QUALITY BY DESIGN APPROACH FOR DEVELOPMENT AND OPTIMIZATION OF DIACEREIN-LOADED TRANSFEROSOMAL CARRIER GEL FOR ENHANCED TRANSDERMAL DELIVERY
DOI:
https://doi.org/10.22159/ijap.2026v18i4.58195Keywords:
Diacerein, Transferosomes, Transdermal drug delivery, Optimization, Permeation enhancementAbstract
Objective: The current study aimed to develop and optimize a diacerein-loaded transferosomal gel for transdermal drug delivery using a box-behnken design (BBD), thereby enhancing bioavailability and reducing systemic side effects.
Methods: Transferosomes were prepared by the rotary thin-film hydration method utilising various ratios of span 80 and phosphatidylcholine (PDC), and optimized using BBD. The independent variables in transferosome preparation were the amount of span 80 and PDC. The dependent variables were entrapment efficiency (EE), drug release, and drug content (DC). Drug and excipient compatibility were determined using differential scanning calorimetry (DSC) and fourier transform infrared spectroscopy (FTIR).The prepared transferosomes were characterized for DC, particle size distribution, EE, zeta potential (ZP), polydispersity index (PDI), in vitro drug release and morphology by scanning electron microscopy (SEM). The optimized diacerein transferosomal formulation was incorporated into a gel and evaluated for pH, spreadability, viscosity, ex vivo skin permeation, and stability.
Results: The optimized formulation had a spherical shape, a vesicular size of 142.6±2.45 nm, a PDI of 0.101±0.012, and an EE of 89.5±2.18%. The optimized transferosomal gel shows720±20µg/cm². h transdermal flow over the skin of albino Wistar rats.SEM demonstrated the rough surface. The drug release kinetics adhered to zero order model, showing a sustained release pattern and confirming improved transdermal penetration of diacerein via transferosomes technology.
Conclusion: Transferosomes are effective nanoscale carriers for diacerein, significantly enhancing the transdermal penetration of diacerein through transferosome technology as confirmed by ex vivo skin permeation studies.
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