姜黄素非离子表面活性剂囊泡的制备优化及质量评价  

Preparation optimization and quality evaluation of curcumin niosomes

作　　者：吕佳琦 刘楠[2] 李明媛 郁彭[1] 郑爱萍[2] LV Jia-qi;LIU Nan;LI Ming-yuan;YU Peng;ZHENG Ai-ping(College of Biotechnology,Tianjin University of Science&Technology,Tianjin 300457,China;China Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850,China)

机构地区：[1]天津科技大学生物工程学院,天津300457 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国医院药学杂志》2022年第15期1546-1552,共7页Chinese Journal of Hospital Pharmacy

摘　　要：目的:通过星点设计-效应面法(central composite design-response surface methodology,CCD-RSM)优化姜黄素非离子表面活性剂囊泡(curcumin niosomes,Cur-Nio)的制备工艺和处方,并进行质量评价。方法:采用薄膜分散-超声法以硬脂山梨坦(Span 60)和胆固醇作为载体材料制备Cur-Nio,以包封率、载药量、平均粒径为考察指标,以总评“归一值”为评价指标优化制备处方。以CCD-RSM选取最佳处方,用二项式进行拟合预测分析,按优化出的处方制备Cur-Nio,考察测定Cur-Nio粒径、PDI和Zeta电位,透射电镜观察Cur-Nio形态,差式扫描热及X-射线衍射分析结构特征及晶型是否有变化,并对其稳定性及体外释放进行考察。结果:Cur-Nio的制备最佳处方及工艺条件为Span 60与胆固醇的质量比值为3.096∶1、水化时间为65 min、水化体积为19.45 mL;优化后的处方制备出的Cur-Nio的平均粒径是(151.70±2.003)nm,PDI为0.21±0.013,Zeta电位为(-45.10±1.40)mV,包封率为(82.91±0.59)%;透射电镜观察Cur-Nio外观圆整;长期存放4℃具有一定稳定性;差式扫描热及X-射线衍射结果表明Cur以无定型或分子状态包裹在囊泡中;体外释放结果表明,与游离姜黄素溶液相比,具有明显缓释效果。结论:通过CCD-RSM优化后的Cur-Nio,制备工艺简单,外观圆整,粒径均匀,具有缓释作用,符合优化试验结果。有效提高了姜黄素的生物活性,可用于进一步研究。OBJECTIVE To optimize the preparation process and formulation of curcumin niosomes(Cur-Nio)by central composite design-response surface methodology,and to evaluate the quality of Cur-Nio.METHODS Cur-Nio was prepared with span 60 and cholesterol as carrier materials by a thin film dispersion method.The encapsulation efficiency,drug loading,and average particle size were used as the evaluation indicators,and the overall evaluation"normalized value"was used as the evaluation index to optimize the preparation of the formulation.The best formulation was selected by CCD-RSM,and the fitting prediction analysis was carried out by binomial.A transmission electron microscope was used to observe the morphology of Cur-Nio,differential scanning calorimetry and X-ray diffraction analysis were applied to studying structural characteristics and crystal form changes,and its stability and in vitro release were investigated as well.RESULTS The optimal formulation and process conditions for the preparation of Cur-Nio were as follows:the mass ratio of Span 60 to cholesterol was 3.096∶1,the hydration time was 65 min,and the hydration volume was 19.45 mL.The average particle size of Cur-Nio prepared by the optimized formulation was(151.70±2.003)nm,the PDI was 0.21±0.013,the Zeta potential was(-45.10±1.40)mV,and the encapsulation efficiency was(82.91±0.59)%.The morphology of Cur-Nio was round under the transmission electron microscope.Cur-Nio showed certain stability when stored at 4℃;differential scanning calorimetry and X-ray diffraction results showed that Cur was encapsulated in the vesicles in an amorphous or molecular state;the in vitro release results showed that compared with free curcumin solution,Cur-Nio had an obvious sustained release effect.CONCLUSION Cur-Nio optimized by CCD-RSM has round morphology and uniform particle size,which conforms to the experimental results of optimization.The biological activity of curcumin is improved effectively,which can be used for further study.

关 键 词：姜黄素 非离子表面活性剂囊泡 星点设计-效应面法 薄膜分散法 质量评价 

分 类 号：R944.9[医药卫生—药剂学]