Alkaline Amino Acid Alternating Copolymers with Potent Antibacterial Properties for the Treatment of Periodontitis

Abstract

Although antibacterial peptides with excellent properties emerge endlessly, the antibacterial peptides with alternating structures have not attracted much attention. In this work, three amino acid alternating copolymers (Orn-Ser, Orn-Gly, and Orn-Val) with similar molecular weights but different hydrophilicity were constructed for the study of antibacterial properties through the solid-phase peptide synthesis (SPPS) method. We found that these three amino acid alternating copolymers showed excellent biocompatibility and broad spectrum antibacterial activity. Nevertheless, they showed slightly different properties due to differences in hydrophilicity and cationic density, for instance, better biocompatibility of Orn-Ser, stronger antibacterial property of Orn-Gly, and a higher selectivity index of Orn-Val. In a rat periodontitis model, Orn-Gly and Orn-Val exhibited remarkable anti-infective performance and significant therapeutic effects. This work is expected to play an important role in the treatment of periodontitis and the rational design of antimicrobial peptides for different applications.

Scalable Fabrication of Polymeric Composite Microspheres to Inhibit Oral Pathogens and Promote Osteogenic Differentiation of Periodontal Membrane Stem Cells

“…Local therapy using drug carriers is gaining immense attention for treating periodontitis. ,− In particular, drug carriers in the form of biodegradable polymeric microspheres have the capability of filling in the deep periodontal pocket and anatomical complexities of the alveolar bone, thereby reducing the total drug dose, enabling controllable drug release, and exhibiting tailored bioactive property and minimal systemic adverse effects. − Xie et al reported a prolonged local antibacterial strategy based on Ag/TiO 2 /alginate (ATA) hydrogel microspheres, which promoted the generation of reactive oxygen species and O 2 under low-level H 2 O 2 to inhibit Porphyromonas gingivalis . In another study, a drug-loading nanocarrier was made by a hydrophobic lipid core (1, 2-distearoyl- sn -glycero-3-phosphoethanolamine-poly­(ethylene glycol) loaded with alpha-lipoic acid and a hydrophilic shell (poly­(amidoamine) dendrimer encapsulating minocycline hydrochloride) .…”