Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers
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...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-06-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/16/6/886 |
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| author | Hadel A. Abo El-Enin Alaa S. Tulbah Hany W. Darwish Rania Salama Ibrahim A. Naguib Heba A. Yassin Hend Mohamed Abdel-Bar |
| author_facet | Hadel A. Abo El-Enin Alaa S. Tulbah Hany W. Darwish Rania Salama Ibrahim A. Naguib Heba A. Yassin Hend Mohamed Abdel-Bar |
| author_sort | Hadel A. Abo El-Enin |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-11T02:02:50Z |
| format | Article |
| id | doaj.art-17a5f40fbcec48428fd9002d70df2787 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-11T02:02:50Z |
| publishDate | 2023-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-17a5f40fbcec48428fd9002d70df27872023-11-18T12:02:56ZengMDPI AGPharmaceuticals1424-82472023-06-0116688610.3390/ph16060886Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid NanocarriersHadel A. Abo El-Enin0Alaa S. Tulbah1Hany W. Darwish2Rania Salama3Ibrahim A. Naguib4Heba A. Yassin5Hend Mohamed Abdel-Bar6Department of Pharmaceutics, National Organization of Drug Control and Research (NODCAR) (Previously), Egyptian Drug Authority (Currently), Giza 12511, EgyptDepartment of Pharmaceutics, College of Pharmacy, Umm Al-Qura University, Makkah 21955, Saudi ArabiaDepartment of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaMacquarie Medical School, Faculty of Medicine, Health and Human Sciences, Macquarie University, Ryde, NSW 2109, AustraliaDepartment of Pharmaceutical Chemistry, College of Pharmacy, Taif University, P.O. Box 11099, Taif 21944, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, Badr University in Cairo (BUC), Badr City, Cairo 11829, EgyptDepartment of Pharmaceutics, Faculty of Pharmacy, University of Sadat City, Menoufia 32897, EgyptThe 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.https://www.mdpi.com/1424-8247/16/6/886intranasalziprasidonelipid–polymer hybridbrain targetingnanocarriers |
| spellingShingle | Hadel A. Abo El-Enin Alaa S. Tulbah Hany W. Darwish Rania Salama Ibrahim A. Naguib Heba A. Yassin Hend Mohamed Abdel-Bar Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers Pharmaceuticals intranasal ziprasidone lipid–polymer hybrid brain targeting nanocarriers |
| title | Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers |
| title_full | Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers |
| title_fullStr | Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers |
| title_full_unstemmed | Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers |
| title_short | Evaluation of Brain Targeting and Antipsychotic Activity of Nasally Administrated Ziprasidone Lipid–Polymer Hybrid Nanocarriers |
| title_sort | evaluation of brain targeting and antipsychotic activity of nasally administrated ziprasidone lipid polymer hybrid nanocarriers |
| topic | intranasal ziprasidone lipid–polymer hybrid brain targeting nanocarriers |
| url | https://www.mdpi.com/1424-8247/16/6/886 |
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