Novel pH-sensitive stearic acid-coated interpenetrating polymer network (IPN) blend microspheres of chitosan and gelatin were prepared by the emulsion cross-linking method using glutaraldehyde for the controlled release (CR) of isoniazid (INH), an antituberculosis drug. Coated as well as uncoated microspheres were developed and characterized by Fourier transform infrared (FTIR) to understand the chemical interactions and formation of the IPN blend structure as well as to confirm successful coating with the stearic acid. X-ray diffraction (XRD) indicated the distribution of INH, while differential scanning calorimetry (DSC) was used for investigating the thermal stability of the IPN blend matrices. Scanning electron microscopy (SEM) was used to distinguish between the morphologies of coated and uncoated microspheres. Coated microspheres were produced in the size range of 52 μm down to 502 nm with encapsulation efficiencies of 65−78%. Equilibrium swelling was studied in pH 1.2 and pH 7.4 buffer media, and the in vitro drug release showed the dependence of drug release on the cross-linking, blend ratio of the IPN matrix as well as stearic acid coating. The variations in the IPN blend ratio and cross-link density controlled the drug release up to 30 h, but the coated microspheres could reduce the burst release in the gastric stomach media, while enhancing in intestinal pH 7.4 media.
This
work reports on the novel development of IPN microparticles of chitosan
(CS) and guar gum (GG) that are enteric coated with NaAlg and magnesium
aluminum silicate (MAS) for controlled release of isoniazid. The matrices
have been characterized by X-ray diffraction (XRD) to understand drug
distribution, DSC for thermal stability, and Fourier transform infrared
spectroscopy (FTIR) for investigating the chemical interactions of
drug with the matrices. Surface morphology was investigated by scanning
electron microscopy. These microparticles exhibited encapsulation
efficiencies from 47 to 58%. Equilibrium swelling as well as in vitro release trends of the formulations studied in pH
1.2 and 7.4 buffer media showed the dependence of drug release on
cross-linking, blend ratio of the matrix and coating, all of which
affected the release time of drug from 1 to 4 h up to 50 h. The coated
microparticles have reduced the burst release in gastric media to
enhance in intestinal media.
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