Title:Self-emulsifying Pellets Prepared by Extrusion/Spheronization: In vitro/In vivo Evaluation
Volume: 10
Issue: 3
Author(s): Mohammad A. Rahman, Mohammad Mujahid and Arshad Hussain
Affiliation:
Keywords:
Absorption, bioavailability, lipid based drug delivery, pellets, extrusion/spheronization, oral delivery.
Abstract: Aims: 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.
Material and Methods: 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).
Results: 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). AUC
0-36h 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).
Conclusion: 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.