Abstract
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.
Highlights
Dental caries is still a major public health problem, which can lead to the loss of teeth
A clear and transparent region was obtained in a wide region of the pseudo-ternary phase diagram and we observed a transition from transparent liquid system (TLS) to transparent viscous system (TVS), opaque viscous system (OVS), and phase separation (PS), with the proportion of the aqueous phase above 20%, tea tree oil (TTO) below 90%, and polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol (PPCA) above 20%
PP is a high molecular weight polymer that forms cross-links with divinyl glycol. It is insoluble in water but at neutral pH, the expansion of the chains when hydrated causes the formation of a strong gel due to neutralization of the carboxylic groups, and provides further stability to the system [14]
Summary
Dental caries is still a major public health problem, which can lead to the loss of teeth. The etiology of dental caries is mainly linked to factors and conditions that encourage the growth of bacteria, especially Streptococcus mutans (S. mutans). The first step of biofilm formation is the adhesion of S. mutans to pellicle-coated tooth surfaces [2]. Studies have evaluated several pharmacologically active molecules, such as peptides, to determine their potential to impede the growth or action of virulence factors, such as adhesins, that are related to the survival of S. mutans in the biofilm surface [3,4]. The antimicrobial peptide p1025 with the amino acid sequence Ac-QLKTADLPAGRDETTSFVLV-NH2 , which is analogous to the 1025–1044 fragments of cellular adhesins of S. mutans, the bacterium responsible for the adhesion and biofilm formation on the oral mucosa, has demonstrated potential to combat dental caries. Et al reported that p1025 inhibited the binding of a cell surface adhesin of
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