School of Pharmacy, Second Military Medical University, Shanghai, PR China; Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fujian, PR China.
School of Pharmacy, Second Military Medical University, Shanghai, PR China.
Nanomedicine. 2014 Feb;10(2):371-80. doi: 10.1016/j.nano.2013.07.018. Epub 2013 Aug 20.
A novel polyethylene glycol 400 (PEG400) mediated lipid nanoemulsion as drug-delivery carrier for paclitaxel (PTX) was successfully developed. The formulation comprised a PEG400 solution of the drug (25mg/mL) that would be mixed with commercially 20% lipid emulsion to form PTX-loaded nanoemulsion (1mg/mL) prior to use. This two-vial formulation of PTX-loaded lipid nanoemulsion (TPLE) could significantly reduce extraction of reticuloendothelial system (RES) organs and increase tumor uptake, and exhibited more potent antitumor efficacy on bearing A2780 or Bcap-37 tumor nude mice compared to conventional PTX-loaded lipid nanoemulsion (CPLE). TPLE did not cause haematolysis and intravenous irritation response yet, and showed the same cytotoxicity against HeLa cells as Taxol®, and its LD50 was 2.7-fold higher than that of Taxol®, suggesting its good safety and druggability. In addition, TPLE displayed distinctly faster release of PTX, a greater proportion of PTX in phospholipids layer and a smaller share in oil phase than CPLE. From the Clinical Editor: This study demonstrates the feasibility and potential advantage of a novel PEG400-mediated two-vial formulation of lipid nanoemulsion as drug carrier for PTX in clinical application for the cancer therapy.
This team of investigators convincingly demonstrates the feasibility and potential advantage of a PEG400-mediated two-vial formulation of lipid nanoemulsion as drug carrier for PTX in cancer therapy, documenting superior safety and faster release of PTX compared to commercially available formulations.
本研究成功开发了一种新型聚乙二醇 400（PEG400）介导的脂质纳米乳液作为紫杉醇（PTX）的药物递送载体。该制剂由药物的 PEG400 溶液（25mg/mL）组成，在使用前将其与市售的 20%脂质乳液混合形成载有 PTX 的纳米乳液（1mg/mL）。这种两瓶装的载有 PTX 的脂质纳米乳液（TPLE）制剂可以显著减少网状内皮系统（RES）器官的提取，增加肿瘤摄取，并在携带 A2780 或 Bcap-37 肿瘤裸鼠的模型中显示出比传统载有 PTX 的脂质纳米乳液（CPLE）更强的抗肿瘤疗效。TPLE 尚未引起溶血和静脉刺激反应，对 HeLa 细胞的细胞毒性与 Taxol®相同，其 LD50 是 Taxol®的 2.7 倍，表明其具有良好的安全性和可药用性。此外，TPLE 显示出比 CPLE 更快的 PTX 释放、更多的 PTX 位于磷脂层和更少的 PTX 位于油相。从临床编辑的角度来看：本研究证明了一种新型的聚乙二醇 400 介导的两瓶装脂质纳米乳液制剂作为 PTX 药物载体在癌症治疗中的临床应用的可行性和潜在优势。
本研究小组令人信服地证明了一种新型的聚乙二醇 400 介导的两瓶装脂质纳米乳液制剂作为 PTX 药物载体在癌症治疗中的可行性和潜在优势，与市售制剂相比，该制剂具有更好的安全性和更快的 PTX 释放。
