Abstract
Purpose: To formulate and evaluate pH-sensitive controlled release cefixime microspheres based on crosslinked chitosan and acryl amide-grafted-poly ethylene glycolMethod: pH sensitive interpenetrating network (IPN) cefixime microspheres based on chitosan, its grafted copolymer, and hydrolyzed grafted copolymer were prepared by precipitation and crosslinking methods. The formulations were characterized by Fourier transform infrared spectroscopy (FTIR),X-ray diffraction(XRD),Differential scanning calorimetry (DSC), Scanning electron microscopy(SEM),Raman spectroscopy for particle size analysis. Swelling ratio, Effect of drug loading on encapsulation efficiencywas investigated. FTIR, SEM, DSC, X-ray diffraction XRD, swelling studies were investigated for controlled drug release of drug at pH 2 and pH 7.4.Results: The microspheres were spherical in shape with a narrow particle size distribution (56 – 124 ìm) and encapsulation efficiency of up to 93 %. The % swelling ratio for blend microspheres of C-PEG are higher than that of plain chitosan in both pH. In both the pH media release was much faster in plain Chitosan microspheres. For instance, only 83% drug was released at 11.5 h for C-grafted copolymer 50 in pH 7.4 media compared to 41% drug released in pH 2 media for the same time whereas 80% drugwas released at 11.5 h for C-grafted copolymer 50 (hydrolyzed) in pH 7.4 media compared to 38% drug released in pH 2. Drug release followed Higuchi release kinetics. FTIR, DSC, XRD data indicate that there was no interaction between the drug and the polymers used.Conclusion: It is evident from this study that chitosan microspheres could be further developed to serve as an effective biodegradable carrier for controlled release of cefixime.Keywords: Chitosan, Polyethylene glycol, Cross-linking, Controlled release, Cefixime.
Highlights
Chitosan is the generic name of a linear random copolymer of β-(1-4) linked –D-glucosamine whose molecular structure comprises a linear backbone linked through glycosidic bonds
Chitosan is mostly hydrophilic and the percentage of acetylated monomers and their distribution in the chains has a critical effect on its solubility and conformation in aqueous media
Due to its unique polymeric cationic character, chitosan-based gels and films have been extensively examined in the pharmaceutical industry for its potential in the development of drug delivery system [5]
Summary
Chitosan is the generic name of a linear random copolymer of β-(1-4) linked –D-glucosamine whose molecular structure comprises a linear backbone linked through glycosidic bonds. Chitosan exhibits pHdependent behavior in solution and some interesting biopharmaceutical properties such as muco-adhesiveness, ability to open, and epithelial tight junction. These characteristics of chitosan have attracted many scientists working in the biomedical field, drug delivery [1,2,3,4]. Due to its unique polymeric cationic character, chitosan-based gels and films have been extensively examined in the pharmaceutical industry for its potential in the development of drug delivery system [5]
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