Antibacterial polypeptide-bioparticle for oral administration: Powder formulation, palatability and in vivo toxicity approach

Author(s)

Ramirez, Carlos A. B. ; Mathews, Patrick D. ; Madrid, Rafael R. M. ; Garcia, Irene T. S. ; Rigoni, Vera L. S. ; Mertins, Omar

• Document type: Journal article
• Source: BIOMATERIALS ADVANCES; v. 153, p. 15-pg., 2023-10-01.

Abstract

The upsurge of bacterial resistance to conventional antibiotics turned a well-recognized public health threat. The need of developing new biomaterials of effective practical use in order to tackle bacterial resistance became urgent. In this study, a submicrometric bioparticle of known antibacterial activity was produced in powder form with suitable texture and appealing characteristics for effective oral administration. Through complex coac-ervating a natural-source antimicrobial polypeptide with chitosan-N-arginine and alginate, the bioactive poly-peptide was physically incorporated to the bioparticle whose structure positively responds to the pH variations found in gastrointestinal tract. The powder formulation presented high palatability that was evaluated using fish as in vivo animal model. A thorough survey of the fish intestinal tissues, following a systematic oral adminis-tration, revealed high penetration potential of the biomaterial through epithelial cells and deeper intestine layers. Despite, no cytotoxic effect was observed in analyzing the tissues through different histology methods. The absence of intestinal damage was corroborated by immune histochemistry, being the integrity of epithelial motor myosin Vb and related traffic proteins preserved. Hematology further endorsed absence of toxicity in blood cells whose morphology was evaluated in detail. The study evidenced the applicability potential of a new biomaterial of appealing and safe oral administration of antibacterial polypeptide. (AU)

• FAPESP's process: 21/00971-2 - Crystalline-phase nano cubosome functionalized with biopolymers: development as a drug carrier and in vivo studies in zebrafish (Danio rerio)
• Grantee: Omar Mertins
• Support Opportunities: Regular Research Grants
• FAPESP's process: 15/23948-5 - Improvement of the polysaccharide chitosan properties for its application in liposomes and giant vesicles
• Grantee: Omar Mertins
• Support Opportunities: Regular Research Grants