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Background <p>Atorvastatin mitigates cardiovascular disorders through potent lipid-lowering, anti-inflammatory, antioxidant, and plaque-stabilizing activities. However, it suffers from limitations of instability in acidic medium, low systemic bioavailability due to extensive hepatic first-pass metabolism, need for higher drug dosages accompanied by systemic toxicity.</p> Methods <p>To overcome the above limitations, the study prepared polymeric and lipid polymer hybrid nanoparticles (LPHNPs) via the ionic gelation method for pulmonary delivery of atorvastatin. The nanoparticles were characterized for physicochemical properties and evaluated for drug release, aerodynamic performance and antihyperlipidemic potential in rabbits.</p> Results <p>The polymeric nanoparticles (PNPs) (234 nm) were significantly smaller than LPHNPs (296 nm). LPHNPs possess curved structure with higher drug loading (96.17 ± 2.38 µg/mg), while PNPs exist as discrete spherical particles. The PNPs have zeta potential of 28 mV that reduced to -16 mV for LPHNPs. The nanoparticles release atorvastatin in sustained fashion via Fickian diffusion. The PNPs achieved significantly higher dispersed fraction (87%) and fine particle fraction (50%) being attributed to its lower Carr’s index (35) and MMAD values (1.38 μm). </p> Conclusion <p>The PNPs were more effective against hyperlipidemia than LPHNPs due to lower particle size, positive zeta potential with higher muco-adhesive properties, making it a potential platform for the systemic delivery of atorvastatin.</p>

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Comparative Analysis of Polymeric and Lipid Polymer Hybrid Nanoparticles: In-Vitro and In-Vivo Analysis for Pulmonary Delivery of Atorvastatin

  • 期刊论文

  • 发表日期：

    2026年6月16日

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  • Kifayat Ullah Shah,
  • Muhammad Usama Ghani Khan,
  • Fahad Y. Sabei,
  • Muhammad Danish Saeed,
  • Firdous Ahmad Burki,
  • Muhammad Yasir Ghani Khan,
  • Awaji Y. Safhi,
  • Ahmad Salawi,
  • Abdullah Alsalhi,
  • Ali Hanbashi

摘要

Background

Atorvastatin mitigates cardiovascular disorders through potent lipid-lowering, anti-inflammatory, antioxidant, and plaque-stabilizing activities. However, it suffers from limitations of instability in acidic medium, low systemic bioavailability due to extensive hepatic first-pass metabolism, need for higher drug dosages accompanied by systemic toxicity.

Methods

To overcome the above limitations, the study prepared polymeric and lipid polymer hybrid nanoparticles (LPHNPs) via the ionic gelation method for pulmonary delivery of atorvastatin. The nanoparticles were characterized for physicochemical properties and evaluated for drug release, aerodynamic performance and antihyperlipidemic potential in rabbits.

Results

The polymeric nanoparticles (PNPs) (234 nm) were significantly smaller than LPHNPs (296 nm). LPHNPs possess curved structure with higher drug loading (96.17 ± 2.38 µg/mg), while PNPs exist as discrete spherical particles. The PNPs have zeta potential of 28 mV that reduced to -16 mV for LPHNPs. The nanoparticles release atorvastatin in sustained fashion via Fickian diffusion. The PNPs achieved significantly higher dispersed fraction (87%) and fine particle fraction (50%) being attributed to its lower Carr’s index (35) and MMAD values (1.38 μm).

Conclusion

The PNPs were more effective against hyperlipidemia than LPHNPs due to lower particle size, positive zeta potential with higher muco-adhesive properties, making it a potential platform for the systemic delivery of atorvastatin.