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Published on: November 14, 2018
Cyclodextrin-Based Quercetin Powders for Potential Nose-to-Brain Transport: Formulation and In Vitro Assessment
Elmina-Marina Saitani1, Paraskevi Papakyriakopoulou1, Theodora Bogri1
1Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimiopolis Zografou, 15771 Athens, Greece.
Spray-dried quercetin (Que) nasal powders using hydroxypropyl-β-cyclodextrin (HPβCD) show enhanced delivery. Formulation optimization with excipients like HPMC and MLMPs can tailor physicochemical properties for improved nose-to-brain drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Quercetin (Que) exhibits antioxidant and neuroprotective effects but suffers from poor solubility and bioavailability.
- Nasal drug delivery offers a direct, non-invasive route to the brain, bypassing first-pass metabolism.
- Hydroxypropyl-β-cyclodextrin (HPβCD) can enhance the solubility and delivery of poorly soluble drugs.
Purpose of the Study:
- To investigate the impact of preparation methods (spray drying vs. lyophilization) and excipients (HPMC, MLMPs) on HPβCD-based nasal Que powder formulations.
- To evaluate the physicochemical properties, structural characteristics, and in vitro diffusion of these nasal powders.
- To optimize Que nasal delivery for enhanced brain targeting.
Main Methods:
- Formulation of Que/HPβCD nasal powders using spray drying and lyophilization.
- Incorporation of hydroxypropyl methylcellulose (HPMC) and mannitol/lecithin microparticles (MLMPs).
- Characterization using TGA, SEM, and in vitro diffusion studies with Franz cells.
Main Results:
- Spray-dried HPβCD/Que powder (F4) demonstrated the highest permeation (0.11 ± 0.01 mg/cm² at 120 min).
- HPMC enhanced thermal stability but decreased Que diffusion due to increased viscosity.
- MLMPs improved powder flow and dose placement but slightly reduced diffusion efficiency.
Conclusions:
- Spray-dried HPβCD-based powders are a promising platform for nasal quercetin delivery.
- HPMC and MLMPs can be strategically used to modulate powder properties and delivery performance.
- This study provides insights into optimizing nasal formulations for enhanced nose-to-brain drug delivery.
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