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.
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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

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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

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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.

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KW - gastro-retentive

KW - gamma scintigraphy

KW - neutron activation

KW - samarium

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

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JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

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