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Preparation, characterization, and in vivo biodistribution study of intranasal 131I-clonazepam-loaded phospholipid magnesome as a promising brain delivery system.
Sayyed, Marwa Eid; El-Motaleb, Mohamed Abd; Ibrahim, Ismail Taha; Rashed, Hassan Medhat; El-Nabarawi, Mohamed Ahmed; Ahmed, Mohamed Abdallah.
Afiliación
  • Sayyed ME; Radio Labeled Compounds Department, Hot Labs Centre, Egyptian Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt. Electronic address: marwaeaea@gmail.com.
  • El-Motaleb MA; Radio Labeled Compounds Department, Hot Labs Centre, Egyptian Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt.
  • Ibrahim IT; Radio Labeled Compounds Department, Hot Labs Centre, Egyptian Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt; Faculty of Pharmacy, Albayan University, Baghdad, Iraq.
  • Rashed HM; Radio Labeled Compounds Department, Hot Labs Centre, Egyptian Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt.
  • El-Nabarawi MA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, P.O. Box 11562, Cairo, Egypt.
  • Ahmed MA; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, P.O. Box 11562, Cairo, Egypt; Department of Pharmaceutics and Industrial Pharmacy, School of Pharmacy, New Giza University, Giza, Egypt.
Eur J Pharm Sci ; 169: 106089, 2022 Feb 01.
Article en En | MEDLINE | ID: mdl-34863872
OBJECTIVE: Clonazepam (CP) is a potent long-acting nitrobenzodiazepine derivative that could be used for targeting peripheral benzodiazepine receptors. Phospholipid magnesome is a new vesicular nanosystem recently developed for brain targeting. Improving the uptake of 131I-CP to the brain might be effective for the diagnosis and/or radiotherapy of certain brain diseases and/or tumors. METHODS: CP was radiolabeled with 131I using direct electrophilic substitution reaction. Quality control of 131I-CP was performed using different techniques. Different formulas of 131I-CP were prepared and characterized according to particle size and polydispersity index. The structural features of the optimized formula were then interpreted using transmission electron microscopy and scanning electron microscopy, whereas pharmacokinetic and in vivo behaviors were estimated using the intravenous and intranasal delivery routes. RESULTS: The heart and blood demonstrated lower uptake of 131I-CP, which inevitably decreased the nontarget effects of radioiodine. Intranasally administered 131I-CP-loaded magnesomes (INMg) had noticeably higher brain uptake (7.1 ± 0.09%ID/g) with rapid onset of action within 5 min and effective pharmacokinetic behavior. INMg had a drug targeting efficiency and nose-to-brain direct transport percentage of 121.1% and 94.6%, respectively as well as a relative bioavailability of 441.04 ± 75.5%. CONCLUSION: The present study showed that 131I-CP-loaded magnesomes can be a beneficial brain-targeting approach for improving the diagnosis and/or radiotherapy of certain brain diseases.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Clonazepam / Radioisótopos de Yodo Idioma: En Revista: Eur J Pharm Sci Asunto de la revista: FARMACIA / FARMACOLOGIA / QUIMICA Año: 2022 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Clonazepam / Radioisótopos de Yodo Idioma: En Revista: Eur J Pharm Sci Asunto de la revista: FARMACIA / FARMACOLOGIA / QUIMICA Año: 2022 Tipo del documento: Article Pais de publicación: Países Bajos