Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific delivery

Scanning electron microscopy (SEM) images of (a) uncoated pectin microspheres and (b) Eudragit‐coated pectin microspheres

This investigation is to find a prolonged or delayed drug release system, exclusively for the treatment of hepatitis‐B to reduce the side effects, which arise when conventional solid dose forms are administered. To pursue this goal, lamivudine‐loaded Eudragit‐coated pectin microspheres have been formulated employing water/oil (W/O) emulsion evaporation strategy. The formulation was optimised using a 3⁴ factorial design. A drug to polymer ratio of 1:2, the surfactant of 1 ml, the volume of 50 ml of processing medium with a stirring speed of 2500 rpm were found to be the optimal parameters to obtain the lamivudine‐loaded Eudragit‐coated pectin microspheres formulation with a high drug entrapment efficiency of 89.44% ± 1.44%. The in vitro release kinetics of lamivudine was a suitable fit to the Higuchi model, indicating a diffusion‐controlled release with anomalous transport. The obtained microspheres were then subjected to different characterisation studies, including scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X‐ray diffraction (XRD). The results of this study clearly indicate that Eudragit‐coated pectin microspheres could be the promising controlled release carriers for colon‐specific delivery of lamivudine in the presence of rat cecal content.

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or continue reading here: Vilas, S. and Thilagar, S. (2021), Formulation and optimisation of lamivudine‐loaded Eudragit^® S 100 polymer‐coated pectin microspheres for colon‐specific delivery. IET Nanobiotechnol. https://doi.org/10.1049/nbt2.12010

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CONCLUSION

Pectin microspheres of lamivudine were successfully prepared by the emulsion dehydration technique using different ratios of the polymer. This method of preparing a solution or suspension of pectin and lamivudine is comparatively easier than other techniques. Our study results suggest that the transmission of Eudragit‐coated pectin‐lamivudine microspheres to the colonic area has great scope. This demonstrates the use of Box‐Behnken Model in optimising formulations for the microsphere. The derived polynomial equation and 3‐D surface plot aid in predicting the values of selected independent variables for the generation of optimum microsphere formulations with the desired properties. The SEM, FT‐IR, DSC, and XRD permitted a structural analysis where the molecular dispersion of the drug inside the polymeric microsphere matrix, which allowed efficient drug incorporation and retention, was observed. Hence, the formulated Eudragit‐coated pectin‐lamivudine microspheres could be used for the efficient treatment of hepatitis B Accordingly, the next step of this investigation has been planned to optimise the parameters that influence the efficacy and bio‐availability in vivo.

excipients formulation