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Article

Oral Formulation Based on Irbesartan Nanocrystals Improve Drug Solubility, Absorbability, and Efficacy

1
Faculty of Pharmacy, Kindai University, 3-4-1 Kowakae, Higashiosaka 577-8502, Osaka, Japan
2
Faculty of Pharmacy, Keio University, 1-5-30 Shibakoen, Minato 105-8512, Tokyo, Japan
3
Research Promotion and Support Headquarters, Center for Clinical Trial and Research Support, Fujita Health University, 1-98 Dengakugakubo, Kutsukake, Toyoake 470-1192, Aichi, Japan
*
Author to whom correspondence should be addressed.
Academic Editors: Márcio Rodrigues and Gilberto Alves
Pharmaceutics 2022, 14(2), 387; https://doi.org/10.3390/pharmaceutics14020387
Received: 8 January 2022 / Revised: 5 February 2022 / Accepted: 8 February 2022 / Published: 10 February 2022
(This article belongs to the Special Issue Pharmacokinetics of Orally Administered Drugs)
We previously reported that the bioavailability (BA) of irbesartan (IRB), a BSC class II drug, was improved by preparing nanocrystalline suspensions. However, nanocrystalline suspensions have chemical and physical instabilities and must be converted into tablets through drying approaches in order to overcome such instabilities. In this study, we attempted to design a molded tablet based on nanocrystalline IRB suspensions (IRB-NP tablet) and investigated the effects of this IRB-NP tablet on blood pressure (BP) in a stroke-prone spontaneously hypertensive (SHR-SP) rat. The IRB-NP tablet (with a hardness of 42.6 N) was developed by combining various additives (methylcellulose, 2-hydroxypropyl-β-cyclodextrin HPβCD, D-mannitol, polyvinylpyrrolidone, and gum arabic) followed by bead-milling and freeze-drying treatments. The mean particle size in the redispersions of the IRB-NP tablet was approximately 118 nm. The solubility and intestinal absorption of IRB in the IRB-NP tablet were significantly enhanced in comparison with the microcrystalline IRB tablet (IRB-MP tablet), and both solubility and clathrin-dependent endocytosis helped improve the low BA of the IRB. In addition, the BP-reducing effect of the IRB-NP tablet was significantly higher than that of the IRB-MP tablet. These results provide useful information for the preservation of nanocrystalline suspensions of BCS class II drugs, such as IRB. View Full-Text
Keywords: irbesartan; nanocrystalline; tablet; intestinal absorption; endocytosis irbesartan; nanocrystalline; tablet; intestinal absorption; endocytosis
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MDPI and ACS Style

Nagai, N.; Ogata, F.; Ike, A.; Shimomae, Y.; Osako, H.; Nakazawa, Y.; Yamamoto, N.; Kawasaki, N. Oral Formulation Based on Irbesartan Nanocrystals Improve Drug Solubility, Absorbability, and Efficacy. Pharmaceutics 2022, 14, 387. https://doi.org/10.3390/pharmaceutics14020387

AMA Style

Nagai N, Ogata F, Ike A, Shimomae Y, Osako H, Nakazawa Y, Yamamoto N, Kawasaki N. Oral Formulation Based on Irbesartan Nanocrystals Improve Drug Solubility, Absorbability, and Efficacy. Pharmaceutics. 2022; 14(2):387. https://doi.org/10.3390/pharmaceutics14020387

Chicago/Turabian Style

Nagai, Noriaki, Fumihiko Ogata, Ayari Ike, Yurisa Shimomae, Hanano Osako, Yosuke Nakazawa, Naoki Yamamoto, and Naohito Kawasaki. 2022. "Oral Formulation Based on Irbesartan Nanocrystals Improve Drug Solubility, Absorbability, and Efficacy" Pharmaceutics 14, no. 2: 387. https://doi.org/10.3390/pharmaceutics14020387

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