Abstract
Backgrounds Curcumin (CUR) is a low-molecular-weight polyphenolic substance obtained from the tuber part of Curcuma 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 (CC50) 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.
Highlights
Hepatitis has caused severe liver diseases and affects the worldwide population in which hepatitis C is the most common type responsible for mortality cases [1, 2]
soy phosphatidylcholine (SPC), egg phosphatidylcholine (EPC), and hydrogenated-soy phosphatidylcholine (HSPC) were from Lipoid GmbH (Germany)
Dulbecco’s modified Eagle medium (DMEM), high glucose was from GIBCO (United Kingdom)
Summary
Hepatitis has caused severe liver diseases and affects the worldwide population in which hepatitis C is the most common type responsible for mortality cases [1, 2]. Patients with hepatitis C are given drugs through various routes, including oral and parenteral delivery. Oral is preferred to parenteral for its benefits when it comes to the easy use for patient compliance. Oral drug delivery systems face major challenges to address various problems such as poor bioavailability and drug targeting [3]. A larger dose is used as compensation to achieve effective plasma drug concentration. It tends to increase the incidence of adverse effects relevant to such high doses
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