1. Phenazopyridine-phthalimide nano-cocrystal: Release rate and oral bioavailability enhancement.
- Author
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Huang Y, Li JM, Lai ZH, Wu J, Lu TB, and Chen JM
- Subjects
- Administration, Oral, Animals, Biological Availability, Drug Liberation, Male, Phenazopyridine blood, Rats, Sprague-Dawley, Nanoparticles chemistry, Phenazopyridine chemistry, Phenazopyridine pharmacokinetics, Phthalimides chemistry, Phthalimides pharmacokinetics
- Abstract
Both cocrystal and nanocrystal technologies have been widely used in the pharmaceutical development for poorly soluble drugs. However, the synergistic effects due to the integration of these two technologies have not been well investigated. The aim of this study is to develop a nano-sized cocrystal of phenazopyridine (PAP) with phthalimide (PI) to enhance the release rate and oral bioavailability of PAP. A PAP-PI nano-cocrystal with particle diameter of 21.4±0.1nm was successfully prepared via a sonochemical approach and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and dynamic light scattering (DLS) analysis. An in vitro release study revealed a significant release rate enhancement for PAP-PI nano-cocrystal as compared to PAP-PI cocrystal and PAP hydrochloride salt. Further, a comparative oral bioavailability study in rats indicated significant improvement in C
max and oral bioavailability (AUC0-∞ ) by 1.39- and 2.44-fold, respectively. This study demonstrated that this novel nano-cocrystal technology can be a new promising option to improve release rate and absorption of poorly soluble compounds in the pharmaceutical industry., (Copyright © 2017 Elsevier B.V. All rights reserved.)- Published
- 2017
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