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Biodegradable Porous Starch Spheres as a Novel Carrier for Enhancement of Dissolution Rate and Oral Bioavailability of Itraconazole

[ Vol. 14 , Issue. 7 ]

Author(s):

Jaywant Pawar*, Meer Tarique Ali, Ritesh Fule, Kailas Moravkar, Madhavsingh Seervi, Sadhana Sathaye and Purnima Amin   Pages 944 - 954 ( 11 )

Abstract:


Background: A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioavailability of Itraconazole as a poorly water-soluble antifungal drug.

Method: BPS was developed by converting native starch from hydrogel to alcogel by solvent exchange method. The developed BPS carrier was characterized by SEM and nitrogen adsorption/desorption analysis to understand surface morphology and porosity distribution respectively. Itraconazole (ITR) was loaded on BPS by adsorption mediated solvent evaporation method, which provides a hydrophilic matrix powder. This causes drug distribution within hydrophilic matrix of porous starch.

Results: Solid-state characterization of optimized batch (ITR/BPS-3) was performed using DSC, PXRD, FTIR, SEM and FTIR chemical imaging. In vitro dissolution and in vivo pharmacokinetic studies were performed to evaluate therapeutic potential of ITR/BPS-3 system. In vitro studies of ITR: BPS-3 system revealed a burst effect in drug release (93%) compared to marketed product, which showed 90% drug release at the end of 60 min compared to 84% of marketed. Moreover, ITR/BPS-3 system showed improved oral bioavailability up to 3.93 fold and marketed product shows 3.12 fold compared to ITR.

Conclusion: This effect is due to high surface area, improved wettability and reduced crystallinity of ITR due to its adsorption into BPS. A successful methodology was reported to prepare BPS from raw starch

Keywords:

Bioavailability, biodegradable porous starch, ITR, Itraconazole, RP-HPLC, solubility.

Affiliation:

Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology Elite Status, Matunga, Mumbai – 400019, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai-400019, Maharashtra, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai-400019, Maharashtra, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai-400019, Maharashtra, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai-400019, Maharashtra, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai-400019, Maharashtra, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Nathalal Parekh Marg, Matunga, Mumbai-400019, Maharashtra

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