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Aminolevulinic acid derivatives and liposome delivery as strategies for improving 5-aminolevulinic acid-mediated photodynamic therapy.

Abstract
Photodynamic Therapy employing 5-aminolevulinic acid (ALA) as a precursor of the photosensitizer Protoporphyrin IX has become a promising approach to treat superficial cancers. However, the hydrophilic nature of the ALA molecule somewhat limits the penetration through the skin as well as all cell membranes. Different attempts are currently under investigation to enhance ALA penetration, such as the development of new synthetic and more lipophilic molecules derived from ALA and the incorporation of ALA into lipophilic vehicles such as liposomes. Among the new synthesized molecules, we can find ALA esters, ALA aminoacid derivatives and ALA dendrimers. In general, there is consensus that the promising results obtained in vitro with ALA esters cannot be reproduced in vivo. However, ALA methyl ester (1) has been widely used for treatment of skin malignancies and ALA hexyl ester (15) proved to be more powerful than ALA in bladder imaging. ALA aminoacid derivatives have been designed to use specific cellular aminopeptidases to targeting tumors, and it was shown that they can be metabolized to ALA with some specificity.
AuthorsAdriana Casas, Alcira Batlle
JournalCurrent medicinal chemistry (Curr Med Chem) Vol. 13 Issue 10 Pg. 1157-68 ( 2006) ISSN: 0929-8673 [Print] United Arab Emirates
PMID16719777 (Publication Type: Journal Article, Review)
Chemical References
  • Esters
  • Liposomes
  • Aminolevulinic Acid
  • Aminopeptidases
Topics
  • Aminolevulinic Acid (administration & dosage, chemistry, therapeutic use)
  • Aminopeptidases (metabolism)
  • Animals
  • Esters (chemistry)
  • Humans
  • Liposomes
  • Photochemotherapy (methods)

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