The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins

Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients re...
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Autor*in:	Siyuan Cao [verfasserIn] Min Zhang [verfasserIn] Minyan Yuan [verfasserIn] Dan Yang [verfasserIn] Mei Zhao [verfasserIn] Shuo Zhang [verfasserIn] Pengjiao Wang [verfasserIn] Rongping Zhang [verfasserIn] Xiuli Gao [verfasserIn]

Format:	E-Artikel
Sprache:	Englisch

Erschienen:	2022

Schlagwörter:	baicalein baicalein‐6‐O‐β‐d‐glucuronide baicalein‐7‐O‐β‐d‐glucuronide Caco‐2 cell transport proteins UDP‐glucuronosyltransferases

Übergeordnetes Werk:	In: Pharmacology Research & Perspectives - Wiley, 2016, 10(2022), 1, Seite n/a-n/a
Übergeordnetes Werk:	volume:10 ; year:2022 ; number:1 ; pages:n/a-n/a

Links:	Link aufrufen Link aufrufen Link aufrufen Journal toc

DOI / URN:	10.1002/prp2.928

Katalog-ID:	DOAJ047774452

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245	1	4	\|a The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins
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520			\|a Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein.
650		4	\|a baicalein
650		4	\|a baicalein‐6‐O‐β‐d‐glucuronide
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650		4	\|a transport proteins
650		4	\|a UDP‐glucuronosyltransferases
653		0	\|a Therapeutics. Pharmacology
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700	0		\|a Minyan Yuan \|e verfasserin \|4 aut
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700	0		\|a Shuo Zhang \|e verfasserin \|4 aut
700	0		\|a Pengjiao Wang \|e verfasserin \|4 aut
700	0		\|a Rongping Zhang \|e verfasserin \|4 aut
700	0		\|a Xiuli Gao \|e verfasserin \|4 aut
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912			\|a GBV_ILN_171
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912			\|a GBV_ILN_213
912			\|a GBV_ILN_224
912			\|a GBV_ILN_230
912			\|a GBV_ILN_285
912			\|a GBV_ILN_293
912			\|a GBV_ILN_602
912			\|a GBV_ILN_636
912			\|a GBV_ILN_2004
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912			\|a GBV_ILN_2106
912			\|a GBV_ILN_2108
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allfields	10.1002/prp2.928 doi (DE-627)DOAJ047774452 (DE-599)DOAJ2b5944fcc91342f3b0f75592f859c065 DE-627 ger DE-627 rakwb eng RM1-950 Siyuan Cao verfasserin aut The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein. baicalein baicalein‐6‐O‐β‐d‐glucuronide baicalein‐7‐O‐β‐d‐glucuronide Caco‐2 cell transport proteins UDP‐glucuronosyltransferases Therapeutics. Pharmacology Min Zhang verfasserin aut Minyan Yuan verfasserin aut Dan Yang verfasserin aut Mei Zhao verfasserin aut Shuo Zhang verfasserin aut Pengjiao Wang verfasserin aut Rongping Zhang verfasserin aut Xiuli Gao verfasserin aut In Pharmacology Research & Perspectives Wiley, 2016 10(2022), 1, Seite n/a-n/a (DE-627)771394683 (DE-600)2740389-0 20521707 nnns volume:10 year:2022 number:1 pages:n/a-n/a https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/article/2b5944fcc91342f3b0f75592f859c065 kostenfrei https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/toc/2052-1707 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_636 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022 1 n/a-n/a
