Formulation and Development of Microsponges Loaded Topical Formulation Containing Non Steroidal Anti-Inflammatory Drug

Abstract

Introduction: Arthritis is a chronic inflammatory condition affecting millions worldwide, leading to extreme pain and inflammation. Available therapies include surgery, laser, and drug treatments like corticosteroids and methotrexate. However, these drugs often cause itching, redness, and heart-related issues. Celecoxib, a COX-2 inhibitor, is used to block inflammation and pain. Microsponge Drug Delivery Systems offer advantages over other technologies like microencapsulation and liposomes, improving solubility of poorly water-soluble drugs like celecoxib. These microsponges are converted into a cream formulation to enhance applicability and patient compliance.

Objectives: The objective was to prepare and assess creams with celecoxib microsponges, a nonsteroidal anti-inflammatory drug for arthritis symptoms. We used the quasi-emulsion solvent diffusion method with Eudragit RS-100 to prepare microsponges with different drug-polymer ratios.

Methods: Drug-loaded microsponges were prepared using the Quasi-emulsion solvent diffusion method. Initially, Eudragit RS 100 was dissolved in dichloromethane, followed by drug addition and ultrasonication at 35°C. This inner phase was then mixed with an outer phase containing polyvinyl alcohol, stirred, and left to form rigid microsponges through solvent evaporation. After filtration, washing, and drying, microsponges were obtained. Key variables were optimized using factorial design. Creams were prepared via oil-in-water emulsion, with heating of aqueous and oil phases over a water bath.

 Results: The results confirmed that celecoxib microsponges significantly increased solubility and met all required limits. Celecoxib-loaded microsponges, formulated with Eudragit RS100, achieved high production yield and drug content. This formulation exhibited prolonged drug release.

Fourier transform infrared and differential scanning calorimetry studies were carried out for pure celecoxib and microsponges

Conclusions: Polymer-based microsponge delivery systems, developed via quasi-emulsion solvent diffusion, offer controlled release of celecoxib. These systems aim to reduce application frequency, hypersensitivity reactions, and improve bioavailability. Creams containing microsponges provide prolonged drug release, promising relief for arthritis symptoms.