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

Denise Murgia,Fabio D’Agostino,Viviana De Caro,Giuseppe Angellotti

doi:10.3390/polym11111801

Denise Murgia, Fabio D’Agostino + Show 2 more

Open Access

https://doi.org/10.3390/polym11111801

Copy DOI

Abstract

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.

Highlights

Bacterial infections are among the most common diseases that could affect the oral mucosae.An immunocompromised state of the oral cavity is related to systemic and local factors that could allow the development of infections
The aim of this work is the formulation, development and characterization of buccal tablets obtained from hydrophilic sponges made by nanostructured lipid carriers (NLC) with curcumin (CUR-NLC) entrapped in a dry hydrophilic matrix loaded with MTR
Nano-encapsulation is highly exploited to promote the administration of substances with a low ability to cross biological membranes, using natural and/or synthetic materials to have a formulation with suitable chemical–physical characteristics

Summary

Introduction

Bacterial infections are among the most common diseases that could affect the oral mucosae.An immunocompromised state of the oral cavity is related to systemic and local factors that could allow the development of infections. Periodontal disease is a bacterial infection associated with the overgrowth of anaerobic organisms and, in certain instances with the micro-aerophilic ones, resulting in chronic inflammation of the gingiva [2]. Their action results in progressive connective tissue loss enhanced by the host’s inflammatory factors, which can lead to tooth loss [3]. In addition to bacterial action, frequently oral lesions are exasperated by the presence of reactive oxygen species (ROS) Their overproduction that is not balanced by an adequate level of antioxidants can prompt oxidative stress damages. The administration of antioxidant substances in periodontal diseases has recently been extensively studied [5]

Objectives

Methods

Results

Conclusion