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Phase behavior and oral bioavailability of amorphous Curcumin
Yogesh B Pawar1, Ganesh Shete, Dharmesh Popat
1Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research (NIPER), SAS Nagar, Punjab 160 062, India.
Summary
The amorphous form of Curcumin (CRM-A) showed improved solubility but limited oral bioavailability due to rapid devitrification in the gastrointestinal tract. Further studies are needed to optimize its delivery.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Amorphous forms enhance solubility and bioavailability of poorly water-soluble drugs.
- Curcumin's therapeutic potential is limited by its poor aqueous solubility and bioavailability.
Purpose of the Study:
- To characterize the thermodynamic and kinetic properties of amorphous Curcumin (CRM-A).
- To evaluate the impact of devitrification on CRM-A's solubility and oral bioavailability.
Main Methods:
- Differential Scanning Calorimetry (DSC) for thermal analysis (Tg, Tm, Cp).
- Powder X-ray Diffraction (PXRD) and Scanning Electron Microscopy (SEM) for structural analysis.
- In vitro solubility and in vivo oral bioavailability studies in animal models.
Main Results:
- CRM-A is a good glass former with a glass transition temperature (Tg) of 342.64 K and moderate crystallization tendency.
- Theoretical solubility advantage of 43.15-folds reduced to 17-folds due to water-induced devitrification.
- CRM-A showed a 1.97-fold increase in Cmax but a non-significant 1.45-fold increase in oral bioavailability (AUC).
Conclusions:
- Rapid devitrification of CRM-A in the gastrointestinal tract limits its oral bioavailability.
- While amorphous curcumin offers solubility benefits, its therapeutic efficacy is constrained by stability issues.
- Strategies to inhibit devitrification are crucial for maximizing the oral bioavailability of amorphous curcumin.
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