Iontophoretic delivery of 5-aminolevulinic acid and its methyl ester using a carbopol gel as vehicle

Journal of Controlled Release : Official Journal of the Controlled Release Society
N MerclinKatarina Edsman

Abstract

The aim of this study was to evaluate a Carbopol gel as a vehicle for iontophoretic delivery of 5-aminolevulinic acid (ALA) and its methyl ester (m-ALA). The formulation was characterized rheologically and the passive diffusion of ALA and m-ALA in the gels was measured. Addition of ALA and m-ALA did not change the rheological behavior of the gel and the diffusion coefficients of ALA and m-ALA were 4.4 +/- 1.2 x 10(-6) and 3.08 +/- 0.7 x 10(-7) cm2 s(-1), respectively. The anodal iontophoretic transport of ALA and m-ALA through porcine skin in vitro was followed for 15 h at a constant current of 0.4 mA. When incorporating ALA in the gel, the steady-state was reached in 10-12 h at a flux level of approx. 65 nmol cm(-2) h(-1) compared to 2.5-4 h and a level of approximately 145 nmol cm(-2) h(-1) for m-ALA. The total amount of m-ALA delivered after 15 h of iontophoresis resulted in a six-fold enhancement over ALA delivery. Iontophoretic delivery from the gel formulation seems to be better than, or comparable to, the passive delivery from formulations commonly used clinically, in spite of the 10-20 times lower concentration of the drug in the gel formulation. The skin uptake after iontophoresis for m-ALA showed a nine-fold increase ...Continue Reading

References

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Apr 11, 2003·Photochemistry and Photobiology·Renata F V LopezRichard H Guy

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Citations

May 22, 2009·Journal of Materials Science. Materials in Medicine·Junling WangBaican Yang
Mar 25, 2011·Expert Opinion on Drug Delivery·Taís GratieriYogeshvar N Kalia
Sep 11, 2007·Journal of Pharmaceutical Sciences·Nadja Grüning, Christel Charlotte Müller-Goymann
Feb 17, 2010·International Journal of Pharmaceutics·Danielle Cristine Almeida Silva de SantanaRenata Fonseca Vianna Lopez
Nov 17, 2015·Journal of Medicinal Chemistry·José A González-DelgadoBruno Sarmento
Jan 24, 2007·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Sarika NamjoshiHeather A E Benson
Nov 17, 2004·Journal of Controlled Release : Official Journal of the Controlled Release Society·N MerclinS Engström
May 17, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·Woo-Dong JangKazunori Kataoka
Dec 2, 2010·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Guilherme M GelfusoRenata F V Lopez
Jan 20, 2010·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Luciana Mattoso Pires de Campos AraújoRenata Fonseca Vianna Lopez

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