Solubility and Pharmacokinetic Profile Improvement of Griseofulvin through Supercritical Carbon Dioxide-Assisted Complexation with HP-Iγ/I-Cyclodextrin

Since griseofulvin was marketed as a non-polyene antifungal antibiotic drug in 1958, its poor water solubility has been an issue for its wide applications, and over the last sixty years, many attempts have been made to increase its water solubility; however, a significant result has yet to be achiev...

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Veröffentlicht in:Molecules (Basel, Switzerland) Switzerland), 2023-10, Vol.28 (21)
Hauptverfasser: Ding, Yili, Cui, Wutong, Zhang, Zhiyuan, Ma, Yanzhi, Ding, Charles, Lin, Yikai, Xu, Zhe
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container_title Molecules (Basel, Switzerland)
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creator Ding, Yili
Cui, Wutong
Zhang, Zhiyuan
Ma, Yanzhi
Ding, Charles
Lin, Yikai
Xu, Zhe
description Since griseofulvin was marketed as a non-polyene antifungal antibiotic drug in 1958, its poor water solubility has been an issue for its wide applications, and over the last sixty years, many attempts have been made to increase its water solubility; however, a significant result has yet to be achieved. Through supercritical carbon dioxide-assisted cyclodextrin complexation with the addition of a trace amount of water-soluble polymer surfactant, the griseofulvin inclusion complex with HP-γ-cyclodextrin was prepared and confirmed. The 1:2 ratio of griseofulvin and HP-γ-cyclodextrin in the complex was determined based on its NMR study. After complexation with HP-γ-cyclodextrin, griseofulvin’s water solubility was increased 477 times compared with that of griseofulvin alone, which is the best result thus far. The complex showed 90% of griseofulvin release in vitro in 10 min, in an in vivo dog pharmacokinetic study; the C[sub.max] was increased from 0.52 µg/mL to 0.72 µg/mL, AUC[sub.0–12] was increased from 1.55 μg·h/mL to 2.75 μg·h/mL, the clearance was changed from 51.78 L/kg/h to 24.16 L/kg/h, and the half-life time was changed from 0.81 h to 1.56 h, indicating the obtained griseofulvin complex can be a more effective drug than griseofulvin alone.
doi_str_mv 10.3390/molecules28217360
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Through supercritical carbon dioxide-assisted cyclodextrin complexation with the addition of a trace amount of water-soluble polymer surfactant, the griseofulvin inclusion complex with HP-γ-cyclodextrin was prepared and confirmed. The 1:2 ratio of griseofulvin and HP-γ-cyclodextrin in the complex was determined based on its NMR study. After complexation with HP-γ-cyclodextrin, griseofulvin’s water solubility was increased 477 times compared with that of griseofulvin alone, which is the best result thus far. 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subjects Carbon dioxide
Ethylenediaminetetraacetic acid
Griseofulvin
title Solubility and Pharmacokinetic Profile Improvement of Griseofulvin through Supercritical Carbon Dioxide-Assisted Complexation with HP-Iγ/I-Cyclodextrin
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