Document Detail

Influence of penetration enhancers on topical delivery of 5-aminolevulinic acid from bioadhesive patches.
MedLine Citation:
PMID:  20636855     Owner:  NLM     Status:  MEDLINE    
OBJECTIVES: The inclusion of chemical penetration enhancers in a novel patch-based system for the delivery of 5-aminolevulinic acid (ALA) was examined in vitro and in vivo. Poor penetration of ALA has been implicated as the primary factor for low response rates achieved with topical ALA-based photodynamic therapy of thicker neoplastic lesions, such as nodular basal cell carcinomas.
METHODS: Several chemical permeation enhancers (dimethylsulfoxide, Labrafac CC, Labrafac PG and Labrafil M1944CS) were incorporated into bioadhesive patches tailored to deliver 19 mg ALA/cm(2).
KEY FINDINGS: In-vitro depth penetration studies into excised porcine skin showed that high concentrations of ALA (>9 micromol/cm(3)) could be delivered to a depth of 1.875 mm. However, inclusion of permeation enhancers did not significantly increase ALA delivery, relative to the control (P > 0.05). In-vivo studies were in strong agreement with in-vitro results, with formulations containing chemical enhancers showing no improvement in delivery compared with the control.
CONCLUSIONS: The patches designed in this work are suited to defineable ALA delivery without the need to immobilise patients for up to 6 h, as is common with the cream-under-occlusion approach. Overall, permeation enhancers were not found to markedly enhance the topical delivery of ALA. However, chemical penetration enhancers may have a greater effect on the delivery of more lipophilic ALA prodrugs, which are thought to primarily permeate the stratum corneum via the intercellular pathway.
Desmond I J Morrow; Paul A McCarron; A David Woolfson; Petras Juzenas; Asta Juzeniene; Vladimir Iani; Johan Moan; Ryan F Donnelly
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  62     ISSN:  2042-7158     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  2010 Jun 
Date Detail:
Created Date:  2010-07-19     Completed Date:  2010-10-26     Revised Date:  2011-09-13    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  England    
Other Details:
Languages:  eng     Pagination:  685-95     Citation Subset:  IM    
School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast, UK.
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MeSH Terms
Administration, Cutaneous
Aminolevulinic Acid / administration & dosage*,  pharmacokinetics
Excipients / chemistry*
Mice, Inbred BALB C
Mice, Nude
Photosensitizing Agents / administration & dosage*,  pharmacokinetics
Skin Absorption*
Reg. No./Substance:
0/Excipients; 0/Photosensitizing Agents; 106-60-5/Aminolevulinic Acid

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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