Bioavailability enhancement and pharmacokinetic profile of an anticancer drug ibrutinib by self-nanoemulsifying drug delivery system. (28th March 2016)

• Record Type: Journal Article
• Authors: Shakeel, Faiyaz; Iqbal, Muzaffar; Ezzeldin, Essam
• Is Part Of: Journal of pharmacy and pharmacology. Volume 68:Number 6(2016:Jun.)
• Page Start: 772
• Page End: 780
• Publication Date: 2016-03-28
• Subjects: bioavailability -- cancer -- drug release -- ibrutinib -- pharmacokinetic; Pharmacy -- Periodicals; Pharmacology -- Periodicals; 615.1
• DOI: 10.1111/jphp.12550
• Languages: English
• ISSNs: 0022-3573

Abstract

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.