FORMULATION, OPTIMIZATION AND EVALUATION OF KETOPROFEN-LOADED EUDRAGIT MICROSPONGES INCORPORATED INTO TABLET DOSAGE FORM
TL;DR
The findings of the study suggest that microsponge technology offers an effective approach for sustained delivery of Ketoprofen by improving drug entrapment, controlling release behavior, enhancing formulation stability, and increasing patient compliance.
Abstract
The present study focused on the formulation, optimization, and evaluation of Ketoprofen-loaded microsponges intended for sustained drug delivery using the quasi-emulsion solvent diffusion method. Ketoprofen, a widely prescribed non-steroidal anti-inflammatory drug (NSAID), is commonly used for the management of pain and inflammatory disorders. However, its short biological half-life and the need for repeated dosing may result in gastrointestinal side effects and reduced patient adherence. To address these limitations, sustained release microsponge tablets were developed using Eudragit RS100 as the rate-controlling polymer and Polyvinyl Alcohol (PVA) as the stabilizing agent. Preformulation studies such as organoleptic evaluation, melting point determination, UV-visible spectroscopy, and FTIR analysis were carried out to confirm the purity and compatibility of the drug with selected excipients. Ketoprofen showed a maximum absorption wavelength at 260 nm and demonstrated good linearity within the concentration range of 2–16 µg/mL. FTIR spectra indicated the absence of any significant interaction between the drug and excipients. The prepared microsponges were characterized for particle size, morphology, production yield, entrapment efficiency, and in-vitro drug release behavior. SEM studies confirmed the formation of spherical, porous, and discrete microsponges with particle size ranging between 9.28 µm and 23.42 µm. Among all formulations, batch F3 exhibited the highest production yield (89.00 ± 0.15%) and maximum loading efficiency (88.60 ± 0.08%). DSC and XRD investigations suggested partial conversion of crystalline Ketoprofen into an amorphous form within the polymeric matrix without any major drug–polymer incompatibility. The optimized microsponge formulation was compressed into tablets and further evaluated for pre-compression and post-compression characteristics. Formulation F3 demonstrated acceptable hardness, low friability, satisfactory drug content, and prolonged drug release of 98.60% over a period of 12 hours. Drug release kinetic studies revealed that the optimized formulation followed Higuchi and Korsmeyer–Peppas release models, indicating diffusion-mediated anomalous drug release. Accelerated stability studies conducted according to ICH guidelines confirmed that the optimized formulation remained stable for three months under prescribed storage conditions. The findings of the study suggest that microsponge technology offers an effective approach for sustained delivery of Ketoprofen by improving drug entrapment, controlling release behavior, enhancing formulation stability, and increasing patient compliance.