spelling	10.1002/prp2.928 doi (DE-627)DOAJ047774452 (DE-599)DOAJ2b5944fcc91342f3b0f75592f859c065 DE-627 ger DE-627 rakwb eng RM1-950 Siyuan Cao verfasserin aut The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein. baicalein baicalein‐6‐O‐β‐d‐glucuronide baicalein‐7‐O‐β‐d‐glucuronide Caco‐2 cell transport proteins UDP‐glucuronosyltransferases Therapeutics. Pharmacology Min Zhang verfasserin aut Minyan Yuan verfasserin aut Dan Yang verfasserin aut Mei Zhao verfasserin aut Shuo Zhang verfasserin aut Pengjiao Wang verfasserin aut Rongping Zhang verfasserin aut Xiuli Gao verfasserin aut In Pharmacology Research & Perspectives Wiley, 2016 10(2022), 1, Seite n/a-n/a (DE-627)771394683 (DE-600)2740389-0 20521707 nnns volume:10 year:2022 number:1 pages:n/a-n/a https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/article/2b5944fcc91342f3b0f75592f859c065 kostenfrei https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/toc/2052-1707 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_636 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022 1 n/a-n/a
allfields_unstemmed	10.1002/prp2.928 doi (DE-627)DOAJ047774452 (DE-599)DOAJ2b5944fcc91342f3b0f75592f859c065 DE-627 ger DE-627 rakwb eng RM1-950 Siyuan Cao verfasserin aut The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein. baicalein baicalein‐6‐O‐β‐d‐glucuronide baicalein‐7‐O‐β‐d‐glucuronide Caco‐2 cell transport proteins UDP‐glucuronosyltransferases Therapeutics. Pharmacology Min Zhang verfasserin aut Minyan Yuan verfasserin aut Dan Yang verfasserin aut Mei Zhao verfasserin aut Shuo Zhang verfasserin aut Pengjiao Wang verfasserin aut Rongping Zhang verfasserin aut Xiuli Gao verfasserin aut In Pharmacology Research & Perspectives Wiley, 2016 10(2022), 1, Seite n/a-n/a (DE-627)771394683 (DE-600)2740389-0 20521707 nnns volume:10 year:2022 number:1 pages:n/a-n/a https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/article/2b5944fcc91342f3b0f75592f859c065 kostenfrei https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/toc/2052-1707 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_636 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022 1 n/a-n/a
allfieldsGer	10.1002/prp2.928 doi (DE-627)DOAJ047774452 (DE-599)DOAJ2b5944fcc91342f3b0f75592f859c065 DE-627 ger DE-627 rakwb eng RM1-950 Siyuan Cao verfasserin aut The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein. baicalein baicalein‐6‐O‐β‐d‐glucuronide baicalein‐7‐O‐β‐d‐glucuronide Caco‐2 cell transport proteins UDP‐glucuronosyltransferases Therapeutics. Pharmacology Min Zhang verfasserin aut Minyan Yuan verfasserin aut Dan Yang verfasserin aut Mei Zhao verfasserin aut Shuo Zhang verfasserin aut Pengjiao Wang verfasserin aut Rongping Zhang verfasserin aut Xiuli Gao verfasserin aut In Pharmacology Research & Perspectives Wiley, 2016 10(2022), 1, Seite n/a-n/a (DE-627)771394683 (DE-600)2740389-0 20521707 nnns volume:10 year:2022 number:1 pages:n/a-n/a https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/article/2b5944fcc91342f3b0f75592f859c065 kostenfrei https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/toc/2052-1707 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_636 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022 1 n/a-n/a
