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一种基于脂质纳米技术的环保绿色配方,用于将亲水性物质递送至皮肤,以治疗和管理色素沉着问题:熊果苷囊泡(Arbusome)。

An eco-friendly and green formulation in lipid nanotechnology for delivery of a hydrophilic agent to the skin in the treatment and management of hyperpigmentation complaints: Arbutin niosome (Arbusome).

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Eastern Mediterranean University, Famagusta, North Cyprus, Turkey.

Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran; Pharmaceutical Sciences Research Centre, Heamoglobinopathy Institute, Mazandaran University of Medical Sciences, Sari, Iran.

出版信息

Colloids Surf B Biointerfaces. 2021 May;201:111616. doi: 10.1016/j.colsurfb.2021.111616. Epub 2021 Feb 8.

DOI:10.1016/j.colsurfb.2021.111616
PMID:33618082
Abstract

The present work designed to improve the skin delivery of arbutin niosome (arbusome) was prepared via an ultrasonic technique. The arbusome formulations were optimized by investigating the effects of the cholesterol:surfactants ratio. To characterize the morphology and solid-state of arbutin in arbusome, differential scanning calorimetry, photon correlation spectroscopy, powder x-ray diffractometer, scanning electron microscopy (SEM), and attenuated total reflectance-Fourier transform infrared spectroscopy were utilized. The findings indicated that adding cholesterol incremented the arbusome's particle size. Further studies proved that the zeta potential and the size of nanoparticles can be modulated by the alterations in the ratio of cholesterol: surfactant. When the cholesterol concentration was high in the formulation, the highest entrapment efficiency was found to be approximately 44 %. Solid-state analysis showed that arbutin in the niosome was in the amorphous state. The skin permeation test indicated the greater quantities of the arbutin in skin layers and the receptor chamber for arbusome gel compared to arbutin simple gel. Furthermore, in vitro cytotoxicity test indicated no cytotoxicity for the improved formulation of niosome containing arbutin. The cell viability (HFF cell line) for niosomal formulation of arbutin was reported to be about 86 %. The formulations were examined in terms of skin irritation on Wistar rats, and non-irritancy of arbutin niosomal gels was indicated. The findings of this work discovered that the manufactured arbusome could be utilized as possible nano-vehicle for the arbutin topical delivery and might open new approaches for the treatment of hyperpigmentation complaints.

摘要

本工作旨在通过超声技术改善熊果苷的皮肤传递。通过考察胆固醇:表面活性剂比例的影响,优化了熊果苷的囊泡配方。为了表征熊果苷在囊泡中的形态和固体状态,利用差示扫描量热法、光相关光谱法、粉末 X 射线衍射仪、扫描电子显微镜(SEM)和衰减全反射傅里叶变换红外光谱法。研究结果表明,添加胆固醇会增加囊泡的粒径。进一步的研究证明,通过改变胆固醇:表面活性剂的比例,可以调节纳米粒子的zeta 电位和粒径。当配方中胆固醇浓度较高时,发现最高包封效率约为 44%。固态分析表明,熊果苷在囊泡中处于无定形态。皮肤渗透试验表明,与熊果苷简单凝胶相比,熊果苷囊泡凝胶在皮肤层和受体室中具有更多的熊果苷。此外,体外细胞毒性试验表明,含有熊果苷的囊泡改良制剂无细胞毒性。熊果苷囊泡制剂的细胞活力(HFF 细胞系)约为 86%。以 Wistar 大鼠为模型,考察了制剂的皮肤刺激性,表明熊果苷囊泡凝胶无刺激性。本研究发现,所制备的熊果苷囊泡可作为熊果苷局部传递的潜在纳米载体,并可能为治疗色素沉着提供新的方法。

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