Optimized mesalamine-loaded polyelectrolyte complex nanoparticles for targeted colon delivery in inflammatory bowel disease treatment: A central composite design approach

Bibliographic Details
Title: Optimized mesalamine-loaded polyelectrolyte complex nanoparticles for targeted colon delivery in inflammatory bowel disease treatment: A central composite design approach
Authors: Iqra Fatima, Ahmad Khan, Abbas Rahdar, Sonia Fathi-karkan, Zelal Kharaba, Francesco Baino
Source: Next Materials, Vol 8, Iss , Pp 100530- (2025)
Publisher Information: Elsevier, 2025.
Publication Year: 2025
Collection: LCC:Technology
Subject Terms: Nanoparticles, Mesalamine, Polyelectrolyte complex, Chitosan, CMC, Eudragit S-100, Technology
More Details: The objective of this study was to develop and optimize mesalamine-loaded polyelectrolyte complex (PEC) nanoparticles for the treatment of inflammatory bowel disease (IBD) using a central composite experimental design. Mesalamine, a pharmaceutical classified as a Biopharmaceutics Classification System (BCS) Class IV drug due to its poor solubility and permeability, short half-life (0.5–2 h), and challenges in patient compliance, was selected as the model drug for this study. PECs were synthesized by titrating sodium carboxymethyl cellulose (Na-CMC) and chitosan, with the experimental compositions determined using Design Expert® 7.0 software. Formulations were optimized by varying concentrations of chitosan and Na-CMC, considering particle size and encapsulation efficiency (EE%) as the response variables. The optimized PEC nanoparticles were subsequently coated with Eudragit S-100 (ES-100) to enable targeted delivery to the colon. The uncoated nanoparticles had a particle size of 234.9 ± 3.8 nm and a zeta potential of 27.90 ± 2.41 mV. After coating, these values were altered to 319.2 ± 4.1 nm and −13.45 ± 4.13 mV, indicating a shift to a slightly negative surface charge, which contributes to the stability and colon-targeting properties of the nanoparticles. Morphological analysis confirmed that the nanoparticles maintained a roughly spherical shape and that the polymer did not chemically interact with the encapsulated drug. The optimized formulation demonstrated an encapsulation efficiency of 62.26 ± 2.03 %. Drug release studies conducted in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) showed that uncoated nanoparticles released 91.2 ± 4.5 % of the drug over 48 h, while coated nanoparticles released 74.9 ± 2.9 %, as determined by ANOVA analysis. These findings suggest that the coating effectively extends mesalamine release over time, making this formulation a promising candidate for targeted IBD therapy.
Document Type: article
File Description: electronic resource
Language: English
ISSN: 2949-8228
Relation: http://www.sciencedirect.com/science/article/pii/S2949822825000486; https://doaj.org/toc/2949-8228
DOI: 10.1016/j.nxmate.2025.100530
Access URL: https://doaj.org/article/fbf50f9cc61b4bc297cc27dffa75c8b0
Accession Number: edsdoj.fbf50f9cc61b4bc297cc27dffa75c8b0
Database: Directory of Open Access Journals
More Details
ISSN:29498228
DOI:10.1016/j.nxmate.2025.100530
Published in:Next Materials
Language:English