Evaluation of Brain Targeting and Mucosal Integrity of Nasally Administrated Nanostructured Carriers of a CNS Active Drug, Clonazepam

Authors

  • Hend Mohamed Abdel-Bar Department of Pharmaceutics, National Organization of Drug Control and Research, Giza, Egypt.
  • Amal Youssef Abdel-Reheem Department of Pharmaceutics, National Organization of Drug Control and Research, Giza, Egypt.
  • Gehanne A.S Awad Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
  • Nahed Daoud Mortada Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

DOI:

https://doi.org/10.18433/J30S31

Abstract

PURPOSE: The aim of the study was to target clonazepam, a CNS active drug, to the brain through the non-invasive intranasal (in) route using of nanocarriers with proven safety METHOD: in clonazepam nanocarriers were prepared by mixing isopropyl myristate, Tween 80, Cremophor EL or lecithin, polyethylene glycol 200, propylene glycol or ethanol in different ratios with water. in-vitro characterization of the nanocarriers was done by various methods including: polarized light microscopy, particle size determination, viscosity measurements and drug release studies. in-vivo study comparing intranasal and intravenous administration was performed. The drug targeting efficiency (DTE %) and direct nose to brain transport percentage (DTP %) were calculated and nasal integrity assessment was carried out. RESULTS: The obtained formulae had particle size below 100 nm favoring rapid direct nose to brain transport and the time for 100% drug release (T100%) depended on systems composition. Plasma Tmax of clonazepam nanostructured carriers varied from 10-30 min., while their brain Tmax did not exceed 10 min, in comparison with 30 min for iv solution. Although there was no significant difference (p>0.05) between the plasma AUC0-∞ of the different tested nanocarriers and intravenous one, the increase in brain AUC 0 -∞ of different nasal formulations in comparison to that of iv administration (3.6 -7.2 fold) confirms direct nose to brain transport via olfactory region. Furthermore, DTE and DTP% confirmed brain targeting of clonazepam following intranasal administration. CONCLUSION: The results confirmed that intranasal nanocarriers were proved to be safe alternative for iv clonazepam delivery with rapid nose to brain transport. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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Author Biographies

Hend Mohamed Abdel-Bar, Department of Pharmaceutics, National Organization of Drug Control and Research, Giza, Egypt.

Department of pharmaceutics

Amal Youssef Abdel-Reheem, Department of Pharmaceutics, National Organization of Drug Control and Research, Giza, Egypt.

Department of pharmaceutics

Gehanne A.S Awad, Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

Department of pharmaceutics and industrial pharmacy

Nahed Daoud Mortada, Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.

Department of pharmaceutics and industrial pharmacy

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Published

2013-07-14

How to Cite

Abdel-Bar, H. M., Abdel-Reheem, A. Y., Awad, G. A., & Mortada, N. D. (2013). Evaluation of Brain Targeting and Mucosal Integrity of Nasally Administrated Nanostructured Carriers of a CNS Active Drug, Clonazepam. Journal of Pharmacy & Pharmaceutical Sciences, 16(3), 456–469. https://doi.org/10.18433/J30S31

Issue

Section

Pharmaceutical Sciences; Review Articles