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<p>Zaltoprofen (ZLT) is a nonsteroidal anti-inflammatory drug (NSAID) with poor oral bioavailability (&lt;20%) due to limited solubility and is associated with gastrointestinal side effects, including gastric discomfort, epigastric pain, and stomatitis. To overcome these drawbacks, a cubosome-based transdermal gel was developed using a Quality by Design (QbD) approach to improve skin permeation and sustain drug release. Cubosomes were prepared by top-down method using glyceryl monooleate (GMO) and Pluronic F-127 (PF127), optimized through a Box–Behnken design with 16 runs. Independent variables were GMO (X1), PF127 (X2), and sonication time (X3), while particle size (PS, Y1), polydispersity index (PDI, Y2), and entrapment efficiency (%EE, Y3) were selected responses. The optimized formulation (F8) was incorporated into a Carbopol 934 gel (ZLT-CUB gel) and evaluated for physicochemical properties, in vitro and ex vivo release, and anti-inflammatory activity using a carrageenan-induced paw edema rat model against diclofenac and marketed formulations. The optimized cubosomes (F8) showed a PS of 260.4 nm, PDI of 0.19, and 61.72% EE, achieving 93.04% release over 24 h. The gel exhibited appropriate pH, viscosity (794.7 ± 5 cps), spreadability (11.45 ± 0.12 g cm/s), and drug content. Diffusion studies showed in vitro release of 80.36% and ex vivo permeation of 55.6%. In vivo studies demonstrated significant anti-inflammatory activity, superior to marketed formulations, along with skin compatibility, absence of irritation, and histological evidence of recovery. Conclusion- The ZLT-loaded cubosomal gel is safe, non-toxic, and demonstrates enhanced efficacy, making it a promising transdermal system for managing inflammatory disorders.</p> Graphical Abstract <p></p>

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Development of Quality by Design Based Novel Zaltoprofen Cubosomal Gel for its improved Anti-Inflammatory Therapy by Transdermal Delivery: Formulation, Characterization, and In Vivo Evaluation

  • 期刊论文

  • 发表日期：

    2026年2月26日

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  • Sujay Hulyalkar,
  • Panchaxari M. Dandagi,
  • Prakash Biradar,
  • Atith Muppayyanamath,
  • Sandeep Kurani

摘要

Zaltoprofen (ZLT) is a nonsteroidal anti-inflammatory drug (NSAID) with poor oral bioavailability (<20%) due to limited solubility and is associated with gastrointestinal side effects, including gastric discomfort, epigastric pain, and stomatitis. To overcome these drawbacks, a cubosome-based transdermal gel was developed using a Quality by Design (QbD) approach to improve skin permeation and sustain drug release. Cubosomes were prepared by top-down method using glyceryl monooleate (GMO) and Pluronic F-127 (PF127), optimized through a Box–Behnken design with 16 runs. Independent variables were GMO (X1), PF127 (X2), and sonication time (X3), while particle size (PS, Y1), polydispersity index (PDI, Y2), and entrapment efficiency (%EE, Y3) were selected responses. The optimized formulation (F8) was incorporated into a Carbopol 934 gel (ZLT-CUB gel) and evaluated for physicochemical properties, in vitro and ex vivo release, and anti-inflammatory activity using a carrageenan-induced paw edema rat model against diclofenac and marketed formulations. The optimized cubosomes (F8) showed a PS of 260.4 nm, PDI of 0.19, and 61.72% EE, achieving 93.04% release over 24 h. The gel exhibited appropriate pH, viscosity (794.7 ± 5 cps), spreadability (11.45 ± 0.12 g cm/s), and drug content. Diffusion studies showed in vitro release of 80.36% and ex vivo permeation of 55.6%. In vivo studies demonstrated significant anti-inflammatory activity, superior to marketed formulations, along with skin compatibility, absence of irritation, and histological evidence of recovery. Conclusion- The ZLT-loaded cubosomal gel is safe, non-toxic, and demonstrates enhanced efficacy, making it a promising transdermal system for managing inflammatory disorders.

Graphical Abstract