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KMID : 0984920100120010121
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Journal of Skin Barrier Research
2010 Volume.12 No. 1 p.121 ~ p.121
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Enhancing Transdermal Delivery of 5-aminolevulinic Acid with Transferosome Using Phospholipids, Lyso-phospholipids and Surfactants
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Han In-Sook
Kim Moon-Kyu
Kim Jeong-Chul
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Abstract
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Photdynamic therapy (PDT) using topical application of 5-aminolevulinic acid (ALA) has been widely applied for the treatment of neoplatic and non-neoplastic cutaneous diseases, including basal cell carcinomas, solar keratosis, psoriasis and acne vulgaris. Since ALA is highly acidic and hydrophilic molecule, we have developed liposomal formulations of ALA to reduce the toxicity and enhance the percutaneous delivery of ALA, accumulating enough PpIX within a limited time to cause PDT. Three types of lipids, S75-3, S100-3, and SL80-3 were used for formulating liposome. The pH of all the liposomal ALA is 5.0~6.5 and the size is 50~200 nm. Most of liposomal formulations gave better ALA penetration than free ALA did. Among them, SL80-3 lipid including 30% of lyso-phospholipids produced excellent results compared with the diphosphatidyl phospholipids of S75- and S100-3. This pattern was proved in the delivery of ALA using Lyso-MPC and DMPC. However, mixed formulation of S75-3 and SL80-3 at the same weight ratio did not enhance the delivery of S75-3 alone and showed much less delivery than SL80-3 did. Humectants of glycerine, propyleneglycol, butyleneglycol and betaine gave little enhancing results, however transferosome system containing surfactants of Tween 20, 60, Brij 72, 76, and 78, contributed to the significant increase of the ALA delivery. Among them, transferosome using SL80-3 and Brij76 showed the best results in both ex vivo ALA delivery and in vivo PpIX biosynthesis.
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KEYWORD
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Aminolevulinic acid, Skin penetration, Transferosome
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