Vegetable Oil-based Hybrid Submicron Particles Loaded with JMV5038: A Promising Formulation against Melanoma |
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| Authors: | Koceïla Doufène Yohan Malki Laure-Anaïs Vincent Pierre Cuq Jean-Marie Devoisselle Nicolas Masurier Anne Aubert-Pouëssel |
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| Affiliation: | 1. Institut Charles Gerhardt Montpellier (ICGM), University of Montpellier, CNRS, ENSCM, Montpellier, France;2. Institut des Biomolécules Max Mousseron (IBMM), University of Montpellier, CNRS, ENSCM, Montpellier, France |
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| Abstract: | The aim of this work was to carry out a preformulation study on JMV5038 as a new potent cytotoxic agent, and to develop its formulation within vegetable oil-based hybrid submicron particles (HNP) in order to obtain a versatile dosage form against melanoma. JMV5038 was first characterized through physico-chemical tests and it exhibited high melting point and logP value, an important pH-sensitivity that led to the formation of well-identified degradation products at low pH, as well as a substantial solubility value in silylated castor oil (ICO). Then, JMV5038-loaded HNP were formulated through a thermostabilized emulsion process based on the sol-gel cross-linking of ICO. They showed high loading efficiency and their in vitro release kinetic assessed in a biorelevant PBS/octanol biphasic system showed a constant sustained release over one month. The cytotoxic activity and cytocompatibility of HNP were evaluated on A375 melanoma cells and NIH 3T3 cells, respectively. JMV5038-loaded HNP exhibited a slightly enhanced cytotoxic activity of JMV5038 on melanoma cells while demonstrating their safety on NIH 3T3 cells. In conclusion, JMV5038-loaded HNP proved to be an efficient and safe drug subcutaneous delivery system that will be interesting to evaluate through preclinical studies. |
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| Keywords: | Diazepine Vegetable oil Lipid-based drug delivery system Melanoma Hybrid particles API" },{" #name" :" keyword" ," $" :{" id" :" kwrd0020" }," $$" :[{" #name" :" text" ," _" :" Active Pharmaceutical Ingredient = drug COSY" },{" #name" :" keyword" ," $" :{" id" :" kwrd0030" }," $$" :[{" #name" :" text" ," _" :" COrrelation SpectroscopY HMBC" },{" #name" :" keyword" ," $" :{" id" :" kwrd0040" }," $$" :[{" #name" :" text" ," _" :" Heteronuclear Multiple Bond Correlation HNP" },{" #name" :" keyword" ," $" :{" id" :" kwrd0050" }," $$" :[{" #name" :" text" ," _" :" Hybrid submicroN Particles HPLC" },{" #name" :" keyword" ," $" :{" id" :" kwrd0060" }," $$" :[{" #name" :" text" ," _" :" High Pressure Liquid Chromatography ICO" },{" #name" :" keyword" ," $" :{" id" :" kwrd0070" }," $$" :[{" #name" :" text" ," _" :" silylated Castor Oil IP" },{" #name" :" keyword" ," $" :{" id" :" kwrd0080" }," $$" :[{" #name" :" text" ," _" :" ImidazoPyridine IPTES" },{" #name" :" keyword" ," $" :{" id" :" kwrd0090" }," $$" :[{" #name" :" text" ," _" :" (3-IsocyanatoPropyl)TriEthoxysilane MAPK/ERK" },{" #name" :" keyword" ," $" :{" id" :" kwrd0100" }," $$" :[{" #name" :" text" ," _" :" Mitogen-Activated Protein Kinases/Extracellular signal-Regulated Kinases MWCO" },{" #name" :" keyword" ," $" :{" id" :" kwrd0110" }," $$" :[{" #name" :" text" ," _" :" Molecular Weight Cut-Off NMR" },{" #name" :" keyword" ," $" :{" id" :" kwrd0120" }," $$" :[{" #name" :" text" ," _" :" Nuclear Magnetic Resonance ORALD" },{" #name" :" keyword" ," $" :{" id" :" kwrd0130" }," $$" :[{" #name" :" text" ," _" :" Open-Ring and Alanine-Loss Derivative (of JMV5038) ORD" },{" #name" :" keyword" ," $" :{" id" :" kwrd0140" }," $$" :[{" #name" :" text" ," _" :" Open-Ring Derivative (of JMV5038) PBS" },{" #name" :" keyword" ," $" :{" id" :" kwrd0150" }," $$" :[{" #name" :" text" ," _" :" Phosphate Buffer Saline RT" },{" #name" :" keyword" ," $" :{" id" :" kwrd0160" }," $$" :[{" #name" :" text" ," _" :" Retention Time SD" },{" #name" :" keyword" ," $" :{" id" :" kwrd0170" }," $$" :[{" #name" :" text" ," _" :" Standard Deviation UPLC (/ MS)" },{" #name" :" keyword" ," $" :{" id" :" kwrd0180" }," $$" :[{" #name" :" text" ," _" :" Ultra Performance Liquid Chromatography (Coupled with Mass Spectrometry) |
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