A Lipid-Based Depot Formulation with a Novel Non-lamellar Liquid Crystal Forming Lipid
| Autor: | Shoko Itakura, Kenji Sugibayashi, Hiroaki Todo, Ichiro Hijikuro, Akie Okada |
|---|---|
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
Glycerol
Male Depot Drug Compounding Mixing (process engineering) Pharmaceutical Science Excipient Biological Availability 02 engineering and technology 030226 pharmacology & pharmacy law.invention Excipients 03 medical and health sciences 0302 clinical medicine Glycerol ester of wood rosin Liquid crystal law medicine Animals Pharmacology (medical) Lamellar structure sustained release Rats Wistar Phospholipids Pharmacology Drug Carriers Chromatography Chemistry Organic Chemistry Lipid-based depot formulation 021001 nanoscience & nanotechnology non-lamellar liquid crystal Sodium salt Liquid Crystals self-assembled structure Drug Liberation Delayed-Action Preparations Molecular Medicine Electron microscope Leuprolide 0210 nano-technology Peptides Biotechnology medicine.drug Research Paper |
| Zdroj: | Pharmaceutical Research |
| ISSN: | 1573-904X 0724-8741 |
| Popis: | Purpose: Non-lamellar liquid crystal (NLLC)-forming lipids have gained attention as a novel component because of their ability to self-assemble upon contact with body fluids. In this study, a novel NLLC-forming lipid, mono-O-(5, 9, 13-trimethyl-4-tetradecenyl) glycerol ester (C17MGE), and a model drug with a middle molecule weight, leuprolide acetate (LA), were used to confirm the usefulness of C17MGE as an excipient for depot formulations with sustained release properties.Methods: A self-constructed depot formulation was prepared by mixing C17MGE and different types of phospholipids. The constructed NLLC structure was evaluated using small angle X-ray analysis and cryo-transmission electron microscopy. In vitro release and blood concentration profiles of LA were investigated.Results: The NLLC structure was confirmed by small angle X-ray analysis. LA release was able to be modified by adding different ratios of various phospholipids to C17MGE. Formulations containing 1, 2-dioleoyl-sn-glycero-3-phosphoglycerol sodium salt with a mixing ratio of 12% or 24% (MDOPG12 or MDOPG24, respectively) exhibited sustained release profiles of LA. In addition, the blood concentration of LA was detected over 21 days or more after administration of MDOPG12, and the absolute bioavailability was calculated to be about 100%.Conclusions: A depot formulation using C17MGE was useful to achieve sustained release of LA. Original Article |
| Databáze: | OpenAIRE |
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