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常规脂质体和聚乙二醇化脂质体作为……的载体

Conventional and PEGylated Liposomes as Vehicles of .

作者信息

Blanco Ian M R, Barbosa Raquel de Melo, Borges Julita M P, de Melo Silvio A B Vieira, El-Bachá Ramon Dos Santos, Viseras César, Severino Patricia, Sanchez-Lopez Elena, Souto Eliana B, Cabral-Albuquerque Elaine

机构信息

Industrial Engineering Program, Polytechnic School, Federal University of Bahia, Salvador 40210-630, Bahia, Brazil.

Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Granada, Campus of Cartuja s/n, 18071 Granada, Spain.

出版信息

Pharmaceutics. 2023 Feb 16;15(2):671. doi: 10.3390/pharmaceutics15020671.

Abstract

Traditional medicine uses resin oils extracted from plants of the genus for several purposes. Resin oils are being studied to understand and profile their pharmacological properties. The aim of this work was to prepare and to characterize conventional and pegylated liposomes incorporating resin oils or the hexanic extract obtained from (copaiba) leaves. The cytotoxic effect of these products was also investigated. Conventional and stealth liposomes with copaiba extract showed similar average diameters (around 126 nm), encapsulation efficiencies greater than 75% and were stable for 90 days. A cytotoxicity test was performed on murine glioma cells and the developed liposomes presented antiproliferative action against these cancer cells at the average concentration of 30 μg/mL. Phytochemicals encapsulated in PEGylated liposomes induced greater reduction in the viability of tumor cells. In addition, bioassay-s measured the cytotoxicity of copaiba resin oil () in liposomes (conventional and PEGylated), which was also checked against pheochromocytoma PC12 cells. Its safety was verified in normal rat astrocytes. The results indicate that liposomes encapsulating copaiba oil showed cytotoxic activity against the studied tumor strains in a dose-dependent fashion, demonstrating their potential applications as a chemotherapeutic bioactive formulation.

摘要

传统医学将从 属植物中提取的树脂油用于多种用途。目前正在对树脂油进行研究,以了解其药理特性并进行剖析。这项工作的目的是制备并表征包裹树脂油或从 (苦配巴)叶中获得的己烷提取物的常规脂质体和聚乙二醇化脂质体。还研究了这些产品的细胞毒性作用。含有苦配巴提取物的常规脂质体和隐形脂质体显示出相似的平均直径(约126 nm),包封率大于75%,并且在90天内稳定。对小鼠胶质瘤细胞进行了细胞毒性测试,所制备的脂质体在平均浓度为30 μg/mL时对这些癌细胞呈现出抗增殖作用。包裹在聚乙二醇化脂质体中的植物化学物质能更大程度地降低肿瘤细胞的活力。此外,生物测定法测定了脂质体(常规脂质体和聚乙二醇化脂质体)中苦配巴树脂油( )的细胞毒性,同时也对嗜铬细胞瘤PC12细胞进行了检测。在正常大鼠星形胶质细胞中验证了其安全性。结果表明,包裹苦配巴油的脂质体对所研究的肿瘤菌株显示出剂量依赖性的细胞毒性活性,证明了它们作为化疗生物活性制剂的潜在应用价值。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4f52/9960246/c611708823ab/pharmaceutics-15-00671-g001.jpg

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