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

Abstract 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...

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Main Authors: Satheesh Vilas, Sivasudha Thilagar
Format: Article
Language:English
Published: Wiley 2021-02-01
Series:IET Nanobiotechnology
Subjects:
Online Access:https://doi.org/10.1049/nbt2.12010
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author Satheesh Vilas
Sivasudha Thilagar
author_facet Satheesh Vilas
Sivasudha Thilagar
author_sort Satheesh Vilas
collection DOAJ
description Abstract 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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spelling doaj-art-7dae63ccd0144e9cb9739aaa1bdba6c82025-08-20T03:35:24ZengWileyIET Nanobiotechnology1751-87411751-875X2021-02-01151909910.1049/nbt2.12010Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific deliverySatheesh Vilas0Sivasudha Thilagar1Department of Environmental Biotechnology Bharathidasan University Tiruchirappalli Tamil Nadu IndiaDepartment of Environmental Biotechnology Bharathidasan University Tiruchirappalli Tamil Nadu IndiaAbstract 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.https://doi.org/10.1049/nbt2.12010biomedical materialsdifferential scanning calorimetrydiffusiondrug delivery systemsdrugsemulsions
spellingShingle Satheesh Vilas
Sivasudha Thilagar
Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific delivery
IET Nanobiotechnology
biomedical materials
differential scanning calorimetry
diffusion
drug delivery systems
drugs
emulsions
title Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific delivery
title_full Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific delivery
title_fullStr Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific delivery
title_full_unstemmed Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific delivery
title_short Formulation and optimisation of lamivudine‐loaded Eudragit® S 100 polymer‐coated pectin microspheres for colon‐specific delivery
title_sort formulation and optimisation of lamivudine loaded eudragit r s 100 polymer coated pectin microspheres for colon specific delivery
topic biomedical materials
differential scanning calorimetry
diffusion
drug delivery systems
drugs
emulsions
url https://doi.org/10.1049/nbt2.12010
work_keys_str_mv AT satheeshvilas formulationandoptimisationoflamivudineloadedeudragits100polymercoatedpectinmicrospheresforcolonspecificdelivery
AT sivasudhathilagar formulationandoptimisationoflamivudineloadedeudragits100polymercoatedpectinmicrospheresforcolonspecificdelivery