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Article

The Biological Fate of Pharmaceutical Excipient β-Cyclodextrin: Pharmacokinetics, Tissue Distribution, Excretion, and Metabolism of β-Cyclodextrin in Rats

by
Kunqian Mu
1,
Kaiwen Jiang
1,
Yue Wang
1,
Zihan Zhao
1,
Song Cang
1,
Kaishun Bi
1,
Qing Li
1 and
Ran Liu
1,2,*
1
School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang 110016, China
2
School of Food and Drug, Shenzhen Polytechnic, 7098 Lau sin Avenue, Shenzhen 518115, China
*
Author to whom correspondence should be addressed.
Molecules 2022, 27(3), 1138; https://doi.org/10.3390/molecules27031138
Submission received: 27 January 2022 / Revised: 5 February 2022 / Accepted: 6 February 2022 / Published: 8 February 2022
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Abstract

β-cyclodextrin has a unique annular hollow ultrastructure that allows encapsulation of various poorly water-soluble drugs in the resulting cavity, thereby increasing drug stability. As a bioactive molecule, the metabolism of β-cyclodextrin is mainly completed by the flora in the colon, which can interact with API. In this study, understanding the in vivo fate of β-cyclodextrin, a LC-MS/MS method was developed to facilitate simultaneous quantitative analysis of pharmaceutical excipient β-cyclodextrin and API dextromethorphan hydrobromide. The established method had been effectively used to study the pharmacokinetics, tissue distribution, excretion, and metabolism of β-cyclodextrin after oral administration in rats. Results showed that β-cyclodextrin was almost wholly removed from rat plasma within 36 h, and high concentrations of β-cyclodextrin distributed hastily to organs with increased blood flow velocities such as the spleen, liver, and kidney after administration. The excretion of intact β-cyclodextrin to urine and feces was lower than the administration dose. It can be speculated that β-cyclodextrin metabolized to maltodextrin, which was further metabolized, absorbed, and eventually discharged in the form of CO2 and H2O. Results proved that β-cyclodextrin, with relative low accumulation in the body, had good safety. The results will assist further study of the design and safety evaluation of adjuvant β-cyclodextrin and promote its clinical development.
Keywords: LC-MS/MS; β-cyclodextrin; pharmacokinetics; tissue distribution; excretion; metabolism LC-MS/MS; β-cyclodextrin; pharmacokinetics; tissue distribution; excretion; metabolism
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MDPI and ACS Style

Mu, K.; Jiang, K.; Wang, Y.; Zhao, Z.; Cang, S.; Bi, K.; Li, Q.; Liu, R. The Biological Fate of Pharmaceutical Excipient β-Cyclodextrin: Pharmacokinetics, Tissue Distribution, Excretion, and Metabolism of β-Cyclodextrin in Rats. Molecules 2022, 27, 1138. https://doi.org/10.3390/molecules27031138

AMA Style

Mu K, Jiang K, Wang Y, Zhao Z, Cang S, Bi K, Li Q, Liu R. The Biological Fate of Pharmaceutical Excipient β-Cyclodextrin: Pharmacokinetics, Tissue Distribution, Excretion, and Metabolism of β-Cyclodextrin in Rats. Molecules. 2022; 27(3):1138. https://doi.org/10.3390/molecules27031138

Chicago/Turabian Style

Mu, Kunqian, Kaiwen Jiang, Yue Wang, Zihan Zhao, Song Cang, Kaishun Bi, Qing Li, and Ran Liu. 2022. "The Biological Fate of Pharmaceutical Excipient β-Cyclodextrin: Pharmacokinetics, Tissue Distribution, Excretion, and Metabolism of β-Cyclodextrin in Rats" Molecules 27, no. 3: 1138. https://doi.org/10.3390/molecules27031138

APA Style

Mu, K., Jiang, K., Wang, Y., Zhao, Z., Cang, S., Bi, K., Li, Q., & Liu, R. (2022). The Biological Fate of Pharmaceutical Excipient β-Cyclodextrin: Pharmacokinetics, Tissue Distribution, Excretion, and Metabolism of β-Cyclodextrin in Rats. Molecules, 27(3), 1138. https://doi.org/10.3390/molecules27031138

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