Characterization and Optimization of Oral Solid Supersaturable Self-emulsifying Drug Delivery System of Cilostazol

Objective: This study aimed to prepare tablets containing solid supersaturable self-emulsifying drug delivery system (S-SEDD) of cilostazol for oral use.

Method: To improve drug dissolution and so bioavailability for cilostazol (calss II drug) as well as reducing the amount of additives (except for drug =50 mg), liquid S-SEDD of cilostazol were prepared. In this study the liquid supersaturable formula was converted into a solid supersaturable self-emulsifying form using different amounts of two different types of the adsorbents (avicel 101 and aerosil 200). Accordingly; six-formulas (SS1-SS6) were prepared and evaluated applying pre-compression evaluation and the best formula was SS3 formula having an amorphous homogenous free-flowing property and used to prepare tablets using direct compression method. Consequently; six tablet formulas (T1-T6) containing different types and amounts of additives were prepared and evaluated applying post-compression parameters and in-vitro drug release.

Result: The best tablet formula was T2 formula which showed high dissolution profile under sink and non-sink condition in comparison to conventional marketed tablet indicating that it kept its supersaturable self-emulsification in-vitro with faster drug release which may lead to improve drug absorption and bioavailability with a fast onset of action.

Conclusion: This work succeeded in converting the prepared cilostazol liquid S-SEDD to solid SEDD which is compressed into an immediate release tablets that disintegrate and spontaneously emulsified to form supersaturable system in the GIT which improved drug solubility, release and consequently may enhance its absorption and bioavailability leading to reducing dose size and drug/excipient size effects.

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Materials: Cilostazol was supplied from Hangzhou Hyper chemicals (China), oleic acid, was obtained from G.C.C., (UK), soluplus were obtained from BASF, Switzerland, transcutol was obtained from Gattefossé Corporation (USA), aerosil 200 and avicel 102 were obtained from Vivapur, Germany and Tween 80 were supplied from CDH (India).

Article information: Ali N. Wannas, Nidhal K. Maraie. Characterization and Optimization of Oral Solid Supersaturable Self-emulsifying Drug Delivery System of Cilostazol. Research Journal of Pharmacy and Technology. 2021; 14(6):3371-6. doi: 10.52711/0974-360X.2021.00586