摘要
目的本研究旨在制备载GNA与PLHSpT的脂质立方液晶纳米粒[Cubs-(GNA+PLHSpT)],并对其理化性质及体外药效学进行研究。方法采用高温乳化蒸发-低温固化法制备同时包裹GNA与PLHSpT的脂质立方液晶纳米粒[Cubs-(GNA+PLHSpT)],通过单因素考察与正交试验等确定最优处方。利用DLS、TEM、DSC、体外释放等体外表征最优处方下[Cubs-(GNA+PLHSpT)]的外观形貌、粒径、粒径分布、Zeta电位、稳定性、包封率、体外释放曲线及累积释放率等物理性质,MTT法检测[Cubs-(GNA+PLHSpT)]对SK-BR-3细胞增殖的抑制作用。结果最优处方下的[Cubs-(GNA+PLHSpT)]平均粒径为(133.7±0.57)nm,多分散系数PDI为(0.171±0.01),Zeta电位为(-12.40±0.41)mV,GNA和PLHSpT包封率分别为(89.70±0.39)%和(87.74±0.71)%,透射电镜显示最优处方下的[Cubs-(GNA+PLHSpT)]呈球形或者类球形,表面无黏连,对SK-BR-3细胞的IC50值为(3.46±0.11)μg·mL^(-1)。结论最优处方下的[Cubs-(GNA+PLHSpT)]粒径分布均匀,药物包封率高,有明显的缓释效果且具有一定的抗肿瘤效果。
Objective To prepare lipid-based cubic liquid crystalline nanoparticles loaded with GNA and PLHSpT[Cubs-(GNA+PLHSpT)]and to determine the[Cubs-(GNA+PLHSpT)]physicochemical properties and in vitro pharmacodynamics.Methods Lipid-based cubic liquid crystalline nanoparticles[Cubs-(GNA+PLHSpT)]that simultaneously encapsulated GNA and PLHSpT were prepared by the emulsification evaporation-low-temperature solidification method.The optimal prescription was determined by single factor and orthogonal test.The appearance morphology,particle size,particle size distribution,Zeta potential,encapsulation efficiency and in vitro cumulative release rate of optimal prescriptions[Cubs-(GNA+PLHSpT)]was determined by DLS,TEM,DSC and in vitro release.MTT method was used to detect the inhibitory effect of[Cubs-(GNA+PLHSpT)]on the proliferation of SK-BR-3 cells.Results The average particle size of[Cubs-(GNA+PLHSpT)]of the optimal prescription was(133.7±0.57)nm,the polydispersity coefficient PDI was(0.171±0.01),and the Zeta potential was(-12.40±0.41)mV,and the encapsulation rates of GNA and PLHSpT were(89.70±0.39)%and(87.74±0.71)%,respectively.Transmission electron microscope showed that[Cubs-(GNA+PLHSpT)]was spherical or quasi-spherical with no adhesion on the surface.The IC50 value for SK-BR-3 cells was(3.46±0.11)μg·mL-1.Conclusion The optimal prescriptions of[Cubs-(GNA+PLHSpT)]show uniform particle size distribution,high drug encapsulation efficiency,obvious sustained-release effect and certain anti-tumor effect.
作者
魏晴
林彤远
王强
王雷
陈卫东
WEI Qing;LIN Tong-yuan;WANG Qiang;WANG Lei;CHEN Wei-dong(School of Pharmacy,Anhui University of Chinese Medicine,Hefei 230012;Department of Pharmacy,Wuhu Hospital Affiliated to East China Normal University(Wuhu Second Hospital),Wuhu Anhui 241100;Key Laboratory of Traditional Chinese Medicine Compound Prescriptions of Anhui Province,Hefei 230012;Institute of Pharmaceutical Preparations,Anhui Academy of Chinese Medical Sciences,Hefei 230012)
出处
《中南药学》
CAS
2022年第2期284-290,共7页
Central South Pharmacy
基金
中华医学会临床药学分会-吴阶平医学基金会科研基金(No.LCYX-Q010)
国家自然科学基金面上项目(No.81773988,No.82073923)。
关键词
脂质立方液晶纳米粒
高温乳化-低温固化法
综合加权评分法
体外表征
抗肿瘤
lipid-based cubic liquid crystalline nanoparticles
emulsification evaporation-low temperature solidification method
comprehensive weighted scoring method
in vitro characterization
antitumor
