Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB Transport
Encapsulation possibilities of an extensively investigated neuroprotective drug (kynurenic acid, KYNA) are studied via lipid-based nanocarriers to increase the blood–brain barrier (BBB) specific permeability. The outcomes of various preparation conditions such as stirring and sonication time, concen...
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2023-09-01
|
| Series: | International Journal of Molecular Sciences |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1422-0067/24/18/14251 |
| _version_ | 1797579700670824448 |
|---|---|
| author | Ádám Juhász Ditta Ungor Norbert Varga Gábor Katona György T. Balogh Edit Csapó |
| author_facet | Ádám Juhász Ditta Ungor Norbert Varga Gábor Katona György T. Balogh Edit Csapó |
| author_sort | Ádám Juhász |
| collection | DOAJ |
| description | Encapsulation possibilities of an extensively investigated neuroprotective drug (kynurenic acid, KYNA) are studied via lipid-based nanocarriers to increase the blood–brain barrier (BBB) specific permeability. The outcomes of various preparation conditions such as stirring and sonication time, concentration of the lipid carriers and the drug, and the drug-to-lipid ratio are examined. Considering the experimentally determined encapsulation efficiency, hydrodynamic diameter, and ζ-potential values, the initial lipid and drug concentration as well as the stirring and sonication time of the preparation were optimized. The average hydrodynamic diameter of the prepared asolectin-(LIP) and water-soluble lipopolymer (WSLP)-based liposomes was found to be ca. 25 and 60 nm under physiological conditions. The physicochemical characterization of the colloidal carriers proves that the preparation of the drug-loaded liposomes was a successful process, and secondary interactions were indicated between the drug molecule and the polymer residues around the WSLP membrane. Dissolution profiles of the active molecule under physiological conditions were registered, and the release of the unformulated and encapsulated drug is very similar. In addition to this outcome, the in vitro polar brain lipid extract (porcine)-based permeability test proved the achievement of two- or fourfold higher BBB specific penetration and lipid membrane retention for KYNA in the liposomal carriers relative to the unformatted drug. |
| first_indexed | 2024-03-10T22:39:52Z |
| format | Article |
| id | doaj.art-fec67ea5e59f4cb9a818c1705c5e2892 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-10T22:39:52Z |
| publishDate | 2023-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-fec67ea5e59f4cb9a818c1705c5e28922023-11-19T11:09:59ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-09-0124181425110.3390/ijms241814251Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB TransportÁdám Juhász0Ditta Ungor1Norbert Varga2Gábor Katona3György T. Balogh4Edit Csapó5Interdisciplinary Excellence Center, Department of Physical Chemistry and Materials Science, University of Szeged, Rerrich B. Sqr. 1, H-6720 Szeged, HungaryMTA-SZTE Lendület “Momentum” Noble Metal Nanostructures Research Group, University of Szeged, Rerrich B. Sqr. 1, H-6720 Szeged, HungaryInterdisciplinary Excellence Center, Department of Physical Chemistry and Materials Science, University of Szeged, Rerrich B. Sqr. 1, H-6720 Szeged, HungaryInstitute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös Str. 6, H-6720 Szeged, HungaryDepartment of Pharmaceutical Chemistry, Semmelweis University, Hőgyes Endre út 9, H-1092 Budapest, HungaryInterdisciplinary Excellence Center, Department of Physical Chemistry and Materials Science, University of Szeged, Rerrich B. Sqr. 1, H-6720 Szeged, HungaryEncapsulation possibilities of an extensively investigated neuroprotective drug (kynurenic acid, KYNA) are studied via lipid-based nanocarriers to increase the blood–brain barrier (BBB) specific permeability. The outcomes of various preparation conditions such as stirring and sonication time, concentration of the lipid carriers and the drug, and the drug-to-lipid ratio are examined. Considering the experimentally determined encapsulation efficiency, hydrodynamic diameter, and ζ-potential values, the initial lipid and drug concentration as well as the stirring and sonication time of the preparation were optimized. The average hydrodynamic diameter of the prepared asolectin-(LIP) and water-soluble lipopolymer (WSLP)-based liposomes was found to be ca. 25 and 60 nm under physiological conditions. The physicochemical characterization of the colloidal carriers proves that the preparation of the drug-loaded liposomes was a successful process, and secondary interactions were indicated between the drug molecule and the polymer residues around the WSLP membrane. Dissolution profiles of the active molecule under physiological conditions were registered, and the release of the unformulated and encapsulated drug is very similar. In addition to this outcome, the in vitro polar brain lipid extract (porcine)-based permeability test proved the achievement of two- or fourfold higher BBB specific penetration and lipid membrane retention for KYNA in the liposomal carriers relative to the unformatted drug.https://www.mdpi.com/1422-0067/24/18/14251liposomekynurenic acidblood–brain barrierdrug release |
| spellingShingle | Ádám Juhász Ditta Ungor Norbert Varga Gábor Katona György T. Balogh Edit Csapó Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB Transport International Journal of Molecular Sciences liposome kynurenic acid blood–brain barrier drug release |
| title | Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB Transport |
| title_full | Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB Transport |
| title_fullStr | Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB Transport |
| title_full_unstemmed | Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB Transport |
| title_short | Lipid-Based Nanocarriers for Delivery of Neuroprotective Kynurenic Acid: Preparation, Characterization, and BBB Transport |
| title_sort | lipid based nanocarriers for delivery of neuroprotective kynurenic acid preparation characterization and bbb transport |
| topic | liposome kynurenic acid blood–brain barrier drug release |
| url | https://www.mdpi.com/1422-0067/24/18/14251 |
| work_keys_str_mv | AT adamjuhasz lipidbasednanocarriersfordeliveryofneuroprotectivekynurenicacidpreparationcharacterizationandbbbtransport AT dittaungor lipidbasednanocarriersfordeliveryofneuroprotectivekynurenicacidpreparationcharacterizationandbbbtransport AT norbertvarga lipidbasednanocarriersfordeliveryofneuroprotectivekynurenicacidpreparationcharacterizationandbbbtransport AT gaborkatona lipidbasednanocarriersfordeliveryofneuroprotectivekynurenicacidpreparationcharacterizationandbbbtransport AT gyorgytbalogh lipidbasednanocarriersfordeliveryofneuroprotectivekynurenicacidpreparationcharacterizationandbbbtransport AT editcsapo lipidbasednanocarriersfordeliveryofneuroprotectivekynurenicacidpreparationcharacterizationandbbbtransport |