Faiyaz Shakeel1,2, Muzaffar Iqbal3,4, Essam Ezzeldin3,4. 1. Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. 2. Center of Excellence in Biotechnology Research (CEBR), King Saud University, Riyadh, Saudi Arabia. 3. Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia. 4. Bioavailability Laboratory, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Abstract
OBJECTIVE: The current studies were undertaken to enhance dissolution and bioavailability/pharmacokinetic profile of a newly approved anticancer drug ibrutinib (IBR) via encapsulation of drug into self-nanoemulsifying drug delivery system (SNEDDS). METHODS: Various SNEDDS formulations of IBR were developed by aqueous phase titration method using Capryol-PGMC (oil phase), Tween-20 (surfactant), Carbitol (cosurfactant) and water (aqueous phase). Developed SNEDDS of IBR was evaluated in vitro for various physicochemical properties and drug release profile. KEY FINDINGS: Based on lowest droplet size (28.7 ± 3.2 nm), least polydispersity (0.123), optimal values of zeta potential (-32.8 mV) and refractive index (1.336), highest % transmittance (98.7 ± 0.2%), highest drug release profile via dialysis membrane (98.9 ± 8.2% after 48 h) and the presence of lowest concentration of Capryol-PGMC (12% w/w), SNEDDS I1 was selected for in-vivo pharmacokinetic/bioavailability studies in female Wistar rats. In-vivo pharmacokinetic studies in rats showed that optimized SNEDDS I1 controlled the absorption of IBR compared with IBR suspension. The bioavailability of IBR from optimized SNEDDS I1 was enhanced around 2.64 times in comparison with IBR suspension. CONCLUSION: These results indicated the potential of developed SNEDDS as an alternative drug delivery system for IBR to enhance its bioavailability and anticancer efficacy.
OBJECTIVE: The current studies were undertaken to enhance dissolution and bioavailability/pharmacokinetic profile of a newly approved anticancer drug ibrutinib (IBR) via encapsulation of drug into self-nanoemulsifying drug delivery system (SNEDDS). METHODS: Various SNEDDS formulations of IBR were developed by aqueous phase titration method using Capryol-PGMC (oil phase), Tween-20 (surfactant), Carbitol (cosurfactant) and water (aqueous phase). Developed SNEDDS of IBR was evaluated in vitro for various physicochemical properties and drug release profile. KEY FINDINGS: Based on lowest droplet size (28.7 ± 3.2 nm), least polydispersity (0.123), optimal values of zeta potential (-32.8 mV) and refractive index (1.336), highest % transmittance (98.7 ± 0.2%), highest drug release profile via dialysis membrane (98.9 ± 8.2% after 48 h) and the presence of lowest concentration of Capryol-PGMC (12% w/w), SNEDDS I1 was selected for in-vivo pharmacokinetic/bioavailability studies in female Wistar rats. In-vivo pharmacokinetic studies in rats showed that optimized SNEDDS I1 controlled the absorption of IBR compared with IBR suspension. The bioavailability of IBR from optimized SNEDDS I1 was enhanced around 2.64 times in comparison with IBR suspension. CONCLUSION: These results indicated the potential of developed SNEDDS as an alternative drug delivery system for IBR to enhance its bioavailability and anticancer efficacy.
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