包载替莫唑胺和索拉非尼PLGA纳米粒的制备及评价

Development and characterization of temozolomide and sorafenib-loaded PLGA nanoparticles

目的制备替莫唑胺和索拉非尼PLGA纳米粒,并对其粒径、形貌、稳定性及体外释放进行考察,探讨其是否可用于抗脑胶质瘤的体内体外研究。方法纳米沉淀法制备替莫唑胺索拉和索拉非尼PLGA纳米粒,测定粒径、电位、形貌、包封率和载药量以及稳定性。结果所得纳米粒的平均粒径为(106.71±0.21)nm、多分散系数为(0.24±0.05),电位(-27.30±1.20)mV,纳米粒呈规则的球状均匀分布,大小均一,表面光滑;PLGA纳米粒中替莫唑胺的包封率及载药量分别为(75.89±3.12)%、(3.61±0.78)%;索拉非尼的包封率及载药率分别为(48.61±1.20)%、(1.50±0.98)%。结论采用纳米沉淀法制备的PLGA纳米粒,呈球形形貌、粒径分布均匀、有良好的稳定性,可用于抗脑胶质瘤的体内体外研究。

Objective To prepare polylactic acid-glycolic acid(PLGA)nanoparticles loaded with temozolomide combined with sorafenib,and to investigate their particle size,morphology,stability and in vitro release,and to explore whether they can be used for in vitro and in vivo studies of anti-glioma.Methods Temozolomide and sorafenib-PLGA nanoparticles were prepared by nano precipitation method.We characterized the pharmaceutical and biological properties of the nanoparticles,including particle size,potential,morphology,encapsulation rate,drug loading and stability were determined.Results The average size of the nanoparticles was(106.71±0.21)nm,the polymer dispersity index was(0.14±0.05),and the Zeta potential was(-27.30±1.20)mV.The nanoparticles showed regular spherical uniform distribution,uniform size and smooth surface.The encapsulation rate and drug loading of temozolomide in PLGA nanoparticles were(75.89±3.12)%and(3.61±0.78)%,respectively.The encapsulation rate and drug loading rate of sorafenib were(48.61±1.20)%and(1.50±0.98)%,respectively.Conclusion The PLGA nanoparticles prepared by nanoprecipitation method,shows spherical shape and uniform size distribution and good stability with high drug loading and entrapment efficiencies,which can be used for in vitro and in vivo anti-glioma research.