Novel perspectives in the tuberculosis treatment: Administration of isoniazid through the skin

International Journal of Pharmaceutics
Thiago CaonMarcos Antônio Segatto Silva

Abstract

Despite its high efficacy in anti-tuberculosis therapy, the oral administration of isoniazid (INH) may lead to poor patient compliance due to hepatotoxicity events. In this context, the transdermal administration of INH was evaluated, for the first time, since this route avoids hepatic first pass effect. INH was applied to porcine skin in Franz diffusion chambers alone and with 5% menthol, limonene or Transcutol(®). Infrared and DSC analyses were selected for mechanistic studies. The transdermal absorption of INH was sufficient to ensure a systemic therapeutic effect. Menthol was not able to improve the absorption of INH, but it increased the drug accumulation in skin compared to the control (1.4-fold). Transcutol(®) reduced permeation flux of INH (2.2-fold) and also increased the amount of drug retained in skin (1.7-fold). Limonene was the most effective excipient since it increased permeation flux of INH (1.5-fold) and lag time was greatly shortened (2.8-fold). DSC and FTIR analyses of limonene-treated skin suggest higher degree of disorder in lipid bilayers. Transdermal delivery of INH was positively correlated with logP of chemical enhancers. INH can be efficiently delivered by skin route and specific excipients may be sele...Continue Reading

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Citations

May 28, 2016·AAPS PharmSciTech·Thiago CaonMarcos Antônio Segatto Silva
Aug 3, 2017·Photodermatology, Photoimmunology & Photomedicine·Haritima JoshiSrinivas Mutalik
Jul 20, 2018·Advanced Pharmaceutical Bulletin·Tasnuva Haque, Md Mesbah Uddin Talukder
May 16, 2021·International Journal of Pharmaceutics·Matheus Aparecido Dos Santos RamosMarlus Chorilli
Jun 3, 2021·International Journal of Environmental Research and Public Health·Afzal HussainMohammad A Almaniea
Sep 4, 2021·Drug Delivery and Translational Research·Lijuan ZengWenting Song

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