[关键词]
[摘要]
目的 制备载和厚朴酚(HK)介孔二氧化硅(MSN)包覆聚吡咯纳米粒(PPy@MSN-HK),考察其体外释放特性。方法 首先制备聚吡咯纳米粒,然后在其表面包裹MSN壳层,再吸附HK,即得PPy@MSN-HK。依次从透射电镜图、粒径、Zeta电位、载药量、包封率、红外光谱分析、体外光热研究及体外释放度等方面进行评价,采用相似因子(f2)法分析释放曲线,并运用多种常用数学模型拟合溶出曲线。结果 透射电镜图显示,制备的MSN包覆聚吡咯纳米粒(PPy@MSN)粒径大小均一,分布均匀,平均粒径为(220.4±4.2)nm,多分散系数为0.042±0.010,Zeta电位为(-21.1±0.8)mV,载药量为(2.58±0.53)%,包封率为(75.04±0.95)%。体外光热实验结果表明,在照射激光功率密度不变的情况下,随着纳米粒质量浓度逐渐增大,纳米粒混悬液温度变化值明显增大,说明PPy@MSN具有良好的光热效应。体外释放实验表明,PPy@MSN-HK与HK原料药的释放曲线不相似,分别以Ritger-Peppas、Logistic方程拟合最佳。原料药释放曲线最接近Ritger-Peppas方程(R2=0.997 32);PPy@MSN-HK释放曲线用Logistic方程拟合最好(R2=0.997 88)。结论 采用水溶液法成功制备了PPy@MSN-HK,为肿瘤治疗提供新的给药策略。
[Key word]
[Abstract]
Objective To prepare a mesoporous silica-coated polypyrrole nanoparticles loaded with honokiol (PPy@MSN-HK) and evaluate their in vitro release behavior.Methods In this study, PPy@MSN-HK was obtained in three steps:First, prepared polypyrrole nanoparticles;Second, coated mesoporous silica shell on its surface;Third, absorbed honokiol.The TEM, particle size, zeta potential, drug loading, infrared spectroscopy, in vitro photothermal properties, and in vitro release characteristics were chosen as indexes to investigate its potential as antitumor nanocarries.The release profiles were analyzed by simulating factor (f2), and the dissolution profiles were fitted by a variety of commonly used mathematical models.Results The results showed that the prepared nanoparticles had uniform particle size and uniform size distribution.The average particle size was (220.4±4.2) nm, polydispersity coefficient was 0.042±0.010, zeta potential was (-21.1±0.8) mV, drug loading was (2.58±0.53)%, and entrapment efficiency was (75.04±0.95)%, respectively.The results of in vitro photothermal experiments showed that with the constant laser power density, the temperature change value of nanoparticles suspension increased with the increase of nanoparticles concentration.This showed that PPy@MSN have a good photothermal effect.In vitro release test revealed that the two release curves were not similar, and fitting best with Ritger-Peppas eqution and Logistic eqution respectively.Conclusion The water solution method could be used to prepare PPy@MSN, which may provide a promising drug delivery strategy for tumor treatment.
[中图分类号]
[基金项目]
重庆市自然科学基金项目(cstc2016jcyjA0068)