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目的 :制备和表征RGD肽修饰的重组高密度脂蛋白(RGD-rHDL)载药纳米粒,考察肿瘤细胞对其摄取作用。方法 :合成RGD与载脂蛋白AⅠ(ApoAⅠ)的偶联物(RGD-ApoAⅠ),并以藤黄酸(GA)作为模型药物,采用薄膜分散法制得GA脂质体(LP-GA),再将RGDApoAⅠ与LP-GA共孵育,制备载有GA的RGD-rHDL纳米粒(RGD-rHDL-GA);随后,对RGD-rHDL-GA进行表征,且采用荧光标记示踪法,通过RGD-rHDL-香豆素-6来考察人肝癌细胞HepG2对载药RGD-rHDL纳米粒的摄取作用。结果 :制备的RGD-rHDL-GA呈现规则圆整的类球形,粒径分布均一[(110.70±3.25)nm],Zeta电位为(-39.21±0.10)mV,包封率为(92.20±0.28)%,载药量为(9.03±0.75)%,且其体外释药缓慢,稳定性良好;RGD-rHDL-香豆素-6的肿瘤细胞摄取率明显高于rHDL-香豆素-6。结论 :rHDL经RGD修饰后可有效促进所载药物进入肿瘤细胞,提高其肿瘤靶向性。
OBJECTIVE: To prepare and characterize RGD-loaded recombinant high-density lipoprotein (RGD-rHDL) drug-loaded nanoparticles for investigating the uptake of tumor cells. Methods: The RGD-Apo AI conjugate of RGD and apolipoprotein AⅠ (ApoAⅠ) was synthesized and GA liposomes (LP-GA) were obtained by using Gambogic acid (GA) RGD-rHDL-GA loaded RG-rHDL nanoparticles (RGD-rHDL-GA) were prepared by co-incubation of RGDApoAⅠ and LP-GA. RGD-rHDL-GA was then characterized by fluorescent labeling with RGD-rHDL - Coumarin-6 to Investigate the uptake of Hepatoma RGD-rHDL Nanoparticles by Human HepG2 Cells. Results: The prepared RGD-rHDL-GA showed a spherical shape with uniform distribution [(110.70 ± 3.25) nm] and Zeta potential of (-39.21 ± 0.10) mV and encapsulation efficiency of (92.20 ± 0.28) %, Drug loading was (9.03 ± 0.75)%, and its slow release in vitro, good stability; RGD-rHDL-coumarin -6 tumor cell uptake rate was significantly higher than rHDL-coumarin -6. Conclusion: RGD modified by RGD can effectively promote the entry of drugs into tumor cells and improve its tumor targeting.