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芒果苷甘醇酯体作为一种治疗银屑病的新型潜在佐剂。

Mangiferin glycethosomes as a new potential adjuvant for the treatment of psoriasis.

机构信息

Department of Pharmacy, Pharmaceutical Technology and Parasitology, Faculty of Pharmacy, University of Valencia, Av. Vicent Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain.

Department of Pharmacy, Pharmaceutical Technology and Parasitology, Faculty of Pharmacy, University of Valencia, Av. Vicent Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain; Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat de València, Av. Vicent Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain.

出版信息

Int J Pharm. 2020 Jan 5;573:118844. doi: 10.1016/j.ijpharm.2019.118844. Epub 2019 Nov 18.

DOI:10.1016/j.ijpharm.2019.118844
PMID:31751638
Abstract

Mangiferin, a natural compound isolated from Mangifera indica L, was incorporated in glycerosomes, ethosomes and alternatively in glycerol-ethanol phospholipid vesicles (glycethosomes). Actually, only glycethosomes were able to stably incorporate the mangiferin that was loaded at increasing concentrations (2, 4, 6, 8 mg/mL). The morphology, size distribution, rheological properties, surface charge and entrapment efficiency of prepared vesicles were deeply measured. All vesicles were mainly spherical, oligolamellar, small in size (145 nm) and negatively charged (-40 mV), as confirmed by cryo-TEM observation and dynamic laser light scattering measurements. The higher concentration of mangiferin (8 mg/mL) allowed an increase of vesicle mean diameter up to ~288 nm. The entrapment efficiency was inversely proportional to the amount of loaded mangiferin. In vitro studies performed by using human abdominal skin, underlined that, the dose-dependent ability of vesicles to promote mangiferin retention in epidermis. In addition, glycethosomes were highly biocompatible and showed a strong ability to protect in vitro the fibroblasts against damages induced by hydrogen peroxide. In vivo results underlined the superior ability of mangiferin loaded glycethosomes respect to the mangiferin dispersion to promote the heal of the wound induced by TPA, confirming their potential application for the treatment of psoriasis or other skin disorders.

摘要

芒果苷是从芒果(Mangifera indica L.)中分离得到的一种天然化合物,被包封于甘油体、醇质体中,或者以替代的方式包封于甘油-乙醇磷脂囊泡(glycethosomes)中。实际上,只有 glycethosomes 能够稳定地包封芒果苷,且随着浓度的增加(2、4、6、8mg/ml)包封量也随之增加。所制备的囊泡的形态、粒径分布、流变学性质、表面电荷和包封效率都进行了深入的测量。所有囊泡主要为球形、寡层、粒径较小(145nm)且带负电荷(-40mV),这一点通过冷冻透射电子显微镜观察和动态激光光散射测量得到了证实。较高浓度的芒果苷(8mg/ml)可使囊泡平均直径增加到~288nm。包封效率与包封的芒果苷量成反比。通过使用人体腹部皮肤进行的体外研究表明,囊泡促进芒果苷在表皮中保留的能力呈剂量依赖性。此外,glycethosomes 具有高度的生物相容性,并显示出强烈的能力,可在体外保护成纤维细胞免受过氧化氢诱导的损伤。体内结果强调了负载芒果苷的 glycethosomes 相对于芒果苷分散体促进 TPA 诱导的伤口愈合的卓越能力,证实了它们在治疗银屑病或其他皮肤疾病方面的潜在应用。

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