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Design and Evaluation of a Self-Emulsifying Drug Delivery System of Aripiprazole

By: Ramya, A. R.
Contributor(s): Preethi, Sudheer.
Publisher: Mumbai Indian Journal of Pharmaceutical Science 2019Edition: Vol.81(6), Nov-Dec.Description: 1089-1098p.Subject(s): PHARMACEUTICSOnline resources: Click here In: Indian journal of pharmaceutical sciencesSummary: The present investigation is aimed at enhancing the solubility and the dissolution rate of aripiprazole by formulating a self-micro emulsifying drug delivery system. The preliminary solubility screening of aripiprazole was determined in oils, surfactants and cosurfactants, respectively. Among those screened, isopropyl myristate, Tween 80 and propylene glycol showed good solubilizing efficiency and were selected for further formulations. A pseudoternary phase diagram was constructed at the ratios of 2:1, 3:1, 4:1 of oil to Smix (surfactant:Tween 80) and cosurfactant (propylene glycol) to find out the self-emulsification region. In vitro dissolution studies of the formulations were carried out in a simulated acidic buffer pH 2.2. A liquid self-micro emulsifying drug delivery system with an optimum composition was converted to solid formulation using crospovidone. Both solid and liquid formulations were evaluated for the cloud point and self-emulsification time. Differential scanning calorimetry endotherm provided confirmation for the amorphisation of the drug. Zeta potential and particle size analysis was carried out on the optimized formula. These studies revealed that the prepared self-micro emulsifying drug delivery system exhibited increased dissolution rate profile in comparison to the pure drug and marketed aripiprazole tablets.
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The present investigation is aimed at enhancing the solubility and the dissolution rate of aripiprazole by formulating a self-micro emulsifying drug delivery system. The preliminary solubility screening of aripiprazole was determined in oils, surfactants and cosurfactants, respectively. Among those screened, isopropyl myristate, Tween 80 and propylene glycol showed good solubilizing efficiency and were selected for further formulations. A pseudoternary phase diagram was constructed at the ratios of 2:1, 3:1, 4:1 of oil to Smix (surfactant:Tween 80) and cosurfactant (propylene glycol) to find out the self-emulsification region. In vitro dissolution studies of the formulations were carried out in a simulated acidic buffer pH 2.2. A liquid self-micro emulsifying drug delivery system with an optimum composition was converted to solid formulation using crospovidone. Both solid and liquid formulations were evaluated for the cloud point and self-emulsification time. Differential scanning calorimetry endotherm provided confirmation for the amorphisation of the drug. Zeta potential and particle size analysis was carried out on the optimized formula. These studies revealed that the prepared self-micro emulsifying drug delivery system exhibited increased dissolution rate profile in comparison to the pure drug and marketed aripiprazole tablets.

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