School of Life and Health Sciences, Aston University, Birmingham, UK.
Strathclyde Institute of Pharmacy and Biomedical Sciences, University of Strathclyde, Glasgow, UK.
J Liposome Res. 2020 Jun;30(2):136-149. doi: 10.1080/08982104.2019.1604746. Epub 2019 May 9.
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.
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。