Cosco Donato, Paolino Donatella, Maiuolo Jessica, Marzio Luisa Di, Carafa Maria, Ventura Cinzia A, Fresta Massimo
Department of Health Sciences, University "Magna Græcia" of Catanzaro, Campus Universitario "S. Venuta", Viale S. Venuta, Germaneto, I-88100 Catanzaro, Italy; IRC FSH - Interregional Research Center for Food Safety & Health, University of Catanzaro "Magna Græcia", Campus Universitario "S. Venuta" - Building of BioSciences, Viale S. Venuta, I-88100 Germaneto, Catanzaro, Italy.
Department of Health Sciences, University "Magna Græcia" of Catanzaro, Campus Universitario "S. Venuta", Viale S. Venuta, Germaneto, I-88100 Catanzaro, Italy.
Int J Pharm. 2015 Jul 15;489(1-2):1-10. doi: 10.1016/j.ijpharm.2015.04.056. Epub 2015 Apr 18.
Ultradeformable liposomes represent useful formulations able to increase the skin permeation of drug compounds. In this study, resveratrol- and 5-fluorouracil-loaded ultradeformable liposomes were investigated for the potential treatment of non-melanoma skin cancer. The in vitro anticancer activity of ultradeformable liposomes was tested on human skin cancer cells through viability-, cell cycle- and apoptosis-analysis. Furthermore, we tested the percutaneous permeation of ultradeformable liposomes using human stratum corneum and viable epidermis. The co-encapsulation of resveratrol and 5-fluorouracil (multi-drug carrier) in ultradeformable liposomes improved their anticancer activity on skin cancer cells as compared to both the free drug form and the single entrapped agents. These multi-drug ultradeformable liposomes arrest cell proliferation in G1/S, thus modifying the action of 5-fluorouracil and increasing the activity of resveratrol. This effect might depend on the ultradeformable liposomes, which may accumulate in deeper skin layers, thus generating a cutaneous depot from which resveratrol and 5-fluorouracil are gradually released. Resveratrol and 5-fluorouracil co-loaded ultradeformable liposomes could be a new nanomedicine for the treatment of squamous cell carcinoma, i.e., actinic keratosis, Bowen's disease, and keratoacanthoma.
超可变形脂质体是能够增加药物化合物皮肤渗透性的有用制剂。在本研究中，对负载白藜芦醇和5-氟尿嘧啶的超可变形脂质体进行了治疗非黑素瘤皮肤癌的潜力研究。通过活力分析、细胞周期分析和凋亡分析，在人皮肤癌细胞上测试了超可变形脂质体的体外抗癌活性。此外，我们使用人体角质层和活表皮测试了超可变形脂质体的经皮渗透。与游离药物形式和单一包封药物相比，超可变形脂质体中共包封白藜芦醇和5-氟尿嘧啶（多药载体）可提高其对皮肤癌细胞的抗癌活性。这些多药超可变形脂质体使细胞增殖停滞在G1/S期，从而改变5-氟尿嘧啶的作用并增强白藜芦醇的活性。这种效应可能取决于超可变形脂质体，其可能积聚在更深的皮肤层中，从而形成一个皮肤贮库，白藜芦醇和5-氟尿嘧啶从该贮库中逐渐释放。负载白藜芦醇和5-氟尿嘧啶的共载超可变形脂质体可能是一种治疗鳞状细胞癌（即光化性角化病、鲍恩病和角化棘皮瘤）的新型纳米药物。
