Manconia Maria, Pendás Jehzabel, Ledón Nurys, Moreira Tomás, Sinico Chiara, Saso Luciano, Fadda Anna Maria
Dipartimento Farmaco Chimico Tecnologico, Universitá di Cagliari, Cagliari, Italy.
J Pharm Pharmacol. 2009 Apr;61(4):423-30. doi: 10.1211/jpp/61.04.0002.
The aim of this work was to investigate the anti-inflammatory activity of C-phycocyanin (C-PC) on skin inflammation after topical administration and the influence of liposomal delivery on its pharmacokinetic properties.
Liposomes of different size and structure were prepared with different techniques using soy phosphatidylcholine and cholesterol. Vesicular dispersions were characterised by transmission electron microscopy, optical and fluorescence microscopy for vesicle formation and morphology, dynamic laser light scattering for size distribution, and Zetasizer for zeta-potential. C-PC skin penetration and permeation experiments were performed in vitro using vertical diffusion Franz cells and human skin treated with either free or liposomal drug dispersed in a Carbopol gel.
The protein was mainly localised in the stratum corneum, while no permeation of C-PC through the whole skin thickness was detected. Two percent C-PC-encapsulating liposomes showed the best drug accumulation in the stratum corneum and the whole skin, higher than that of the corresponding free 2% C-PC gel. Moreover, skin deposition of liposomal C-PC was dose dependent since skin accumulation values increased as the C-PC concentration in liposomes increased. The topical anti-inflammatory activity of samples was evaluated in vivo as inhibition of croton oil-induced or arachidonic acid-induced ear oedema in rats.
The results showed that C-PC can be successfully used as an anti-inflammatory drug and that liposomal encapsulation is effective in improving its anti-inflammatory activity.
本研究旨在探讨藻蓝蛋白(C-PC)局部给药后对皮肤炎症的抗炎活性以及脂质体递送对其药代动力学性质的影响。
采用不同技术,以大豆磷脂酰胆碱和胆固醇制备不同大小和结构的脂质体。通过透射电子显微镜、光学显微镜和荧光显微镜对囊泡形成和形态进行表征,利用动态激光光散射测定粒径分布,使用Zetasizer测定zeta电位。采用垂直扩散Franz细胞和用人皮肤进行体外C-PC皮肤渗透和透过实验,皮肤分别用分散在卡波姆凝胶中的游离或脂质体药物处理。
该蛋白主要定位于角质层,未检测到C-PC透过全层皮肤。2%包封C-PC的脂质体在角质层和全层皮肤中显示出最佳的药物蓄积,高于相应的游离2% C-PC凝胶。此外,脂质体C-PC的皮肤沉积呈剂量依赖性,因为随着脂质体中C-PC浓度的增加,皮肤蓄积值升高。通过抑制巴豆油诱导或花生四烯酸诱导的大鼠耳部水肿,在体内评估样品的局部抗炎活性。
结果表明,C-PC可成功用作抗炎药物,脂质体包封可有效提高其抗炎活性。