Abstract

Aiming to target vitamin D receptors (VDR) expressed in melanoma cells, vitamin D₃ functionalized hybrid lipid-polymer nanoparticles (HNP-VDs) comprising a poly(lactic-co-glycolic acid) (PLGA) core and a lipid shell composed of hydrogenated soy phosphatidylcholine (HSPC), cholesterol (CHOL) and 1,2-disteroyl-sn-glycero-3-phosphaethanolamine-N[succinyl(polyethyleneglycol)-2000 (DSPE-PEG₂₀₀₀) were synthesized. The nanocarriers were optimized to a lipid surface area coverage of 97%. In vitro drug release studies showed an initial burst release in the first 24 h followed by diffusive transport. Finally, cellular uptake experiments demonstrated that the HNP-VDs efficiently targeted B16 melanoma cells, thus resulting in a promising vehicle to deliver therapeutics for the melanoma treatment.

摘要

为了靶向在黑色素瘤细胞中表达的维生素 D 受体 (VDR)，维生素 D ₃功能化的混合脂质聚合物纳米颗粒 (HNP-VD) 包含聚（乳酸-乙醇酸共聚物）（PLGA）核和由氢化物组成的脂质壳合成了大豆磷脂酰胆碱 (HSPC)、胆固醇 (CHOL) 和 1,2-二硬脂酰-sn-甘油-3-磷酸乙醇胺-N[琥珀酰(聚乙二醇)-2000 (DSPE-PEG ₂₀₀₀ )。纳米载体经过优化，脂质表面积覆盖率为 97%。体外药物释放研究表明，在最初的 24 小时内出现初始突释，然后是扩散运输。最后，细胞摄取实验表明，HNP-VDs 有效地靶向 B16 黑色素瘤细胞，从而为黑色素瘤治疗提供了一种有前途的载体。