摘要
目的制备载姜黄素两亲性星状聚酯纳米粒(Cur-NPs),以解决其稳定性差、生物利用度低等问题。方法通过开环聚合反应和酯化反应合成两亲性星状聚酯(DPE-PCL-m PEG)作为纳米粒的载体材料,傅立叶变换显微红外光谱(FT-IR)、1H-NMR和凝胶渗透色谱(GPC)表征确定其结构和相对分子质量。溶剂挥发法制备Cur-NPs,考察其粒径、ξ电位、载药量、包封率。对Cur-NPs进行稳定性、体外释放、材料安全性、体外抗肿瘤和细胞摄取能力考察。结果成功合成DPE-PCLm PEG,制备的Cur-NPs平均粒径为(86.00±2.01)nm,ξ电位为(-9.40±0.09)m V,包封率为(95.51±1.23)%,载药量为(5.52±0.54)%。Cur-NPs具有良好的稳定性和缓释能力。细胞毒性、细胞摄取和体外抗肿瘤实验表明,空白纳米粒(blankNPs)具有良好的生物安全性;相对于姜黄素溶液,Cur-NPs对人胶质瘤U251细胞的生长抑制作用更明显,并且具有更强的入胞能力。结论Cur-NPs理化性质理想,能有效提高药物体外生物活性,为姜黄素的临床应用提供了新的解决方案。
Objective Curcumin loaded amphiphilic star-shaped polyester nanoparticles(Cur-NPs)were prepared to improve the bioavailability of curcumin.Methods Amphiphilic star-shaped polymers(DPE-PCL-m PEG)were synthesized by ring-opening polymerization and esterification and used as the polymer precursor of nanoscale drug carrier.The structures of polymers were characterized by FT-IR spectroscopy and 1H-NMR.The molecular weights of polymers were determined via GPC.Cur-NPs were prepared by solvent evaporation.The physicochemical properties such as particle size,zeta potential,drug loading,encapsulation efficiency,stability,in vitro drug release behavior and cytotoxicity,anti-proliferation efficacy and cellular uptake of Cur-NPs were studied.Results DPE-PCL-m PEG was successfully synthesized.The particle size,ξpotential,encapsulation efficiency and drug loading of Cur-NPs was(86.00±2.01)nm,ξpotential(-9.40±0.09)mV,(95.51±1.23)%and(5.52±0.54)%,respectively.In addition,the nanoparticles exhibited good stability and sustained release ability.In vitro cytotoxicity demonstrated that blank nanoparticles(blank-NPs)had favorable biosafety.Cur-NPs exhibited stronger anti-proliferation efficacy and better cellular uptake ability against U251 cell.Conclusion Cur-NPs with ideal physicochemical properties were successfully prepared.This novel nanocarrier system can effectively improve the bioavailability of curcumin and have potential applications in drug delivery.
作者
洪伟勇
王金明
王海英
周雪峰
郭钫元
杨根生
HONG Wei-yong;WANG Jin-ming;WANG Hai-ying;ZHOU Xue-feng;GUO Fang-yuan;YANG Gen-sheng(Department of Pharmcy,Taizhou Municipal Hospital,Taizhou 318000,China;College of Pharmaceutical Sciences,Zhejiang University of Technology,Hangzhou 310032,China)
出处
《中草药》
CAS
CSCD
北大核心
2021年第8期2237-2246,共10页
Chinese Traditional and Herbal Drugs
基金
国家自然科学基金项目(22078297)
浙江省自然科学基金项目(LY19B060012)
浙江省药学会医院药学专项科研基金项目(2017ZYY28)
浙江省药学会医院药学专项科研基金项目(2016ZYY35)
台州市科技计划项目(1901ky49)。