DESIGN AND CHARACTERIZATION OF LULICONAZOLE-ENCAPSULATED TRANSFEROSOMES IN THERMOSENSITIVE OCULAR GEL
DOI:
https://doi.org/10.22159/ijap.2025v17i6.55006Keywords:
Transferosomes, Luliconazole (LCZ), Box-behnken design, Zeta potetail, In situ gelAbstract
Objective: The present study develops and optimizes a thermosensitive in-situ gel containing Luliconazole-loaded transferosomes (LCZ-TFs) to improve ocular bioavailability and therapeutic efficacy through enhanced permeation and prolonged retention.
Methods: Transferosomes (TFs) were prepared using the thin film hydration method. To optimize the formulation, a Box-Behnken design was used to study the effects of three variables: the concentration of soya phosphatidylcholine (SPC), Tween 80, and chloroform and evaluated for their influence on vesicle size, polydispersity index (PDI), and percentage entrapment efficiency (EE). Zeta potential and Transmission Electron Microscopy (TEM) analysis were performed for optimized formulation. The optimized transferosome was incorporated into the thermosensitive in-situ gel containing Pluronic F127 (15% w/v) and Pluronic F68 (1% w/v) and evaluated for in vitro drug release using a membrane diffusion technique and ex vivo permeation studies on goat cornea using a modified Franz diffusion cell.
Results: The optimized TFs showed a particle size of 205.5 nm, PDI of 0.236, and EE of 77.43%. The zeta potential was recorded at −53.9 mV, indicating good stability. TEM revealed well-formed spherical vesicles. Drug release studies demonstrated a sustained release profile from the transferosomes in situ gel with release kinetics following first-order kinetics and Higuchi model mechanisms. In ex vivo permeation studies, the transferosomes in situ gel showed a 1.68-fold higher permeation than the conventional gel. The formulation passed sterility and isotonicity tests and retained antifungal activity comparable to a marketed product, as shown by its zone of inhibition. Additionally, the hen’s egg test–chorioallantoic membrane (HET-CAM) test confirmed the gel was non-irritant and safe for ocular use.
Conclusion: Overall, the transferosomes in situ gel significantly improved ocular retention and prolonged the drug's release, which enhances the therapeutic effectiveness of Luliconazole in treating fungal keratitis.
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