Abstract
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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Acknowledgements
The present study was supported in part by a Grant-in-Aid for Young Scientists (B) (25860127) from the Japan Society for the Promotion of Sciences (JSPS).
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All animal experiments were performed according to the guidelines of the Tokyo University of Pharmacy and Life Sciences. The study was approved by the Tokyo University of Pharmacy and Life Sciences Committee on the Care and Use of Laboratory Animals (approval number: P13-42 and P14-69).
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Takizawa, Y., Furuno, Y. & Hayashi, M. Effects of polyvinylpyrrolidone (K90) on membrane permeation via the transcellular route in the rat jejunum. J. Pharm. Investig. 51, 311–316 (2021). https://doi.org/10.1007/s40005-021-00514-2
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DOI: https://doi.org/10.1007/s40005-021-00514-2