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胡椒堿-壳聚糖包被脂质体的配方:特性描述和体外细胞毒性评价。

Formulation of Piperine-Chitosan-Coated Liposomes: Characterization and In Vitro Cytotoxic Evaluation.

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

Central Laboratory, Research Center, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia.

出版信息

Molecules. 2021 May 29;26(11):3281. doi: 10.3390/molecules26113281.

Abstract

The present research work is designed to prepare and evaluate piperine liposomes and piperine-chitosan-coated liposomes for oral delivery. Piperine (PPN) is a water-insoluble bioactive compound used for different diseases. The prepared formulations were evaluated for physicochemical study, mucoadhesive study, permeation study and in vitro cytotoxic study using the MCF7 breast cancer cell line. Piperine-loaded liposomes (PLF) were prepared by the thin-film evaporation method. The selected liposomes were coated with chitosan (PLFC) by electrostatic deposition to enhance the mucoadhesive property and in vitro therapeutic efficacy. Based on the findings of the study, the prepared PPN liposomes (PLF3) and chitosan coated PPN liposomes (PLF3C1) showed a nanometric size range of 165.7 ± 7.4 to 243.4 ± 7.5, a narrow polydispersity index (>0.3) and zeta potential (-7.1 to 29.8 mV). The average encapsulation efficiency was found to be between 60 and 80% for all prepared formulations. The drug release and permeation study profile showed biphasic release behavior and enhanced PPN permeation. The in vitro antioxidant study results showed a comparable antioxidant activity with pure PPN. The anticancer study depicted that the cell viability assay of tested PLF3C2 has significantly ( < 0.001)) reduced the IC when compared with pure PPN. The study revealed that oral chitosan-coated liposomes are a promising delivery system for the PPN and can increase the therapeutic efficacy against the breast cancer cell line.

摘要

本研究工作旨在制备和评价胡椒碱脂质体和胡椒碱-壳聚糖包被脂质体用于口服给药。胡椒碱(PPN)是一种水溶性生物活性化合物,用于治疗不同的疾病。所制备的制剂进行了理化性质研究、粘膜粘附研究、渗透研究和体外细胞毒性研究,使用 MCF7 乳腺癌细胞系。胡椒碱负载脂质体(PLF)通过薄膜蒸发法制备。选择的脂质体通过静电沉积用壳聚糖(PLFC)包被,以增强粘膜粘附性和体外治疗效果。根据研究结果,所制备的 PPN 脂质体(PLF3)和壳聚糖包被的 PPN 脂质体(PLF3C1)显示出纳米尺寸范围为 165.7 ± 7.4 至 243.4 ± 7.5,较窄的多分散指数(>0.3)和zeta 电位(-7.1 至 29.8 mV)。所有制备的制剂的平均包封效率在 60%到 80%之间。药物释放和渗透研究结果显示,具有双相释放行为和增强的 PPN 渗透。体外抗氧化研究结果表明,与纯 PPN 相比,具有相当的抗氧化活性。抗癌研究表明,与纯 PPN 相比,测试的 PLF3C2 的细胞活力测定显著(<0.001)降低了 IC。该研究表明,口服壳聚糖包被的脂质体是 PPN 的一种有前途的递药系统,可以提高对乳腺癌细胞系的治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0c1/8198173/57ff823b3d5e/molecules-26-03281-g001.jpg

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