FORMULATION AND EVALUATION OF MICROEMULSION CONTAINING DESLORATADINE FOR INTRANASAL DELIVER

Abstract

prepared to attain enhanced solubility and fast release through intranasal delivery. Desloratadine saturated solubility was determined in different oils, surfactants and cosurfactants. Triacetin and Tween 80 were selected as oily phase and surfactant respectively. Regarding the cosurfactant, Transcutol and Propylene Glycol were used separately in two comparative systems. Pseudoternary phase diagrams were constructed to identify the microemul- sion regions. Visual inspection, pH, viscosity, drug content, morphology, particle size, percentage transmittance and in-vitro release were character- ized for the selected Desloratadine loaded microemulsion formulations. The pharmacological evaluation of the selected formulae was carried through experimental induction of allergy using palm grains in white albino female rats and Lorafast® syrup was used for comparison. Plasma histamine and plasma eosinophil peroxidase concentrations were evaluated as well as his- topathological examination of rat nasal mucosa. An increase in the micro- emulsion region in pseudoternary phase diagrams was observed when using Transcutol compared to Propylene Glycol. However, Desloratadine micro- emulsion formulation containing (5% Triacetin, 15% Tween 80, 30% Pro- pylene Glycol and 50% Distilled Water) displayed highest rate of drug re- lease (100.77±0.90% within 60 minutes) and smallest particle size (16.43±1.80nm). The chosen Desloratadine microemulsion formulations succeeded to reduce significantly the plasma histamine and eosinophil pe- roxidase levels. The results revealed that the developed microemulsion has great potential for intranasal delivery of Desloratadine.