Nanocrytals-Mediated Oral Drug Delivery: Enhanced Bioavailability of Amiodarone

The aim of this study was to improve the saturation solubility, dissolution profile and oral bioavailability of amiodarone hydrochloride (AMH), a highly lipophilic drug. Stabilizer (Pluronic F-127)-coated AMH nanocrystals (AMH-NCs) were developed by a combination of antisolvent precipitation and hom...

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Published in:Pharmaceutics 2022-06, Vol.14 (6), p.1300
Main Authors: Awan, Anum Munir, Farid, Arshad, Shah, Shefaat Ullah, Khan, Dildar, Ur Rehman, Fiza, Dar, Muhammad Junaid, Iftikhar, Tayyaba, Ghazanfar, Shakira, Galanakis, Charis M, Alamri, Abdulhakeem S, Asdaq, Syed Mohammed Basheeruddin, Shah, Kifayat Ullah
Format: Article
Language:English
Subjects:
amiodarone HCl
Bioavailability
bioavailability enhancement
drug delivery
Drug dosages
Fourier transforms
Homogenization
Nanocrystals
Optimization
Particle size
pluronic F-127
Solvents
Surfactants
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Summary:The aim of this study was to improve the saturation solubility, dissolution profile and oral bioavailability of amiodarone hydrochloride (AMH), a highly lipophilic drug. Stabilizer (Pluronic F-127)-coated AMH nanocrystals (AMH-NCs) were developed by a combination of antisolvent precipitation and homogenization techniques. The optimized formulation comprised pluronic F-127 and AMH at the concentration of 4% and 2% w/v, respectively. The particle size (PS), zeta potential (ZP) and polydispersity index (PDI) of the optimized formulation was found to be 221 ± 1.2 nm, 35.3 mV and 0.333, respectively. The optimized formulation exhibited a rough surface morphology with particles in colloidal dimensions and a significant reduction in crystallinity of the drug. AMH-NCs showed a marked increase in the saturation solubility as well as rapid dissolution rate when compared with the AMH and marketed product. The stability study displayed that the formulation was stable for 3 months, with no significant change in the PS, ZP and PDI. The in vivo pharmacokinetic study demonstrated the ability of AMH-NCs to significantly (p < 0.05) improve the oral bioavailability (2.1-fold) of AMH in comparison with AMH solution, indicating that the production of AMH-NCs using a combination of antisolvent precipitation and homogenization techniques could enhance the bioavailability of the drug.
ISSN:1999-4923
1999-4923
DOI:10.3390/pharmaceutics14061300