SMART BIOSURFACTANT NANOCARRIERS: ROS-LABILE ORAL DELIVERY SYSTEM FOR ENHANCED CELECOXIB EFFICACY IN RHEUMATOID ARTHRITIS
DOI:
https://doi.org/10.22159/ijap.2026v18i2.57021Keywords:
Rheumatoid arthritis, Celecoxib, Nanostructured lipid carriers, Sophorolipid, ROS-responsive delivery, Anti-inflammatory therapyAbstract
Objective: The chronic autoimmune illness known as rheumatoid arthritis (RA) is typified by joint destruction, oxidative stress, and ongoing inflammation. The selective COX-2 inhibitor celecoxib is useful in the treatment of RA, although its lack of disease-specific targeting, low oral bioavailability, and poor solubility restrict its effectiveness. In order to increase absorption, offer inflammation-triggered release, and boost treatment effectiveness in RA, this study set out to create a sophorolipid-stabilized, ROS-labile nanostructured lipid carrier (NLC) system for oral celecoxib administration.
Methods: Using microfluidic ethanol injection, NLCs were created with thioketal (TK)-PEG-cholesterol integrated at the interface and sophorolipid acting as a biosurfactant. Mucus penetration, epithelial transport, hemocompatibility, ROS-triggered release, and in vitro pharmacological activity in LPS-stimulated macrophages were all assessed, along with the formulation's physicochemical and interfacial characteristics.
Results: Optimized NLCs displayed a size of 138±6 nm, PDI<0.2, zeta potential −21 mV, and encapsulation efficiency>90%. Under ROS exposure, drug release reached ~83% at 12 h versus ~21% in controls. SL-NLCs showed 3-fold higher mucus diffusivity and significantly improved Caco-2 permeability (P_app 5.7×10⁻⁶ cm/s). In vitro studies demonstrated superior cytokine suppression (TNF-α ↓68%, IL-6 ↓62%) and COX-2 downregulation. Hemolysis was<3%, indicating excellent biocompatibility.
Conclusion: With improved absorption, inflammation-specific release, and strong anti-inflammatory action, ROS-labile, sophorolipid-stabilized NLCs offer a secure and efficient oral delivery system for celecoxib that may find therapeutic use in RA.
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