allfieldsSound	10.1002/prp2.928 doi (DE-627)DOAJ047774452 (DE-599)DOAJ2b5944fcc91342f3b0f75592f859c065 DE-627 ger DE-627 rakwb eng RM1-950 Siyuan Cao verfasserin aut The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins 2022 Text txt rdacontent Computermedien c rdamedia Online-Ressource cr rdacarrier Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein. baicalein baicalein‐6‐O‐β‐d‐glucuronide baicalein‐7‐O‐β‐d‐glucuronide Caco‐2 cell transport proteins UDP‐glucuronosyltransferases Therapeutics. Pharmacology Min Zhang verfasserin aut Minyan Yuan verfasserin aut Dan Yang verfasserin aut Mei Zhao verfasserin aut Shuo Zhang verfasserin aut Pengjiao Wang verfasserin aut Rongping Zhang verfasserin aut Xiuli Gao verfasserin aut In Pharmacology Research & Perspectives Wiley, 2016 10(2022), 1, Seite n/a-n/a (DE-627)771394683 (DE-600)2740389-0 20521707 nnns volume:10 year:2022 number:1 pages:n/a-n/a https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/article/2b5944fcc91342f3b0f75592f859c065 kostenfrei https://doi.org/10.1002/prp2.928 kostenfrei https://doaj.org/toc/2052-1707 Journal toc kostenfrei GBV_USEFLAG_A SYSFLAG_A GBV_DOAJ SSG-OLC-PHA GBV_ILN_20 GBV_ILN_22 GBV_ILN_23 GBV_ILN_24 GBV_ILN_31 GBV_ILN_39 GBV_ILN_40 GBV_ILN_60 GBV_ILN_62 GBV_ILN_63 GBV_ILN_65 GBV_ILN_69 GBV_ILN_73 GBV_ILN_74 GBV_ILN_95 GBV_ILN_105 GBV_ILN_110 GBV_ILN_151 GBV_ILN_161 GBV_ILN_170 GBV_ILN_171 GBV_ILN_206 GBV_ILN_213 GBV_ILN_224 GBV_ILN_230 GBV_ILN_285 GBV_ILN_293 GBV_ILN_602 GBV_ILN_636 GBV_ILN_2004 GBV_ILN_2005 GBV_ILN_2006 GBV_ILN_2007 GBV_ILN_2009 GBV_ILN_2010 GBV_ILN_2011 GBV_ILN_2014 GBV_ILN_2026 GBV_ILN_2027 GBV_ILN_2034 GBV_ILN_2037 GBV_ILN_2038 GBV_ILN_2044 GBV_ILN_2048 GBV_ILN_2049 GBV_ILN_2050 GBV_ILN_2055 GBV_ILN_2056 GBV_ILN_2057 GBV_ILN_2059 GBV_ILN_2061 GBV_ILN_2068 GBV_ILN_2088 GBV_ILN_2106 GBV_ILN_2108 GBV_ILN_2110 GBV_ILN_2111 GBV_ILN_2118 GBV_ILN_2122 GBV_ILN_2143 GBV_ILN_2144 GBV_ILN_2147 GBV_ILN_2148 GBV_ILN_2152 GBV_ILN_2153 GBV_ILN_2232 GBV_ILN_2336 GBV_ILN_2470 GBV_ILN_2507 GBV_ILN_2522 GBV_ILN_4012 GBV_ILN_4035 GBV_ILN_4037 GBV_ILN_4046 GBV_ILN_4112 GBV_ILN_4125 GBV_ILN_4126 GBV_ILN_4242 GBV_ILN_4249 GBV_ILN_4251 GBV_ILN_4305 GBV_ILN_4306 GBV_ILN_4307 GBV_ILN_4313 GBV_ILN_4322 GBV_ILN_4323 GBV_ILN_4324 GBV_ILN_4325 GBV_ILN_4326 GBV_ILN_4333 GBV_ILN_4334 GBV_ILN_4335 GBV_ILN_4336 GBV_ILN_4338 GBV_ILN_4367 GBV_ILN_4700 AR 10 2022 1 n/a-n/a
language	English
source	In Pharmacology Research & Perspectives 10(2022), 1, Seite n/a-n/a volume:10 year:2022 number:1 pages:n/a-n/a
sourceStr	In Pharmacology Research & Perspectives 10(2022), 1, Seite n/a-n/a volume:10 year:2022 number:1 pages:n/a-n/a
format_phy_str_mv	Article
institution	findex.gbv.de
topic_facet	baicalein baicalein‐6‐O‐β‐d‐glucuronide baicalein‐7‐O‐β‐d‐glucuronide Caco‐2 cell transport proteins UDP‐glucuronosyltransferases Therapeutics. Pharmacology
isfreeaccess_bool	true
container_title	Pharmacology Research & Perspectives
authorswithroles_txt_mv	Siyuan Cao @@aut@@ Min Zhang @@aut@@ Minyan Yuan @@aut@@ Dan Yang @@aut@@ Mei Zhao @@aut@@ Shuo Zhang @@aut@@ Pengjiao Wang @@aut@@ Rongping Zhang @@aut@@ Xiuli Gao @@aut@@
publishDateDaySort_date	2022-01-01T00:00:00Z
hierarchy_top_id	771394683
id	DOAJ047774452
language_de	englisch
fullrecord	<?xml version="1.0" encoding="UTF-8"?><collection xmlns="http://www.loc.gov/MARC21/slim"><record><leader>01000caa a22002652 4500</leader><controlfield tag="001">DOAJ047774452</controlfield><controlfield tag="003">DE-627</controlfield><controlfield tag="005">20230502234112.0</controlfield><controlfield tag="007">cr uuu---uuuuu</controlfield><controlfield tag="008">230227s2022 xx \|\|\|\|\|o 00\| \|\|eng c</controlfield><datafield tag="024" ind1="7" ind2=" "><subfield code="a">10.1002/prp2.928</subfield><subfield code="2">doi</subfield></datafield><datafield tag="035" ind1=" " ind2=" "><subfield code="a">(DE-627)DOAJ047774452</subfield></datafield><datafield