The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity
The natural peptide somatostatin has hormonal and cytostatic effects exerted by the binding to specific receptors in various tissues. Therapeutic uses are strongly prevented by its very short biological half-life of 1–2 min due to enzymatic hydrolysis, therefore encapsulation methodologies are explo...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-08-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/24/17/3085 |
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| author | Anna Vita Larocca Gianluca Toniolo Silvia Tortorella Marios G. Krokidis Georgia Menounou Giuseppe Di Bella Chryssostomos Chatgilialoglu Carla Ferreri |
| author_facet | Anna Vita Larocca Gianluca Toniolo Silvia Tortorella Marios G. Krokidis Georgia Menounou Giuseppe Di Bella Chryssostomos Chatgilialoglu Carla Ferreri |
| author_sort | Anna Vita Larocca |
| collection | DOAJ |
| description | The natural peptide somatostatin has hormonal and cytostatic effects exerted by the binding to specific receptors in various tissues. Therapeutic uses are strongly prevented by its very short biological half-life of 1–2 min due to enzymatic hydrolysis, therefore encapsulation methodologies are explored to overcome the need for continuous infusion regimes. Multilamellar liposomes made of natural phosphatidylcholine were used for the incorporation of a mixture of somatostatin and sorbitol dissolved in citrate buffer at pH = 5. Lyophilization and reconstitution of the suspension were carried out, showing the flexibility of this preparation. Full characterization of this suspension was obtained as particle size, encapsulation efficiency and retarded release properties in aqueous medium and human plasma. Liposomal somatostatin incubated at 37 °C in the presence of Fe(II) and (III) salts were used as a biomimetic model of drug-cell membrane interaction, evidencing the free radical processes of peroxidation and isomerization that transform the unsaturated fatty acid moieties of the lipid vesicles. This study offers new insights into a liposomal delivery system and highlights molecular reactivity of sulfur-containing drugs with its carrier or biological membranes for pharmacological applications. |
| first_indexed | 2024-12-10T16:23:28Z |
| format | Article |
| id | doaj.art-1505fdb093584283bee4d7fe23b7b657 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-10T16:23:28Z |
| publishDate | 2019-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-1505fdb093584283bee4d7fe23b7b6572022-12-22T01:41:43ZengMDPI AGMolecules1420-30492019-08-012417308510.3390/molecules24173085molecules24173085The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical ReactivityAnna Vita Larocca0Gianluca Toniolo1Silvia Tortorella2Marios G. Krokidis3Georgia Menounou4Giuseppe Di Bella5Chryssostomos Chatgilialoglu6Carla Ferreri7R&D Laboratory, Lipinutragen srl, Via Piero Gobetti 101, 40129 Bologna, ItalyInstitute of Nanoscience and Nanotechnology, N.C.S.R. “Demokritos”, 15310 Agia Paraskevi Attikis, GreeceISOF, Consiglio Nazionale delle Ricerche, Via P. Gobetti 101, 40129 Bologna, ItalyInstitute of Nanoscience and Nanotechnology, N.C.S.R. “Demokritos”, 15310 Agia Paraskevi Attikis, GreeceISOF, Consiglio Nazionale delle Ricerche, Via P. Gobetti 101, 40129 Bologna, ItalyDi Bella Foundation, Via G. Marconi 51, 40122 Bologna, ItalyR&D Laboratory, Lipinutragen srl, Via Piero Gobetti 101, 40129 Bologna, ItalyR&D Laboratory, Lipinutragen srl, Via Piero Gobetti 101, 40129 Bologna, ItalyThe natural peptide somatostatin has hormonal and cytostatic effects exerted by the binding to specific receptors in various tissues. Therapeutic uses are strongly prevented by its very short biological half-life of 1–2 min due to enzymatic hydrolysis, therefore encapsulation methodologies are explored to overcome the need for continuous infusion regimes. Multilamellar liposomes made of natural phosphatidylcholine were used for the incorporation of a mixture of somatostatin and sorbitol dissolved in citrate buffer at pH = 5. Lyophilization and reconstitution of the suspension were carried out, showing the flexibility of this preparation. Full characterization of this suspension was obtained as particle size, encapsulation efficiency and retarded release properties in aqueous medium and human plasma. Liposomal somatostatin incubated at 37 °C in the presence of Fe(II) and (III) salts were used as a biomimetic model of drug-cell membrane interaction, evidencing the free radical processes of peroxidation and isomerization that transform the unsaturated fatty acid moieties of the lipid vesicles. This study offers new insights into a liposomal delivery system and highlights molecular reactivity of sulfur-containing drugs with its carrier or biological membranes for pharmacological applications.https://www.mdpi.com/1420-3049/24/17/3085liposomal somatostatinretarded deliveryfree radicalsisomerizationtrans lipidperoxidation |
| spellingShingle | Anna Vita Larocca Gianluca Toniolo Silvia Tortorella Marios G. Krokidis Georgia Menounou Giuseppe Di Bella Chryssostomos Chatgilialoglu Carla Ferreri The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity Molecules liposomal somatostatin retarded delivery free radicals isomerization trans lipid peroxidation |
| title | The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity |
| title_full | The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity |
| title_fullStr | The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity |
| title_full_unstemmed | The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity |
| title_short | The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity |
| title_sort | entrapment of somatostatin in a lipid formulation retarded release and free radical reactivity |
| topic | liposomal somatostatin retarded delivery free radicals isomerization trans lipid peroxidation |
| url | https://www.mdpi.com/1420-3049/24/17/3085 |
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