Preparation and ex vivo investigation of an injectable microparticulate formulation for gastrointestinal mucosa polyp resection

• Published in: European journal of pharmaceutics and biopharmaceutics 2022-09, Vol.178, p.25-34
• Main Authors: Moles-Aranda, Cristina, Pérez-González, Noelia, Calpena-Campmany, Ana C., Martín-Villena, María J., Otero-Espinar, Francisco J., Severino, Patricia, Souto, Eliana B., Morales-Molina, José A., Clares-Naveros, Beatriz
• Format: Article
• Language: English
• Subjects: Alginate microparticles; Endoscopic submucosal dissection (ESD); Endoscopic submucosal resection (ESR); Injectable polymeric solution; Mucosal elevation
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/j.ejpb.2022.07.012

[Display omitted] Endoscopic submucosal dissection (ESD) and endoscopic submucosal resection (EMR) are non-invasive endoscopic techniques. They allow an early excised gastrointestinal (GI) mucosal precancerous lessions. For their application is necessary to use a submucosal injection that lifts the area to excise. The main objective of this study was the preparation of a microparticulate-based fluid for injection in the GI submucosa. Alginate microparticles (MPs) were developed by the solvent displacement technique and characterized by particle size, surface electrical properties, swelling, degradation, rheology, adhesion, leakage, syringeablity and stability. Furthermore, their potential to form a submucosal cushion was assayed in porcine stomach mucosa and porcine colon mucosa. Results showed MPs sizes below 160 μm, negative surface charge around −50 mV at pH = 6, high rates of swelling and good adhesion. The microparticulate-based fluid exhibited pseudoplastic behavior following the Ostwald-de Waele rheological model. A brief force is sufficient for its injection through a syringe. Finally, formulations were able to provide a submucosa elevation of 1.70 cm for more than 90 min and 120 min in the porcine stomach and colon, respectively.