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载 EGCG 的变形控释脂质体的细胞内摄取用于皮肤癌。

Intracellular uptake of EGCG-loaded deformable controlled release liposomes for skin cancer.

机构信息

School of Life and Health Sciences, Aston University, Birmingham, UK.

Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK.

出版信息

J Liposome Res. 2020 Jun;30(2):136-149. doi: 10.1080/08982104.2019.1604746. Epub 2019 May 9.

Abstract

Caucasian population groups have a higher propensity to develop skin cancer, and associated clinical interventions often present substantial financial burden on healthcare services. Conventional treatments are often not suitable for all patient groups as a result of poor efficacy and toxicity profiles. The primary objective of this study was to develop a deformable liposomal formulation, the properties of which being dictated by the surfactant Tween 20, for the dermal cellular delivery of epigallocatechin gallatein (EGCG), a compound possessing antineoplastic properties. The results demonstrated a significant ( ≤ 0.05) decrease in liposome deformability index (74 ± 8 to 37 ± 7) as Tween 20 loading increased from 0 to 10% w/w, indicating an increase in elasticity. EGCG release over 24-h demonstrated Tween 20 incorporation directly increased release from 13.7% ± 1.1% to 94.4% ± 4.9% (for 0 and 10% w/w Tween 20 respectively). Finally, we demonstrated DilC-loaded deformable liposomes were localized intracellularly within human dermal fibroblast and keratinocyte cells within 2 h. Thus, it was evident that deformable liposomes may aid drug penetration into dermal cells and would be useful in developing a controlled-release formulation.

摘要

白种人群体更倾向于患上皮肤癌,相关的临床干预措施往往会给医疗保健服务带来巨大的经济负担。由于疗效和毒性特征不佳,常规治疗方法并不适合所有患者群体。本研究的主要目的是开发一种变形脂质体配方,其特性由表面活性剂吐温 20 决定,用于将表没食子儿茶素没食子酸酯(EGCG)递送至皮肤细胞,EGCG 是一种具有抗肿瘤特性的化合物。结果表明,随着吐温 20 负载量从 0 增加到 10%w/w,脂质体变形性指数(74 ± 8 至 37 ± 7)显著(≤0.05)降低,表明弹性增加。在 24 小时内释放 EGCG 表明,吐温 20 的掺入直接增加了释放率,从 13.7% ± 1.1%增加到 94.4% ± 4.9%(分别为 0 和 10%w/w 吐温 20)。最后,我们证明了负载 DilC 的变形脂质体在 2 小时内被定位在人皮肤成纤维细胞和角质形成细胞内的细胞内。因此,很明显,变形脂质体可以帮助药物渗透到皮肤细胞中,并有助于开发控释制剂。

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