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Fabrication, Evaluation, In Vivo Pharmacokinetic and Toxicological Analysis of pH-Sensitive Eudragit S-100-Coated Hydrogel Beads: a Promising Strategy for Colon Targeting

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A Correction to this article was published on 25 March 2022

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Abstract

The aim of present research aims to fabricate a system of enteric coating of hydrogel beads with pH-sensitive polymer, which shows solubility at pH > 7, and explore their potential to target the colon for drug delivery. Hydrogel beads were fabricated through the extrusion-dripping technique followed by ion gelation crosslinking. Moreover, freeze-thaw cycle was implemented for crosslinking of polyvinyl alcohol (PVA)/Ca-alginate blend beads. The oil-in-oil solvent evaporation method was adopted for the Eudragit coating of hydrogel beads using different coat: core ratios (4:1 or 8:1). Coated and uncoated hydrogel beads were evaluated by in vitro physicochemical properties, swelling and drug release behaviours, and in vivo pharmacokinetics, swelling, and toxicity evaluation. Diclofenac sodium was loaded as an experimental drug. Drug entrapment efficiency for the PVA/Ca-alginate beads was calculated as 98%, and for Ca-alginate beads, it came out to a maximum of 74%. Drug release study at various pH suggested that, unlike uncoated hydrogel beads, the coated beads delay the release of diclofenac sodium in low pH of the gastric and intestinal environment, thus targeting the colon for the drug release. It was concluded that Eudragit S-100-coated hydrogel beads could serve as a more promising and reliable way to target the colon for drug delivery.

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Authors and Affiliations

  1. Department of Pharmaceutics, The Islamia University of Bahawalpur, Railway Road Campus, Bahawalpur, Pakistan

    Sadia Rehman, Hina Shoukat, Asadullah Madni & Qazi Adnan Jameel

  2. Department of Pharmacy, The University of Lahore, Gujrat Campus, GT Road, Gujrat, Pakistan

    Nazar Muhammad Ranjha

  3. Department of Mechanical Engineering, Universiti Teknologi PETRONAS, Seri Iskandar,, Malaysia

    Faiz Ahmad

  4. Department of Mechanical Engineering, COMSATS University Islamabad, Sahiwal Campus, Sahiwal, Pakistan

    M. Rafi Raza

  5. Department of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan

    Abdul Majeed & Nasreen Ramzan

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  1. Sadia Rehman
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Rehman, S., Ranjha, N.M., Shoukat, H. et al. Fabrication, Evaluation, In Vivo Pharmacokinetic and Toxicological Analysis of pH-Sensitive Eudragit S-100-Coated Hydrogel Beads: a Promising Strategy for Colon Targeting. AAPS PharmSciTech 22, 209 (2021). https://doi.org/10.1208/s12249-021-02082-y

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