Purpose: The investigation was aimed at developing micellar nanocarriers for nose-to-brain delivery of zolmitriptan with the objective to investigate the pathway involved in the drug transport.
Methods: The micellar nanocarrier was successfully formulated and characterized for particle size and shape by multi-angle dynamic light scattering, small angle neutron scattering and cryo-transmission electron microscopy. Toxicity and biodistribution studies were carried out in rat. The distribution of the nasally administered labeled micellar nanocarrier in various regions of the rat brain was determined using the brain localization and autoradiography studies.
Results: Micellar nanocarrier of zolmitriptan, with size of around 23 nm, was successfully formulated. The spherical nature of the nanocarrier was confirmed using DLS, SANS and cryo-TEM. Toxicity studies indicated the safety for administration in the nasal cavity. In vivo biodistribution studies indicated the superiority of the developed nanocarrier for brain targeting when compared with the intravenous and nasal solutions of the drug. Brain localization and autoradiography studies illustrated the distribution of the drug in various regions of the brain and revealed a possible nose-to-brain transport pathway for the labeled drug.
Conclusion: The investigation indicated the potential of the developed nanocarrier as an effective new-generation vehicle for brain targeting of zolmitriptan.
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http://dx.doi.org/10.1007/s11095-009-0041-x | DOI Listing |
Acta Biomater
December 2024
Shanghai Frontiers Science Center of Drug Target Identification and Delivery, School of Pharmaceutical Sciences, Shanghai Jiao Tong University, Shanghai 200240, China; National Key Laboratory of Innovative Immunotherapy, Shanghai Jiao Tong University, Shanghai 200240, China. Electronic address:
The activation of STING pathway has emerged as a promising strategy in cancer immunotherapy. However, challenges associated with unfavorable physicochemical properties and potential off-target toxicities have limited the application of STING agonists. Here, we develop an amphiphilic and cationic charged porphyrin-polymer to electrostatically load the STING agonist (MSA-2) within a micellar structure, thereby enhancing carrier compatibility and drug-loading content of MSA-2.
View Article and Find Full Text PDFFood Chem
March 2025
Department of Food Science, Aarhus University, Agro Food Park 48, 8200 Aarhus N, Denmark.
In this study, the bioaccessibility and bioavailability of curcumin encapsulated into different lupin protein isolate-based carriers was evaluated by coupling an in vitro gastrointestinal digestion (INFOGEST) with an in vitro co-culture absorption model, Caco-2/HT29-MTX, consisting of both absorptive and mucus producing cells. A targeted ultrahigh-performance quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS) method was applied to monitor the fate of curcumin post digestion and absorption, specifically analyzing the apical, cellular, and basolateral fractions. Lupin protein nanoparticles, obtained by desolvation, protected curcumin from degradation better than oil in water (O/W) emulsions stabilized with lupin protein isolate.
View Article and Find Full Text PDFBiomacromolecules
January 2025
Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska 68198, United States.
Curr Drug Targets
November 2024
Department of Pharmacy, Teerthanker Mahaveer College of Pharmacy, Teerthanker Mahaveer University, Moradabad (UP)-244001, India.
Pharm Dev Technol
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Bezmialem Vakif University, Fatih, Istanbul, Turkey.
Polymeric micelles were prepared for the delivery of donepezil, a leading Alzheimer's disease drug, to enhance its transport across the blood-brain barrier (BBB). Poly(ethylene glycol)--poly(-butyl methacrylate) amphiphilic block copolymers were synthesized reversible addition-fragmentation chain transfer (RAFT) polymerization. The polymers were characterized by gel permeation chromatography and nuclear magnetic resonance spectroscopy.
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