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脂质组学:亲脂性和亲水性药物静脉给药的潜在载体。

Lipomics: A Potential Carrier for the Intravenous Delivery of Lipophilic and Hydrophilic Drugs.

作者信息

Ramírez-Hernández David, Juárez-Osornio Carlos, Izquierdo-Sánchez Vanessa, Figueroa-Rodríguez Pavel A, Organista-Nava Jorge, Gómez-Gómez Yazmín, Medina Luis Alberto

机构信息

Facultad de Química, Universidad Nacional Autónoma de México, Mexico City 04510, Mexico.

Unidad de Investigación Biomédica en Cáncer INCan-UNAM, Instituto Nacional de Cancerología, Mexico City 14080, Mexico.

出版信息

Pharmaceutics. 2022 Aug 8;14(8):1651. doi: 10.3390/pharmaceutics14081651.

Abstract

In the present work, we propose the development of a novel carrier that does not need organic solvents for its preparation and with the potential for the intravenous delivery of lipophilic and hydrophilic drugs. Named lipomics, this is a mixed colloid of micelles incorporated within a liposome. This system was designed through ternary diagrams and characterized by physicochemical techniques to determine the particle size, zeta potential, shape, morphology, and stability properties. The lipomics were subjected to electron microscopy (SEM, TEM, and STEM) to evaluate their physical size and morphology. Finally, pharmacokinetic studies were performed by radiolabeling the lipomics with Technetium-99m chelated with BMEDA to evaluate the in vivo biodistribution through techniques of molecular imaging (microSPECT/CT) in rats. Radiolabeling efficiency was used to compare the encapsulation efficiency of the hydrophilic and lipophilic molecules in lipomics and liposomes. According to the results, lipomics are potentially carriers of lipophilic and hydrophilic drugs.

摘要

在本研究中,我们提出开发一种新型载体,其制备过程无需有机溶剂,具有静脉注射亲脂性和亲水性药物的潜力。这种载体名为脂质组学,是一种包裹在脂质体内的混合胶束胶体。该系统通过三元相图设计,并采用物理化学技术进行表征,以确定粒径、zeta电位、形状、形态和稳定性。脂质组学通过电子显微镜(SEM、TEM和STEM)进行评估,以确定其物理尺寸和形态。最后,通过用与BMEDA螯合的锝-99m对脂质组学进行放射性标记,在大鼠中进行药代动力学研究,以通过分子成像技术(microSPECT/CT)评估其体内生物分布。放射性标记效率用于比较脂质组学和脂质体中亲水性和亲脂性分子的包封效率。根据结果,脂质组学有可能成为亲脂性和亲水性药物的载体。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d29d/9412689/068962e1ec4a/pharmaceutics-14-01651-g001.jpg

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