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

    Keywords

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

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