植物乳糜微粒作为木樨草素靶向肝癌的双重纳米载体：体外评价与药效学。
Phytochylomicron as a dual nanocarrier for liver cancer targeting of luteolin: in vitro appraisal and pharmacodynamics.
机构信息
Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy & Drug Manufacturing, Pharos University in Alexandria, Alexandria, Egypt.
出版信息
Nanomedicine (Lond). 2018 Jan;13(2):209-232. doi: 10.2217/nnm-2017-0220. Epub 2017 Dec 4.
AIM
A novel luteolin (LUT) loaded dual bionanocarrier 'phytochylomicron' was elaborated to allow LUT injectable delivery and liver cancer targeting.
METHODS
LUT-phospholipid complex was prepared and loaded into chylomicron nanocarrier. Then phytochylomicron underwent physicochemical characterization, cell culture and pharmacodynamics studies on a new liver-tumor model.
RESULTS
Phytochylomicron showed sustained release pattern with minimum drug leakage until reaching the liver. Cell culture studies showed high growth inhibition of Hep G2 cells with 2.6-fold enhancement in cellular uptake. Pharmacodynamics demonstrated enhanced tumor growth inhibition (sixfold) with a significant tumor size reduction. Finally, cell culture results demonstrated an excellent correlation with pharmacodynamics confirming the obtained findings.
CONCLUSION
A novel phytochylomicron nanosystem was successfully elaborated with promising characteristics that promoted injectable LUT delivery and liver cancer targeting. [Formula: see text].
目的
研制了一种新型的叶黄素（LUT）负载双仿生纳米载体“植物乳糜微粒”，以实现 LUT 的可注射递药和肝癌靶向。
方法
制备 LUT-磷脂复合物并将其载入乳糜微粒纳米载体中。然后对植物乳糜微粒进行理化性质表征、细胞培养和新的肝癌模型药效学研究。
结果
植物乳糜微粒呈现出最小药物泄漏的持续释放模式，直到到达肝脏。细胞培养研究表明，Hep G2 细胞的生长抑制率很高，细胞摄取增加了 2.6 倍。药效学研究表明，肿瘤生长抑制增强了六倍，肿瘤体积显著缩小。最后，细胞培养结果与药效学结果具有极好的相关性，证实了所得结果。
结论
成功研制了一种具有良好特性的新型植物乳糜微粒纳米系统，促进了 LUT 的可注射递药和肝癌靶向。
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