Fabrication of oral nanovesicle in-situ gel based on Epigallocatechin gallate phospholipid complex: Application in dental anti-caries

The conventional anti-caries agents exhibit many shortcomings such as poor stability, low efficacy or short residence time in the oral environment, it is urgent to develop efficacy treatments to prevent dental caries. As the most active polyphenols from tea, Epigallocatechin gallate (EGCG) shows rem...

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Bibliographic Details
Published in:European journal of pharmacology 2021-04, Vol.897, p.173951-173951, Article 173951
Main Authors: Xu, Xiaodi, Dai, Zihan, Zhang, Zilin, Kou, Xianyong, You, Xiangyu, Sun, Hongmei, Guo, Huilin, Liu, Mingxing, Zhu, Hongda
Format: Article
Language:English
Subjects:
Administration, Oral
Anti-Bacterial Agents - administration & dosage
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Anti-caries
Bacterial Adhesion - drug effects
Biofilms - drug effects
Biofilms - growth & development
Cariostatic Agents - administration & dosage
Cariostatic Agents - chemistry
Cariostatic Agents - pharmacology
Catechin - administration & dosage
Catechin - analogs & derivatives
Catechin - chemistry
Catechin - pharmacology
Dental Caries - microbiology
Dental Caries - prevention & control
Drug Carriers
Drug Compounding
Drug Liberation
Drug Stability
EGCG
Gels
Kinetics
Nanoparticles
Nanovesicle
Phospholipid complex
Phospholipids - chemistry
Staphylococcus aureus - drug effects
Staphylococcus aureus - growth & development
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Summary:The conventional anti-caries agents exhibit many shortcomings such as poor stability, low efficacy or short residence time in the oral environment, it is urgent to develop efficacy treatments to prevent dental caries. As the most active polyphenols from tea, Epigallocatechin gallate (EGCG) shows remarkable anti-cariogenic bioactivity. However, the poor stability and low bioavailability of EGCG limit its potential application. This study aimed to fabricate nanovesicles in-situ gel based on EGCG phospholipid complex in order to increase its stability and efficacy. The formation of EGCG phospholipid complex was characterized by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The ethanol injection method was used to prepare the EGCG-loaded nanovesicles, an optimal ratio of Poloxamer407 (P407) and Poloxamer188 (P188) as in-situ gel matrix was selected to fabricate oral nanovesicles in-situ gel. EGCG-loaded nanovesicle in-situ gel based on the phospholipid complex had uniform spherical shape without any agglomeration. The discrete nanoparticle with a size (131.44 ± 4.24 nm) and a negative zeta potential value at −30.7 ± 0.5 mV possessed good physical stability and high entrapment efficiency (83.66 ± 3.2%). The formulation exhibited a strong antibacterial activity on S. mutans, which could reduce acid production and tooth surface adhesion. In addition, EGCG formulation could inhibit the formation of glucan and biofilm from S. mutans by suppressing the activity of glycosyltransferase enzymes (GTF). In conclusion, the EGCG-loaded nanovesicle in-situ gel holds great promise as an efficient anti-cariogenic formulation for topical oral delivery.
ISSN:0014-2999
1879-0712
DOI:10.1016/j.ejphar.2021.173951