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Abstract
FABRICATION AND PHYSICOCHEMICAL EVALUATION OF MICROSPHERE-BASED TAZAROTENE DELIVERY SYSTEMS
Sumit Kumar Das*, Prateek Jain, Hemant Agrawal, Naveen Gupta
ABSTRACT
Tazarotene is a topical retinoid widely used in the treatment of psoriasis, acne, and other dermatological disorders; however, its poor aqueous solubility and instability limit its therapeutic effectiveness and patient compliance. The present study aimed to fabricate and evaluate Tazarotene-loaded microspheres using Eudragit RS100 as a polymeric carrier system to achieve controlled drug release, enhanced stability, and improved topical delivery. Pre-formulation studies were carried out to investigate the physicochemical properties of Tazarotene, including organoleptic characteristics, solubility profile, melting point, pH, λ max determination, calibration curve, and FTIR analysis. The drug exhibited maximum absorbance and showed compatibility with formulation components. Microspheres were prepared by the emulsion solvent evaporation method using Eudragit RS100, sodium CMC, Tween 80, and chloroform. Five formulations (MSF1–MSF5) were developed by varying the polymer concentration. The prepared microspheres were evaluated for physical appearance, particle size, zeta potential, surface morphology, entrapment efficiency, in vitro drug release, release kinetics, and stability studies. Among all formulations, MSF4 was identified as the optimized formulation, exhibiting a particle size of 282.2 nm, zeta potential of 68.9 mV, and entrapment efficiency of 92.83%. SEM analysis revealed that the microspheres were spherical, smooth, porous, and uniformly distributed, indicating successful encapsulation and stable formulation characteristics. The in vitro drug release study demonstrated a sustained and controlled release pattern; with 98.97% cumulative drug release over 12 hours. Release kinetic analysis showed that the formulation predominantly followed the Higuchi diffusion model (R² = 0.991), indicating diffusion-controlled drug release from the polymeric matrix. Stability studies performed under ICH guidelines for 90 days revealed minimal changes in particle size and entrapment efficiency under both room temperature and accelerated conditions, confirming excellent formulation stability. The findings of the study suggest that Eudragit RS100-based Tazarotene microspheres provide an effective controlled-release topical delivery system with improved physicochemical stability, sustained drug release, and enhanced therapeutic potential for dermatological applications.
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