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One of the main reasons for treatment failure and variability in cellular response, despite the drug being at a therapeutically effective concentration in the plasma, is the development of multidrug resistance to therapeutic medications mediated by drug transporters.
The therapeutically effective concentration of clarithromycin, 5 mg/ml, was achieved using tocopherol succinate (TS) combined with oleic acid as lipophilic counterions.
Thus, it was exhibited that compound 4c showed strong cytotoxicity selectivity to human hepatocellular carcinoma cells in vitro at the therapeutically effective concentration.
Although the daily intake of EGCG through regular tea drinking may not reach a therapeutically effective concentration, it should be noted that tea and coffee also contain many other polyphenolic antioxidants.
ZB497 is shown to have a unique advantage in that it can reach therapeutically effective concentration of 4-OHT at a fraction of the dose that would be required if tamoxifen or 4-OHT is administered.
Amphotericin B, when administered systemically, does not reach a therapeutically effective concentration at the site of infection with Pythium insidiosum and can be associated with adverse effects such as nephrotoxicity and anaemia [ 16, 17].
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The other vitamin K-dependent proteins of the clotting cascade, protein S and C, are present in therapeutically effective concentrations to provide antithrombotic effects.
Regional overactivity of efflux transporters at the BBB is thought to contribute to drug resistance by impeding therapeutically effective concentrations of antiepileptic drugs at their sites of action [2].
These data demonstrate that the poloxamer 188-coated PLGA nanoparticles enable delivery of doxorubicin across the blood-brain barrier in the therapeutically effective concentrations.
Together with the data obtained previously, the results of the present study unequivocally demonstrate that PLGA nanoparticles coated with poloxamer 188 enable brain delivery of agents that cannot independently permeate across the blood-brain barrier in therapeutically effective concentrations.
Voriconazole achieves therapeutically effective concentrations in the epithelial lining fluid after standard doses [ 71- 73].
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Justyna Jupowicz-Kozak
CEO of Professional Science Editing for Scientists @ prosciediting.com