tag="035" ind1=" " ind2=" "><subfield code="a">(DE-599)DOAJ2b5944fcc91342f3b0f75592f859c065</subfield></datafield><datafield tag="040" ind1=" " ind2=" "><subfield code="a">DE-627</subfield><subfield code="b">ger</subfield><subfield code="c">DE-627</subfield><subfield code="e">rakwb</subfield></datafield><datafield tag="041" ind1=" " ind2=" "><subfield code="a">eng</subfield></datafield><datafield tag="050" ind1=" " ind2="0"><subfield code="a">RM1-950</subfield></datafield><datafield tag="100" ind1="0" ind2=" "><subfield code="a">Siyuan Cao</subfield><subfield code="e">verfasserin</subfield><subfield code="4">aut</subfield></datafield><datafield tag="245" ind1="1" ind2="4"><subfield code="a">The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins</subfield></datafield><datafield tag="264" ind1=" " ind2="1"><subfield code="c">2022</subfield></datafield><datafield tag="336" ind1=" " ind2=" "><subfield code="a">Text</subfield><subfield code="b">txt</subfield><subfield code="2">rdacontent</subfield></datafield><datafield tag="337" ind1=" " ind2=" "><subfield code="a">Computermedien</subfield><subfield code="b">c</subfield><subfield code="2">rdamedia</subfield></datafield><datafield tag="338" ind1=" " ind2=" "><subfield code="a">Online-Ressource</subfield><subfield code="b">cr</subfield><subfield code="2">rdacarrier</subfield></datafield><datafield tag="520" ind1=" " ind2=" "><subfield code="a">Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. 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callnumber-first	R - Medicine
author	Siyuan Cao
spellingShingle	Siyuan Cao misc RM1-950 misc baicalein misc baicalein‐6‐O‐β‐d‐glucuronide misc baicalein‐7‐O‐β‐d‐glucuronide misc Caco‐2 cell misc transport proteins misc UDP‐glucuronosyltransferases misc Therapeutics. Pharmacology The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins
authorStr	Siyuan Cao
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topic_title	RM1-950 The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins baicalein baicalein‐6‐O‐β‐d‐glucuronide baicalein‐7‐O‐β‐d‐glucuronide Caco‐2 cell transport proteins UDP‐glucuronosyltransferases
topic	misc RM1-950 misc baicalein misc baicalein‐6‐O‐β‐d‐glucuronide misc baicalein‐7‐O‐β‐d‐glucuronide misc Caco‐2 cell misc transport proteins misc UDP‐glucuronosyltransferases misc Therapeutics. Pharmacology
topic_unstemmed	misc RM1-950 misc baicalein misc baicalein‐6‐O‐β‐d‐glucuronide misc baicalein‐7‐O‐β‐d‐glucuronide misc Caco‐2 cell misc transport proteins misc UDP‐glucuronosyltransferases misc Therapeutics. Pharmacology
topic_browse	misc RM1-950 misc baicalein misc baicalein‐6‐O‐β‐d‐glucuronide misc baicalein‐7‐O‐β‐d‐glucuronide misc Caco‐2 cell misc transport proteins misc UDP‐glucuronosyltransferases misc Therapeutics. Pharmacology
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title	The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins
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title_full	The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins
author_sort	Siyuan Cao
journal	Pharmacology Research & Perspectives
journalStr	Pharmacology Research & Perspectives
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author_browse	Siyuan Cao Min Zhang Minyan Yuan Dan Yang Mei Zhao Shuo Zhang Pengjiao Wang Rongping Zhang Xiuli Gao
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author-letter	Siyuan Cao
doi_str_mv	10.1002/prp2.928
