Solid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release

A synthetic dual-target mu opioid peptide receptor/delta opioid peptide receptor anti-nociceptive ligand, named LP2, has emerged as a promising candidate for the management of acute and/or persistent pain, but its lipophilicity limits further developments as a therapeutic agent. In this work, to all...

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Autores principales:	Angelo Spadaro, Lorella Pasquinucci, Miriam Lorenti, Ludovica Maria Santagati, Maria Grazia Sarpietro, Rita Turnaturi, Carmela Parenti, Lucia Montenegro
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	solid lipid nanoparticles diastereoisomers LP2 multitarget ligand opioids anti-nociceptive agents Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/102302aa0a4c48a2987cd36f2ca7f7f8
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spelling	oai:doaj.org-article:102302aa0a4c48a2987cd36f2ca7f7f82021-11-11T15:17:34ZSolid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release10.3390/app1121102502076-3417https://doaj.org/article/102302aa0a4c48a2987cd36f2ca7f7f82021-11-01T00:00:00Zhttps://www.mdpi.com/2076-3417/11/21/10250https://doaj.org/toc/2076-3417A synthetic dual-target mu opioid peptide receptor/delta opioid peptide receptor anti-nociceptive ligand, named LP2, has emerged as a promising candidate for the management of acute and/or persistent pain, but its lipophilicity limits further developments as a therapeutic agent. In this work, to allow designing aqueous formulations of LP2 for parenteral administration, solid lipid nanoparticles (SLNs) were investigated as LP2 nanocarriers. LP2-loaded SLNs were prepared by the phase-inversion temperature method, showing good technological properties (small mean particle, size, low polydispersity index, good stability). As LP2 was a diastereoisomeric mixture of 2<i>R</i>/2<i>S</i>-LP2, an HPLC method was developed to identify and quantify each diastereoisomer, and this method was used to assess LP2 in vitro release from SLNs. The developed method, based on reverse-phase chromatography using an isocratic mobile phase consisting of 50% methanol and 50% triethanolamine at 0.3% (pH = 3 with trifluoroacetic acid), allowed efficient separation of 2<i>R</i>- and 2<i>S</i>-LP2 peaks and reliable quantification with intra- and inter-day precision and accuracy within the acceptability limit, expressed as relative standard deviation set at ≤15%. The results of this study suggest that the incorporation of LP2 into SLNs could be a promising strategy to design suitable formulations for further pharmacological studies involving LP2.Angelo SpadaroLorella PasquinucciMiriam LorentiLudovica Maria SantagatiMaria Grazia SarpietroRita TurnaturiCarmela ParentiLucia MontenegroMDPI AGarticlesolid lipid nanoparticlesdiastereoisomersLP2multitarget ligandopioidsanti-nociceptive agentsTechnologyTEngineering (General). Civil engineering (General)TA1-2040Biology (General)QH301-705.5PhysicsQC1-999ChemistryQD1-999ENApplied Sciences, Vol 11, Iss 10250, p 10250 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	solid lipid nanoparticles diastereoisomers LP2 multitarget ligand opioids anti-nociceptive agents Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999
spellingShingle	solid lipid nanoparticles diastereoisomers LP2 multitarget ligand opioids anti-nociceptive agents Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999 Angelo Spadaro Lorella Pasquinucci Miriam Lorenti Ludovica Maria Santagati Maria Grazia Sarpietro Rita Turnaturi Carmela Parenti Lucia Montenegro Solid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release
description	A synthetic dual-target mu opioid peptide receptor/delta opioid peptide receptor anti-nociceptive ligand, named LP2, has emerged as a promising candidate for the management of acute and/or persistent pain, but its lipophilicity limits further developments as a therapeutic agent. In this work, to allow designing aqueous formulations of LP2 for parenteral administration, solid lipid nanoparticles (SLNs) were investigated as LP2 nanocarriers. LP2-loaded SLNs were prepared by the phase-inversion temperature method, showing good technological properties (small mean particle, size, low polydispersity index, good stability). As LP2 was a diastereoisomeric mixture of 2<i>R</i>/2<i>S</i>-LP2, an HPLC method was developed to identify and quantify each diastereoisomer, and this method was used to assess LP2 in vitro release from SLNs. The developed method, based on reverse-phase chromatography using an isocratic mobile phase consisting of 50% methanol and 50% triethanolamine at 0.3% (pH = 3 with trifluoroacetic acid), allowed efficient separation of 2<i>R</i>- and 2<i>S</i>-LP2 peaks and reliable quantification with intra- and inter-day precision and accuracy within the acceptability limit, expressed as relative standard deviation set at ≤15%. The results of this study suggest that the incorporation of LP2 into SLNs could be a promising strategy to design suitable formulations for further pharmacological studies involving LP2.
format	article
author	Angelo Spadaro Lorella Pasquinucci Miriam Lorenti Ludovica Maria Santagati Maria Grazia Sarpietro Rita Turnaturi Carmela Parenti Lucia Montenegro
author_facet	Angelo Spadaro Lorella Pasquinucci Miriam Lorenti Ludovica Maria Santagati Maria Grazia Sarpietro Rita Turnaturi Carmela Parenti Lucia Montenegro
author_sort	Angelo Spadaro
title	Solid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release
title_short	Solid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release
title_full	Solid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release
title_fullStr	Solid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release
title_full_unstemmed	Solid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release
title_sort	solid lipid nanoparticles as carriers for the synthetic opioid lp2: characterization and in vitro release
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/102302aa0a4c48a2987cd36f2ca7f7f8
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Solid Lipid Nanoparticles as Carriers for the Synthetic Opioid LP2: Characterization and In Vitro Release

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