Abstract
The aim of this study was to develop a stable aqueous formulation containing a combination of doxycycline and monocaprin in clinically relevant concentrations. Increase in expression of Matrix metalloproteinases (MMPs) and microbial role in oral diseases is well established and the combination of above active ingredients could be potentially beneficial in treatment of oral mucosal conditions. The hydrogels containing different concentrations of doxycycline and monocaprin in the presence and absence of stabilizing excipients were developed and their stabilities were studied at 4 °C for up to 1 year. The drug–drug interaction was evaluated using Fourier-transform infrared spectroscopy (FTIR). The addition of monocaprin on doxycycline in situ hydrogel’s mucoadhesiveness, texture properties and drug release mechanism was studied. The addition of monocaprin negatively affected the doxycycline stability and was concentration dependent, whereas monocaprin was stable up to 1 year. Doxycycline did not interfere with the anti-Candidal activity of monocaprin. Furthermore, the presence of monocaprin significantly affected the formulation hardness, compressibility and adhesiveness. Monocaprin and doxycycline release followed zero order kinetics and the release mechanism was, by anomalous (non-Fickian) diffusion. The addition of monocaprin increased the drug release time and altered the release mechanism. It is possible to stabilize doxycycline in the presence of monocaprin up to 1 year at 4 °C.
Highlights
The oral mucosa is accessible and convenient site for local drug delivery
Doxycycline did not interfere with the anti-Candidal activity of monocaprin
The aim of this study was to incorporate monocaprin to doxycycline hydrogels and to study the effect of monocaprin on doxycycline stability as well as to stabilize active ingredients as doxycycline is susceptible to oxidation and epimerization [11] whereas, monocaprin is susceptible to hydrolysis and cleavage of fatty acid i.e., capric acid from glycerol and acyl-migration in solutions [22]
Summary
The oral mucosa is accessible and convenient site for local drug delivery. The oral mucosa is up to 4000 times more permeable relative to the skin [1,2]. Has excellent vasculature for drug diffusion into the systemic circulation through capillaries and venous drainage and thereby prevent the drugs from the harsh gastrointestinal environment as well as avoiding the first-pass metabolism. This route may reduce the systemic side effects. Virtual lack of Langerhans cells makes the oral mucosa tolerant to potential allergens and less susceptible to toxicity from locally applied agents [3].
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