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用于增强药物和化妆品成分经皮渗透的壳聚糖纳米颗粒。

Chitosan nanoparticles for enhancing drugs and cosmetic components penetration through the skin.

作者信息

Ta Quynh, Ting Jessica, Harwood Sophie, Browning Nicola, Simm Alan, Ross Kehinde, Olier Ivan, Al-Kassas Raida

机构信息

School of Pharmacy and Biomolecular Science, Faculty of Science, Liverpool John Moores University, James Parsons Building, Byrom St, Liverpool, L3 3AF, UK.

Faculty of Science, Liverpool John Moores University, James Parsons Building, Byrom St, Liverpool, L3 3AF, UK.

出版信息

Eur J Pharm Sci. 2021 May 1;160:105765. doi: 10.1016/j.ejps.2021.105765. Epub 2021 Feb 16.

DOI:10.1016/j.ejps.2021.105765
PMID:33607243
Abstract

Chitosan nanoparticles (CT NPs) have attractive biomedical applications due to their unique properties. This present research aimed at development of chitosan nanoparticles to be used as skin delivery systems for cosmetic components and drugs and to track their penetration behaviour through pig skin. CT NPs were prepared by ionic gelation technique using sodium tripolyphosphate (TPP) and Acacia as crosslinkers. The particle sizes of NPs appeared to be dependent on the molecular weight of chitosan and concentration of both chitosan and crosslinkers. CT NPs were positively charged as demonstrated by their Zeta potential values. The formation of the nanoparticles was confirmed by FTIR and DSC. Both SEM and TEM micrographs showed that both CT-Acacia and CT:TPP NPs were smooth, spherical in shape and are distributed uniformly with a size range of 200nm to 300 nm. The CT:TPP NPs retained an average of 98% of the added water over a 48-hour period. CT-Acacia NPs showed high moisture absorption but lower moisture retention capacity, which indicates their competency to entrap polar actives in cosmetics and release the encapsulated actives in low polarity skin conditions. The cytotoxicity studies using MTT assay showed that CT NPs made using TPP or Acacia crosslinkers were similarly non-toxic to the human dermal fibroblast cells. Cellular uptake study of NPs observed using live-cell imaging microscopy, proving the great cellular internalisation of CT:TPP NPs and CT-Acacia NPs. Confocal laser scanning microscopy revealed that CT NPs of particle size 530nm containing fluorescein sodium salt as a marker were able to penetrate through the pig skin and gather in the dermis layer. These results show that CT NPs have the ability to deliver the actives and cosmetic components through the skin and to be used as cosmetics and dermal drug delivery system.

摘要

壳聚糖纳米颗粒(CT NPs)因其独特的性质而具有吸引人的生物医学应用。本研究旨在开发用作化妆品成分和药物皮肤递送系统的壳聚糖纳米颗粒,并追踪其通过猪皮的渗透行为。采用离子凝胶化技术,使用三聚磷酸钠(TPP)和阿拉伯胶作为交联剂制备CT NPs。纳米颗粒的粒径似乎取决于壳聚糖的分子量以及壳聚糖和交联剂的浓度。CT NPs的Zeta电位值表明其带正电荷。通过傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)证实了纳米颗粒的形成。扫描电子显微镜(SEM)和透射电子显微镜(TEM)照片均显示,CT-阿拉伯胶和CT:TPP NPs均表面光滑、呈球形,且均匀分布,粒径范围为200nm至300nm。CT:TPP NPs在48小时内平均保留了98%的添加水分。CT-阿拉伯胶NP显示出高吸湿能力但较低的保湿能力,这表明它们能够在化妆品中包封极性活性成分,并在低极性皮肤条件下释放包封的活性成分。使用MTT法进行的细胞毒性研究表明,使用TPP或阿拉伯胶交联剂制备的CT NPs对人皮肤成纤维细胞同样无毒。使用活细胞成像显微镜观察纳米颗粒的细胞摄取研究,证明了CT:TPP NPs和CT-阿拉伯胶NP具有很强的细胞内化能力。共聚焦激光扫描显微镜显示,含有荧光素钠盐作为标记物的粒径为530nm的CT NPs能够穿透猪皮并聚集在真皮层。这些结果表明,CT NPs有能力通过皮肤递送活性成分和化妆品成分,并用作化妆品和皮肤药物递送系统。

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