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

Drug Deliv. 2016 Nov;23(9):3257-3265. doi: 10.3109/10717544.2016.1170247. Epub 2016 Apr 11.

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.

Keywords: Chronotherapeutic systems; cyclodextrins; drug stability; nano-encapsulation; oral delivery.

Publication types

  • Review

MeSH terms

  • Acetates / administration & dosage*
  • Acetates / chemistry*
  • Acetates / metabolism
  • Administration, Oral
  • Anti-Asthmatic Agents / administration & dosage
  • Anti-Asthmatic Agents / chemistry
  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry
  • Biological Availability
  • Chemistry, Pharmaceutical / methods
  • Cyclopropanes
  • Drug Delivery Systems / methods
  • Humans
  • Leukotriene Antagonists / administration & dosage
  • Leukotriene Antagonists / chemistry
  • Quinolines / administration & dosage*
  • Quinolines / chemistry*
  • Quinolines / metabolism
  • Sulfides

Substances

  • Acetates
  • Anti-Asthmatic Agents
  • Anti-Inflammatory Agents
  • Cyclopropanes
  • Leukotriene Antagonists
  • Quinolines
  • Sulfides
  • montelukast