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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
Solubility and dissolution rate of progesterone-cyclodextrin-polymer systems.
Malika Lahiani-Skiba1, Cécile Barbot, Frédéric Bounoure
1Laboratoire de Pharmacie Galénique et Biopharmacie, ADEN-UPRES EA 3234, UFR de Médecine-Pharmacie, 22 Boulevard Gambetta, 76183, Rouen Cedex, France.
Drug Development and Industrial Pharmacy
|October 3, 2006
Summary
Improving progesterone oral bioavailability, this study enhanced its solubility and dissolution rates using cyclodextrin inclusion complexes and ternary systems with PEG 6000. These methods significantly boost progesterone
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Materials Science
Background:
- Progesterone, a steroid hormone, exhibits poor water solubility, limiting its oral bioavailability.
- Cyclodextrins (CDs) are widely used to enhance the solubility and dissolution of poorly soluble drugs.
- Derivatized CDs and ternary complexes offer advanced strategies for drug formulation.
Purpose of the Study:
- To improve the solubility and dissolution rate of progesterone.
- To evaluate the efficacy of various cyclodextrin derivatives (HPbeta-CD, HPgamma-CD, PMbeta-CD, SBEbeta-CD) in forming inclusion complexes with progesterone.
- To investigate the potential of ternary complexes involving beta-CD and PEG 6000 to further enhance progesterone's dissolution properties.
Main Methods:
- Preparation of progesterone-cyclodextrin inclusion complexes using freeze-drying and precipitation methods.
- Higuchi phase solubility studies to determine complex stability constants.
- Dissolution rate studies of binary and ternary systems.
- Characterization of drug-excipient interactions using Differential Scanning Calorimetry (DSC) and Fourier Transform-Infrared Spectroscopy (FT-IR).
Main Results:
- Hydroxypropyl-beta-CD (HPbeta-CD) and permethyl-beta-CD (PMbeta-CD) showed the highest efficiency in solubilizing progesterone among the tested CDs.
- Progesterone dissolution rates were significantly increased with HPbeta-CD, PMbeta-CD, and gamma-CD compared to beta-CD.
- Ternary complexes of progesterone/beta-CD with PEG 6000 demonstrated considerably enhanced dissolution rates, particularly at 5% and 10% concentrations.
- DSC and FT-IR confirmed progesterone's inclusion within cyclodextrin cavities and its dispersion in PEG for ternary systems.
Conclusions:
- HPbeta-CD and PMbeta-CD are effective for progesterone solubilization.
- Ternary complexation with PEG 6000 significantly enhances the dissolution rate of progesterone/beta-CD systems.
- These advanced cyclodextrin-based systems show great promise for improving oral bioavailability of poorly soluble drugs like progesterone.
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