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Formulation and In Vivo Evaluation of Ticagrelor Self- Nanoemulsifying Drug Delivery Systems.

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BACKGROUND Ticagrelor (TGR) being antiplatelet agent belongs to BCS class IV drug with low solubility and permeability that undergoes first-pass metabolism leads to reduced bioavailability of 36%. OBJECTIVE The main… Click to show full abstract

BACKGROUND Ticagrelor (TGR) being antiplatelet agent belongs to BCS class IV drug with low solubility and permeability that undergoes first-pass metabolism leads to reduced bioavailability of 36%. OBJECTIVE The main goal of the present study was to develop TGR SNEDDS for improving solubility and oral bioavailability. METHODS An oil, surfactant and co-surfactant (miglyol 810, brij 35 and lauro glycol FCC) were chosen based on the maximum solubility of TGR. The chosen vehicles were mixed in varying ratios and agitated mildly and transmittance values more than 80 were noted and used for constructing pseudo ternary phase diagram. Formulations that passed stability testing were evaluated for % transmission, drug content and in vitro drug release analysis. In-vivo bioavailability studies of optimized SNEDDS were performed in wistar rats. RESULTS From evaluation studies of TGR, formulation F13 with maximum drug release of 98.99% in 60 minutes that is higher than 31.99 % of pure drug is considered the optimised formulation. The particle size, Z average and zeta potential of the optimized TGR formulation F13 was 289.6 nm, 185.1 nm and -18.3 mV respectively. The FTIR and SEM studies do not indicate any drug excipient interaction and confirm nanosize and stable for 3 months. From in vivo bioavailability studies in rats, the Cmax of optimized TGR SNEDDS (302.43±4.78ng/ml) was higher than pure TGR suspension (47.32±2.75ng/ml) and optimized SNEDDS exhibited 5 folds increased oral bioavailability than pure drug. CONCLUSION Hence, the results revealed that application of SNEDDS formulation technique for TGR increased solubility and oral bioavailability.

Keywords: ticagrelor; bioavailability; formulation; drug; solubility; tgr

Journal Title: Pharmaceutical nanotechnology
Year Published: 2020

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