Nanodispersions of taxifolin

impact of solid-state properties on dissolution behavior

Aleksander Shikov, Olga Pozharitskaya, Inna Miroshnyk, Sabiruddin Mirza, Irina Urakova, Samuli Hirsjärvi, Valery Makarov, Jyrki Heinämäki, Jouko Yliruusi, Raimo Hiltunen

    Tutkimustuotos: ArtikkelijulkaisuArtikkeliTieteellinenvertaisarvioitu

    Kuvaus

    Nanosizing is an advanced formulation approach to address the issues of poor aqueous solubility of active pharmaceutical ingredients. Here we present a procedure to prepare a nanoparticulate formulation with the objective to enhance dissolution kinetics of taxifolin dihydrate, a naturally occurring flavonoid with antioxidant, anti-inflammatory, and hepatoprotective activities. Polyvinylpirrolidone was selected as a carrier and the solid nanodispersions of varying compositions were prepared by a co-precipitation technique followed by lyophilization. The formulation technology reported herein resulted in aggregate-free, spherical particles with the mean size of about 150 nm, as observed by scanning electron microscopy and measured by photon correlation spectroscopy. Furthermore, the co-precipitation process caused taxifolin dihydrate to convert into an amorphous form as verified by X-ray powder diffraction, differential scanning calorimetry, hot stage microscopy and Raman spectroscopy. Finally, in vitro dissolution behavior of the nanodispersion of taxifolin was shown to be superior to that of either pure drug or a drug-polymer physical mixture, reaching 90% of taxifolin released after 30 min. Such enhanced drug release kinetics from the nanodispersion was attributed to both the reduced particle size and the loss of crystallinity. (C) 2009 Elsevier B.V. All rights reserved.
    Alkuperäiskielienglanti
    LehtiInternational Journal of Pharmaceutics
    Vuosikerta377
    Numero1-2
    Sivut148-152
    Sivumäärä5
    ISSN0378-5173
    DOI - pysyväislinkit
    TilaJulkaistu - 2009
    OKM-julkaisutyyppiA1 Alkuperäisartikkeli tieteellisessä aikakauslehdessä, vertaisarvioitu

    Lainaa tätä

    Shikov, A., Pozharitskaya, O., Miroshnyk, I., Mirza, S., Urakova, I., Hirsjärvi, S., ... Hiltunen, R. (2009). Nanodispersions of taxifolin: impact of solid-state properties on dissolution behavior. International Journal of Pharmaceutics, 377(1-2), 148-152. https://doi.org/10.1016/j.ijpharm.2009.04.044
    Shikov, Aleksander ; Pozharitskaya, Olga ; Miroshnyk, Inna ; Mirza, Sabiruddin ; Urakova, Irina ; Hirsjärvi, Samuli ; Makarov, Valery ; Heinämäki, Jyrki ; Yliruusi, Jouko ; Hiltunen, Raimo. / Nanodispersions of taxifolin : impact of solid-state properties on dissolution behavior. Julkaisussa: International Journal of Pharmaceutics. 2009 ; Vuosikerta 377, Nro 1-2. Sivut 148-152.
    @article{f193cc1587fc4a3d82bd9c6e869943d3,
    title = "Nanodispersions of taxifolin: impact of solid-state properties on dissolution behavior",
    abstract = "Nanosizing is an advanced formulation approach to address the issues of poor aqueous solubility of active pharmaceutical ingredients. Here we present a procedure to prepare a nanoparticulate formulation with the objective to enhance dissolution kinetics of taxifolin dihydrate, a naturally occurring flavonoid with antioxidant, anti-inflammatory, and hepatoprotective activities. Polyvinylpirrolidone was selected as a carrier and the solid nanodispersions of varying compositions were prepared by a co-precipitation technique followed by lyophilization. The formulation technology reported herein resulted in aggregate-free, spherical particles with the mean size of about 150 nm, as observed by scanning electron microscopy and measured by photon correlation spectroscopy. Furthermore, the co-precipitation process caused taxifolin dihydrate to convert into an amorphous form as verified by X-ray powder diffraction, differential scanning calorimetry, hot stage microscopy and Raman spectroscopy. Finally, in vitro dissolution behavior of the nanodispersion of taxifolin was shown to be superior to that of either pure drug or a drug-polymer physical mixture, reaching 90{\%} of taxifolin released after 30 min. Such enhanced drug release kinetics from the nanodispersion was attributed to both the reduced particle size and the loss of crystallinity. (C) 2009 Elsevier B.V. All rights reserved.",
    author = "Aleksander Shikov and Olga Pozharitskaya and Inna Miroshnyk and Sabiruddin Mirza and Irina Urakova and Samuli Hirsj{\"a}rvi and Valery Makarov and Jyrki Hein{\"a}m{\"a}ki and Jouko Yliruusi and Raimo Hiltunen",
    year = "2009",
    doi = "10.1016/j.ijpharm.2009.04.044",
    language = "English",
    volume = "377",
    pages = "148--152",
    journal = "International Journal of Pharmaceutics",
    issn = "0378-5173",
    publisher = "Elsevier Scientific Publ. Co",
    number = "1-2",

