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Background <p>Meloxicam is a potent non-steroidal anti-inflammatory drug (NSAID) widely prescribed for Osteoarthritis and Rheumatoid arthritis. However, its clinical efficacy via the oral route is severely compromised by its poor aqueous solubility, high first-pass metabolism, and frequent gastrointestinal adverse effects. Furthermore, conventional topical administration is often ineffective due to the drug’s inability to penetrate the stratum corneum barrier. To overcome these limitations, this research utilized a Quality by Design (QbD) methodology to develop and optimize Meloxicam-loaded polymeric nanoparticles for transdermal delivery, aiming to enhance solubility and ensure direct, localized therapeutic action while minimizing systemic toxicity.</p> Methods <p>Nanoparticles were formulated using a modified solvent evaporation method, utilizing Soluplus as a stabilizer and PLGA as the biodegradable matrix former. Critical formulation parameters, PLGA and Soluplus concentrations, were screened through FMEA and correlated using a central composite design (CCD) to maximize entrapment efficiency (% EE) and drug release while minimizing particle size. The nanoparticles were evaluated for FTIR, DSC, XRD, TEM etc. Stability of the optimal batch was determined.</p> Results <p>Through risk assessment study, the amount of PLGA and Soluplus were found critical. The optimal formulation derived from CCD demonstrated a high entrapment efficiency (84.56%), a compact particle size (155.51 nm), and a sustained drug release profile (96.54% over 12 h). FTIR investigations confirmed drug polymer compatibility with no significant interactions. DSC and XRD confirmed entrapment of drug inside nanoparticles or conversion of crystalline to amorphous structure. Stability studies indicated no significant alteration in formulation characteristics over time. The nanostructure was further validated by Transmission Electron Microscopy (TEM), which revealed distinct, spherical nanoparticles with smooth surfaces and a size range of 100–200 nm.</p> Conclusion <p>These study indicate that the optimized PLGA-Soluplus nanoparticles effectively facilitate passage through the stratum corneum, enabling continuous delivery of Meloxicam to deeper, arthritis affected tissues.</p>

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Design, Formulation, and Characterization of Meloxicam Loaded PLGA Nanoparticles Using a Quality by Design Approach for Optimized Therapeutic Efficacy in Arthritis Management

  • 期刊论文

  • 发表日期：

    2026年3月16日

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  • Ankur Patel,
  • Hardik Rana,
  • Rahil Bhura

摘要

Background

Meloxicam is a potent non-steroidal anti-inflammatory drug (NSAID) widely prescribed for Osteoarthritis and Rheumatoid arthritis. However, its clinical efficacy via the oral route is severely compromised by its poor aqueous solubility, high first-pass metabolism, and frequent gastrointestinal adverse effects. Furthermore, conventional topical administration is often ineffective due to the drug’s inability to penetrate the stratum corneum barrier. To overcome these limitations, this research utilized a Quality by Design (QbD) methodology to develop and optimize Meloxicam-loaded polymeric nanoparticles for transdermal delivery, aiming to enhance solubility and ensure direct, localized therapeutic action while minimizing systemic toxicity.

Methods

Nanoparticles were formulated using a modified solvent evaporation method, utilizing Soluplus as a stabilizer and PLGA as the biodegradable matrix former. Critical formulation parameters, PLGA and Soluplus concentrations, were screened through FMEA and correlated using a central composite design (CCD) to maximize entrapment efficiency (% EE) and drug release while minimizing particle size. The nanoparticles were evaluated for FTIR, DSC, XRD, TEM etc. Stability of the optimal batch was determined.

Results

Through risk assessment study, the amount of PLGA and Soluplus were found critical. The optimal formulation derived from CCD demonstrated a high entrapment efficiency (84.56%), a compact particle size (155.51 nm), and a sustained drug release profile (96.54% over 12 h). FTIR investigations confirmed drug polymer compatibility with no significant interactions. DSC and XRD confirmed entrapment of drug inside nanoparticles or conversion of crystalline to amorphous structure. Stability studies indicated no significant alteration in formulation characteristics over time. The nanostructure was further validated by Transmission Electron Microscopy (TEM), which revealed distinct, spherical nanoparticles with smooth surfaces and a size range of 100–200 nm.

Conclusion

These study indicate that the optimized PLGA-Soluplus nanoparticles effectively facilitate passage through the stratum corneum, enabling continuous delivery of Meloxicam to deeper, arthritis affected tissues.