Development and optimization of polymeric nanosponges for enhanced delivery of diflunisal in rheumatoid arthritis

Abstract

Rheumatoid arthritis damages the synovial membrane, and diflunisal, a nonsteroidal anti-inflammatory drug (NSAID) with poor solubility, faces delivery challenges. Nanosponges enhance diflunisals solubility improving its bioavailability; in addition it improved its stability and controls its release. Current research focuses on developing polymeric nanosponges (DIF-NS) through emulsion solvent evaporation, optimized by central composite design.

The optimized DIF-NS were further loaded into a carbopol 940 gel (DIF-NS-gel) and evaluated. The optimized BNS showed spherical morphology, % CDR (Percentage cumulative drug release) of 84.9 ± 1.6 within 12 hours and % entrapment efficiency of 82.45 % ± 1.2, a % practical yield of 75 % ± 2.2 with a particle size of 120.1 ± 8.5 nm, zeta potential -29 ± 3.2 mv, and a PDI of 0.348± 0.015. The drug excipient compatibility study was carried out by using FTIR. The sharp peak obtained in the DSC and XRD proves the drug’s crystalline nature.

The DIF-NS-gel exhibited sustained release and enhanced ex-vivo permeation compared to plain diflunisal gel. In a CFA-induced rheumatoid arthritis rabbit model, it significantly reduced inflammation for a prolonged duration. These findings highlight its potential for effective long-term rheumatoid arthritis management.

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Materials

DIF (98%) was acquired from Otto Chemie Pvt Ltd., Mumbai. Ethyl Cellulose (7cps) (EC), Polyvinyl Alcohol (PVA), and Carbopol 940 were sourced from Research Lab, Mumbai. Cellophane was purchased from HiMedia Laboratories, Mumbai, India. Double distilled water, essential for the formulations, was prepared using an in-house double distillation unit. Acetonitrile and methanol were sourced from Merck, while potassium dihydrogen phosphate was obtained from Ranchem Pvt Ltd Mumbai. Complete Freund’s adjuvant (CFA) was purchased from SIGMA-ALDRICH (F5881-10mL) (PCode 1003552933; SLCN3573), stored at 2 to 8 °C, and used to induce arthritis in rats.

Aher, K. B., Bhosale, S., Bhavar, G. B., Habeeb, M., & You, H. W. (2024). Development and optimization of polymeric nanosponges for enhanced delivery of diflunisal in rheumatoid arthritis. International Journal of Nano Dimension. https://doi.org/10.57647/j.ijnd.2025.1602.16

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