The cariogenic bacterium Streptococcus mutans attaches to tooth surfaces via a cell surface adhesin termed streptococcal antigen I/II (SA I/II). Mapping studies identified an adhesion epitope within residues 1025-1044. A synthetic peptide (p1025) spanning these residues inhibited adhesion of S. mutans in vitro and was tested in an in vivo human streptococcal adhesion model. Direct application of p1025 to the teeth prevented recolonisation of the oral cavity by S. mutans but not Actinomyces naeslundii. This review also describes various other adhesion-inhibiting peptides have been identified in vitro. We suggest that adhesion-blocking synthetic peptides may provide novel anti-infective agents. Topical application of such peptides at mucosal surfaces does not provide sustained selective pressure and in contrast to antibiotics, may not induce resistance.

Molecules3区 · 化学

Design and Characterization of a Novel p1025 Peptide-Loaded Liquid Crystalline System for the Treatment of Dental Caries

3区 · 化学

ArticleOA

作者: Cilli, Eduardo ; Calixto, Giovana ; Garcia, Matheus ; Chiavacci, Leila ; Chorilli, Marlus

Dental caries, mainly caused by the adhesion of Streptococcus mutans to pellicle-coated tooth surfaces, is an important public health problem worldwide. A synthetic peptide (p1025) corresponding to residues 1025–1044 of the adhesin can inhibit this binding. Peptides are particularly susceptible to the biological environment; therefore, a p1025 peptide-loaded liquid crystalline system (LCS) consisting of tea tree oil as the oil phase, polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol as the surfactant, and water or 0.5% polycarbophil polymer dispersions as the aqueous phase was employed as a drug delivery platform. This system exhibited anticaries and bioadhesive properties and provided a protective environment to p1025 at the site of action, thereby modulating its action, prolonging its contact with the teeth, and decreasing the frequency of administration. LCSs were characterized by polarized light microscopy (PLM), small-angle X-ray scattering (SAXS), and rheological, texture, and bioadhesive tests. PLM and SAXS revealed the presence of hexagonal liquid crystalline phases and microemulsions. Rheological analyses demonstrated that the addition of polymer dispersions favored characteristics such as shear thinning and thixotropy, hence improving buccal application. Bioadhesion tests showed that polymer dispersions contributed to the adhesion onto the teeth. Taken together, LCS could provide a novel pharmaceutical nanotechnology platform for dental caries treatment.

International Journal of Nanomedicine

Development and characterization of p1025-loaded bioadhesive liquid-crystalline system for the prevention of <em>Streptococcus mutans </em>biofilms

Article

作者: Dos Santos, Vanessa Rodrigues ; Aida, Kelly Limi ; Calixto, Giovana Maria Fioramonti ; Chorilli, Marlus ; Duque, Cristiane ; Massunari, Loiane

Formation of a dental biofilm by Streptococcus mutans can cause dental caries, and remains a costly health problem worldwide. Recently, there has been a growing interest in the use of peptidic drugs, such as peptide p1025, analogous to the fragments 1025-1044 of S. mutans cellular adhesin, responsible for the adhesion and formation of dental biofilm. However, peptides have physicochemical characteristics that may affect their biological action, limiting their clinical performance. Therefore, drug-delivery systems, such as a bioadhesive liquid-crystalline system (LCS), may be attractive strategies for peptide delivery. Potentiation of the action of LCS can be achieved with the use of bioadhesive polymers to prolong their residence on the teeth. In line with this, three formulations - polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol, oleic acid, and Carbopol C974P in different combinations (F1C, F2C, and F3C) were developed to observe the influence of water in the LCS, with the aim of achieving in situ gelling in the oral environment. These formulations were assessed by polarized light microscopy, small-angle X-ray scattering, rheological analysis, and in vitro bioadhesion analysis. Then, p1025 and a control (chlorhexidine) were incorporated into the aqueous phase of the formulation (F + p1025 and F + chlorhexidine), to determine their antibiofilm effect and toxicity on epithelial cells. Polarized light microscopy and small-angle X-ray scattering showed that F1C and F2C were LCS, whereas F3C was a microemulsion. F1C and F2C showed pseudoplastic behavior and F3C Newtonian behavior. F1C showed the highest elastic and bioadhesive characteristics compared to other formulations. Antibiofilm effects were observed for F + p1025 when applied in the surface-bound salivary phase. The p1025-loaded nanostructured LCS presented limited cytotoxicity and effectively reduced S. mutans biofilm formation, and could be a promising p1025-delivery strategy to prevent the formation of S. mutans dental biofilm.

100 项与 P-1025 相关的药物交易

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