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目的制备并优化田蓟苷固体脂质纳米粒(T-SLNs),对其理化性质及体外吸收和转运进行考察。方法采用高剪切乳化超声法制备了T-SLNs,利用星点设计-效应面法(CCD-RSM)对其制备工艺进行了优化,并对其平均粒径、多分散性指数(PDI)、Zeta电位、形态、包封率及体外释放等特性进行了考察,使用Caco-2细胞模型模拟小肠上皮细胞,对T-SLNs在Caco-2细胞中的吸收和转运进行了考察。结果 T-SLNs的最佳制备工艺:药脂比(质量比)0.11,大豆卵磷脂与脂质质量比1.26,聚山梨酯-80用量50.5 mg/m L,所制备的T-SLNs外观呈球形或类球形,大小相近,分散均匀,平均粒径为(86.40±0.62)nm,PDI为0.165±0.080,Zeta电位为(-24.2±0.6)m V,包封率为(89.81±1.07)%,在磷酸盐缓冲溶液(p H 6.8)中48 h累积释放率为(98.72±1.57)%。T-SLNs在Caco-2细胞模型中的吸收和转运均高于田蓟苷组。结论高剪切乳化超声法制备T-SLNs的工艺稳定可行,制备的T-SLNs具有较小的粒径和较高的包封率,相同浓度下T-SLNs在Caco-2细胞模型中的吸收和转运均高于田蓟苷组。
Objective To prepare and optimize the thymidine solid lipid nanoparticles (T-SLNs), its physical and chemical properties and in vitro absorption and transport were investigated. Methods T-SLNs were prepared by high-shear emulsification sonication. The preparation process was optimized by CCD-RSM. The average particle size, polydispersity index (PDI) Zeta potential, morphology, entrapment efficiency and in vitro release. The Caco-2 cell model was used to simulate intestinal epithelial cells and the absorption and transport of T-SLNs in Caco-2 cells were investigated. Results The optimal preparation process of T-SLNs was as follows: the ratio of drug to lipid (mass ratio) was 0.11, the ratio of soybean lecithin to lipid was 1.26, and the dosage of polysorbate-80 was 50.5 mg / mL. The appearance of T-SLNs was spherical The average particle size was (86.40 ± 0.62) nm, the PDI was 0.165 ± 0.080, the zeta potential was (-24.2 ± 0.6) m V, the encapsulation efficiency was (89.81 ± 1.07)%, The cumulative release rate at 48 h in phosphate buffer solution (p H 6.8) was (98.72 ± 1.57)%. The uptake and transport of T-SLNs in the Caco-2 cell model were higher than those in the thymidine group. Conclusion The preparation of T-SLNs by high-shear emulsification ultrasound is stable and feasible. T-SLNs prepared by this method have smaller particle size and higher entrapment efficiency. The absorption of T-SLNs in the Caco-2 cell model at the same concentration And translocation were higher than thymidine group.