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KMID : 1146920210510030311
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Journal of Pharmaceutical Investigation
2021 Volume.51 No. 3 p.311 ~ p.316
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Effects of polyvinylpyrrolidone (K90) on membrane permeation via the transcellular route in the rat jejunum
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Takizawa Yusuke
Furuno Yuka
Hayashi Masahiro
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Abstract
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Purpose: Although pharmaceutical excipients do not affect the membrane permeation of active drugs, some have been shown to influence absorption-regulating factors. However, limited information is currently available on the effects of pharmaceutical excipients on membrane permeation via passive transcellular transport, which is the main membrane permeation route of many drugs.
Methods: We herein focused on polyvinylpyrrolidone (PVP) (K90), which is used as a diluent and binder in pharmaceutical formulations, and examined its effects on passive transport via the transcellular route in the rat jejunum using the in vitro sac method.
Results: The membrane permeation of β-naphthol, a passive transcellular marker, was increased by the co-existence of 0.02 w/v % PVP (K90). However, PVP (K90)-induced increases in membrane permeation were not observed following a pre-incubation with PVP (K90). Therefore, PVP (K90)-induced increases in membrane permeation may be attributed to a drug-excipient interaction, but not a mucosal membrane-excipient interaction.
Conclusion: PVP (K90) affected membrane transport via the transcellular route in the rat jejunum. However, since the coexistence of PVP (K90) did not influence membrane protein expression levels or cause membrane lesions, the absorption of active drugs may be regulated by the optimal application of PVP (K90).
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KEYWORD
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Polyvinylpyrrolidone (K90), Passive transport, Transcellular route, Pharmaceutical excipient, Unstirred water layer
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