Systematic Development of Bicalutamide Immediate Release Pellets Using Aeroperl and Non-MCC Extruder Aid

Author(s): Hardik Rana*, Hussain Hasan, Mukesh Gohel, Vaishali Thakkar, Tejal Gandhi

Journal Name: Current Drug Therapy

Volume 15 , Issue 5 , 2020

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Graphical Abstract:


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.

Keywords: Bicalutamide, liquisolid technique, aeroperl 300 pharma, MCC to mannitol ratio, disintegration, pellets.

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Article Details

Year: 2020
Published on: 22 January, 2021
Page: [482 - 492]
Pages: 11
DOI: 10.2174/1574885515999200424082315
Price: $65

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