Abstract

In the present work, we report for the first time the complex coacervation of carboxymethyl sago pulp (CMSP) with gelatine for sustained drug delivery. Toluene saturated with glutaraldehyde and aqueous aluminum chloride was employed as cross-linkers. Measurements of zeta potential confirm neutralization of two oppositely charged colloids due to complexation, which was further supported by infrared spectroscopy. The coacervates encapsulated a model drug ibuprofen and formed microcapsules with a loading of 29%–56% w/w and an entrapment efficiency of 85%–93% w/w. Fresh coacervates loaded with drug had an average diameter of 10.8 ± 1.93 µm (n = 3 ± s.d.). The coacervates could encapsulate only the micronized form of ibuprofen in the absence of surfactant. Analysis through an optical microscope evidenced the encapsulation of the drug in wet spherical coacervates. Scanning electron microscopy revealed the non-spherical geometry and surface roughness of dried drug-loaded microcapsules. X-ray diffraction, differential scanning calorimetry and thermal analysis confirmed intact and crystalline ibuprofen in the coacervates. Gas chromatography indicated the absence of residual glutaraldehyde in the microcapsules. Dual cross-linked microcapsules exhibited a slower release than mono-cross-linked microcapsules and could sustain the drug release over the period of 6 h following Fickian diffusion.

Highlights

  • One of the most crucial innovations in recent years is the conversion of plant waste into useful products

  • In the present work, complex coacervation of Carboxymethyl sago pulp (CMSP) with gelatin is attempted for microencapsulation and sustained drug delivery

  • Drug-loaded coacervates were evaluated for loading/entrapment efficiency, particle size/distribution, optical and field emission scanning electron microscopy (FE-SEM), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), residual glutaraldehyde and in vitro release

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Summary

Introduction

One of the most crucial innovations in recent years is the conversion of plant waste into useful products. CMSP bead was exploited for colon targeted drug delivery of 5-aminosalicylic acid [4]. These CMSP beads were prepared by ionotropic gelation followed by radiation cross-linking. This method yields larger particles and need radiation facilities. In the present work, complex coacervation of CMSP with gelatin is attempted for microencapsulation and sustained drug delivery. The concentration of colloids, physicochemical properties of the drug being encapsulated, cross-linking agents and pH at which coacervation takes places are the most important parameters to obtain the final product [9]. Ibuprofen is encapsulated in CMSP/gelatine complex coacervates using glutaraldehyde as the cross-linking agent. Drug-loaded coacervates were evaluated for loading/entrapment efficiency, particle size/distribution, optical and field emission scanning electron microscopy (FE-SEM), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), X-ray diffraction (XRD), residual glutaraldehyde and in vitro release

Materials
Preparation of Carboxymethyl Sago Pulp
Preparation of Micronized Ibuprofen
Drug Loading and Entrapment Efficiency
Particle Size Analysis and Zeta Potential Measurement
Optical and Field Emission Scanning Electron Microscopy
X-Ray Diffractometry
2.10. Differential Scanning Calorimetry
2.12. In Vitro Release
2.13. Test for Residual Glutaraldehyde
Complex Coacervation and m-INN Encapsulation
Particle Size and Zeta Potential Analysis
Fourier Transform Infrared Spectroscopy Studies
Differential Scanning Calorimetry
Thermogravimetric Analysis
Optical Microscopy and FESEM
In Vitro Drug Release
Release Kinetics
3.10. Residual Glutaraldehyde
Conclusions
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