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<p>This study aims to formulate amino acid-based nanotherapeutics for the effective treatment of chronic obstructive pulmonary disease (COPD). For this purpose, L-Arginine (Arg) was glycosylated with glucose (Glu) via Millard reaction and then integrated into Roflumilast (Rof) loaded self-nanoemulsifying drug delivery system (SNEDDS). A selective phosphodiesterase-4 inhibitor (PDE-4), Rof, is an anti-inflammatory drug that is clinically used to treat COPD, and was integrated into an SNEDDS formulation to improve its solubilization, stability, and targeted therapeutic efficacy. The developed SNEDDS were characterized for physicochemical and in-vivo characterization. SNEDDS displayed 192 ± 1.23&#xa0;nm size with 30 ± 1.4 mV zeta potential, and 0.24 ± 0.5 PDI. Moreover, Arg-Glu-Rof-loaded SNEDDS resulted in favorable mucoadhesion properties along with 90% drug entrapment efficiency and 85% efficient drug release in 12&#xa0;h. The optimized SNEDDS demonstrated outstanding biocompatibility, hemocompatibility, and enhanced cellular uptake analysis. The most significant bacterial inhibition was observed with prepared SNEDDS formulation, having reduced optical density values of 0.45, thus indicating dispersion of bacteria as compared to the control. Additionally, the defensive effect of SNEDDS formulation helped in protecting the lungs from chronic infection, as indicated by histopathological studies. Collectively, this study highlights the therapeutic effectiveness of targeted SNEDDS formulation as an advanced and efficient delivery system for COPD management.</p>

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Formulation and Characterization of Arginine Decorated Self-nanoemulsifying Drug Delivery System of Roflumilast against Chronic Obstructive Pulmonary Disease

  • 期刊论文

  • 发表日期：

    2026年3月17日

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  • Iqra Khan,
  • Rabia Arshad,
  • Waqar Aman,
  • Tahir Maqbool,
  • Waqas Ahmad,
  • Abdul Malik,
  • Mohammad Shamsul Ola,
  • Sara Aiman

摘要

This study aims to formulate amino acid-based nanotherapeutics for the effective treatment of chronic obstructive pulmonary disease (COPD). For this purpose, L-Arginine (Arg) was glycosylated with glucose (Glu) via Millard reaction and then integrated into Roflumilast (Rof) loaded self-nanoemulsifying drug delivery system (SNEDDS). A selective phosphodiesterase-4 inhibitor (PDE-4), Rof, is an anti-inflammatory drug that is clinically used to treat COPD, and was integrated into an SNEDDS formulation to improve its solubilization, stability, and targeted therapeutic efficacy. The developed SNEDDS were characterized for physicochemical and in-vivo characterization. SNEDDS displayed 192 ± 1.23 nm size with 30 ± 1.4 mV zeta potential, and 0.24 ± 0.5 PDI. Moreover, Arg-Glu-Rof-loaded SNEDDS resulted in favorable mucoadhesion properties along with 90% drug entrapment efficiency and 85% efficient drug release in 12 h. The optimized SNEDDS demonstrated outstanding biocompatibility, hemocompatibility, and enhanced cellular uptake analysis. The most significant bacterial inhibition was observed with prepared SNEDDS formulation, having reduced optical density values of 0.45, thus indicating dispersion of bacteria as compared to the control. Additionally, the defensive effect of SNEDDS formulation helped in protecting the lungs from chronic infection, as indicated by histopathological studies. Collectively, this study highlights the therapeutic effectiveness of targeted SNEDDS formulation as an advanced and efficient delivery system for COPD management.