研究动态
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通过微流控方法合成和表征负载紫杉醇的聚乙二醇化脂质体。

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

发表日期:2023 Nov 06
作者: Eman Jaradat, Edward Weaver, Adam Meziane, Dimitrios A Lamprou
来源: MOLECULAR PHARMACEUTICS

摘要:

对于癌症治疗,紫杉醇 (PX) 具有一些局限性,包括溶解度有限和非靶向作用。将 PX 加载到纳米脂质体中以增强 PX 溶解度并作为药物递送系统靶向其递送,有可能克服这些限制。与其他制备脂质体的常规方法相比,微流体系统用于配制负载 PX 的聚乙二醇化脂质体。研究了改变水相和脂相之间的流速比 (FRR) 对粒径和多分散指数 (PDI) 的影响。此外,还研究了改变聚乙二醇 (PEG) 脂质比例对粒径、PDI、稳定性、包封率​​ (EE%) 和释放曲线的影响。通过动态光散射、FTIR 光谱和 AFM 分析了所得制剂的理化特性。本工作旨在利用微流控技术生产直径<200 nm、低PDI < 0.25、高均质性和可行的28天稳定性的聚乙二醇化PX负载脂质体。结果表明FRR和PEG脂质比例对空脂质体的理化特性有显着影响。在所制备的制剂中,两种制剂可产生尺寸可控、低 PDI 且稳定的脂质体,这使得它们更适合 PX 封装。两种配方的平均 EE % >90%,并且 PEG 脂质比例的变化对 EE % 略有影响;据报道,不同药物浓度下 PX 的堆积程度较高。不同 PEG 脂质比例的释放曲线有所不同。
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.