Speaker at Pharmaceutics and Drug Delivery Systems 2022 - Ibrahim A. Alsarra
King Saud University, Saudi Arabia
Title : Self-nanoemulsifying drug delivery system (SNEDDS) of apremilast: In-vitro evaluation and pharmacokinetic studies


Psoriatic arthritis is an autoimmune disease of the joints; it can lead to persistent inflammation, joint damage and disability. Apremilast (APR) was the first FDA-approved oral anti-psoriatic arthritis drug. It APR immediate release tablets Otezla® have 20-33% bioavailability compared to APR absolute bioavailability 73%. APR-SNEDDS were formulated to enhance APR’s solubility, dissolution and oral bioavailability. The assay of drug was carried out using a validated HPLC method. The standard plot obtained linearity in the concentration range of (0.1 to 100 µg/ml) with R2= 0.9991. Using Lauraglycol-FCC as the oil phase, de-ionized water as the aqueous phase, tween-80 as the surfactant and transcutol-HP as the cosurfactant, nine APR-SNEDDS were developed namely (F1-F9) by spontaneous emulsification method. Various thermodynamic tests were carried out on APR-SNEDDS. Stable SNEDDS were characterized then subjected to in-vitro drug release studies via dialysis membrane. The optimum formulation was F9 which showed the maximum in-vitro drug release (94.9%) over 24h was furtherly investigated in in-vivo studies. F9 was composed of 15% oil, 60% Smix, and 25% water had the lowest droplet size (17.505 ± 0.247 nm), low PDI (0.147 ± 0.014), low ZP (-13.35 mV), highest %T (99.15 ± 0.131) and optimum increases in the relative bioavailability (703.66%) compared to APR suspension (100%) over 24h. These findings represented APR-SNEDDS as a possible alternative delivery system for APR and for future studies to evaluate the major factors that influence the encapsulation efficiency and stability of APR. Moreover, the application of APR-SNEDDS for oral delivery, efficacy and safety assessments.


Professor Ibrahim A. Alsarra received his Bachelor of Pharmacy (B.S.), in 1996 from College of Pharmacy, King Saud University, Kingdom of Saudi Arabia and his Doctor of Philosophy (Ph.D.) in Pharmaceutical Biotechnology and Drug Formulation Development, Division of Pharmaceutical Sciences, School of Pharmacy, University of Missouri-Kansas City, Missouri, USA. He joined King Saud University in 2002 and is currently the Assistant Secretary for Research and Scientific Affairs, Arab Pharmacists Union as well as the Deputy Director for Research and Technical Affairs, Centre of Excellence in Biotechnology Research; the only biotechnology center in Saudi Arabia, King Saud University.