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Applying Different Techniques to Improve the Bioavailability of Candesartan Cilexetil Antihypertensive Drug

Authors Aly UF, Sarhan HA, Ali TFS, Sharkawy HAEB

Received 5 February 2020

Accepted for publication 27 April 2020

Published 14 May 2020 Volume 2020:14 Pages 1851—1865


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 2

Editor who approved publication: Dr Qiongyu Guo

Usama Farghaly Aly,1 Hatem Abdel-monsef Sarhan,1 Taha FS Ali,2 Hosny Abd El-Bakey Sharkawy1

1Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Minia, Egypt; 2Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, Minia, Egypt

Correspondence: Usama Farghaly Aly
Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Assuit Agriculture Road, P.O: 61519, Minia, Egypt
Tel +20 100110868
Fax +20 862369075

Purpose: The objective of this study was to compare different techniques to enhance the solubility and dissolution rate, and hence the bioavailability of candesartan cilexetil.
Methods: To achieve this target, various techniques were employed such as solid dispersions, inclusion complexes, and preparation of candesartan nanoparticles. Following the preparations, all samples were characterized for their physicochemical properties, and the samples of the best results were subjected to further bioavailability studies.
Results: Results of dissolution studies revealed an increase in the dissolution rate of all samples. The highest dissolution rate was achieved using solid dispersion of the drug with PVP K-90 (1:4). Physicochemical investigations (XR, DSC, and FT-IR) suggested formation of hydrogen bonding and changing in the crystalline structure of the drug. Regarding the inclusion complexes, more stable complex was formed between HP-β-CD and CC compared to β-CD, as indicated by phase solubility diagrams. Antisolvent method resulted in the preparation of stable nanoparticles, as indicated by ζ potential, with average particle size of 238.9 ± 19.25 nm using PVP K-90 as a hydrophilic polymer. The best sample that gave the highest dissolution rate (CC/PVP K-90 1:4) was allowed for further pharmacokinetic studies using UPLC MS/MS assay of rabbit plasma. Results showed a significant increase in the bioavailability of CC from ∼ 15% to ∼ 48%.
Conclusion: The bioavailability of CC was significantly improved from ∼ 15% to ∼ 48% when formulated as SDs with PVP K-90 with 1:4 drug:polymer ratio.

Keywords: solid dispersion, inclusion complex, nanoparticles, pharmacokinetics, UPLC MS/MS

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