eprintid: 14620
rev_number: 2
eprint_status: archive
userid: 1
dir: disk0/00/01/46/20
datestamp: 2023-11-10 03:29:12
lastmod: 2023-11-10 03:29:12
status_changed: 2023-11-10 01:57:23
type: article
metadata_visibility: show
creators_name: Rehman, S.
creators_name: Ranjha, N.M.
creators_name: Shoukat, H.
creators_name: Madni, A.
creators_name: Ahmad, F.
creators_name: Raza, M.R.
creators_name: Jameel, Q.A.
creators_name: Majeed, A.
creators_name: Ramzan, N.
title: Fabrication, Evaluation, In Vivo Pharmacokinetic and Toxicological Analysis of pH-Sensitive Eudragit S-100-Coated Hydrogel Beads: a Promising Strategy for Colon Targeting
ispublished: pub
keywords: calcium alginate; calcium chloride; diclofenac; eudragit; hexane; hydrogel; polyvinyl alcohol; alginic acid; glucuronic acid; hexuronic acid; methylmethacrylate-methacrylic acid copolymer; microsphere; polymethacrylic acid derivative, animal experiment; animal model; aqueous solution; Article; AUC (0-8 h); body weight variation; chemical binding; controlled study; cross linking; drug blood level; drug delivery system; drug release; drug solubility; encapsulation; enteric coated tablet; fluid intake; food intake; in vitro study; in vivo study; maximum concentration; maximum plasma concentration; mean residence time; microencapsulation; mortality rate; nonhuman; pH; pharmacokinetic parameters; qualitative analysis; rabbit model; swelling; time to maximum plasma concentration; toxicity testing; toxicology; colon; hydrogel; pH, Alginates; Colon; Glucuronic Acid; Hexuronic Acids; Hydrogels; Hydrogen-Ion Concentration; Microspheres; Polymethacrylic Acids
note: cited By 11
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. Graphical abstractFigure not available: see fulltext.. © 2021, American Association of Pharmaceutical Scientists.
date: 2021
publisher: Springer Science and Business Media Deutschland GmbH
official_url: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85111296344&doi=10.1208%2fs12249-021-02082-y&partnerID=40&md5=a15d5608208746bf1e3df40ce2dcec9e
id_number: 10.1208/s12249-021-02082-y
full_text_status: none
publication: AAPS PharmSciTech
volume: 22
number: 6
refereed: TRUE
issn: 15309932
citation:   Rehman, S. and Ranjha, N.M. and Shoukat, H. and Madni, A. and Ahmad, F. and Raza, M.R. and Jameel, Q.A. and Majeed, A. and Ramzan, N.  (2021) 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 (6).   ISSN 15309932