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 |