Systemic Design and Evaluation of Ticagrelor-Loaded Nanostructured Lipid Carriers for Enhancing Bioavailability and Antiplatelet Activity.

ABSTRACT: Ticagrelor (TGL), a P2Y₁₂ receptor antagonist, is classified as biopharmaceutics classification system (BCS) class IV drug due to its poor solubility and permeability, resulting in low oral bioavailability. Nanostructured lipid carriers (NLC) are an efficient delivery system for the improvement of bioavailability of BCS class IV drugs. Hence, we prepared TGL-loaded NLC (TGL-NLC) to enhance the oral bioavailability and antiplatelet activity of TGL with a systemic design approach. The optimized TGL-NLC with Box-Behnken design showed a small particle size of 87.6 nm and high encapsulation efficiency of 92.1%. Scanning electron microscope (SEM), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) were performed to investigate the characteristics of TGL-NLC.

SUBMITTER: Son GH 

PROVIDER: S-EPMC6572397 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature