摘要
目的制备色胺酮纳米胶束,改善色胺酮的水溶性,并进行体外性质考察。方法以二硬脂酰基磷脂酰乙醇胺-聚乙二醇2000(DSPE-PEG2000)为载体,用溶剂挥发法制备色胺酮纳米胶束,通过正交实验筛选制备胶束的最佳条件,核磁共振氢谱(1 HNMR)验证色胺酮包载于纳米胶束,用芘荧光探针法测定其临界胶束浓度(CMC),用紫外分光光度计测定其包封率和载药率,动态光散射法测定胶束的粒径,以粒径、外观形态和包封率为指标考察胶束的稳定性。结果色胺酮纳米胶束的CMC为8.93×10-6mol·L^(-1),色胺酮与聚合物投药比为0.442 9∶1(mol∶mol),真空干燥1h,水化5min时,胶束的包封率为32.24%±1.37%,载药率为5.468%±0.39%。色胺酮纳米胶束平均粒径为112.5nm,平均分散系数为0.208,4℃条件下胶束可稳定15d以上。结论制备色胺酮纳米胶束,将色胺酮的溶解度提高至1.625mmol·L^(-1),为改善色胺酮生物利用度的研究奠定了基础。
Objective To prepare and characterize the tryptanthrin-loaded nano-micelles and improve the solubility of tryptanthrin.Methods 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy（polyethyleneglycol）-2000]（DSPE-PEG2000）was used as the carrier to prepare tryptanthrin-loaded nano-micelles.Optimal conditions for preparation of micelles were found through orthogonal experiments.Tryptanthrin-loaded nano-micelles were prepared by using solvent evaporation method.The critical micelle concentration（CMC）of polymer micelles was measured by pyrene fluorescence probe method.The entrapment efficiency and drug loading were charactered by UV spectrophotometry.Size and distribution were evaluated through dynamic light scattering method.Particle size,morphology and encapsulation efficiency were used to investigate the stability of micelles.Results The CMC of tryptanthrin-loaded nano-micelles was 8.93×10-6 mol·L^-1.When the dosage ratio of copolymer and tryptanthrin was 0.442 9∶1（mol∶mol）,vacuum during 1h,hydration smin,the encapsulation efficiency of micelles prepared under the optimal conditions was 32.24%±1.37%,and the drug loading efficiency was 5.468%±0.39%.The average particle size was 112.5nm,and the average dispersion coefficient was 0.208.The micelles could be kept for more than 15 dat 4 ℃,indicating excellent stability.Conclusion Tryptanthrin-loaded nano-micelles were obtained using solvent evaporation method,the solubility of tryptanthrin in water was improved to 1.625mmol·L^-1.Tryptanthrin-loaded nano-micelles improved its solubility,which laid a foundation for the research of improving its bioavailability.
出处
《西北药学杂志》
CAS
2016年第3期277-281,共5页
Northwest Pharmaceutical Journal
基金
国家自然科学基金项目(编号:81271687)
