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<p>The current study aims to develop, optimize, and characterize metformin-loaded aspasomal serum (MET-ASPs serum) for topical application. MET-ASPs were formulated via the thin-film hydration method. MET-ASPs were developed via Quality by Design (QbD), where batches were screened using a Plackett–Burman Design and optimized using Box Behnken Design with JMP 18 Pro Software. Optimized MET-ASPs displayed a spherical morphology, with particle size of 197.9 ± 0.02&#xa0;nm, polydispersity index of 0.448 ± 0.019, zeta potential of -40.8 ± 10.8&#xa0;mV, and % entrapment of 31.66 ± 1.73%, respectively. The in vitro drug release study demonstrated a prolonged release of MET (94.15 ± 5.09%) over 5&#xa0;h, following Weibull model kinetics. At the same time, the DPPH assay showed that the antioxidant potential of MET-ASPs was 96.66 ± 0.22%, comparable to that of ascorbic acid, a standard antioxidant. Also, the optimized MET-ASPs showed no toxicity towards NIH/3T3 fibroblast cells, whereas they showed cytotoxicity towards B16F0 melanoma cells and a high % of cellular ROS inhibition and melanogenesis inhibition ability. Thereafter, MET-ASPs were loaded in serum for practical applicability, which displayed desired spreadability (7.99 ± 0.42 mm<sup>2</sup>/g) and viscosity (399.23 ± 34.56&#xa0;mPa&#xa0;s). Ex vivo skin permeation and retention studies demonstrated greater permeation and retention of MET from MET-ASPs serum in the stratum corneum and viable skin layers. Moreover, the topical application of MET-ASPs serum in SD rats displayed minimal irritation. In a nutshell, MET-ASPs serum may serve as a promising topical nanocarrier for the enhanced delivery of MET. Further pre-clinical and clinical studies are needed to determine the therapeutic efficacy of MET-ASPs serum.</p> Graphical Abstract <p></p>

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A Quality-by-Design Driven Development and Characterization of Metformin-Loaded Aspasomal Serum for Topical Application

  • 期刊论文

  • 发表日期：

    2026年8月4日

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  • Shruti Patil,
  • Sandeep Kr Maharana,
  • Biswajit Rout,
  • Shyam Sudhakar Gomte,
  • Aakanchha Jain

摘要

The current study aims to develop, optimize, and characterize metformin-loaded aspasomal serum (MET-ASPs serum) for topical application. MET-ASPs were formulated via the thin-film hydration method. MET-ASPs were developed via Quality by Design (QbD), where batches were screened using a Plackett–Burman Design and optimized using Box Behnken Design with JMP 18 Pro Software. Optimized MET-ASPs displayed a spherical morphology, with particle size of 197.9 ± 0.02 nm, polydispersity index of 0.448 ± 0.019, zeta potential of -40.8 ± 10.8 mV, and % entrapment of 31.66 ± 1.73%, respectively. The in vitro drug release study demonstrated a prolonged release of MET (94.15 ± 5.09%) over 5 h, following Weibull model kinetics. At the same time, the DPPH assay showed that the antioxidant potential of MET-ASPs was 96.66 ± 0.22%, comparable to that of ascorbic acid, a standard antioxidant. Also, the optimized MET-ASPs showed no toxicity towards NIH/3T3 fibroblast cells, whereas they showed cytotoxicity towards B16F0 melanoma cells and a high % of cellular ROS inhibition and melanogenesis inhibition ability. Thereafter, MET-ASPs were loaded in serum for practical applicability, which displayed desired spreadability (7.99 ± 0.42 mm2/g) and viscosity (399.23 ± 34.56 mPa s). Ex vivo skin permeation and retention studies demonstrated greater permeation and retention of MET from MET-ASPs serum in the stratum corneum and viable skin layers. Moreover, the topical application of MET-ASPs serum in SD rats displayed minimal irritation. In a nutshell, MET-ASPs serum may serve as a promising topical nanocarrier for the enhanced delivery of MET. Further pre-clinical and clinical studies are needed to determine the therapeutic efficacy of MET-ASPs serum.

Graphical Abstract