DESIGN, OPTIMIZATION AND CHARACTERIZATION OF AZELNIDIPINE LOADED SELF MICRO-EMULSIFYING DRUG DELIVERY SYSTEM USING D-OPTIMAL MIXTURE DESIGN
DOI:
https://doi.org/10.22159/ijap.2026v18i3.57826Keywords:
Azelnidipine, SMEDDS, Ternary plot, D-optimal mixture design, Adsorption, BioavailabilityAbstract
Objective: Azelnidipine, a BCS Class II calcium channel blocker, exhibits poor water solubility and limited oral bioavailability (22%) due to extensive first-pass metabolism. This study aimed to enhance its absorption by formulating it into a Self Micro-emulsifying Drug Delivery System (SMEDDS) and further converting it into a solid dosage form.
Methods: The SMEDDS was developed using Capmul MCM C8 (oil), Transcutol HP (surfactant), and Tween 80 (co-surfactant) depending on the results of solubility study. A ternary phase diagram identified the microemulsification region, while a D-optimal mixture design was used to optimize the formulation. The liquid SMEDDS was then converted into a solid powder using Aeroperl 300 as an adsorbing agent and ultimately converted into a tablet dosage form.
Result: The optimized liquid SMEDDS exhibited a droplet size of 96.71 nm, solubility of 26.2 mg/mL, and emulsification time of 41 seconds. It was subsequently adsorbed onto a porous carrier to produce a solid SMEDDS. Scanning Electron Microscopy (SEM) analysis confirmed that the solid particles were discrete and non-agglomerated. In-vitro drug release studies showed significantly enhanced release profiles for both liquid and solid SMEDDS compared to the marketed tablet available. The formulation also remained stable under accelerated storage conditions (45 °C ± 2 °C and 75% ± 5% RH).
Conclusion: Overall, SMEDDS effectively improved the solubility, dissolution rate, and stability of Azelnidipine. The application of D-optimal design enabled precise optimization of the formulation, supporting its potential as a promising strategy for enhancing the oral bioavailability of poorly water-soluble drugs.
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