Micellar Nanocarriers: Potential Nose-to-Brain Delivery of Zolmitriptan as Novel Migraine Therapy
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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.
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.
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.
The investigation indicated the potential of the developed nanocarrier as an effective new-generation vehicle for brain targeting of zolmitriptan.
KEY WORDSautoradiography biodistribution brain targeting micellar nanocarrier zolmitriptan
The authors are thankful to Archarchem Pharmaceuticals Pvt. Ltd. and Chokhani Pharmaceutical Ltd. for the gift sample of zolmitriptan; Gattefosse, Mumbai, India and BASF India Ltd. for the gift sample of excipients; and Aptar Pharma India Pvt. Ltd., Mumbai, India for the kind gift of Equadel™ Pump. The authors are grateful to Lalit Borde and Dr. Krishanu Ray from Tata Institute of Fundamental Research, Mumbai, India; Prof. Katarina Edwards, Uppsala University, Uppsala, Sweden; and Prof. Ishi Talmon, Haifa, Israel for conducting the cryo-TEM analysis. The authors are thankful to Dr. P. A. Hassan, Dr. V. K. Aswal for DLS and SANS analysis, and Dr. Tanuja Shet for authoradiography Studies. Ratnesh Jain is thankful to the Board of Research in Nuclear Sciences (Sanction No. 2006/35/11/BRNS), Department of Atomic Energy, Gov’t of India, for providing the funding to execute the research.
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