Disulfiram thermosensitive in-situ gel based on solid dispersion for cataract

Publication date: Available online 23 April 2018Source: Asian Journal of Pharmaceutical SciencesAuthor(s): Chunjuan Zhang, Tonghua Xu, Donglei Zhang, Wei He, Siling Wang, Tongying JiangAbstractTo improve the corneal permeability and water-solubility of disulfiram (DSF), which is an ocular drug for cataract, P188 was selected as a matrix to prepare solid dispersion of DSF (DSFSD) by hot melt method. The DSFSD was characterized by DSC, XRD, and IR, and the results suggested that DSF was amorphous in DSFSD. The DSFSD was added to borate buffer solution (BBS) contained 20% poloxamer P407 and 1.2% poloxamer P188 to form in-situ gel. In vitro and in vivo experiments revealed that DSFSD combined with in-situ gel (DSFSD/in-situ gel) increased the residence time and the amount of DSF penetrated through the corneal. The pharmacodynamics studies exhibited DSFSD/in-situ gel delayed the development of selenium-induced cataract at some content. These results investigated that DSFSD/in-situ gel as a drug delivery system can improve DSF ocular permeability.Graphical abstractDisulfiram solid dispersion was prepared by hot melt method. DSFSD/in-situ gel was also prepared through adjustment of the ratio of P407 to the P188, in-situ gel turned into semisolid at the temperature around eye and then covered the corneal. Which could increase the residence time and the amount of DSF penetrated through the corneal.
Source: Asian Journal of Pharmaceutical Sciences - Category: Drugs & Pharmacology Source Type: research