    }

    Shikov, A, Pozharitskaya, O, Miroshnyk, I, Mirza, S, Urakova, I, Hirsjärvi, S, Makarov, V, Heinämäki, J, Yliruusi, J & Hiltunen, R 2009, 'Nanodispersions of taxifolin: impact of solid-state properties on dissolution behavior', International Journal of Pharmaceutics, Vuosikerta 377, Nro 1-2, Sivut 148-152. https://doi.org/10.1016/j.ijpharm.2009.04.044

    Nanodispersions of taxifolin : impact of solid-state properties on dissolution behavior. / Shikov, Aleksander; Pozharitskaya, Olga; Miroshnyk, Inna; Mirza, Sabiruddin; Urakova, Irina; Hirsjärvi, Samuli; Makarov, Valery; Heinämäki, Jyrki; Yliruusi, Jouko; Hiltunen, Raimo.

    julkaisussa: International Journal of Pharmaceutics, Vuosikerta 377, Nro 1-2, 2009, s. 148-152.

    Tutkimustuotos: ArtikkelijulkaisuArtikkeliTieteellinenvertaisarvioitu

    TY - JOUR

    T1 - Nanodispersions of taxifolin

    T2 - impact of solid-state properties on dissolution behavior

    AU - Shikov, Aleksander

    AU - Pozharitskaya, Olga

    AU - Miroshnyk, Inna

    AU - Mirza, Sabiruddin

    AU - Urakova, Irina

    AU - Hirsjärvi, Samuli

    AU - Makarov, Valery

    AU - Heinämäki, Jyrki

    AU - Yliruusi, Jouko

    AU - Hiltunen, Raimo

    PY - 2009

    Y1 - 2009

    N2 - Nanosizing is an advanced formulation approach to address the issues of poor aqueous solubility of active pharmaceutical ingredients. Here we present a procedure to prepare a nanoparticulate formulation with the objective to enhance dissolution kinetics of taxifolin dihydrate, a naturally occurring flavonoid with antioxidant, anti-inflammatory, and hepatoprotective activities. Polyvinylpirrolidone was selected as a carrier and the solid nanodispersions of varying compositions were prepared by a co-precipitation technique followed by lyophilization. The formulation technology reported herein resulted in aggregate-free, spherical particles with the mean size of about 150 nm, as observed by scanning electron microscopy and measured by photon correlation spectroscopy. Furthermore, the co-precipitation process caused taxifolin dihydrate to convert into an amorphous form as verified by X-ray powder diffraction, differential scanning calorimetry, hot stage microscopy and Raman spectroscopy. Finally, in vitro dissolution behavior of the nanodispersion of taxifolin was shown to be superior to that of either pure drug or a drug-polymer physical mixture, reaching 90% of taxifolin released after 30 min. Such enhanced drug release kinetics from the nanodispersion was attributed to both the reduced particle size and the loss of crystallinity. (C) 2009 Elsevier B.V. All rights reserved.

    AB - Nanosizing is an advanced formulation approach to address the issues of poor aqueous solubility of active pharmaceutical ingredients. Here we present a procedure to prepare a nanoparticulate formulation with the objective to enhance dissolution kinetics of taxifolin dihydrate, a naturally occurring flavonoid with antioxidant, anti-inflammatory, and hepatoprotective activities. Polyvinylpirrolidone was selected as a carrier and the solid nanodispersions of varying compositions were prepared by a co-precipitation technique followed by lyophilization. The formulation technology reported herein resulted in aggregate-free, spherical particles with the mean size of about 150 nm, as observed by scanning electron microscopy and measured by photon correlation spectroscopy. Furthermore, the co-precipitation process caused taxifolin dihydrate to convert into an amorphous form as verified by X-ray powder diffraction, differential scanning calorimetry, hot stage microscopy and Raman spectroscopy. Finally, in vitro dissolution behavior of the nanodispersion of taxifolin was shown to be superior to that of either pure drug or a drug-polymer physical mixture, reaching 90% of taxifolin released after 30 min. Such enhanced drug release kinetics from the nanodispersion was attributed to both the reduced particle size and the loss of crystallinity. (C) 2009 Elsevier B.V. All rights reserved.

    U2 - 10.1016/j.ijpharm.2009.04.044

    DO - 10.1016/j.ijpharm.2009.04.044

    M3 - Article

    VL - 377

    SP - 148

    EP - 152

    JO - International Journal of Pharmaceutics

    JF - International Journal of Pharmaceutics

    SN - 0378-5173

    IS - 1-2

    ER -