| Influence of penetration enhancers on topical delivery of 5-aminolevulinic acid from bioadhesive patches. | |
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MedLine Citation:
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PMID: 20636855 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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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:
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Type: Journal Article |
Journal Detail:
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Title: The Journal of pharmacy and pharmacology Volume: 62 ISSN: 2042-7158 ISO Abbreviation: J. Pharm. Pharmacol. Publication Date: 2010 Jun |
Date Detail:
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Created Date: 2010-07-19 Completed Date: 2010-10-26 Revised Date: 2011-09-13 |
Medline Journal Info:
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Nlm Unique ID: 0376363 Medline TA: J Pharm Pharmacol Country: England |
Other Details:
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Languages: eng Pagination: 685-95 Citation Subset: IM |
Affiliation:
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School of Pharmacy, Queen's University Belfast, Medical Biology Centre, 97 Lisburn Road, Belfast, UK. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Adhesiveness Administration, Cutaneous Aminolevulinic Acid / administration & dosage*, pharmacokinetics Animals Excipients / chemistry* Female Mice Mice, Inbred BALB C Mice, Nude Photosensitizing Agents / administration & dosage*, pharmacokinetics Skin Absorption* Swine |
| Chemical | |
Reg. No./Substance:
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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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