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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Gefitinib-cyclodextrin inclusion complexes: physico-chemical characterization and dissolution studies.
Y-H Phillip Lee1, Sateesh Sathigari, Y-J Jean Lin
1Department of Pharmacal Sciences, Harrison School of Pharmacy, Auburn University, Auburn, AL, USA.
Drug Development and Industrial Pharmacy
|July 31, 2009
Summary
Gefitinib
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Gefitinib, an anticancer drug, exhibits poor aqueous solubility, limiting oral absorption.
- Cyclodextrins (CDs) offer a strategy to enhance gefitinib's solubility and dissolution rate.
Purpose of the Study:
- To investigate the complexation of gefitinib with hydroxypropyl beta-cyclodextrin (HPbetaCD) and randomly methylated beta-cyclodextrin (RMbetaCD).
- To characterize the inclusion complexes in both liquid and solid states.
- To evaluate the impact of polymers on gefitinib-CD complex properties.
Main Methods:
- Phase solubility studies were performed to characterize liquid-state complexes.
- Solid-state inclusion complexes were prepared using freeze-drying.
- Complex characterization involved X-ray diffractometry (X-RD) and differential scanning calorimetry (DSC).
Main Results:
- Gefitinib formed stable complexes with HPbetaCD and RMbetaCD, with high association constants.
- Amorphous solid-state complexes significantly increased gefitinib's solubility and dissolution rate.
- Incorporation of polymers like polyvinyl pyrrolidone (PVP) and hydroxypropyl methylcellulose (HPMC) further enhanced solubility and dissolution.
Conclusions:
- Gefitinib forms stable inclusion complexes with HPbetaCD and RMbetaCD.
- Complexation with CDs and incorporation of polymers effectively improves gefitinib's solubility and dissolution rate.
- These findings suggest a promising approach for enhancing gefitinib oral bioavailability.
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