Evaluation of brain targeting and antipsychotic activity of nasally administrated ziprasidone lipid–polymer hybrid nanocarriers

Hadel A. Abo El-Enin, Alaa S. Tulbah, Hany W. Darwish, Rania Salama, Ibrahim A. Naguib, Heba A. Yassin, Hend Mohamed Abdel-Bar

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)
74 Downloads (Pure)

Abstract

The feasibility of using lipid-polymer hybrid (LPH) nanocarriers as a potential platform for the intranasal delivery of ziprasidone (ZP), a second-generation antipsychotic, was explored. Different ZP-loaded LPH composed of a PLGA core and cholesterol-lecithin lipid coat were prepared using a single step nano-precipitation self-assembly technique. Modulation of polymer, lipid and drug amounts, as well as stirring-speed-optimized LPH with a particle size of 97.56 ± 4.55 nm and a ZP entrapment efficiency (EE%) of 97.98 ± 1.22%. The brain deposition and pharmacokinetics studies proved the efficiency of LPH to traverse the blood-brain barrier (BBB) following intranasal delivery with a 3.9-fold increase in targeting efficiency compared to the intravenous (IV) ZP solution with a direct nose-to-brain transport percentage (DTP) of 74.68%. The ZP-LPH showed enhanced antipsychotic activity in terms of animals' hypermobility over an IV drug solution in schizophrenic rats. The obtained results showed that the fabricated LPH was able to improve ZP brain uptake and proved its antipsychotic efficiency.

Original languageEnglish
Article number886
Pages (from-to)1-17
Number of pages17
JournalPharmaceuticals
Volume16
Issue number6
DOIs
Publication statusPublished - 15 Jun 2023

Bibliographical note

Copyright the Author(s) 2023. Version archived for private and non-commercial use with the permission of the author/s and according to publisher conditions. For further rights please contact the publisher.

Keywords

  • intranasal
  • ziprasidone
  • lipid–polymer hybrid
  • brain targeting
  • nanocarriers

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