Original articleBioavailability of tobramycin after oral delivery in FVB mice using CRL-1605 copolymer, an inhibitor of P-glycoprotein
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Thiomers: Influence of molecular mass and thiol group content of poly(acrylic acid) on efflux pump inhibition
2015, International Journal of PharmaceuticsCitation Excerpt :Moreover, in vivo studies showed an increase in relative bioavailability of paclitaxel for 6.3-fold in rats. Another group used CRL-105 copolymer of polyoxypropylene and polyoxyethylene blocks to increase the absorption of P-gp substrates amikacin and tobramycin in vivo in rats (Jagannath et al., 1999; Banerjee et al., 2000). In the past decade a new generation of polymers—thiolated polymers—has emerged as a promising new type of polymeric excipients for use in oral pharmaceutical formulations.
Hydroxypropyl-Sulfobutyl-β-Cyclodextrin improves the oral bioavailability of edaravone by modulating drug efflux pump of enterocytes
2014, Journal of Pharmaceutical SciencesCitation Excerpt :However, these Pgp inhibitors were not enough to increase intracellular concentrations of anticancer drugs in clinical trials. On the contrary, Pgp inhibitors were also employed to improve the bioavailability of Pgp substrates.45-47 Nevertheless, some shortages have been considered accompanying with these effects, including the adverse effect owing to their pharmacological activities.
Intranasal delivery of streptomycin sulfate (STRS) loaded solid lipid nanoparticles to brain and blood
2014, International Journal of PharmaceuticsCitation Excerpt :Nevertheless, several factors like dose related toxicity, development of resistance and poor patient compliance due to the invasive therapy (streptomycin is given intramuscularly) limit its widespread use. Need for parenteral therapy is attributed to loss of its bioactivity in the acidic pH of the stomach due to ionization, poor permeability across intestinal epithelium due to its highly hydrophilic nature (log p = −6.7), a high molecular weight (1457.4 Da) and its proneness to P-gp efflux (Banerjee et al., 2000). It is indicated that STRS cannot reach across the (<10% of the administered dose) normal human brain due to its inability to cross intact blood brain barrier (BBB), while >25% of the administered STRS may reach brain in patients with tubercular meningitis due to the disruption of the BBB.
Polymers influencing transportability profile of drug
2013, Saudi Pharmaceutical JournalCitation Excerpt :Furthermore, it has been demonstrated that the efflux pump inhibitory effect of pluronics gets reduced when its concentration reaches toward critical micelle concentration (CMC). Banerjee et al. (2000) and Jagannath et al. (1999), in separate studies have demonstrated the PGP efflux pump inhibitory activity of CRL-1605 copolymer to improve tobramycin and amikacin oral uptake. Kabanov et al. (2003) have discussed different mechanisms behind the efflux pump inhibitory activity of pluronics and its role in the delivery of efflux pump substrates across BBB.
Enhanced oral bioavailability of paclitaxel in pluronic/LHR mixed polymeric micelles: Preparation, in vitro and in vivo evaluation
2012, European Journal of Pharmaceutical SciencesCitation Excerpt :It was shown that pluronic inhibited the P-gp efflux system in Caco-2 monolayers, resulting in a significant enhancement of absorption and permeability of rhodamine 123 (Batrakova et al., 1998, 1999). Furthermore, increased oral uptake of tobramicin and amikacin which could be P-gp substrates was observed in the presence of poloxamer CRL-1605 (Banerjee et al., 2000; Jagannath et al., 1999). Another study has shown that pluronic F68 can improve the pharmacokinetics of orally administered drugs that are P-gp and/or CYP3A4 substrates in vivo such as rifampicin, celiprolol and midazolam (Ma et al., 2011; Huang et al., 2008).
Drug transporters in the lung - Do they play a role in the biopharmaceutics of inhaled drugs?
2010, Journal of Pharmaceutical Sciences