摘要
制备大黄素纳米结构脂质载体(emodin nanostructured lipid carriers,ED-NLC),并对其进行质量评价。依据单因素试验结果,以大黄素投药量、肉豆蔻酸异丙酯用量和乳化剂泊洛沙姆188用量为考察因素,纳米粒粒径、包封率和载药量为考察指标,采用Box-Behnken响应面法优化处方,并对最优处方制备的纳米粒进行外观形态、粒径和体外释放的考察。最终确定ED-NLC的最优处方大黄素为3.27 mg,肉豆蔻酸异丙酯为148.68 mg,泊洛沙姆188为173.48 mg。乳化-超声分散法制备ED-NLC,透射电镜观察ED-NLC呈类球形,粒度分布均匀,粒径(97.02±1.55)nm,聚合物分散系数0.21±0.01,Zeta电位(-38.96±0.65)mV,包封率90.41%±0.56%,载药量1.55%±0.01%。差示扫描量热仪(differential scanning calorimeter,DSC)结果表明大黄素可能以分子或无定形状态被包裹进纳米结构脂质载体中。体外释药具有明显的缓释特征,体外释药模型符合一级释药方程。Box-Behnken响应面法拟合模型精准可靠,最优处方制备的ED-NLC粒径分布集中,包封率高,为后续ED-NLC体内研究奠定基础。
Emodin nanostructured lipid carriers(ED-NLC)were prepared and their quality was evaluated in vitro.Based on the results of single-factor experiments,the ED-NLC formulation was optimized by Box-Behnken response surface method with the dosages of emodin,isopropyl myristate and poloxamer 188 as factors and the nanoparticle size,encapsulation efficiency and drug loading as evaluation indexes.Then the evaluation was performed on the morphology,size and in vitro release of the nanoparticles prepared by emulsification-ultrasonic dispersion method in line with the optimal formulation,i.e.,3.27 mg emodin,148.68 mg isopropyl myristate and 173.48 mg poloxamer 188.Under a transmission electron microscope(TEM),ED-NLC were spherical and their particle size distribution was uniform.The particle size of ED-NLC was(97.02±1.55)nm,the polymer dispersion index 0.21±0.01,the zeta potential(-38.96±0.65)mV,the encapsulation efficiency 90.41%±0.56%and the drug loading 1.55%±0.01%.The results of differential scanning calorimeter(DSC)indicated that emodin may be encapsulated into the nanostructured lipid carriers in molecular or amorphous form.In vitro drug release had obvious characteristics of slow release,which accorded with the first-order drug release equation.The fitting model of Box-Behnken response surface methodology was proved accurate and reliable.The optimal formulation-based ED-NLC featured concentrated particle size distribution and high encapsulation efficiency,which laid a foundation for the follow-up study of ED-NLC in vivo.
作者
韩德恩
辛玉凤
位恒超
祝侠丽
刘雅敏
田萍
HAN De-en;XIN Yu-feng;WEI Heng-chao;ZHU Xia-li;LIU Ya-min;TIAN Ping(School of Pharmacy,Henan University of Chinese Medicine,Zhengzhou 450046,China;Henan Research Center for Special Processing Technology of Chinese Medicine,Zhengzhou 450046,China;Henan Academy of Chinese Medicine,Zhengzhou 450004,China)
出处
《中国中药杂志》
CAS
CSCD
北大核心
2022年第4期913-921,共9页
China Journal of Chinese Materia Medica
基金
国家自然科学基金项目(81803740)
河南省高等学校重点科研项目(18A350007)。
