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Disulfiram thermosensitive in-situ gel based on solid dispersion for cataract
Chunjuan Zhang1, Tonghua Xu1, Donglei Zhang2
1Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, China.
Asian Journal of Pharmaceutical Sciences
|February 28, 2020
Summary
This study developed a novel drug delivery system for disulfiram (DSF) to treat cataracts. The new system, disulfiram solid dispersion in an in-situ gel, significantly enhanced ocular permeability and delayed cataract development.
Area of Science:
- Ophthalmology
- Pharmaceutics
- Materials Science
Background:
- Disulfiram (DSF) is an ocular drug for cataract, but its corneal permeability and water-solubility are limited.
- Developing effective drug delivery systems is crucial for improving ocular drug efficacy.
Purpose of the Study:
- To enhance the corneal permeability and water-solubility of disulfiram (DSF).
- To develop a novel in-situ gel formulation for ocular drug delivery of DSF.
Main Methods:
- Disulfiram solid dispersion (DSFSD) was prepared using poloxamer 188 (P188) via a hot melt method.
- DSFSD was incorporated into a borate buffer solution with poloxamer 407 and P188 to form an in-situ gel.
- Characterization included DSC, XRD, and IR; in vitro and in vivo studies assessed corneal penetration and pharmacodynamics.
Main Results:
- Characterization confirmed DSF was in an amorphous state within the DSFSD.
- The DSFSD/in-situ gel formulation demonstrated increased residence time and corneal penetration of DSF.
- Pharmacodynamic studies showed the formulation delayed the progression of selenium-induced cataracts.
Conclusions:
- The developed DSFSD/in-situ gel system effectively improves DSF's ocular permeability.
- This novel drug delivery system holds promise for enhanced cataract treatment.

