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目的评价载O-(氯乙酰-氨甲酰基)烟曲霉醇(TNP-470)甲氧基聚乙二醇-聚乳酸(mPEG-PLA)纳米粒的载药量、包封率、粒径、电位、形态、体外释放及活性。方法采用单乳法制备载TNP-470的mPEG-PLA纳米粒,透射电镜观察纳米粒形态,马尔文激光粒度仪测定其粒径分布及Zeta电位,高效液相色谱仪(HPLC)法测定纳米粒包封率、载药量及体外释药特性;CCK-8试剂盒检测对人脐静脉内皮细胞(HUVEC)的细胞毒作用;细胞划痕试验检测对HUVEC细胞迁移力的影响。结果制备的载TNP-470纳米粒为类球形,平均粒径131.25nm,Zeta电位-14.17mV,包封率66.24%,载药量3.31%,制剂72h体外累计释药百分率为60.15%,细胞增殖和划痕实验表明载TNP-470纳米粒能够显著抑制HUVEC细胞的增殖和迁移。结论对难溶性不稳定药物TNP-470制得的纳米粒具有合适的粒径及包封率,可提高其在水相中的浓度,并达到缓释作用,同时保留有原有的生物活性。
OBJECTIVE To evaluate the drug loading, entrapment efficiency, and particle size of mPEG-PLA nanoparticles loaded with O- (chloroacetyl-carbamoyl) fumagillol (TNP-470) Potential, morphology, in vitro release and activity. Methods Monolayer method was used to prepare mPEG-PLA nanoparticles loaded with TNP-470. The morphology of nanoparticles was observed by transmission electron microscopy. The particle size distribution and Zeta potential were measured by Malvern laser particle sizer. The nanoparticles were determined by high performance liquid chromatography (HPLC) Encapsulation efficiency, drug loading and release characteristics in vitro. Cytotoxicity of CCK-8 kit to human umbilical vein endothelial cells (HUVECs) was detected. Cell scratch assay was used to determine the effect of HUVEC migration. Results The prepared nanoparticles loaded TNP-470 nanoparticles were spherical in shape with an average particle diameter of 131.25 nm, a zeta potential of -14.17 mV, an encapsulation efficiency of 66.24% and a drug loading capacity of 3.31%. The cumulative drug release percentage was 60.15% Scratch experiments showed that TNP-470 nanoparticles could significantly inhibit the proliferation and migration of HUVECs. Conclusion Nanoparticles prepared from TNP-470, a poorly soluble and unstable drug, have suitable particle size and entrapment efficiency, which can increase their concentration in the aqueous phase and achieve sustained release, while retaining the original biological activity.