Montelukast medicines of today and tomorrow: from molecular pharmaceutics to technological formulations

Abstract

Montelukast sodium is a leukotriene antagonist of growing interest as an alternative therapy for asthma across different age groups due to its bronchoprotective, anti-inflammatory and anti-allergic properties. Currently, montelukast is commercialized only in oral solid dosage forms, which are the favorite of adult patients but may pose challenges in administration to children of young age or patients suffering from dysphagia. This review presents a comprehensive revision of scientific reports and patents on emerging strategies for the delivery of montelukast. A common ground to these reports is the pursue of an enhanced montelukast performance, by increasing its bioavailability and physico-chemical stability. A wide variety of strategies can be found, from the formation of supramolecular adducts with cyclodextrins to encapsulation in nanoparticles and liposomes. The new dosage forms for montelukast are designed for non-enteric absorption, some for absorption in the oral cavity and another two being for local action in the nasal mucosa or in the pulmonary epithelium. The review describes the emerging delivery strategies to circumvent the current limitations to the use of montelukast that are expected to ultimately lead to the development of more patient-compliant dosage forms.

Montelukast promotes mitochondrial biogenesis via CREB/PGC-1α in human bronchial epithelial cells

“…Administration of montelukast plays important roles in improving pulmonary function and reducing the risk of exacerbation in patients with asthma. In addition to its bronchoprotective effect, montelukast has exhibited antiinflammatory and anti-allergic properties in various tissues and cells [18]. However, the physiological function of montelukast on mitochondrial function in human bronchial epithelial cells remains undefined.…”

Metal-free quinolylation of the primary amino groups of amino acid derivatives and peptides with dihydrooxazolo[3,2-a]quinoliniums

“…20 Several strategies have been developed for the chemical modification of primary amino groups in amino acid derivatives and peptides, including acetylation, [21][22][23] alkylation, 24 oximation, [25][26][27] arylation 28 and quinonylation. 29 The quinoline skeleton is a prevalent structure in small-molecule drugs, including quinine sulfate (antimalarial), 30 montelukast sodium (asthma), 31 and saquinavir (anti-HIV). 32 Furthermore, the quinolylation of primary amino groups can also be used to generate peptide-drug conjugates (PDCs) and is thus important in the development of both peptide and PDC drugs.…”

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“…Emerging delivery strategies are being pursued to circumvent the current limitations to the use of MKS. [10] The polymers and excipients used in this study were Pluronic F127, a thermosensitive polymer (approved by FDA as a food additive), Xyloglucan (from tamarind seeds) as an ice crystal stabilizer, Sorbitol (10-17%) as a sweetener, viscosity enhancer and sodium benzoate (0.1%) as preservative. [11][12][13][14][15][16][17][18][19] The aim of this work was to develop a liquid oral in situ gelling formulation of MKS for sustained delivery, better bioavailability, and patient compliance.…”