Inhaled deep eutectic solvent based-nanoemulsion of pirfenidone in idiopathic pulmonary fibrosis
Copyright © 2022 Elsevier B.V. All rights reserved..
Pirfenidone (PRF), the first FDA-approved drug to treat idiopathic pulmonary fibrosis (IPF) and formulated as an oral dosage form, has many side effects. To enhance the therapeutic effect, we discovered a high-load nanoemulsion using a novel deep eutectic solvent (DES) and developed an inhalation drug with improved bioavailability. The DES of PRF and N-acetylcysteine were discovered, and their physicochemical properties were evaluated in this study. The mechanism of DES formation was confirmed by FT-IR and 1H NMR and suggested to involve hydrogen bonding. The DES nanoemulsion in which the nano-sized droplets were dispersed is optimized by mixing the DES and distilled water in a ratio. The in vivo pharmacokinetic study showed that the pulmonary route of administration is superior to that of the oral route, and the DES nanoemulsion is superior to that of the PRF solution in achieving better bioavailability and lung distribution. The therapeutic effect of PRF for IPF could be confirmed through in vivo pharmacodynamics studies, including lung function assessment, enzyme-linked immunosorbent assay, histology, and micro-computed tomography using the bleomycin-induced IPF rat model. In addition, the pulmonary route administration of PRF is advantageous in reducing the toxicity risk.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:352 |
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| Enthalten in: |
Journal of controlled release : official journal of the Controlled Release Society - 352(2022) vom: 01. Dez., Seite 570-585 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Kang, Ji-Hyun [VerfasserIn] |
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| Links: |
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| Themen: |
D7NLD2JX7U |
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| Anmerkungen: |
Date Completed 06.12.2022 Date Revised 12.12.2022 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.jconrel.2022.10.045 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM348557914 |
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| 245 | 1 | 0 | |a Inhaled deep eutectic solvent based-nanoemulsion of pirfenidone in idiopathic pulmonary fibrosis |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2022 Elsevier B.V. All rights reserved. | ||
| 520 | |a Pirfenidone (PRF), the first FDA-approved drug to treat idiopathic pulmonary fibrosis (IPF) and formulated as an oral dosage form, has many side effects. To enhance the therapeutic effect, we discovered a high-load nanoemulsion using a novel deep eutectic solvent (DES) and developed an inhalation drug with improved bioavailability. The DES of PRF and N-acetylcysteine were discovered, and their physicochemical properties were evaluated in this study. The mechanism of DES formation was confirmed by FT-IR and 1H NMR and suggested to involve hydrogen bonding. The DES nanoemulsion in which the nano-sized droplets were dispersed is optimized by mixing the DES and distilled water in a ratio. The in vivo pharmacokinetic study showed that the pulmonary route of administration is superior to that of the oral route, and the DES nanoemulsion is superior to that of the PRF solution in achieving better bioavailability and lung distribution. The therapeutic effect of PRF for IPF could be confirmed through in vivo pharmacodynamics studies, including lung function assessment, enzyme-linked immunosorbent assay, histology, and micro-computed tomography using the bleomycin-induced IPF rat model. In addition, the pulmonary route administration of PRF is advantageous in reducing the toxicity risk | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Deep eutectic solvents | |
| 650 | 4 | |a Idiopathic pulmonary fibrosis | |
| 650 | 4 | |a Inhalation | |
| 650 | 4 | |a Nanoemulsions | |
| 650 | 4 | |a Pirfenidone | |
| 650 | 7 | |a pirfenidone |2 NLM | |
| 650 | 7 | |a D7NLD2JX7U |2 NLM | |
| 650 | 7 | |a Deep Eutectic Solvents |2 NLM | |
| 650 | 7 | |a Pyridones |2 NLM | |
| 700 | 1 | |a Yang, Min-Seok |e verfasserin |4 aut | |
| 700 | 1 | |a Kwon, Taek Kwan |e verfasserin |4 aut | |
| 700 | 1 | |a Kim, Dong-Wook |e verfasserin |4 aut | |
| 700 | 1 | |a Park, Chun-Woong |e verfasserin |4 aut | |
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