Effect of Alkyl Chain Length and Unsaturation of the Phospholipid on the Physicochemical Properties of Lipid Nanoparticles

Chemical & Pharmaceutical Bulletin
Yuka FunakoshiShigeru Itai

Abstract

Previously, we developed lipid nanoparticles (LNs) containing poorly water-soluble drugs using two types of phospholipids, a neutral phospholipid (hydrogenated soybean phosphatidylcholine) and a negatively-charged phospholipid (dipalmitoylphosphatidylglycerol), with mean particle sizes of less than 100 nm. Here, we studied the effects of alkyl chain length and unsaturation of neutral and negatively-charged phospholipids on the physicochemical properties of LNs. Three neutral phospholipids, dimyristoylphosphatidylcholine, dipalmitoylphosphatidylcholine and distearoylphosphatidylcholine, having different alkyl chain lengths, were compared. The mean particle size of the LNs increased with the alkyl chain length, while the concentration of the drug entrapped in the LNs decreased. The particle size of all of the LNs could be maintained at less than 100 nm for 1 month in cool and dark conditions, with the LNs with longer alkyl chain lipids showing greater stability. In the unsaturated phospholipids, the double bond in the alkyl chain of dioleoylphosphatidylcholine and dierucoylphosphatidylcholine did not affect the physicochemical properties of the LNs. The negatively-charged phospholipids dipalmitoylphosphatidylglycerol and distearo...Continue Reading

References

Oct 19, 2004·International Journal of Pharmaceutics·A R MohammedY Perrie
Jan 18, 2006·Journal of Controlled Release : Official Journal of the Controlled Release Society·Jun-ichi JinnoToshikiro Kimura
Feb 8, 2006·Chemical & Pharmaceutical Bulletin·Seitaro KamiyaTakashi Sonobe
Dec 18, 2007·International Journal of Pharmaceutics·Seitaro KamiyaTakashi Sonobe
May 19, 2009·International Journal of Pharmaceutics·Hiroyuki OhshimaShigeru Itai
Dec 28, 2010·International Journal of Pharmaceutics·Sudhir VermaDiane J Burgess
Apr 30, 2013·International Journal of Pharmaceutics·Yuka FunakoshiShigeru Itai
May 3, 2014·Chemical & Pharmaceutical Bulletin·Ranjan Kumar BarmanShigeru Itai

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Citations

Jan 5, 2017·Chemical & Pharmaceutical Bulletin·Md Ashraf AliShigeru Itai
Apr 5, 2021·Materials Science & Engineering. C, Materials for Biological Applications·Disha N MoholkarKiran D Pawar

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