ArticlePharmaceutical research2025
Pharmacokinetic Assessment of Drug Efflux from Erythrocytes Loaded with Corticosteroid Esters.
Article in Pharmaceutical research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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2 authors.
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Abstract
purposeDrugs can be found in erythrocytes (RBC) in accordance with their physicochemical and specific binding properties, but particularly high concentrations can be attained using an ex vivo hypotonic pre-swelling method. Pharmacokinetic (PK) methodology and characterization of in vivo data for RBC-loaded corticosteroid prodrugs was sought.
methodsThree studies providing in vitro and in vivo assessments of the pharmacokinetics of steroid ester prodrugs loaded into RBC were found. A PK model involving three fractional input rates and two-compartment disposition was applied.
resultsAfter their sodium phosphate ester pro-drugs were loaded into RBC and dosed intravenously, dexamethasone (DEX) and betamethasone (BET) plasma concentrations were markedly prolonged with three phases in humans and animals. For DEX in humans, a PK model accounted for the typical biexponential disposition of the active steroid and for input of a large fraction (0.72) released within 1 h, a small fraction (0.27) released over several hours (t
conclusionsThe proposed PK methodology well characterized the input properties of RBC-loaded controlled-release formulations of corticosteroids in animal and humans in context of the flip-flop kinetics of the released drug. The model may be relevant to other types of RBC-loaded therapeutic agents.
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