Decrease of liposomal size and retarding effect on fluconazole skin permeation by lysine derivatives.

J Pharm Sci

Research Platform Characterisation of Drug Delivery Systems on Skin and Investigation of Involved Mechanisms, University of Vienna, Vienna, Austria.

Published: July 2011

AI Article Synopsis

  • Liposomes are effective for delivering drugs through the skin due to their ability to modify how drugs are distributed in the body.
  • A study used lysine derivatives (Lys-5 and Lys-7) to enhance the structure of liposomes containing fluconazole and analyzed their impact on drug permeability.
  • Results showed that these oligopeptides caused a structural change in the liposomes, reducing their size by 10% to 40% and slowing down the skin absorption of fluconazole.

Article Abstract

Liposomes are ideal dermal drug delivery systems because of their ability to alter the biodistribution profile of incorporated drugs. In a novel approach to optimize the liposomal microstructure, lysine derivatives were employed. The effect of the oligopeptides Lys-5 and Lys-7 on the structure as well as on the skin permeation of the antimycotic drug fluconazole in 1,2-dipalmitoyl-sn-glycero-3-phosphocholine vesicles was studied using a variety of techniques. It was demonstrated by addition of the shift reagent praseodymium(III)chloride and subsequent (31)P NMR measurements that the liposomes produced consisted mainly of unilamellar vesicles. This was confirmed by cryo-transmission electron microscopy. The addition of Lys-5 and Lys-7 induced a structural change resulting in a decrease in particle size between 10% and 40% and a retarding effect on fluconazole skin permeation.

Download full-text PDF

Source
http://dx.doi.org/10.1002/jps.22513DOI Listing

Publication Analysis

Top Keywords

skin permeation
12
retarding fluconazole
8
fluconazole skin
8
lysine derivatives
8
lys-5 lys-7
8
decrease liposomal
4
liposomal size
4
size retarding
4
permeation lysine
4
derivatives liposomes
4

Similar Publications

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!