Development of Long Acting Depot Injection of Iloperidone by SABER Technology

Abstract

The present investigations report the application of SABER® technology in the development of a one-month depot injection of iloperidone. SABER® is a new in situ gel formulation technology for sustained release drug delivery, which precludes the use of large amounts of toxic organic solvents in the formulation. Traditionally in the in situ gel forming technology-based depot injections, expensive polymers such as polylactic acid and poly(lactic-co-glycolic acid), and a class 2 solvent like N-methyl-2-pyrrolidone have been used to control the rate of drug release and dissolve the drug and polymer, respectively. In the present investigations, however, no such release retarding polymers were used, moreover, the formulation was developed using a limited amount of dimethylsulphoxide, a class 3 solvent. Formulation variables were optimized by D-optimal mixture design to obtain the depot formulation with a consistent drug release for one month. The composition of sucrose acetate isobutyrate, and dimethylsulphoxide were taken as input variables and cumulative drug release at various time points as response variables. The optimized formulation contained 81.718 % sucrose acetate isobutyrate and 18.282 % dimethylsulphoxide and produced a consistent drug release profile with 85.71 % cumulative drug release in 30 days without any significant burst release.