探讨大麻二酚包封脂质体对其理化性质和生物相容性的影响。

IF 6.5 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Drug Delivery Pub Date : 2025-12-01 Epub Date: 2025-02-06 DOI:10.1080/10717544.2025.2460666
Inga Jurgelane, Karina Egle, Andra Grava, Dana Galkina, Margarita Brante, Maksims Melnichuks, Marite Skrinda-Melne, Girts Salms, Arita Dubnika
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引用次数: 0

摘要

大麻二酚(CBD)因其在各种情况下的治疗特性而得到认可。然而,CBD有限的水溶性和对环境胁迫的敏感性阻碍了其有效性和生物利用度。包封在药物输送系统,特别是脂质体中,提供了一个很有前途的解决方案。本研究旨在利用商用脂质二硬脂酰磷脂酰胆碱(dsc)和二棕榈酰磷脂酰胆碱(DPPC)和1,2二硬脂酰sn-甘油-3磷酸乙醇胺- n-[羰基-氨基(聚乙二醇)-4300](铵盐)(DSPE-PEG)制备含CBD的脂质体,并进行体外研究-细胞活力和CBD释放。采用薄膜水合法制备脂质体,并利用傅里叶变换红外光谱(FT-IR)、动态光散射(DLS)和扫描透射电镜(STEM)对脂质体进行了表征。DLS分析显示,CBD的掺入减少了23-53%的脂质体大小,这取决于脂质体的大小。包封效率依次为:DPPC CBD(63%)体外细胞活力实验显示空白脂质体无细胞毒性。然而,装载CBD的脂质体显著降低了含有CBD脂质体的特定类型的细胞活力。DSPE-PEG的加入提高了脂质体的包封效率和稳定性,使DSPC DSPE-PEG CBD脂质体更适合CBD的长期释放。与其他研究相比,将CBD包封在脂质体中可以提高其生物利用度,使较低浓度的CBD直接递送到细胞中,从而导致细胞活力的明显变化。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Exploring the effects of cannabidiol encapsulation in liposomes on their physicochemical properties and biocompatibility.

Cannabidiol (CBD) is recognized for its therapeutic properties in various conditions. However, CBD's limited water solubility and sensitivity to environmental stresses hinder its efficacy and bioavailability. Encapsulation in drug delivery systems, particularly liposomes, offers a promising solution. This study aims to prepare CBD-containing liposomes using commercially used lipids distearoyl phosphatidylcholine (DSPC) and dipalmitoyl phosphatidylcholine (DPPC), and 1,2 distearoyl-sn-glycero-3 phosphoethanolamine-N-[carbonyl-amino(polyethylene glycol)-4300] (ammonium salt) (DSPE-PEG) and to perform in vitro studies - cell viability and CBD release. Liposomes were synthesized using thin-film hydration method, and characterized by Fourier-transform infrared (FT-IR) spectroscopy, dynamic light scattering (DLS), and scanning transmission electron microscopy (STEM). DLS analysis revealed that CBD incorporation reduced liposome size by 23-53%, depending on the liposomes. Encapsulation efficiency followed the order: DPPC CBD (63%) < DSPC CBD (74%) < DSPC DPPC CBD (81%) < DSPC DSPE-PEG CBD (87%). CBD release profiles indicated that DPPC CBD liposomes released the highest CBD amount initially, while DSPC DSPE-PEG CBD exhibited sustained release, achieving 79% release over 504 h. In vitro cell viability tests showed that blank liposomes were non-cytotoxic. However, CBD-loaded liposomes significantly reduced cell viability for defined type of CBD containing liposomes. The inclusion of DSPE-PEG improved encapsulation efficiency and liposome stability, making DSPC DSPE-PEG CBD liposomes more suitable for long-term CBD release. Compared to other studies, encapsulation of CBD in liposomes enhances its bioavailability, allowing lower concentrations of CBD to be directly delivered to cells, resulting in observable changes in cell viability.

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来源期刊
Drug Delivery
Drug Delivery 医学-药学
CiteScore
11.80
自引率
5.00%
发文量
250
审稿时长
3.3 months
期刊介绍: Drug Delivery is an open access journal serving the academic and industrial communities with peer reviewed coverage of basic research, development, and application principles of drug delivery and targeting at molecular, cellular, and higher levels. Topics covered include all delivery systems including oral, pulmonary, nasal, parenteral and transdermal, and modes of entry such as controlled release systems; microcapsules, liposomes, vesicles, and macromolecular conjugates; antibody targeting; protein/peptide delivery; DNA, oligonucleotide and siRNA delivery. Papers on drug dosage forms and their optimization will not be considered unless they directly relate to the original drug delivery issues. Published articles present original research and critical reviews.
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