHEN Da-wei* (School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China) ABSTRACT: OBJECTIVE To study the preparation of Curcumin-long cirvulating-liposome injection. METHODS. The liposomes were prepared by ethanol infusion technique. On the basis of preliminary experiments, taking the encapsulation efficiency and size distribution as index, adopted the single factor prescription for the identification of factors affecting Cur-Liposome. Orthogonal design was employed to screen best prescription of Curcumin long-circulating liposome. RESULTS. The best prescription of the curcumin long-circulating liposome (Cur-PEG-L): the weight ratio of Cur to SPC is 5:1, the weight ratio of SPC to Cholest is 13:1, the weight ratio of PEG2000-Chol to SPC is 5%(mol/mol), the pH of buffer solution is 5.0 and the iron strength of water phase is 20 mmol?L-1. The mean diameters of liposomes were （136±18）nm, The Zeta potential was -17.7mv. The entrapment efficiency was （88.27±2.16）%. The release of Cur-PEG-L was significantly delayed. CONCLUSION Curcumin long-circulating liposome can be prepared according to the optimum formulation. KEY WORDS: Curcumin; long-circulating liposome; ethanol infusion technique; release in vitro 姜黄素（Curcumin）具有抗炎[1]、抗氧化[2]、降血脂[3]、抗动脉粥样硬化[4]、抗肿瘤[5]、抗HIV病毒等作用，且毒性很低。近年研究表明[1-8]，姜黄素可影响肿瘤发生、发展的各个阶段（始发、促进和演进），并可通过抑制血管生成达到抗肿瘤侵袭和转移的目的。作为一种良好发展前景的抗癌药物，姜黄素在肿瘤预防和治疗方面已经引起人们的重视，成为研究热点，美国国立肿瘤研究所已将其列为第三代癌化学预防药[9]。但姜黄素难溶于水，在体外也容易被氧化，体内被快速代谢，体内半衰期短，难以静脉给药，故目前没有稳定性较好的药物剂型，口服的姜黄素大部分也在胃肠道内被代谢失活