Gamma scintigraphic evaluation of the fate of microcrystalline chitosan granules in human stomach

Mia Säkkinen (Corresponding Author), Janne Marvola, Hanna Kanerva, Maija Lindevall, Maija Lipponen, Tommi Kekki, Aapo Ahonen, Martti Marvola

    Research output: Contribution to journalArticleScientificpeer-review

    34 Citations (Scopus)

    Abstract

    In several reports of in vitro studies it has been suggested that the mucoadhesive chitosans could be of value in preparing gastro-retentive formulations. The aim of this study was to obtain direct in vivo evidence of whether microcrystalline chitosan (MCCh) formulations acted as gastro-retentive systems in humans. Neutron-activation-based gamma scintigraphy was used to study gastric residence times of MCCh granules in healthy male volunteers. Possible effects of neutron irradiation on the properties of the MCCh granules were studied in advance, in vitro. In vivo gamma scintigraphic evaluations were carried out with the subjects in a fasted state, using granules containing 95% (F1) or 40% (F2) of MCCh of molecular weight 150 kDa. Reference formulation (F3) was lactose granules. The reference granules passed rapidly from the stomach (mean t50% 0.5±0.3 h (n=5)). MCCh in granules prolonged gastric residence times of the formulations in only a few cases (in one volunteer in the F1 group (n=4) and in two volunteers in the F2 group (n=5)). Maximum individual t50% values were 2.1 h (F1) and 2.3 h (F2). It was concluded that the in vivo mucoadhesion of MCCh formulations is erratic, and that the formulations studied are not reliable gastro-retentive drug delivery systems.
    Original languageEnglish
    Pages (from-to)133 - 143
    Number of pages11
    JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
    Volume57
    Issue number1
    DOIs
    Publication statusPublished - 2004
    MoE publication typeA1 Journal article-refereed

    Fingerprint

    Chitosan
    Stomach
    Neutrons
    Volunteers
    Drug Delivery Systems
    Lactose
    Radionuclide Imaging
    Healthy Volunteers
    Molecular Weight

    Keywords

    • microcrystalline chitosan
    • mucoadhesion
    • gastro-retentive
    • gamma scintigraphy
    • neutron activation
    • samarium

    Cite this

    Säkkinen, Mia ; Marvola, Janne ; Kanerva, Hanna ; Lindevall, Maija ; Lipponen, Maija ; Kekki, Tommi ; Ahonen, Aapo ; Marvola, Martti. / Gamma scintigraphic evaluation of the fate of microcrystalline chitosan granules in human stomach. In: European Journal of Pharmaceutics and Biopharmaceutics. 2004 ; Vol. 57, No. 1. pp. 133 - 143.
    @article{195eedd5ecaa46a3998174fe2788db38,
    title = "Gamma scintigraphic evaluation of the fate of microcrystalline chitosan granules in human stomach",
    abstract = "In several reports of in vitro studies it has been suggested that the mucoadhesive chitosans could be of value in preparing gastro-retentive formulations. The aim of this study was to obtain direct in vivo evidence of whether microcrystalline chitosan (MCCh) formulations acted as gastro-retentive systems in humans. Neutron-activation-based gamma scintigraphy was used to study gastric residence times of MCCh granules in healthy male volunteers. Possible effects of neutron irradiation on the properties of the MCCh granules were studied in advance, in vitro. In vivo gamma scintigraphic evaluations were carried out with the subjects in a fasted state, using granules containing 95{\%} (F1) or 40{\%} (F2) of MCCh of molecular weight 150 kDa. Reference formulation (F3) was lactose granules. The reference granules passed rapidly from the stomach (mean t50{\%} 0.5±0.3 h (n=5)). MCCh in granules prolonged gastric residence times of the formulations in only a few cases (in one volunteer in the F1 group (n=4) and in two volunteers in the F2 group (n=5)). Maximum individual t50{\%} values were 2.1 h (F1) and 2.3 h (F2). It was concluded that the in vivo mucoadhesion of MCCh formulations is erratic, and that the formulations studied are not reliable gastro-retentive drug delivery systems.",
    keywords = "microcrystalline chitosan, mucoadhesion, gastro-retentive, gamma scintigraphy, neutron activation, samarium",
    author = "Mia S{\"a}kkinen and Janne Marvola and Hanna Kanerva and Maija Lindevall and Maija Lipponen and Tommi Kekki and Aapo Ahonen and Martti Marvola",
    year = "2004",
    doi = "10.1016/S0939-6411(03)00097-3",
    language = "English",
    volume = "57",
    pages = "133 -- 143",
    journal = "European Journal of Pharmaceutics and Biopharmaceutics",
    issn = "0939-6411",
    publisher = "Elsevier",
    number = "1",

