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KMID : 0613820210310050502
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Journal of Life Science
2021 Volume.31 No. 5 p.502 ~ p.510
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Development of Solid Self-nanoemulsifying Drug Delivery Systems of Ticagrelor Using Porous Carriers
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Choi Hyung-Joo
Kim Kyeong-Soo
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Abstract
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The objective of this study was to develop a novel ticagrelor-loaded self-nanoemulsifying drug delivery system with an enhanced solubility and dissolution rate. Numerous oils and surfactants were screened, then medium chain triglyceride (MCT) oil and the surfactants polyoxyethylene sorbitan monooleate (Tween 80) and Labrafil M1944CS were selected for the preparation of the ticagrelor-loaded self-nanoemulsifying drug delivery system. A pseudo-ternary phase diagram was constructed to detect the nanoemulsion region. Of the various formulations tested, the liquid SNEDDS, composed of MCT (oil), Tween 80 (surfactant), and Labrafil M1944CS (cosurfactant) at a weight ratio of 20/70/10 produced the smallest emulsion droplet size (around 20.56±0.70 nm). Then, particle size, polydispersity, and zeta potential were measured using drugs containing liquid SNEDDS. The selected ticagrelor- loaded liquid SNEDDS was spray-dried to convert it into a ticagrelor-loaded solid SNEDDS with a suitable inert carrier, such as silicon dioxide, calcium silicate, or magnesium aluminometasilicate. The solid SNEDDS was characterized by scanning electron microscopy, transmission electron microscopy, and in vitro dissolution studies. SEM, PXRD, and DSC results suggested that amorphous ticagrelor was present in the solid SNEDDS. Also, the solid SNEDDS significantly increased the dissolution rate of ticagrelor. In particular, the emulsion particle size and the polydispersity index of the solid SNEDDS using silicon dioxide (SS1) as a carrier was the smallest among the evaluated solid SNEDDS, and the flowability and compressibility result of the SS1 was the most suitable for the manufacturing of solid dosage forms. Therefore, solid SNEDDS using silicon dioxide (SS1) could be a potential nano-sized drug delivery system for the poorly water-soluble drug ticagrelor.
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KEYWORD
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Dissolution, porous carrier, SNEDDS, solubility, ticagrelor
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