Formulation of cilostazol spherical agglomerates by crystallo-co-agglomeration technique and optimization using
Sanjeevani Shekhar Deshkar1, Govind R Borde1, Rupali N Kale1
1Department of Pharmaceutics, Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pune, Maharashtra, India.
International Journal of Pharmaceutical Investigation
|April 26, 2018
Summary
Crystallo-co-agglomeration significantly improved cilostazol solubility and dissolution. Optimized formulations enhanced drug release and bioavailability for this poorly soluble drug.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
Background:
- Spherical agglomeration is a novel technique to enhance drug flow and dissolution.
- Cilostazol, a BCS Class II drug, exhibits poor solubility and limited bioavailability.
- This study focuses on improving cilostazol's properties via crystallo-co-agglomeration.
Purpose of the Study:
- To enhance the solubility and dissolution rate of cilostazol using crystallo-co-agglomeration.
- To investigate the impact of polymer concentration on spherical agglomerate formation.
- To evaluate the physicochemical and performance characteristics of the developed agglomerates.
Main Methods:
- Cilostazol agglomerates were prepared using hydroxypropyl methylcellulose E 50 (HPMC E50), polyvinyl pyrrolidone K30 (PVP K30), and polyethylene glycol 6000.
- A 3^2 factorial design was employed to study the influence of polymer concentration.
- Characterization included particle size, yield, drug content, solubility, in vitro dissolution, FTIR, SEM, DSC, and XRD.
Main Results:
- An optimized formulation (F3) showed a mean agglomerate size of 210.0 ± 0.56 μm with excellent flow properties.
- A 15-fold increase in aqueous solubility and complete drug release within 60 minutes were achieved.
- SEM confirmed drug microcrystals, FTIR indicated no chemical changes, and DSC/XRD revealed a crystalline to amorphous transformation, enhancing solubility.
Conclusions:
- Crystallo-co-agglomeration is an effective approach for improving the solubility and dissolution of poorly soluble drugs like cilostazol.
- The study demonstrates the potential of this technique for enhancing drug bioavailability.
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