Self-emulsifying Pellets Prepared by Extrusion/Spheronization: In vitro/In vivo Evaluation.

Abstract

The purpose of the current study was to investigate the feasibility of producing solid self-emulsifying pellets using the extrusion/spheronization technique with an aim to increase the bioavailability of selected drug and also to encounter the problems associated with liquid lipid formulations. Selfemulsifying formulations are experiencing a very active development as reflected by the numerous publications and patents being granted on these systems. The patents on self-emulsifying formulation (US20036630150) and (US20006054136) helped in selecting the drug and excipients. These pellets were prepared using liquid SNEDDS (24.59 % LBF M 2125 CS + Maisine35-1; 1:1 ratio) (oil), 50.27 % Labrasol (surfactant) and 25.13% Lauroglycol 90 (cosurfactant), adsorbent (silicon dioxide), pellet forming excipient (microcrystalline cellulose), binder (pregelatinized starch), disintegrant (croscarmelose sodium) and lubricant (corn starch). The resulting self-emulsified pellets loaded with about 32% liquid SNEDDS exhibited uniform pellet size and round shape, droplet size distribution following self-emulsification was nearly same to the liquid SNEDDS (26.5 nm and 24.8 nm, respectively). The in vitro release was significantly higher than the plain drug (p<0.01). AUC0-36h of sertraline from the pellets showed about 5-fold greater than the plain drug and no significant difference compared with the liquid SNEDDS (p>0.05). In conclusion, spherical pellets with low friability and self-emulsifying properties can be produced by the standard extrusion/spheronization technique. The pellets are capable of transferring lipophilic compounds into the aqueous phase and have a high potential to increase the oral absorption of lipophilic drugs.