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用于抗丙型肝炎病毒的载姜黄素脂质体固体凝胶的制剂设计与细胞毒性

Formulation Design and Cell Cytotoxicity of Curcumin-Loaded Liposomal Solid Gels for Anti-Hepatitis C Virus.

作者信息

Yusuf Helmy, Novitasari Erlyn K D D, Purnami Ni L W, Mahbub Adhe W, Sari Retno, Setyawan Dwi

机构信息

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Airlangga University, Jl. Mulyorejo, Surabaya 60115, Indonesia.

出版信息

Adv Pharmacol Pharm Sci. 2022 Mar 7;2022:3336837. doi: 10.1155/2022/3336837. eCollection 2022.

Abstract

BACKGROUNDS

Curcumin (CUR) is a low-molecular-weight polyphenolic substance obtained from the tuber part of species. Anti-inflammatory and anti-hepatitis C virus (HCV) activities have been associated with CUR. However, its poor aqueous solubility and low systemic bioavailability have been the challenges in improving the therapeutic efficacy of curcumin.

AIM

The study aimed to produce CUR-loaded liposomal solid gels as anti-HCV delivery systems. Parameters including the physical characteristics and the cell cytotoxicity properties were evaluated.

METHODS

The freeze-drying technique was applied to manufacture the CUR-loaded liposomal solid gels. Scanning electron microscopy (SEM), X-ray diffractometry (XRD), and differential thermal analysis (DTA) were involved to reveal the characteristics of the solid gels. Such characteristics were as follows: the morphology and the microscopic structure of the solid gels, the crystallinity structure of the curcumin, and the thermal properties of the mixtures. Furthermore, their cell cytotoxicity was investigated using a Huh7it cell line.

RESULTS

The SEM images confirmed that curcumin liposomes were intact and trapped in the solid gel matrix. The XRD data showed flat patterns diffractograms of the formulations, confirming the transformation of CUR from crystalline to amorphous form. The DTA thermograms showed a single melting endothermic peak at a higher temperature around 200°C, indicating a single-phase transition of the mixtures. The XRD and DTA data revealed the molecular dispersion of CUR in the developed formulations. The cytotoxicity data provided as cell cytotoxicity 50 (CC) for all formulations were ≥25 mg. These data confirmed that the developed liposomal solid gels were not cytotoxic to Huh7it cell line, indicating that the anti-HCV activity would be through a specific pathway and not by its toxicity.

CONCLUSION

The CUR-loaded liposomal solid gels exhibited the potential and offered an alternative dosage form to improve the therapeutic efficacy of curcumin as an anti-HCV.

摘要

背景

姜黄素(CUR)是从姜黄属植物的块茎部分获得的低分子量多酚类物质。抗炎和抗丙型肝炎病毒(HCV)活性与姜黄素有关。然而,其较差的水溶性和低全身生物利用度一直是提高姜黄素治疗效果的挑战。

目的

本研究旨在制备负载姜黄素的脂质体固体凝胶作为抗HCV递送系统。评估包括物理特性和细胞毒性特性在内的参数。

方法

采用冷冻干燥技术制备负载姜黄素的脂质体固体凝胶。通过扫描电子显微镜(SEM)、X射线衍射仪(XRD)和差示热分析(DTA)揭示固体凝胶的特性。这些特性如下:固体凝胶的形态和微观结构、姜黄素的结晶结构以及混合物的热性质。此外,使用Huh7it细胞系研究其细胞毒性。

结果

SEM图像证实姜黄素脂质体完整并被困在固体凝胶基质中。XRD数据显示制剂的衍射图谱呈平坦模式,证实姜黄素从结晶形式转变为无定形形式。DTA热重曲线在约200°C的较高温度下显示出单一的熔融吸热峰,表明混合物发生单相转变。XRD和DTA数据揭示了姜黄素在开发的制剂中的分子分散。所有制剂的细胞毒性数据以细胞毒性50(CC)表示均≥25mg。这些数据证实所开发的脂质体固体凝胶对Huh7it细胞系无细胞毒性,表明抗HCV活性将通过特定途径而非其毒性发挥作用。

结论

负载姜黄素的脂质体固体凝胶具有潜力,并提供了一种替代剂型,以提高姜黄素作为抗HCV药物的治疗效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/651f/8920649/3543c20042f7/APS2022-3336837.001.jpg

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