Dapsone (DAP)is a bactericidal agent used in the treatment of leprosy, caused by Mycobacterium leprae. Despite its therapeutic potential, DAP has low solubility, which results in allow therapeutic index and a high microbial resistance. Recently, new approaches were used to increase the DAP solubility. In particular, the use of interpenetrating polymer network (IPN)-hydrogels based chitosan (CS)for the controlled release of DAP provides some advantages because they can modify their swelling properties and network structures as a response to environmental stimuli. The aim of this study was to synthesize and physicochemically characterize pH-responsive chitosan/polymer hydrogels to control the release of DAP. For this reason, different combination of polymers, such as polyvinyl pyrrolidone, polyethylene glycol and hydroxypropyl methylcellulose, and concentrations of the cross-linking agents (glutaraldehyde)were used and then blended to the CS. The resulting hydrogels were evaluated in terms of physicochemical and swelling properties, rheological analysis and in vitro release of DAP at different pHs (1.2–6.8). Hydrogels were further characterized by Fourier transformed infrared (FT-IR)spectroscopy and scanning electron microscopy (SEM)analysis. pH-responsive DAP-loaded hydrogels may represent the set-up for developing potential oral formulations for the treatment of leprosy caused by Mycobacterium leprae.

pH-responsive chitosan based hydrogels affect the release of dapsone: Design, set-up, and physicochemical characterization

Cristiano M. C.;Paolino D.;Celia C.
2019-01-01

Abstract

Dapsone (DAP)is a bactericidal agent used in the treatment of leprosy, caused by Mycobacterium leprae. Despite its therapeutic potential, DAP has low solubility, which results in allow therapeutic index and a high microbial resistance. Recently, new approaches were used to increase the DAP solubility. In particular, the use of interpenetrating polymer network (IPN)-hydrogels based chitosan (CS)for the controlled release of DAP provides some advantages because they can modify their swelling properties and network structures as a response to environmental stimuli. The aim of this study was to synthesize and physicochemically characterize pH-responsive chitosan/polymer hydrogels to control the release of DAP. For this reason, different combination of polymers, such as polyvinyl pyrrolidone, polyethylene glycol and hydroxypropyl methylcellulose, and concentrations of the cross-linking agents (glutaraldehyde)were used and then blended to the CS. The resulting hydrogels were evaluated in terms of physicochemical and swelling properties, rheological analysis and in vitro release of DAP at different pHs (1.2–6.8). Hydrogels were further characterized by Fourier transformed infrared (FT-IR)spectroscopy and scanning electron microscopy (SEM)analysis. pH-responsive DAP-loaded hydrogels may represent the set-up for developing potential oral formulations for the treatment of leprosy caused by Mycobacterium leprae.
2019
Anti-leprosy drugs
Controlled release
Dapsone
Oral drug delivery systems
pH-responsive hydrogels
Swelling property
Chemical Phenomena
Chitosan
Dapsone
Drug Carriers
Hydrogels
Hydrogen-Ion Concentration
Leprosy
Rheology
Drug Liberation
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/20.500.12317/65274
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