    }

    Gamma scintigraphic evaluation of the fate of microcrystalline chitosan granules in human stomach. / Säkkinen, Mia (Corresponding Author); Marvola, Janne; Kanerva, Hanna; Lindevall, Maija; Lipponen, Maija; Kekki, Tommi; Ahonen, Aapo; Marvola, Martti.

    In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 57, No. 1, 2004, p. 133 - 143.

    Research output: Contribution to journalArticleScientificpeer-review

    TY - JOUR

    T1 - Gamma scintigraphic evaluation of the fate of microcrystalline chitosan granules in human stomach

    AU - Säkkinen, Mia

    AU - Marvola, Janne

    AU - Kanerva, Hanna

    AU - Lindevall, Maija

    AU - Lipponen, Maija

    AU - Kekki, Tommi

    AU - Ahonen, Aapo

    AU - Marvola, Martti

    PY - 2004

    Y1 - 2004

    N2 - In several reports of in vitro studies it has been suggested that the mucoadhesive chitosans could be of value in preparing gastro-retentive formulations. The aim of this study was to obtain direct in vivo evidence of whether microcrystalline chitosan (MCCh) formulations acted as gastro-retentive systems in humans. Neutron-activation-based gamma scintigraphy was used to study gastric residence times of MCCh granules in healthy male volunteers. Possible effects of neutron irradiation on the properties of the MCCh granules were studied in advance, in vitro. In vivo gamma scintigraphic evaluations were carried out with the subjects in a fasted state, using granules containing 95% (F1) or 40% (F2) of MCCh of molecular weight 150 kDa. Reference formulation (F3) was lactose granules. The reference granules passed rapidly from the stomach (mean t50% 0.5±0.3 h (n=5)). MCCh in granules prolonged gastric residence times of the formulations in only a few cases (in one volunteer in the F1 group (n=4) and in two volunteers in the F2 group (n=5)). Maximum individual t50% values were 2.1 h (F1) and 2.3 h (F2). It was concluded that the in vivo mucoadhesion of MCCh formulations is erratic, and that the formulations studied are not reliable gastro-retentive drug delivery systems.

    AB - In several reports of in vitro studies it has been suggested that the mucoadhesive chitosans could be of value in preparing gastro-retentive formulations. The aim of this study was to obtain direct in vivo evidence of whether microcrystalline chitosan (MCCh) formulations acted as gastro-retentive systems in humans. Neutron-activation-based gamma scintigraphy was used to study gastric residence times of MCCh granules in healthy male volunteers. Possible effects of neutron irradiation on the properties of the MCCh granules were studied in advance, in vitro. In vivo gamma scintigraphic evaluations were carried out with the subjects in a fasted state, using granules containing 95% (F1) or 40% (F2) of MCCh of molecular weight 150 kDa. Reference formulation (F3) was lactose granules. The reference granules passed rapidly from the stomach (mean t50% 0.5±0.3 h (n=5)). MCCh in granules prolonged gastric residence times of the formulations in only a few cases (in one volunteer in the F1 group (n=4) and in two volunteers in the F2 group (n=5)). Maximum individual t50% values were 2.1 h (F1) and 2.3 h (F2). It was concluded that the in vivo mucoadhesion of MCCh formulations is erratic, and that the formulations studied are not reliable gastro-retentive drug delivery systems.

    KW - microcrystalline chitosan

    KW - mucoadhesion

    KW - gastro-retentive

    KW - gamma scintigraphy

    KW - neutron activation

    KW - samarium

    U2 - 10.1016/S0939-6411(03)00097-3

    DO - 10.1016/S0939-6411(03)00097-3

    M3 - Article

    VL - 57

    SP - 133

    EP - 143

    JO - European Journal of Pharmaceutics and Biopharmaceutics

    JF - European Journal of Pharmaceutics and Biopharmaceutics

    SN - 0939-6411

    IS - 1

    ER -