Abstract
A novel nanocrystal system of montelukast (MTK) was designed to improve the transdermal delivery, while ensuring chemical stability of the labile compound. MTK nanocrystal suspension was fabricated using acid-base neutralization and ultra-sonication technique and was characterized as follows: approximately 100 nm in size, globular shape, and amorphous state. The embedding of MTK nanocrystals into xanthan gum-based hydrogel caused little changes in the size, shape, and crystalline state of the nanocrystal. The in vitro drug release profile from the nanocrystal hydrogel was comparable to that of the conventional hydrogel because of the rapid dissolution pattern of the drug nanocrystals. The drug degradation under visible exposure (400–800 nm, 600,000 lux·h) was markedly reduced in case of nanocrystal hydrogel, yielding only 30% and 50% amount of cis-isomer and sulfoxide as the major degradation products, as compared to those of drug alkaline solution. Moreover, there was no marked pharmacokinetic difference between the nanocrystal and the conventional hydrogels, exhibiting equivalent extent and rate of drug absorption after topical administration in rats. Therefore, this novel nanocrystal system can be a potent tool for transdermal delivery of MTK in the treatment of chronic asthma or seasonal allergies, with better patient compliance, especially in children and elderly.
Highlights
Montelukast (MTK) is a selective leukotriene receptor antagonist that has been commonly prescribed in the treatment of chronic asthma and symptoms of seasonal allergies in children and adults [1,2,3]
A novel nanocrystal system of MTK was lucratively prepared by acid-base neutralization and ultra-sonication method
Drug nanocrystals stabilized by Polyvinylpyrrolidone K30 (PVP K30) polymer were approximately 130 nm in size, globular shaped, and were in amorphous state
Summary
Montelukast (MTK) is a selective leukotriene receptor antagonist that has been commonly prescribed in the treatment of chronic asthma and symptoms of seasonal allergies in children and adults [1,2,3]. MTK is clinically being investigated as a novel medication in the treatment of Alzheimer’s disease in elderly people [4]. Considering its frequent prescription to children in the age group of 6–24 months [7] and potential dosing in elderly patients with difficulty in swallowing, the transdermal dosage form can be an alternative for better patient compliance. MTK is extremely susceptible to light- or oxygen-induced degradation, and mainly breaks down into sulfoxide and cis-isomer by the oxidation of the mercapto group and by isomerization of the double bond, respectively. The penetration of this lipophilic compound (log P > 8.0) across the relevant skin layer and the absorption into the bloodstream are strictly restricted by the “brick and mortar” structure of stratum corneum [12,13,14,15,16]
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