The effect of distribution of momethazone furoat in emulsions on its anti-inflammatory action

A. M. Lyapunova, O. P. Bezugla, V. V. Libina, O. V. Timchenko, T. V. Andrianova

Abstract


Aim. To study distribution of mometasone furoate (MF) in emulsions of the 1st (o/w) and 2nd (w/o) types with different excipients, as well as to conduct a comparative experimental study of the anti-inflammatory effect of 0.1 % creams of MF with these emulsions as a vehicle.

Materials and methods. When studying its solubility, distribution between phases and solubilization by surfactant micelles the method of liquid chromatography was used for assay of MF; optical microscopy was used for determination of the disperse system type. The anti-inflammatory activity was studied on the dextran-induced rat paw edema and aerosol-induced rat paw edema.

Results. The solubility of MF in various hydrophilic and lipophilic solvents, distribution between the liquid paraffin and the hydrophilic solvent hexylene glycol–water (8:2), as well as solubilization by micelles of surfactants have been studied, it allows to predict the disperse state, distribution and localization of MF in emulsions of type 1 and 2, which are the vehicles for soft dosage forms. The dispersed state of MF in emulsions of type 1 and 2 has been confirmed by optical microscopy. The anti-inflammatory activity of 0.1 % Mometasone cream (a vehicle – o/w emulsion where MF is mostly in the form of a suspension) and 0.1 % Elocom® cream (a vehicle – w/o emulsion where MF is mostly dissolved in a dispersed hydrophilic phase) was studied. It has been determined that the dynamics of the anti-inflammatory effects (AE) for both drugs differs depending on the type of inflammatory edema; however, both drugs compared have a similar dynamics of AE under conditions of the same edema. It indicates that the type and concentration of glucocorticosteroid is a determining pharmaceutical factor for AE dynamic. Under conditions of the dextran-induced rat paw edema there is a pronounced tendency towards a higher AE in case of 0.1 % Mometasone cream (a vehicle – o/w emulsion) compared to 0.1 % Elocom® cream (a vehicle – w/o emulsion). It indicates the impact of differences in the pharmaceutical factors of these drugs on the efficiency of their anti-inflammatory activity. In the conditions of an aerosol-induced rat paw edema AE of 0.1 % Mometasone cream (a vehicle – o/w emulsion) basically corresponds to AE of 0.1 % Elocom® cream (a vehicle – w/o emulsion).

Conclusions. According to the results of the research the cream with MF and the o/w emulsion as a vehicle should be used in the acute phase of the inflammatory process accompanied with exudation, while the cream or ointment with the w/o emulsion as a vehicle – for the treatment of chronic dermatoses accompanied with a dry skin.


Keywords


mometasone furoate; solvent; emulsion; cream; distribution; pharmaceutical factor; edema; rats; anti-inflammatory effect

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DOI: https://doi.org/10.24959/cphj.17.1441

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