Synthesis and Characterization of Paclitaxel-Loaded PEGylated Liposomes by the Microfluidics Method

脂质体 分散性 聚乙二醇化 聚乙二醇 粒径 PEG比率 药物输送 化学 溶解度 动态光散射 色谱法 水溶液 微流控 材料科学 化学工程 纳米技术 纳米颗粒 有机化学 物理化学 财务 工程类 经济
作者
Eman Jaradat,Edward Weaver,Adam Meziane,Dimitrios A. Lamprou
出处
期刊:Molecular Pharmaceutics [American Chemical Society]
卷期号:20 (12): 6184-6196 被引量:10
标识
DOI:10.1021/acs.molpharmaceut.3c00596
摘要

For cancer therapy, paclitaxel (PX) possesses several limitations, including limited solubility and untargeted effects. Loading PX into nanoliposomes to enhance PX solubility and target their delivery as a drug delivery system has the potential to overcome these limitations. Over the other conventional method to prepare liposomes, a microfluidic system is used to formulate PX-loaded PEGylated liposomes. The impact of changing the flow rate ratio (FRR) between the aqueous and lipid phases on the particle size and polydispersity index (PDI) is investigated. Moreover, the effect of changing the polyethylene glycol (PEG) lipid ratio on the particle size, PDI, stability, encapsulation efficiency % (EE %), and release profile is studied. The physicochemical characteristics of the obtained formulation were analyzed by dynamic light scattering, FTIR spectroscopy, and AFM. This work aims to use microfluidic technology to produce PEGylated PX-loaded liposomes with a diameter of <200 nm, low PDI < 0.25 high homogeneity, and viable 28 day stability. The results show a significant impact of FRR and PEG lipid ratio on the empty liposomes' physicochemical characteristics. Among the prepared formulations, two formulations produce size-controlled, low PDI, and stable liposomes, which make them preferable for PX encapsulation. The average EE % was >90% for both formulations, and the variation in the PEG lipid ratio affected the EE % slightly; a high packing for PX was reported at different drug concentrations. A variation in the release profiles was notified for the different PEG lipid ratios.

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