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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
Inclusion complex of colchicine in hydroxypropyl-β-cyclodextrin tenders better solubility and improved
Ritu Chauhan1, Jitender Madan, Dinesh Kaushik
1Department of Pharmaceutics, Hindu College of Pharmacy, Sonepat, Haryana, India.
Context:
Colchicine (CLC) causes cell death by destabilizing the tubulin unit. However, it ionizes at physiological pH resultant low bioavailability and therapeutic efficacy.
Objectives:
We have attempted to augment the bioavailability of CLC by fabricating the inclusion complex with hydroxypropyl-β-cyclodextrin (HP-β-CD).
Materials And Methods:
CLC-HP-β-CD inclusion complex was prepared and evaluated with Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, scanning electron microscopy, (1)H nuclear magnetic resonance ((1)H NMR) spectroscopy and rotating frame overhauser enhancement spectroscopy (ROESY). Oral bioavailability of CLC-HP-β-CD inclusion complex was analyzed using high performance liquid chromatography method.
Results And Discussion:
Our phase-solubility data indicated the formation of a stable complex with K(c) ~0.31 mM(-1) at pH 7.4. (1)H NMR ascertains that NHCOCH(3) moiety of CLC enters in the HP-β-CD cavity and deshielded the H-3 and H-5 protons. ROESY also correlates the H(f) and H(g) of CLC with H-3 and H-5 protons of HP-β-CD and indicates that H(f) and H(g) protons of CLC are present either as cis and/or trans form in CLC-HP-β-CD inclusion complex. Pharmacokinetic studies showed a 1.82-fold increase in absolute bioavailability of CLC upon complexation.
Conclusion:
CLC-HP-β-CD inclusion complex may potentially be used as a viable formulation of CLC.
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