Abstract
The controlled release of diclofenac sodium (DFNa) from a chitosan-oxidized konjac glucomannan (CTS-OKG) polymer film was studied. Konjac glucomannan (KGM) was initially oxidized by sodium periodate and then cross-linked to CTS via imine bonds (–C=N–) to form the new CTS-OKG copolymer. The DFNa loaded CTS-OKG polymers were characterized by Fourier transformed infrared spectroscopy (FT-IR) and X-ray diffractometry (XRD). Finally, the release profiles of DFNa from the CTS-OKG polymer matrices were evaluated in a simulated gastrointestinal fluid system comprised of two hours in simulated gastric fluid (SGF; pH 1.2) followed by 24 h in simulated intestinal fluid (SIF; pH 7.4). A 1:2:1 (w/w/w) ratio of CTS:OKG:DFNa prepared at room temperature for 3 hours gave the highest % encapsulation efficiency (EE) of 95.6 ± 0.6 and resulted in a minimal release of DFNa (<1% over 2 h) in SGF (pH 1.2) and a significantly improved sustained release in SIF (pH 7.4) with ~6% and 19% release over 8 and 24 h, respectively), some 15- and five-fold lower than that of the two commercial DFNa preparations, Diclosian and Voltaren. This formulation may be used for further study as a long term intestine controlled release drug model (at least 3 days).
Highlights
Chitosan (CTS) is the deacetylated form of chitin, a natural polymer from the exoskeleton of crustaceans, insects and cell walls of fungi and is as a waste product from marine aquaculture products like prawns/shrimps
We report on the oxidation of konjac glucomannan (KGM) with periodate to form the oxidized product (OKG) as a macromolecular cross-linking agent for CTS to replace the traditional toxic glutaraldehyde and prepare composite polymer films for controlled release drug delivery
The oxidation reaction of KGM by sodium periodate can be monitored with attenuated total reflectance Fourier transformed infrared spectroscopy (FT-IR)
Summary
Chitosan (CTS) is the deacetylated form of chitin, a natural polymer from the exoskeleton of crustaceans, insects and cell walls of fungi and is as a waste product from marine aquaculture products like prawns/shrimps. The most common side effects of DFNa are undesirable, being gastric ulcers, gastrointestinal bleeding, blood dyscrasia, anaphylaxis and depression of renal function, making more efficient delivery systems that avoid the initial high dose spikes highly desirable [2,3] In this scenario, the ideal system will protect the drug with minimal release in the acidic gastric environment, but with a complete off-loading of the DFNa at a sustained slow release in the intestine. We report on the oxidation of konjac glucomannan (KGM) with periodate to form the oxidized product (OKG) as a macromolecular cross-linking agent for CTS to replace the traditional toxic glutaraldehyde and prepare composite polymer films for controlled release drug delivery
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