Trans-ungual delivery of itraconazole hydrochloride by iontophoresis. (July 2015)

• Record Type: Journal Article
• Authors: Kushwaha, Avadhesh; Jacob, Melissa; Shiva Kumar, H. N.; Hiremath, Shobharani; Aradhya, Sacchidanand; Repka, Michael A.; Murthy, S. Narasimha
• Is Part Of: Drug development and industrial pharmacy. Volume 41:Number 7(2015:Jul.)
• Page Start: 1089
• Page End: 1094
• Publication Date: 2015-07
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmaceutical industry -- Periodicals; Drug Industry -- Periodicals; Technology, Pharmaceutical -- Periodicals; 615.05
• DOI: 10.3109/03639045.2014.927481
• Languages: English
• ISSNs: 0363-9045

Abstract

<abstract> <title>Abstract</title> <p>Itraconazole (ITR) is a potent antifungal drug. However, poor aqueous solubility limits its permeation ability across the human nail plate. Therefore, in this project, ITR was converted to hydrochloride salt (ITR-HCl) to improve its solubility and to render it amenable to iontophoresis. ITR-HCl was characterized by spectroscopic methods and antifungal efficacy was evaluated in comparison to the base. <italic>In vitro</italic> and <italic>ex vivo</italic> transport studies (passive and iontophoresis) were carried out across the porcine hoof membrane and excised human cadaver toe using two different protocols; continuous delivery of drug for 24 h and pulsed delivery of drug for 3 days (8 h/day). The antifungal efficacy of ITR-HCL was comparable to ITR. Iontophoresis was found to be more effective than passive mode of delivery of ITR-HCL. In both iontophoresis as well as passive mode of delivery, the pulsed protocol resulted in more ungual and trans-ungual delivery of drug than continuous protocol. ITR-HCL could be delivered into and across the nail plate by iontophoresis. Human cadaver toe appears to be a good model to investigate the ungual delivery of drugs.</p> </abstract>