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. 2018 Nov;13(6):527-535.
doi: 10.1016/j.ajps.2018.02.010. Epub 2018 Apr 23.

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

Chunjuan Zhang  1 , Tonghua Xu  1 , Donglei Zhang  2 , Wei He  2 , Siling Wang  1 , Tongying Jiang  1
Affiliations

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

Chunjuan Zhang et al. Asian J Pharm Sci. 2018 Nov.

Abstract

To 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.

Keywords: Anti-cataract; Disulfiram; In-situ gel; Permeability; Solid dispersion.

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Figures

Image, graphical abstract
Graphical abstract
Fig 1
Fig. 1
XRD patterns of DSF, P188, physical mixture and DSFSD.
Fig 2
Fig. 2
Thermol analysis of (A) DSC thermograms of DSF, P188, physical mixture and DSFSD; (B) TGA results of DSF, P188, physical mixture and DSFSD.
Fig 3
Fig. 3
IR spectrograms of DSF, P188, physical mixture and DSFSD.
Fig 4
Fig. 4
DDC cumulative amount of formulation 1:3, 1:5, 1:7 and DSF.
Fig 5
Fig. 5
(A) In vitro cumulative release for the pure drug DSF, physical mixture, DSFSD in sink conditioned release; (B) In vitro cumulative release for the pure drug DSF and DSFSD in STF.
Fig 6
Fig. 6
(A) Corrosional curves and (B) Cumulative release curves of contrast, non-BBS, BBS at initial time; (C) Corrosional stability and (D) Cumulative release stability of DSFSD/in-situ gel in 0, 1, 3, 6 month.
Fig 7
Fig. 7
Fluorescence imaging of Rhodamine B on precorneal at different time of (A) DSFSD in-situ gels group and (B) DSFSD suspensions group.
Fig 8
Fig. 8
Histopathology microscopy of the ocular tissues including the conjunctiva (A and D), the corneal (B and E) and the iris (C and F) after treatment for 7 days, (A–C) normal saline as control, (D–F) DSFSD/ in situ gel.
Fig 9
Fig. 9
Imagine of anti-cataract effect in different groups including blank control group, model control group, DSF suspensions group, DSFSD suspensions and DSFSD/in-situ gel group.
Fig 10
Fig. 10
Calculation cataract scale in different groups including blank control group, model control group, DSF suspension group, DSFSD suspension and DSFSD/in-situ gel group.
See this image and copyright information in PMC

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