Background: The Microcrystalline Cellulose is called as a gold standard for the manufacture
of pellets. The poor disintegration leads to incomplete drug release that restricts the use of
MCC in the immediate-release formulation.
Objective: The present work aims to explore non-MCC extruder aid for pellet formulation and
solubility modulation potential of Aeroperl® 300 Pharma.
Methods: Bicalutamide (BCL) was selected as a model BCS class-II drug. The solubility of BCL
was assessed in different vehicles such as polyethylene glycol, propylene glycol, and Tween by
carrying out phase solubility study. The suitable vehicle was selected based on the higher solubility
of BCL. The vehicle was further adsorbed on newer adsorbent Aeroperl® 300 Pharma to formulate
liquisolid granules. The liquisolid granules were further incorporated into the pellet using mannitol
and microcrystalline cellulose as an extruder aid. Box-Behnken design was adopted for the optimization
of formulation considering MCC: mannitol ratio, the concentration of HPMC and spheronizer
speed as independent factors whereas drug release at 30 min, disintegration time and aspect ratio were
selected as dependent variables. The pellets were evaluated for different evaluation parameters.
Results: Propylene glycol was selected for the formulation of liquisolid technique based on the
results of the phase solubility study. Propylene glycol containing BCL was adsorbed on Aeroperl
300 Pharma. The optimized batch was selected exploring the Design-Expert software by considering
the limits of different responses. Pellet had excellent flowability. Friability was found to be
within the range (<1%). Pellets were found to be spherical and had pores on the surfaces.
Conclusion: Liquisolid granules containing newer solubilizer Aeroperl was found to be a promising
approach for the improvement in the solubility of the drug. The use of mannitol with MCC has a
profound effect on disintegration time, without altering flow property and other parameters. No
patents were reported on the combination of Bicalutamide, mannitol and Aeroperl. The critical finding
of the present work is to use mannitol as an extruder aid to fasten the disintegration leads to
complete drug release within a short period of time. Aeroperl and Mannitol, MCC: mannitol ratio,
the concentration of HPMC and spheronizer speed were found to be significant and had the potential
effect in pellet formulation.