摘要
目的制备载姜黄素两亲性星状聚酯纳米粒,并对其理化特性、毒性及体外释药性能进行初步研究。方法通过开环聚合法制备两亲性星状聚酯(PET-PCL)作为药物载体,通过MTT比色法检测材料毒性。采用微通道界面沉淀法制备载药纳米粒,单因素考察实验筛选最优工艺;动态光散射法(DLS)测定粒径及其分布;紫外分光光度法测定其包封率和载药量;透析法测定其体外释放特性。结果姜黄素纳米粒(Cur-NPs)制备的最佳工艺:水相流速为0.5 m L·min^(-1),脂相流速为0.5 m L·min^(-1),水相质量浓度为1.0 mg·m L^(-1),脂相质量浓度为6.0 mg·m L^(-1),药物质量浓度为0.6 mg·m L^(-1)。纳米粒粒径为(180.3±4.05)nm,分布指数为(0.060±0.055 1),Zeta电位为(^(-1)2.1±1.04)m V,包封率为(90.12±0.824)%,载药量为(4.40±0.080)%,96 h释药期内累积释药率为(72.89±3.001)%,PET-PCL与L929细胞共培后细胞存活率为(81.05±1.223)%。结论该方法制备的载姜黄素两亲性星状聚酯纳米粒简便可行,具有较好的控释效果,在药物递送领域具有潜在的应用价值。
OBJECTIVE To prepare the cureumin-loaded amphiphilic star-shaped polyester nanoparticles（Cur-NPs） and evaluate its physieoehemieal property, toxicity and release behavior in vitro. METHODS Poly （pentaerythrotol）-poly （e-Caprolaetone） （ab- breviated as PET-PCL） , a new amphiphilie star-shaped poly ester material, as drug carrier was successfully synthesized by ring-open- ing polymerization. The toxicity of PET-PCL was determined by MTT method. Drug-loading nanopartieles were prepared by microchan- nel interface precipitation, and the optimal prescription was screened by single factor experiment. The particle size and the particle dis- persion index was measured by dynamic light scattering（DLS） techniques. The encapsulation efficiency and drug loading content were determined by UV spectrophotometry. The in vitro release behavior was investigated by dynamic dialysis. RESULTS The optimal preparation for nanoparticles was listed as follows： water flow rate was 0. 5 mL ·min-l , lipid phase flow rate was 0. 5 mL· min-1 , a- queous phase concentration was 1 mg · mL- 1 , lipid phase concentration was 6. 0 mg· mL- 1, and drug concentration was 0. 6 mg · mL-1. The particle size was （180. 3 ±4. 05） nm, the Zeta potential was （ -12. 1 ± 1.04）mV; drug encapsulation efficiency was （90. 12±0. 824）% ; drug loading content was （4. 40 ± 0. 080）% ; the amount of cumulated drug released in 96 h was （72.89 ± 3. 001 ） %. Survival rate of L929 cells with PET-PCL were （ 81.05 ± 1. 223） %. CONCLUSION The curcumin-loaded amphiphilic star-shaped polyester nanoparticles prepared by this method are simple and feasible, and have a better controlled release property, have potential application value in the field of drug delivery.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2018年第2期114-121,共8页
Chinese Pharmaceutical Journal
基金
国家自然科学基金资助项目(21376223)
关键词
姜黄素
微通道界面沉淀法
纳米粒
体外释放
curcumin
microchannel interface precipitation method
nanoparticle
in vitro release
