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Open AccessArticle

Bioadhesive Matrix Tablets Loaded with Lipophilic Nanoparticles as Vehicles for Drugs for Periodontitis Treatment: Development and Characterization

1
Dipartimento di Discipline Chirurgiche, Oncologiche e Stomatologiche, Università degli Studi di Palermo, 90127 Palermo, Italy
2
Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, 90123 Palermo, Italy
3
Istituto per lo Studio degli Impatti Antropici e Sostenibilità dell’Ambiente Marino, Consiglio Nazionale delle Ricerche (IAS – CNR), Campobello di Mazara, 91021 Trapani, Italy
*
Author to whom correspondence should be addressed.
Polymers 2019, 11(11), 1801; https://doi.org/10.3390/polym11111801
Received: 16 October 2019 / Revised: 29 October 2019 / Accepted: 30 October 2019 / Published: 2 November 2019
(This article belongs to the Special Issue Medical Application of Polymer-Based Composites)
Periodontitis treatment is usually focused on the reduction or eradication of periodontal pathogens using antibiotics against anaerobic bacteria, such as metronidazole (MTR). Moreover, recently the correlation between periodontal diseases and overexpression of reactive oxygen species (ROS) led to the introduction of antioxidant biomolecules in therapy. In this work, bioadhesive buccal tablets, consisting of a hydrophilic matrix loaded with metronidazole and lipophilic nanoparticles as a vehicle of curcumin, were developed. Curcumin (CUR)-loaded nanostructured lipid carriers (NLC) were prepared using glycyrrhetic acid, hexadecanol, isopropyl palmitate and Tween®80 as a surfactant. As method, homogenization followed by high-frequency sonication was used. After dialysis, CUR-NLC dispersion was evaluated in terms of drug loading (DL, 2.2% w/w) and drug recovery (DR, 88% w/w). NLC, characterized by dynamic light scattering and scanning electron microscopy (SEM), exhibited a spherical shape, an average particle size of 121.6 nm and PDI and PZ values considered optimal for a colloidal nanoparticle dispersion indicating good stability of the system. Subsequently, a hydrophilic sponge was obtained by lyophilization of a gel based on trehalose, Natrosol and PVP-K90, loaded with CUR-NLC and MTR. By compression of the sponge, matrix tablets were obtained and characterized in term of porosity, swelling index, mucoadhesion and drugs release. The ability of the matrix tablets to release CUR and MTR when applied on buccal mucosa and the aptitude of actives to penetrate and/or permeate the tissue were evaluated. The data demonstrate the ability of NLC to promote the penetration of CUR into the lipophilic domains of the mucosal membrane, while MTR can penetrate and permeate the mucosal tissue, where it can perform a loco-regional antibacterial activity. These results strongly support the possibility of using this novel matrix tablet for delivering MTR together with CUR for topical treatment of periodontal diseases. View Full-Text
Keywords: buccal matrix tablets; nanostructured lipid carriers; NLC; metronidazole; curcumin; oral mucosal drug delivery; buccal delivery; hydrophilic sponge; periodontitis; oral disease buccal matrix tablets; nanostructured lipid carriers; NLC; metronidazole; curcumin; oral mucosal drug delivery; buccal delivery; hydrophilic sponge; periodontitis; oral disease
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MDPI and ACS Style

Murgia, D.; Angellotti, G.; D’Agostino, F.; De Caro, V. Bioadhesive Matrix Tablets Loaded with Lipophilic Nanoparticles as Vehicles for Drugs for Periodontitis Treatment: Development and Characterization. Polymers 2019, 11, 1801.

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