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title_sort	pharmaceutical excipient peg400 affect the absorption of baicalein in caco‐2 monolayer model by interacting with udp‐glucuronosyltransferases and efflux transport proteins
callnumber	RM1-950
title_auth	The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins
abstract	Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein.
abstractGer	Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein.
abstract_unstemmed	Abstract The bioavailability of drugs is often related to intestinal metabolism and transport mechanisms. In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. We initially found that baicalein in the Caco‐2 monolayer would be metabolized into glucuronide conjugates BG and B6G under the action of UGT1A8 and UGT1A9 on the endoplasmic reticulum membrane, and then mainly excreted to different sides by acting of MRP and BCRP. The addition of PEG400 significantly accelerated the metabolism of B in Caco‐2 cells and increased the penetration of BG and B6G. Furthermore, PEG400 also significantly decreased the efflux ratio of BG and B6G, which was the evidence of the interaction with the efflux transporters. In the in vitro intestinal microsome regeneration system, low concentration PEG400 decreased the Km value of UGT1A8 and UGT1A9 (key enzymes that mediate the production of BG and B6G); high concentration PEG400 enhanced the Vmax value of UGT1A8 and UGT1A9. In conclusion, our results determined that PEG400 interacted with some UGTs and efflux transporters, which were the main factors affecting the absorption of baicalein.
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title_short	The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins
url	https://doi.org/10.1002/prp2.928 https://doaj.org/article/2b5944fcc91342f3b0f75592f859c065 https://doaj.org/toc/2052-1707
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author2	Min Zhang Minyan Yuan Dan Yang Mei Zhao Shuo Zhang Pengjiao Wang Rongping Zhang Xiuli Gao
author2Str	Min Zhang Minyan Yuan Dan Yang Mei Zhao Shuo Zhang Pengjiao Wang Rongping Zhang Xiuli Gao
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callnumber-subject	RM - Therapeutics and Pharmacology
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doi_str	10.1002/prp2.928
callnumber-a	RM1-950
up_date	2024-07-03T14:03:41.231Z
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In previous studies, pharmaceutical excipients were recognized as inert substances in clinical safety evaluations. However, a large number of studies have shown that pharmaceutical excipients regulate the metabolism and transport of drugs in the body and improve the bioavailability. The pharmaceutical excipient polyethylene glycol 400 (PEG400) as a good solubilizer and surfactant has the potential to improve the bioavailability of drugs. The combined action of UDP‐glucuronosyltransferases (UGTs) and efflux transport proteins is responsible for the intestinal disposition and poor bioavailability of baicalein. Our aim is to study the effect of PEG400 on the absorption of baicalein on the Caco‐2 monolayer, and confirm the interaction of PEG400 with UGTs (UGT1A8 and UGT1A9) and efflux transports. 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The pharmaceutical excipient PEG400 affect the absorption of baicalein in Caco‐2 monolayer model by interacting with UDP‐glucuronosyltransferases and efflux transport proteins

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