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. 2016 Jan 28;21(2):158.
doi: 10.3390/molecules21020158.

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

Giovana Maria Fioramonti Calixto  1 , Matheus Henrique Garcia  2 , Eduardo Maffud Cilli  3 , Leila Aparecida Chiavacci  4 , Marlus Chorilli  5
Affiliations

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

Giovana Maria Fioramonti Calixto et al. Molecules. .

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.

Keywords: bioadhesive polymers; dental caries; liquid crystalline system; nanostructured drug delivery systems; tea tree oil.

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Conflict of interest statement

The authors declare no conflict of interest. The funding sponsors had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, and in the decision to publish the results.

Figures

Figure 1
Figure 1
(A) Ternary phase diagram of polyoxypropylene-(5)-polyoxyethylene-(20)-cetyl alcohol (PPCA), tea tree oil (TTO), and water. F1-A, F2-A, and F3-A were the selected formulations for characterization; (B) Ternary phase diagram of PPCA, TTO, and 0.5% polycarbophil (PP) dispersion. F1-P, F2-P, and F3-P were the selected formulations for characterization. PS: Phase separation; OVS: opaque viscous systems; TLS: transparent liquid systems; and TVS: transparent viscous systems.
Figure 2
Figure 2
Polarized light microscopy photomicrographs of the formulations F1-A, F2-A, F3-A, F1-P, F2-P, and F3-P. Magnification 20×.
Figure 3
Figure 3
Small-angle X-ray scattering analysis of F1A, F2A, and F3A (a) and F1P, F2P, and F3P (b).
Figure 4
Figure 4
(a) Flow rheograms of the formulations F1-A, F2-A, and F3-A; (b) Flow rheograms of the formulations F1-P, F2-P, and F3-P. Closed symbol represents the upcurve and open symbol represents the downcurve. Standard deviations have been omitted for clarity; however, in all cases, the coefficient of variation of triplicate analyses was less than 10%. Data were collected at 37 ± 0.5 °C.
Figure 5
Figure 5
Bioadhesion of F1-A, F2-A, F3-A, F1-P, F2-P, and F3-P. Each value represents the mean (±SD) of at least seven replicates. Data were collected at 37 ± 0.5 °C.
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