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Efficacy of a resveratrol nanoformulation based on a commercially available liposomal platform
International Journal of Pharmaceutics ( IF 5.8 ) Pub Date : 2021-09-14 , DOI: 10.1016/j.ijpharm.2021.121086
Carla Caddeo 1 , Daniela Lucchesi 2 , Xavier Fernàndez-Busquets 3 , Donatella Valenti 1 , Giuseppe Penno 2 , Anna Maria Fadda 1 , Laura Pucci 4
Affiliation  

Scalability is one of the important factors slowing down or even impeding the clinical translation of nanoparticle-based systems. The latter need to be manufactured at a high level of quality, with batch-to-batch reproducibility, and need to be stable after the manufacturing process, during long-term storage and upon clinical administration. In this study, a vesicular formulation intended for cutaneous applications was developed by the easy reconstitution of a commercially available liposomal platform. Resveratrol, a naturally occurring compound with potent antioxidant activity, and Tween80, a hydrophilic non-ionic surfactant, were included in the formulation. The physico-chemical properties of the vesicles were assessed using light scattering and cryogenic transmission electron microscopy. Nanosized (around 80 nm) spherical and elongated, unilamellar vesicles were produced, with remarkable storage stability. The incorporation of resveratrol in the vesicular system did not alter its strong antioxidant activity, as demonstrated by antioxidant colorimetric assays (DPPH and FRAP). Furthermore, the resveratrol liposomes were cytocompatible with fibroblasts and capable of protecting skin cells from oxidative stress by reducing both endogenous and chemically induced reactive oxygen species more effectively than free resveratrol. Therefore, the proposed formulation, based on the use of a commercially available liposomal platform, represents an easy-to-prepare, reproducible, up-scaled and efficient means of delivering resveratrol and potentiating its biological activity in vitro.



中文翻译:

基于市售脂质体平台的白藜芦醇纳米制剂的功效

可扩展性是减缓甚至阻碍基于纳米粒子的系统临床转化的重要因素之一。后者需要以高质量水平制造,具有批次间的重现性,并且需要在制造过程后、长期储存期间和临床给药期间保持稳定。在这项研究中,通过对市售脂质体平台的轻松重构,开发了一种用于皮肤应用的囊泡制剂。配方中包含白藜芦醇(一种具有强抗氧化活性的天然化合物)和 Tween80(一种亲水性非离子表面活性剂)。使用光散射和低温透射电子显微镜评估囊泡的物理化学性质。纳米尺寸(约 80 nm)球形和细长形,产生单层囊泡,具有显着的储存稳定性。正如抗氧化比色测定(DPPH 和 FRAP)所证明的那样,在囊泡系统中加入白藜芦醇并没有改变其强大的抗氧化活性。此外,白藜芦醇脂质体与成纤维细胞具有细胞相容性,并且能够通过比游离白藜芦醇更有效地减少内源性和化学诱导的活性氧物质来保护皮肤细胞免受氧化应激。因此,基于使用市售脂质体平台,所提出的制剂代表了一种易于制备、可重复、规模扩大且有效的白藜芦醇递送方式并增强其生物活性 正如抗氧化比色测定(DPPH 和 FRAP)所证明的那样,在囊泡系统中加入白藜芦醇并没有改变其强大的抗氧化活性。此外,白藜芦醇脂质体与成纤维细胞具有细胞相容性,并且能够通过比游离白藜芦醇更有效地减少内源性和化学诱导的活性氧物质来保护皮肤细胞免受氧化应激。因此,基于使用市售脂质体平台,所提出的制剂代表了一种易于制备、可重复、规模扩大且有效的白藜芦醇递送方式并增强其生物活性 正如抗氧化比色测定(DPPH 和 FRAP)所证明的那样,在囊泡系统中加入白藜芦醇并没有改变其强大的抗氧化活性。此外,白藜芦醇脂质体与成纤维细胞具有细胞相容性,并且能够通过比游离白藜芦醇更有效地减少内源性和化学诱导的活性氧物质来保护皮肤细胞免受氧化应激。因此,基于使用市售脂质体平台,所提出的制剂代表了一种易于制备、可重复、规模扩大且有效的白藜芦醇递送方式并增强其生物活性 白藜芦醇脂质体与成纤维细胞具有细胞相容性,并且能够通过比游离白藜芦醇更有效地减少内源性和化学诱导的活性氧物质来保护皮肤细胞免受氧化应激。因此,基于使用市售脂质体平台,所提出的制剂代表了一种易于制备、可重复、规模扩大且有效的白藜芦醇递送方式并增强其生物活性 白藜芦醇脂质体与成纤维细胞具有细胞相容性,并且能够通过比游离白藜芦醇更有效地减少内源性和化学诱导的活性氧来保护皮肤细胞免受氧化应激。因此,基于使用市售脂质体平台,所提出的制剂代表了一种易于制备、可重复、规模扩大且有效的白藜芦醇递送方式并增强其生物活性体外

更新日期:2021-09-19
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