Next Article in Journal
Synthesis of Novel 2-(Het)arylpyrrolidine Derivatives and Evaluation of Their Anticancer and Anti-Biofilm Activity
Next Article in Special Issue
Converging Fate of the Oxidation and Reduction of 8-Thioguanosine
Previous Article in Journal
Melatonin Inhibits Apoptosis and Oxidative Stress of Mouse Leydig Cells via a SIRT1-Dependent Mechanism
Previous Article in Special Issue
Why Does the Type of Halogen Atom Matter for the Radiosensitizing Properties of 5-Halogen Substituted 4-Thio-2′-Deoxyuridines?
Open AccessFeature PaperArticle

The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity

1
R&D Laboratory, Lipinutragen srl, Via Piero Gobetti 101, 40129 Bologna, Italy
2
Institute of Nanoscience and Nanotechnology, N.C.S.R. “Demokritos”, 15310 Agia Paraskevi Attikis, Greece
3
ISOF, Consiglio Nazionale delle Ricerche, Via P. Gobetti 101, 40129 Bologna, Italy
4
Di Bella Foundation, Via G. Marconi 51, 40122 Bologna, Italy
*
Author to whom correspondence should be addressed.
These authors contributed equally to the work.
Present address: Università di Bologna, Dipartimento di Chimica Industriale, Viale del Risorgimento 4, 40136 Bologna, Italy.
Academic Editor: Chryssostomos Chatgilialoglu
Molecules 2019, 24(17), 3085; https://doi.org/10.3390/molecules24173085
Received: 10 August 2019 / Revised: 19 August 2019 / Accepted: 22 August 2019 / Published: 25 August 2019
(This article belongs to the Special Issue Biomimetic Radical Chemistry and Applications)
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. View Full-Text
Keywords: liposomal somatostatin; retarded delivery; free radicals; isomerization; trans lipid; peroxidation liposomal somatostatin; retarded delivery; free radicals; isomerization; trans lipid; peroxidation
Show Figures

Graphical abstract

MDPI and ACS Style

Larocca, A.V.; Toniolo, G.; Tortorella, S.; Krokidis, M.G.; Menounou, G.; Di Bella, G.; Chatgilialoglu, C.; Ferreri, C. The Entrapment of Somatostatin in a Lipid Formulation: Retarded Release and Free Radical Reactivity. Molecules 2019, 24, 3085.

Show more citation formats Show less citations formats
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop