Enhanced percutaneous permeability of diclofenac using a new U-type dilutable microemulsion

Drug Development and Industrial Pharmacy
Marina ShevachmanAmnon C Sintov

Abstract

Enhanced systemic absorption in vivo and percutaneous penetration in vitro was demonstrated after transdermal administration of diclofenac sodium formulated in U-type microemulsion. Diclofenac sodium was solubilized in a typical four-component system consisting of an oil, polyoxyethylene-10EO-oleyl alcohol (Brij 96V) as the surfactant, and 1-hexanol along water dilution line W46 (40 wt % surfactant and 60 wt % oil phase before water titration). Viscosity and small angle X-ray scattering measurements have evidenced bicontinuous structures within water fractions of 0.25 and 0.5 along the dilution line. Self-diffusion NMR studies showed that drug molecules accumulated in the interfacial film and, to some extent, dissolved in the oil. Relative to a commercial macro-emulsion cream (Voltaren Emulgel), microemulsions containing paraffin oil or isopropyl myristate increased the in vivo transdermal penetration rate of diclofenac by two order of magnitude, whereas the rat plasma levels were increased by one order of magnitude. The in vitro data obtained from excised rat skin were comparable to the in vivo results, but suffered from discrepancies from the ideal in vivo-in vitro correlation, which might be explained by optimal in vitro con...Continue Reading

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Citations

Sep 17, 2009·AAPS PharmSciTech·Adnan AzeemSushama Talegaonkar
Mar 5, 2014·Pharmaceutics·Luciana B Lopes
Jul 3, 2015·Drug Development and Industrial Pharmacy·Maha Nasr, Sameh Abdel-Hamid
Nov 19, 2008·Drug Development and Industrial Pharmacy·Adnan AzeemSushama Talegaonkar
Jun 16, 2010·Drug Development and Industrial Pharmacy·Pao-Chu WuYi-Hung Tsai
Aug 4, 2009·Journal of Colloid and Interface Science·S K MehtaK K Bhasin
May 29, 2009·Colloids and Surfaces. B, Biointerfaces·Orit AmsalemNissim Garti
Feb 12, 2010·Pharmaceutical Development and Technology·Mrunali R PatelBharat G Patel
Feb 7, 2015·International Journal of Pharmaceutics·Amnon C Sintov
Jun 20, 2016·Cellular Immunology·Karsten GogollPeter Langguth
Jun 23, 2012·Langmuir : the ACS Journal of Surfaces and Colloids·Gurpreet KaurSurinder K Mehta
Dec 23, 2016·The Journal of Physical Chemistry. B·Muhammad Faizan NazarMuhammad Zubair
Nov 29, 2020·Colloids and Surfaces. B, Biointerfaces·Eva Abramov, Nissim Garti

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