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Hydrophobic ion pair loaded self-emulsifying drug delivery system (SEDDS): A novel oral drug delivery approach of cromolyn sodium for management of bronchial asthma.
Metadata
Journalinternational journal of pharmaceutics4.845Date
2020 Jun 04
4 months ago
Type
Journal Article
Volume
2020-Jul-30 / 585 : 119494
Author
Asfour MH 1, Kassem AA 2, Salama A 3, Abd El-Alim SH 2
Affiliation
  • 2. Pharmaceutical Technology Department, National Research Centre, El-Buhouth St, Dokki, Cairo 12622, Egypt.
  • 3. Pharmacology Department, National Research Centre, El-Buhouth St, Dokki, Cairo 12622, Egypt.
Doi
PMIDMESH
Abstract
The aim of the present study is to develop a self-emulsifying drug delivery system (SEDDS) for the hydrophobic ion pair (HIP) complex of cromolyn sodium (CS), in order to enhance its intestinal absorption and biological activity. Two ion pairing agents (IPAs) were investigated: hexadecyl pyridininum chloride (HPC) and myristyl trimethyl ammonium bromide (MTAB). The optimum binding efficiency for complexation between investigated IPAs and CS was observed at a molar ratio of 1.5:1, where CS binding efficiency was found to be 76.10 ± 2.12 and 91.37 ± 1.73% for MTAB and HPC, respectively. The two prepared complexes exhibited a significant increase in partition coefficient indicating increased lipophilicity. The optimized CS-HIP complex was incorporated into SEDDS formulations. SEDDS formulations F2 (40% oleic acid, 40% BrijTM98, 20% propylene glycol) and F3 (25% oleic acid, 50% BrijTM98, 25% propylene glycol) exhibited nanometric droplet diameters with monodisperse distribution and nearly neutral zeta potential values. Ex vivo intestinal permeation study, using the non-everted gut sac technique, revealed a significantly higher cumulative amount of permeated drug, after 2 h, for F2 and F3 (53.836 and 77.617 µg/cm2, respectively) compared to 8.649 µg/cm2 for plain CS solution. The in vivo evaluation of plain CS solution compared to F2 and F3 was conducted in an ovalbumin sensitization-induced bronchial asthma rat model. Lung function parameters (tidal volume and peak expiratory flow), biochemical parameters (interleukin-5, immunoglobulin-E, myeloperoxidase and airway remodelling parameters) were assessed in addition to histopathological examination. The results indicated the superiority of F3 followed by F2 compared to plain CS solution for prophylaxis of bronchial asthma in rats.
Keywords: Airway remodelling Bronchial asthma Cromolyn sodium Hydrophobic ion pairing Self-emulsifying drug delivery system
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4.8
Int J Pharminternational journal of pharmaceutics
Metadata
LocationNetherlands
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