Pharmaceutics
A Mesalazine-Aloperine Co-Amorphous System for Simultaneous Dissolution Enhancement, Permeability Improvement, and Synergistic Anti-Ulcerative Colitis Activity: A Combined Pharmaceutics and Network Pharmacology Study
By Su H, Guo N, Yuan S and 4 others.
Abstract
Background/Objectives: Mesalazine (MSZ), the first-line therapy for ulcerative colitis (UC), is a BCS Class IV drug limited by poor aqueous solubility and low intestinal permeability, which together restrict colonic drug delivery and therapeutic efficacy. This study aimed to develop a co-amorphous (CAM) system of MSZ and aloperine (ALO) to enhance MSZ dissolution and permeation while achieving anti-UC synergy.
Methods
The MSZ-ALO CAM system was prepared via solvent evaporation and characterized by PXRD, DSC, FTIR, and 1H NMR. Equilibrium solubility, intrinsic dissolution rate (IDR), and in vitro permeability were assessed under biorelevant pH conditions. Physical stability was evaluated under long-term and accelerated conditions. Network pharmacology predicted potential therapeutic targets and synergistic mechanisms.