DESIGN OF EXPERIMENT-BASED CANDESARTAN CILEXETIL NANOCRYSTALS LOADED SOLID DISPERSION FOR ORAL DRUG DELIVERY SYSTEM: OPTIMIZATION, IN VITRO/IN VIVO EVALUATION

SONALI VIJAYKUMAR MAGDUM; PRAMODKUMAR JAYKUMAR SHIROTE

doi:10.22159/ajpcr.2025v18i8.54604

Authors

SONALI VIJAYKUMAR MAGDUM Department of Pharmaceutics, Dr. J. J. Magdum Pharmacy College, Jaysingpur, Maharashtra, India
PRAMODKUMAR JAYKUMAR SHIROTE Department of Pharmaceutical Chemistry, Dr. Bapuji Salunkhe Institute of Pharmacy, Miraj, Maharashtra, India.

DOI:

https://doi.org/10.22159/ajpcr.2025v18i8.54604

Keywords:

Candesartan cilexetil, Nanocrystal, Solid dispersion, Eudragit RLPO, Oral bioavailability

Abstract

Objective: The current study aimed to develop and characterize a nanocrystal-based solid dispersion of Candesartan Cilexetil (CC) to improve its solubility and bioavailability.

Methods: CC-loaded nanosuspension was prepared using the solvent precipitation method, employing Eudragit RLPO, and polyvinyl alcohol as a stabilizer. The resulting nano-sized lyophilized powder was then incorporated into a solid dispersion using the kneading method with crospovidone as a super-disintegrant. A 32 factorial design was used for optimization, with the amount of nanosuspension powder (X1) and concentration of superdisintegrant agent (X2) as independent variables. Evaluations included drug content (%), drug release (DR %), zeta potential (ZP), and other characterization techniques.

Results: The optimized formulation, CCSD9, exhibited a particle size of 264 nm, a ZP of 20.32 mV, a DR rate of 99.45%, and a polydispersity index (PDI) of 0.365. Transmission electron microscopy analysis revealed drug nanocrystal agglomeration, possibly due to the water removal process. Differential scanning calorimetry analysis indicated a minor change in crystallinity, likely due to lactose presence, and confirmed no significant drug-excipient interaction. A 6-month stability trial was conducted.

Conclusion: The solvent precipitation method proved to be an efficient approach for developing CC nanocrystal-based solid dispersion with a lower particle size. The nanosizing technique successfully encapsulated CC within the polymer matrix, enhancing DR and stability.

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