Related Experiment Video
Updated: Jun 17, 2026

Uptake of New Lipid-coated Nanoparticles Containing Falcarindiol by Human Mesenchymal Stem Cells
Published on: February 9, 2019
Ascorbyl dipalmitate/PEG-lipid nanoparticles as a novel carrier for hydrophobic drugs
Kunikazu Moribe1, Sunao Maruyama, Yutaka Inoue
1Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba 263-8522, Japan. moribe@p.chiba-u.ac.jp
Abstract:
L-ascorbyl 2,6-dipalmitate (ASC-DP), a fatty ester derivative of ascorbic acid, is poorly soluble in water and does not spontaneously form micelles or liposomal structures in water. In this study, we attempted to prepare an ASC-DP/surfactant nano-sized complex as a carrier for hydrophobic drugs. Samples were prepared by hydrating a solvent-evaporated film of ASC-DP/surfactant at a molar ratio of 1:1. Among the surfactants tested, distearoylphosphatidylethanolamine-polyethylene glycol 2000 (DSPE-PEG) was found to form stable nanoparticles with ASC-DP (average particle size: ca. 67 nm). Several hydrophobic drugs were incorporated in the ASC-DP/DSPE-PEG nanoparticles. Stability, toxicity, and blood residence of the drug-containing ASC-DP/DSPE-PEG nanoparticles were evaluated using amphotericin B (AmB) as the model drug. By intravenously administering mice with the formulations, we determined the minimum lethal dose of Fungizone, a formulation of AmB solubilized with sodium deoxycholate, was 3.0 mg/kg, while that of AmB/ASC-DP/DSPE-PEG nanoparticles was 10.0 mg/kg. When 2.0 mg/kg, Fungizone was administered, the mice showed higher renal and hepatic toxicities. Intravenously administered AmB/ASC-DP/DSPE-PEG nanoparticles demonstrated higher concentration in plasma than Fungizone. Thus, the ASC-DP/DSPE-PEG nanoparticle system appears to be a promising delivery system for hydrophobic drugs.
Related Concept Videos
Bioavailability Enhancement: Drug Permeability Enhancement
Site-Targeted Drug Delivery Systems: Polymeric Carriers
Ophthalmic Drug Delivery Systems
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
Modified-Release Drug Delivery Systems: Site-Targeted

