Castangia Ines, Nácher Amparo, Caddeo Carla, Valenti Donatella, Fadda Anna Maria, Díez-Sales Octavio, Ruiz-Saurí Amparo, Manconi Maria
Dept. Scienze della Vita e dell'Ambiente, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.
Dept. of Pharmacy and Pharmaceutical Technology, University of Valencia, Avda Vicente Andrés Estellés s/n, 46100-Burjassot, Valencia, Spain; Instituto de Reconocimiento Molecular y Desarrollo Tecnológico, Centro Mixto Universidad Politécnica de Valencia-Universidad de Valencia, Spain.
Acta Biomater. 2014 Mar;10(3):1292-300. doi: 10.1016/j.actbio.2013.11.005. Epub 2013 Nov 15.
In the present work biocompatible quercetin and curcumin nanovesicles were developed as a novel approach to prevent and restore skin tissue defects on chronic cutaneous pathologies. Stable and suitable quercetin- and curcumin-loaded phospholipid vesicles, namely liposomes and penetration enhancer-containing vesicles (PEVs), were prepared. Vesicles were made from a highly biocompatible mixture of phospholipids and alternatively a natural polyphenol, quercetin or curcumin. Liposomes were obtained by adding water, while PEVs by adding polyethylene glycol 400 and Oramix®CG110 to the water phase. Transmission electron microscopy, cryogenic-transmission electron microscopy and small- and wide-angle X-ray scattering showed that vesicles were spherical, oligo- or multilamellar and small in size (112-220 nm). In vitro and in vivo tests underlined a good effectiveness of quercetin and curcumin nanovesicles in counteracting phorbol ester 12-O-tetradecanoylphorbol-13-acetate (TPA) induced lesions and inflammation. Myeloperoxydase activity, used to gauge inflammation, was markedly inhibited by quercetin liposomes (59%) and curcumin liposomes and polyethylene glycol (PEG)-PEVs (∼ 68%). Histology showed that PEG-PEVs provided an extensive re-epithelization of the TPA-damaged skin, with multiple layers of thick epidermis. In conclusion, nanoentrapped polyphenols prevented the formation of skin lesions abrogating the various biochemical processes that cause epithelial loss and skin damage.
在本研究中，开发了具有生物相容性的槲皮素和姜黄素纳米囊泡，作为预防和修复慢性皮肤病变中皮肤组织缺陷的新方法。制备了稳定且合适的负载槲皮素和姜黄素的磷脂囊泡，即脂质体和含渗透增强剂的囊泡（PEV）。囊泡由磷脂与天然多酚（槲皮素或姜黄素）的高度生物相容性混合物制成。通过向水相中加水获得脂质体，而通过向水相中加入聚乙二醇400和Oramix®CG110获得PEV。透射电子显微镜、低温透射电子显微镜以及小角和广角X射线散射表明，囊泡呈球形，为寡层或多层结构，且尺寸较小（112 - 220 nm）。体外和体内试验强调了槲皮素和姜黄素纳米囊泡在对抗佛波酯12 - O - 十四酰佛波醇 - 13 - 乙酸酯（TPA）诱导的损伤和炎症方面具有良好的效果。用于评估炎症的髓过氧化物酶活性被槲皮素脂质体（59%）、姜黄素脂质体和聚乙二醇（PEG） - PEV（约68%）显著抑制。组织学显示，PEG - PEV使TPA损伤的皮肤实现了广泛的再上皮化，形成了多层厚表皮。总之，纳米包封的多酚通过消除导致上皮细胞丧失和皮肤损伤的各种生化过程，预防了皮肤病变的形成。
