Biopharmaceutics

Biography

Biography: Pompilia Ispas-Szabo

Abstract

Macromolecular self-assembly represents an interesting way to produce materials for various therapeutic applications (targeted drug delivery, bioactive encapsulation). Considerable interest relates to the design of polymer- or peptide-based self-assembled biomaterials due to the possibility to generate different specific properties by new arrangements at molecular level. Differently from existing approaches which explore mainly the drug-excipient association in order to improve solubility, we are proposing a new alternative – the drug-drug self-assembling, using two different active molecules. Mesalamine (5-aminosalicylic acid, MES) is an efficacious active ingredient used for the long-term therapy of inflammatory bowel disease. However, its oral administration is frequently associated with systemic side effects caused by drug absorption in the upper gastrointestinal tract. Sucralfate (SUC) is a non-systemic site protector prescribed in the treatment of inflammation and gastric ulceration. The anti-inflammatory action of MES in association with bioadhesiveness and mucosal healing properties of SUC were considered promising for the development of a new compound containing both molecules, aimed as an improved treatment of ulcerative colitis. The present case investigated the capacity of the two active agents to interact and generate a new and stable entity via self-assembling. Spray-drying was used to co-process the two active principles from an aqueous mixture. Preliminary in vitro studies with oral solid dosage forms based on the obtained MES-SUC complexes have shown a controlled MES release, opening the perspective of a new colon-targeted delivery system and a novel class of compounds with therapeutic application in inflammatory bowel diseases.