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Intratracheal Administration of Dry Powder Formulation in Mice
Published on: July 25, 2020
Quercetin solid lipid microparticles: a flavonoid for inhalation lung delivery
Santo Scalia1, Mehra Haghi, Vanessa Losi
1Department of Chemical and Pharmaceutical Sciences, University of Ferrara, via Fossato di Mortara 17, 44121 Ferrara, Italy.
Summary
Researchers developed solid lipid microparticles (SLMs) for quercetin inhalation. These non-toxic SLMs showed enhanced quercetin diffusion, suggesting potential for improved lung drug delivery.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Nanotechnology
Background:
- Quercetin, a flavonoid, possesses antioxidant and anti-inflammatory properties.
- Pulmonary drug delivery offers direct targeting and avoids first-pass metabolism.
- Developing stable, inhalable formulations for quercetin is crucial for its therapeutic application.
Purpose of the Study:
- To formulate quercetin as dry powder solid lipid microparticles (SLMs) for direct pulmonary administration.
- To characterize the physicochemical properties and in vitro performance of quercetin SLMs.
- To evaluate the toxicity and cellular transport of quercetin SLMs in a lung model.
Main Methods:
- Solid lipid microparticles (SLMs) containing quercetin were prepared using tristearin and phosphatidylcholine via o/w emulsification and phase inversion.
- Characterization included morphology, drug loading (15.5%), encapsulation efficiency (71.4%), particle size, humidity response, crystallinity, thermal behavior, and respirable fraction.
- In vitro toxicity and transport across a Calu-3 cell monolayer were assessed using a modified twin-stage impinger.
Main Results:
- Quercetin SLMs were successfully formulated as a dry powder with a fine particle fraction of 20.5% (≤4.46μm), suitable for inhalation.
- The SLMs exhibited linear kinetic absorption across the Calu-3 cell monolayer (22.32% over 4h).
- Quercetin SLMs demonstrated no significant toxicity, and no apical to basolateral transport of micronized quercetin was observed.
Conclusions:
- The developed quercetin SLMs are suitable for inhalation drug delivery.
- The lipid and emulsifying excipients in SLMs appear to enhance quercetin diffusion.
- Further research is needed to fully elucidate the mechanisms behind enhanced quercetin diffusion.
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