Effect of Doxycycline Microencapsulation on Buccal Films: Stability, Mucoadhesion and In Vitro Drug Release.

Venu Gopal Reddy Patlolla,William Peter Holbrook,Sveinbjörn Gizurarson,Thordis Kristmundsdottir,Nikolina Popovic

doi:10.3390/gels7020051

Venu Gopal Reddy Patlolla, William Peter Holbrook + Show 3 more

Open Access

https://doi.org/10.3390/gels7020051

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Journal: Gels	Publication Date: Apr 28, 2021
Citations: 6	License type: CC BY 4.0

Affiliation: University of Iceland, University of Malawi

Abstract

The aim of this work was to stabilize doxycycline in mucoadhesive buccal films at room temperature (25 °C). Since doxycycline is susceptible to degradation such as oxidation and epimerization, tablets are currently the only formulation that can keep the drug fully stable at room temperature, while liquid formulations are limited to refrigerated conditions (4 °C). In this study, the aim was to make formulations containing subclinical (antibiotic) doxycycline concentration that can act as matrix metalloproteinase inhibitors (MMPI) and can be stored at temperatures such as 25 °C. Here, doxycycline was complexed with excipients using three techniques and entrapped into microparticles that were stored at 4 °C, 25 °C and 40 °C. Effect of addition of precomplexed doxycycline microparticles on films: stability mucoadhesion capacity, tensile strength, swelling index and in vitro release was studied. The complexation efficiency between drug-excipients, microparticles and films was studied using Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). Two of the films were found to be stable at 4 °C but the film containing microparticle composed of precomplexed doxycycline with β-cyclodextrin, MgCl2, sodium thiosulfate, HPMC and Eudragit® RS 12.5 was found to be stable at 25 °C until 26 weeks. The addition of microparticles to the films was found to reduce the mucoadhesive capacity, peak detachment force, tensile strength and elasticity, but improved the stability at room temperature.

Highlights

There is a need for topical drug delivery systems that can be used to treat oral conditions and is able to tolerate the harsh conditions inside the mouth
Since doxycycline is susceptible to degradation such as oxidation and epimerization, tablets are currently the only formulation that can keep the drug fully stable at room temperature, while liquid formulations are limited to refrigerated conditions (4 ◦ C)
Some oral conditions could benefit from barrier properties of the buccal films, while compounds like doxycycline that acts as a matrix metalloproteinase (MMP) inhibitor may be delivered as well

Summary

Introduction

There is a need for topical drug delivery systems that can be used to treat oral conditions and is able to tolerate the harsh conditions inside the mouth. There is a clear benefit, that by treating such conditions locally, systemic side effects will be reduced as well as presystemic elimination of molecules [1]. The buccal mucosa is robust and tolerant to numerous compounds such as potential allergens [2] and is accessible for topical formulations. Some oral conditions could benefit from barrier properties of the buccal films, while compounds like doxycycline that acts as a matrix metalloproteinase (MMP) inhibitor may be delivered as well. Apart from MMP inhibition, these conditions require some barrier protective layer that could prevent further exacerbation from mechanical movements of the mouth

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