Griseofulvin Nanosuspension: A Quality by Design Approach to Enhance the Dissolution Performance

Sarah Salim Oleiwi; Ghaidaa Sulaiman Hameed

doi:10.54133/ajms.v10i1.2693

Authors

Sarah Salim Oleiwi Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq https://orcid.org/0009-0009-9278-006X
Ghaidaa Sulaiman Hameed Department of Pharmaceutics, College of Pharmacy, Mustansiriyah University, Baghdad, Iraq https://orcid.org/0000-0003-1470-6808

DOI:

https://doi.org/10.54133/ajms.v10i1.2693

Keywords:

Box–Behnken design, Cryoprotectant, Lyophilization , Nanosuspension , Particle size, Stability

Abstract

Background: Griseofulvin (GF) is a BCS class II antifungal drug characterized by poor aqueous solubility with low and variable oral bioavailability, which affects its therapeutic performance. Objective: This study aimed to optimize a stable griseofulvin nanosuspension (NS) using an ultrasonication-assisted antisolvent precipitation method combined with a Quality by Design (QbD) approach. Methods: Preliminary stabilizer screening identified polyvinylpyrrolidone K30 (PVP) and sodium lauryl sulfate (SLS) as the most effective electrosteric stabilizer system. Box–Behnken design was used to study the effects of surfactant and polymer percent, in addition to sonication time, on particle size (PS) and polydispersity index (PDI). The optimized nanosuspension was lyophilized using trehalose or mannitol. as cryoprotectants. Physicochemical characterization was performed using particle size analysis, zeta potential, PXRD, DSC, and FTIR, while solubility, dissolution, and stability studies were also conducted. Results: The optimized formulation exhibited 264±32.7 nm as PS, a PDI of 0.246±0.02, an entrapment efficiency of 91±3.44%, and a zeta potential of −28.7 mV, indicating good colloidal stability. Trehalose provided superior redispersibility and demonstrated significantly enhanced solubility and rapid dissolution, achieving 96% drug release within 15 min, compared with mannitol. Solid-state characterization confirmed a marked reduction in crystallinity and partial amorphization of GF. Stability studies confirmed acceptable physicochemical stability under accelerated storage conditions. Conclusions: Overall, the developed griseofulvin nanosuspension represents a promising strategy for improving the solubility and dissolution behavior of poorly water-soluble drugs

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