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Open AccessArticle

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

1
College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99, Daehak-ro, Yuseong-gu, Daejeon 34134, Korea
2
Present affiliation: Korea United Pharmaceutical Co. Ltd., 25-23, Nojangongdan-gil. Jeondong-myeon, Sejong 30011, Korea
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2019, 11(5), 222; https://doi.org/10.3390/pharmaceutics11050222
Received: 15 April 2019 / Revised: 3 May 2019 / Accepted: 6 May 2019 / Published: 8 May 2019
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. Furthermore, TGL-NLC exhibited biocompatible cytotoxicity against Caco-2 cells. Cellular uptake of TGL-NLC was 1.56-fold higher than that of raw TGL on Caco-2 cells. In pharmacokinetic study, the oral bioavailability of TGL-NLC was 254.99% higher than that of raw TGL. In addition, pharmacodynamic study demonstrated that the antiplatelet activity of TGL-NLC was superior to that of raw TGL, based on enhanced bioavailability of TGL-NLC. These results suggest that TGL-NLC can be applied for efficient oral absorption and antiplatelet activity of TGL. View Full-Text
Keywords: ticagrelor; nanostructured lipid carrier; design of experiments; Box–Behnken design; bioavailability; antiplatelet activity ticagrelor; nanostructured lipid carrier; design of experiments; Box–Behnken design; bioavailability; antiplatelet activity
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Son, G.-H.; Na, Y.-G.; Huh, H.W.; Wang, M.; Kim, M.-K.; Han, M.-G.; Byeon, J.-J.; Lee, H.-K.; Cho, C.-W. Systemic Design and Evaluation of Ticagrelor-Loaded Nanostructured Lipid Carriers for Enhancing Bioavailability and Antiplatelet Activity. Pharmaceutics 2019, 11, 222.

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