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Bioavailability Enhancement: Drug Stability Enhancement and GI Retention01:05

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Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
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After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
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Updated: May 27, 2026

Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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Ibuprofen-phospholipid solid dispersions: improved dissolution and gastric tolerance.

M Delwar Hussain1, Vipin Saxena, James F Brausch

  • 1Department of Pharmaceutical Sciences, Irma Lerma Rangel College of Pharmacy, Texas A&M University Health Science Center, 1010 West Avenue B, Kingsville, TX, USA. hussain@pharmacy.tamhsc.edu

International Journal of Pharmaceutics
|November 22, 2011
PubMed
Summary

Solid dispersions with dimyristoylphosphatidyl-glycerol (DMPG) significantly enhanced ibuprofen dissolution and bioavailability. Ibuprofen-DMPG solid dispersions also reduced gastric irritation in rats.

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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients
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Published on: August 9, 2022

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Pharmacology

Background:

  • Ibuprofen is a widely used nonsteroidal anti-inflammatory drug (NSAID).
  • NSAIDs like ibuprofen are associated with gastrointestinal toxicity.
  • Improving ibuprofen's dissolution rate and reducing its gastric side effects are key pharmaceutical challenges.

Purpose of the Study:

  • To investigate the impact of various phospholipids on ibuprofen's in vitro dissolution.
  • To evaluate the in vivo gastrointestinal toxicity of ibuprofen when formulated as solid dispersions with phospholipids.
  • To determine the optimal phospholipid for enhancing ibuprofen's pharmaceutical properties.

Main Methods:

  • Preparation of solid dispersions of ibuprofen with different phospholipids.
  • In vitro dissolution testing of ibuprofen and its solid dispersions.
  • In vivo assessment of gastric mucosal irritation in rats using solid dispersions.
  • X-ray diffraction and scanning electron microscopy for characterizing solid dispersions.

Main Results:

  • Most phospholipids improved ibuprofen dissolution; dimyristoylphosphatidyl-glycerol (DMPG) showed the greatest effect.
  • The ibuprofen-DMPG system (9:1 ratio) increased ibuprofen dissolution extent by 69% and the initial rate sevenfold.
  • Solid dispersion with DMPG significantly reduced gastric mucosal irritation in rats compared to ibuprofen alone.
  • Characterization revealed smaller ibuprofen crystallite size and uniform distribution in DMPG solid dispersions.

Conclusions:

  • Solid dispersions of ibuprofen with phospholipids, particularly DMPG, enhance dissolution rates and extent.
  • The ibuprofen-DMPG solid dispersion demonstrates reduced gastrointestinal toxicity, suggesting improved bioavailability and safety.
  • Phospholipid-based solid dispersions offer a promising strategy for improving ibuprofen's therapeutic profile.