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Using laser microporation to improve transdermal delivery of diclofenac: Increasing bioavailability and the range of therapeutic applications

Heinrich, Arne
Published in European journal of pharmaceutics and biopharmaceutics. 2011, vol. 78, no. 3, p. 408-14
Abstract The objective of the study was to investigate the effect of laser microporation, using P.L.E.A.S.E.® technology, on diclofenac delivery kinetics. Skin transport of diclofenac was studied from aqueous solution, propylene glycol and marketed formulations across intact and laser-porated porcine and human skins; cumulative permeation and skin deposition were quantified by HPLC. After 24h, cumulative diclofenac permeation across skins with 150, 300, 450 and 900 shallow pores (50-80 μm) was 3.7-, 7.5-, 9.2- and 13-fold superior to that across untreated skin. It was also found to be linearly dependent on laser fluence; Permeation (μg/cm(2))=11.35*Fluence (J/cm(2))+352.3; r(2)=0.99. After 24h, permeation was 539.6 ± 78.1, 934.5 ± 451.5, 1451.9 ± 151.3 and 1858.6 ± 308.5 μg/cm(2), at 22.65, 45.3, 90.6 and 135.9 J/cm(2), respectively. However, there was no statistically significant effect of laser fluence on skin deposition. Diclofenac delivery from marketed gel formulations was also significantly higher across laser-porated skins (e.g. for Solaraze, cumulative permeation after 24h across treated (900 pores/135.9 J/cm(2)) and untreated skin was 974.9 ± 368.8 and 8.2 ± 3.8 μg/cm(2), respectively. Diclofenac delivery from Solaraze across laser-porated porcine and human skins was also shown to be statistically equivalent. The results demonstrated that laser microporation significantly increased diclofenac transport from both simple and semi-solid formulations through porcine and human skin and that pore depth and pore number could modulate delivery kinetics. A similar improvement in topical diclofenac delivery in vivo may increase the number of potential therapeutic applications.
Keywords Administration, CutaneousAnimalsAnti-Inflammatory Agents, Non-Steroidal/administration & dosage/chemistry/pharmacokinetics/therapeutic useDiclofenac/administration & dosage/chemistry/pharmacokinetics/therapeutic useDrug CompoundingDrug Delivery Systems/methodsDrug StabilityEarHumansLasersSkin/metabolismSkin AbsorptionSwine
PMID: 21397689
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BACHHAV, Yogeshwar, HEINRICH, Arne, KALIA, Yogeshvar. Using laser microporation to improve transdermal delivery of diclofenac: Increasing bioavailability and the range of therapeutic applications. In: European journal of pharmaceutics and biopharmaceutics, 2011, vol. 78, n° 3, p. 408-14. doi: 10.1016/j.ejpb.2011.03.006 https://archive-ouverte.unige.ch/unige:22833

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Deposited on : 2012-09-11

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