Why the study?
Ticagrelor is used to inhibit platelet aggregation in acute coronary syndrome, but poor solubility and low bioavailability limit its in vivo efficacy.
Does a ticagrelor-loaded self-microemulsifying drug delivery system improve oral bioavailability and antiplatelet activity compared to raw ticagrelor suspension in rats?
Population
Caco-2 cells and rats
Comparison
Ticagrelor-loaded self-microemulsifying drug delivery system vs raw ticagrelor suspension or Brilinta
Design
Preclinical formulation and pharmacokinetic study
Key result
An optimized ticagrelor-loaded SMEDDS formulation at 5 mg/kg achieved a similar area under the inhibitory curve for antiplatelet activity as a 10 mg/kg dose of raw ticagrelor suspension in rats.
Authors
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Half-dose ticagrelor-SMEDDS matches suspension antiplatelet effect in rats; leaves open clinical translation and human outcomes.
Does a ticagrelor-loaded self-microemulsifying drug delivery system improve oral bioavailability and antiplatelet activity compared to raw ticagrelor suspension in rats?
Absolute Event Rate: 907.8% vs 907%
A novel self-microemulsifying drug delivery system for ticagrelor significantly enhanced its oral bioavailability and antiplatelet efficacy in a preclinical rat model.
Na et al. (2019) studied Acute coronary syndrome (preclinical model). Ticagrelor-loaded SMEDDS (TCG-SM) vs. Raw ticagrelor suspension (10 mg/kg) was evaluated on Area under the inhibitory curve for antiplatelet activity. An optimized ticagrelor-loaded SMEDDS formulation at 5 mg/kg achieved a similar area under the inhibitory curve for antiplatelet activity as a 10 mg/kg dose of raw ticagrelor suspension in rats.
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