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Montelukast microsuspension with hypromellose for improved stability and oral absorption

Ha Ryeong Lee1, Hyun Jin Park1, Jun Soo Park1

  • 1College of Pharmacy, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan, Chungnam 330-714, Republic of Korea.

International Journal of Biological Macromolecules
|May 29, 2021
PubMed

Insights

Formulating montelukast (MTK) microsuspensions with hypromellose (HPMC) improved drug stability and dissolution. These novel oral liquid preparations showed significantly enhanced bioavailability in rats, offering better patient compliance for asthma and Alzheimer's treatment.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Pharmacokinetics

Background:

  • Oral montelukast (MTK) is a standard treatment for asthma and rhinitis.
  • MTK is under investigation for Alzheimer's dementia treatment.
  • Patient compliance with current MTK formulations can be improved.

Purpose of the Study:

  • To develop novel microsuspension (MS)-based oral liquid preparations of MTK.
  • To evaluate drug-polymer interactions, physicochemical stability, dissolution, and pharmacokinetics.
  • To enhance patient compliance through improved oral absorption.

Main Methods:

  • Formulation of MTK microsuspensions using hypromellose (HPMC) as a polymeric suspending agent.
  • Evaluation of drug-polymer interactions using Raman spectrometry.
  • Assessment of physicochemical stability, dissolution profiles, and in vivo pharmacokinetic studies in rats.

Main Results:

  • HPMC addition significantly suppressed amorphous MTK crystallization and aggregation, improving stability.
  • MTK microsuspensions with HPMC demonstrated enhanced dissolution rates compared to crystalline forms.
  • Optimized HPMC-based MS showed over 80% higher bioavailability in rats versus marketed granules.

Conclusions:

  • Novel MTK-loaded microsuspensions with HPMC offer improved physicochemical stability and dissolution.
  • These liquid preparations demonstrate superior oral absorption and bioavailability.
  • MTK microsuspensions represent a promising alternative for enhanced patient compliance and therapeutic efficacy.
Keywords:
CrystallinityHypromelloseMicrosuspensionMontelukastPharmacokineticsStability

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