Liposomes are one of the best drug delivery systems. They can favourably alter the pharmacokinetics and pharmacodynamics of the encapsulated drugs. There are many factors like liposome composition, drug-bilayer interactions and encapsulation method which have a direct influence on drug leakage from liposomes and indirect on antitumour activity of the drug [1].

In this study we decided to prepare liposomal formulations of epirubicin (EPI) loaded in the lipid vesicles via ascorbic acid and ammonium ascorbate gradients [2]. We investigated physical state of the drug inside the vesicles using circular dichroism and Cryo-TEM microsopy and correlate it with in vitro cytotoxic activity of the prepared liposomal formulations of EPI on l breast cancer cell lines. We also show that developed in our laboratory gradient based on vitamin C protect healthy cells against Epirubicin cytotoxicity. To increase anticancer activity of developed liposomal forlmulation we used folic acid to active targeting of liposomes. The folate receptors over-expressed in many tumours are being intensively studied as a target to enhance the selectivity of drug delivery to cancer cells [3]. In vitro activity of the liposomal formulation was studied on 4T1 murine mammary cancer cells, which are highly physiological mouse model that closely resembles breast cancer in human. Prepared liposomal formulation showed great anticancer activity because of the active targeting and physical state of the drug inside the vesicles which allows to fast drug release from the liposomes and kill cancer cells.

The research was supported by Wroclaw Research Centre EIT+ under the project „Biotechnologies and advanced medicaltechnologies ”– BioMed (POIG.01.01.02-02-003/08) financed from the European Regional Development Fund (Operational Programme Innovative Economy, 1.1.2).

References:

1. Gubernator J (2011) Active methods of drug loading into liposomes: recent strategies for stable drug entrapment and increased in vivo activity. Expert Opin Drug Deliv 8: 565-580.
2. Lipka D, Gubernator J, Filipczak N, Barnert S, Suss R, et al. (2013) Vitamin C-driven epirubicin loading into liposomes. Int J Nanomedicine 8: 3573-3585.
3. Watanabe K, Kaneko M, Maitani Y (2012) Functional coating of liposomes using a folate-polymer conjugate to target folate receptors. Int J Nanomedicine 7: 3679-3688.

• Legal notice:
  

  Copyright (c) Pielaszek Research, all rights reserved.
  The above materials, including auxiliary resources, are subject to Publisher's copyright and the Author(s) intellectual rights. Without limiting Author(s) rights under respective Copyright Transfer Agreement, no part of the above documents may be reproduced without the express written permission of Pielaszek Research, the Publisher. Express permission from the Author(s) is required to use the above materials for academic purposes, such as lectures or scientific presentations.
  In every case, proper references including Author(s) name(s) and URL of this webpage: https://science24.com/paper/31195 must be provided.