ArticleDrug metabolism and disposition: the biological fate of chemicals2007
Improvement of the oral drug absorption of topotecan through the inhibition of intestinal xenobiotic efflux transporter, breast cancer resistance protein, by excipients.
Article in Drug metabolism and disposition: the biological fate of chemicals, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 103 citations in OpenAlex.
- Polyethylene glycol 400 enhances the bioavailability of a BCS class III drug (ranitidine) in male subjects but not females.Pharmaceutical research · 2008Trial
- Pluronic F-68 and F-127 Based Nanomedicines for Advancing Combination Cancer Therapy.Pharmaceutics · 2023Review
- Article
- Dual Inhibition of P-gp and BCRP Improves Oral Topotecan Bioavailability in Rodents.Pharmaceutics · 2021Article
- Human non‑small cell lung cancer cells can be sensitized to camptothecin by modulating autophagy.International journal of oncology · 2018Article
- The Effects of Pharmaceutical Excipients on Gastrointestinal Tract Metabolic Enzymes and Transporters-an Update.The AAPS journal · 2016Article
- Degradable Controlled-Release Polymers and Polymeric Nanoparticles: Mechanisms of Controlling Drug Release.Chemical reviews · 2016Review
- San-Huang-Xie-Xin-Tang Constituents Exert Drug-Drug Interaction of Mutual Reinforcement at Both Pharmacodynamics and Pharmacokinetic Level: A Review.Frontiers in pharmacology · 2016Review
- Formulation strategies for drug delivery of tacrolimus: An overview.International journal of pharmaceutical investigation · 2012Article
- Pharmacokinetic modeling to assess factors affecting the oral bioavailability of the lactone and carboxylate forms of the lipophilic camptothecin analogue AR-67 in rats.Pharmaceutical research · 2012Article
- Physiologically based pharmacokinetic model for topotecan in mice.Journal of pharmacokinetics and pharmacodynamics · 2011Article
- Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells.Pharmaceutical research · 2010Article
- Xenobiotic, bile acid, and cholesterol transporters: function and regulation.Pharmacological reviews · 2010Review
- A Novel Docetaxel-Loaded Poly (ε-Caprolactone)/Pluronic F68 Nanoparticle Overcoming Multidrug Resistance for Breast Cancer Treatment.Nanoscale research letters · 2009Article
- Pluronic block copolymers: evolution of drug delivery concept from inert nanocarriers to biological response modifiers.Journal of controlled release : official journal of the Controlled Release Society · 2008Review
- A novel nanocapsule delivery system to overcome intestinal degradation and drug transport limited absorption of P-glycoprotein substrate drugs.Pharmaceutical research · 2008Article
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Recently, breast cancer resistance protein (BCRP/ABCG2) has been shown to limit the oral absorption of its substrates in the intestine. The purpose of this study was to examine whether excipients can be used as inhibitors of BCRP, to improve the oral drug absorption of BCRP substrates. In wild-type mice, Pluronic P85 and Tween 20, given orally 15 min before topotecan administration, increased the area under the plasma concentration-time curve (AUC) of topotecan after oral administration (2.0- and 1.8-fold, respectively). In contrast, Pluronic P85 and Tween 20 were less effective (no significant difference) on the AUC of topotecan after oral administration in Bcrp (-/-) mice (1.2- and 1.2-fold, respectively). Pluronic P85 and Tween 20 given orally did not affect significantly the AUC of topotecan after intravenous administration in wild-type and Bcrp (-/-) mice. Moreover, we determined the mucosal-to-serosal absorptive transport of topotecan using everted mouse ileum. Pluronic P85 and Tween 20 significantly increased the intestinal absorption rate of topotecan in everted sacs from wild-type mice whereas, in everted sacs from Bcrp (-/-) mice, the absorption rate was 2.1-fold greater than that in wild-type mice, and these excipients were not significantly effective. There was no significant difference in the intestinal P-glycoprotein (P-gp) expression and serosal-to-mucosal secretory transport of rhodamine 123, a typical P-gp substrate. Taken together, these results suggest that Pluronic P85 and Tween 20 can improve the oral bioavailability of BCRP substrates by inhibiting BCRP function in the small intestine.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.