학술논문

Polyionic complexes of chitosan-N-arginine with alginate as pH responsive and mucoadhesive particles for oral drug delivery applications.
Document Type
Article
Source
International Journal of Biological Macromolecules. Apr2020, Vol. 148, p550-564. 15p.
Subject
*ORNAMENTAL fishes
*SURFACE charges
*FRESHWATER fishes
*ELECTROSTATIC interaction
*INTESTINAL mucosa
Language
ISSN
0141-8130
Abstract
The production of efficient micro and nanoparticles of pH-responsive and mucoadhesive properties is of high scrutiny. We produced a drug carrier bioparticle providing such structural features. Thereby, protonated chitosan bearing chemically bonded arginine was interacted with ionized alginate, leading to the assembling of colloidal particles of specific characteristics. Ideally, the ratio of chitosan-arginine monomers to alginate monomer is 1.6 when the biopolymers are highly charged, providing electrostatic interaction with Gibbs energy compensation around −14 kcal/mol. Both size and surface charge of the bioparticle respond to pH variation, leading to structures of nano to micro hydrodynamic diameters and of positive, nearly neutral and negative zeta potential, with nanoscopic structure changing from mass to surface fractals. The inclusion of two hydrophobic model drugs provided some specific physicochemical features. Following freeze-drying, the bioparticles present both irregular shape and surface morphology, but an overall similar dry structure. An in vivo study of oral administration to teleost fish revealed that the bioparticles attain the intestine mucus and further, the interaction with the intestinal mucosa is timely dependent thanks to the mucoadhesive property. The in vivo study endorsed that the bioparticle provides high compliance to freshwater ornamental fish, highlighting it as a material of promising application. • A robust bioparticle enabled to reach and accumulate in the intestinal organ is produced. • The balance between carboxyl, amino and guanidinium groups provides outstanding physical characteristics to the bioparticle. • The composite particle formulation, containing the cell penetrating arginine, provides local mucosal interaction. • The biomaterial shows high in vivo acceptability by three species of teleost fish. [ABSTRACT FROM AUTHOR]