Fang Yi-Ping, Tsai Yi-Hung, Wu Pao-Chu, Huang Yaw-Bin
Graduate Institute of Pharmaceutical Sciences, College of Pharmacy, Kaohsiung Medical University, Kaohsiung, Taiwan.
Int J Pharm. 2008 May 22;356(1-2):144-52. doi: 10.1016/j.ijpharm.2008.01.020. Epub 2008 Jan 19.
Topical photodynamic therapy (PDT) with 5-aminolevulinic acid (ALA) is an alternative therapy for many non-melanoma skin cancers. The major limitation of this therapy, however, is the low permeability of ALA through the stratum corneum (SC) of the skin. The objective of the present work was to characterize ethosomes containing ALA and to enhance the skin production of protoporphyrin IX (PpIX), compared to traditional liposomes. Results showed that the average particle sizes of the ethosomes were less than those of liposomes. Moreover, the entrapment efficiency of ALA in the ethosome formulations was 8-66% depending on the surfactant added. The particle size of the ethosomes was still approximately <200 nm after 32 days of storage. An in vivo animal study observed the presence of PpIX in the skin by confocal laser scanning microscopy (CLSM). The results indicated that the penetration ability of ethosomes was greater than that of liposomes. The enhancements of all the formulations were ranging from 11- to 15-fold in contrast to that of control (ALA in an aqueous solution) in terms of PpIX intensity. In addition, colorimetry detected no erythema in the irradiated skin. The results demonstrated that the enhancement ratio of ethosome formulations did not significantly differ between the non-irradiated and irradiated groups except for PE/CH/SS, which may have been due to a photobleaching effect of the PDT-irradiation process.
外用5-氨基酮戊酸(ALA)光动力疗法(PDT)是许多非黑素瘤皮肤癌的替代疗法。然而,该疗法的主要局限性在于ALA透过皮肤角质层(SC)的渗透性较低。本研究的目的是对含ALA的醇质体进行表征,并与传统脂质体相比,提高皮肤中原卟啉IX(PpIX)的生成。结果表明,醇质体的平均粒径小于脂质体。此外,根据添加的表面活性剂不同,ALA在醇质体制剂中的包封率为8%-66%。储存32天后,醇质体的粒径仍约<200 nm。一项体内动物研究通过共聚焦激光扫描显微镜(CLSM)观察到皮肤中存在PpIX。结果表明,醇质体的渗透能力大于脂质体。就PpIX强度而言,与对照组(ALA水溶液)相比,所有制剂的增强倍数在11至15倍之间。此外,比色法检测到照射皮肤无红斑。结果表明,除PE/CH/SS外,非照射组和照射组醇质体制剂的增强率无显著差异,这可能是由于PDT照射过程的光漂白效应所致。