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用于姜黄素经皮给药的双纳米结构脂质载体/水凝胶系统

Dual Nanostructured Lipid Carriers/Hydrogel System for Delivery of Curcumin for Topical Skin Applications.

作者信息

Calderon-Jacinto Rosa, Matricardi Pietro, Gueguen Virginie, Pavon-Djavid Graciela, Pauthe Emmanuel, Rodriguez-Ruiz Violeta

机构信息

ERRMECe Laboratory, Biomaterials for Health Group, CY Cergy Paris Université, Maison Internationale de la Recherche, I MAT, 1 rue Descartes, 95031 Neuville sur Oise, France.

Department of Drug Chemistry and Technologies, Sapienza University of Rome, P.le Aldo Moro 5, 00185 Rome, Italy.

出版信息

Biomolecules. 2022 Jun 3;12(6):780. doi: 10.3390/biom12060780.

Abstract

This work focuses on the development and evaluation of a dual nanostructured lipid carrier (NLC)/Carbopol-based hydrogel system as a potential transporter for the topical delivery of curcumin to the skin. Two populations of different sized negatively charged NLCs (P1, 70-90 nm and P2, 300-350 nm) were prepared and characterized by means of dynamic light scattering. NLCs presented an ovoid platelet shape confirmed by transmission electron microscopy techniques. Curcumin NLC entrapment efficiency and release profiles were assessed by HPLC (high pressure liquid chromatography) and spectrophotometric methods. Preservation and enhancement of curcumin (CUR) antioxidant activity in NLCs (up to 7-fold) was established and cell viability assays on fibroblasts and keratinocytes indicated that CUR-NLCs are non-cytotoxic for concentrations up to 10 μM and exhibited a moderate anti-migration/proliferation effect (20% gap reduction). CUR-NLCs were then embedded in a Carbopol-based hydrogel without disturbing the mechanical properties of the gel. Penetration studies on Franz diffusion cells over 24 h in CUR-NLCs and CUR-NLCs/gels demonstrated an accumulation of CUR in Strat-M membranes of 22% and 5%, respectively. All presented data support the use of this new dual CUR-NLC/hydrogel system as a promising candidate for adjuvant treatment in topical dermal applications.

摘要

本研究聚焦于开发和评估一种基于双纳米结构脂质载体(NLC)/卡波姆的水凝胶系统,作为姜黄素经皮给药的潜在载体。制备了两种不同尺寸的带负电荷的NLC群体(P1,70 - 90纳米和P2,300 - 350纳米),并通过动态光散射进行表征。通过透射电子显微镜技术证实NLC呈卵形血小板形状。采用高效液相色谱(HPLC)和分光光度法评估姜黄素NLC的包封率和释放曲线。确定了NLC中姜黄素(CUR)抗氧化活性的保留和增强(高达7倍),对成纤维细胞和角质形成细胞的细胞活力测定表明,浓度高达10 μM时,CUR - NLC无细胞毒性,并表现出中等的抗迁移/增殖作用(间隙减少20%)。然后将CUR - NLC包埋在基于卡波姆的水凝胶中,且不影响凝胶的机械性能。在Franz扩散池上进行的24小时渗透研究表明,CUR在CUR - NLC和CUR - NLC/凝胶中的Strat - M膜中的累积量分别为22%和5%。所有呈现的数据均支持将这种新型双CUR - NLC/水凝胶系统用作局部皮肤应用辅助治疗的有前景候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/99c4/9221280/0471e9816157/biomolecules-12-00780-g001.jpg

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