Trans resveratrol loaded DSPE PEG 2000 coated liposomes: An evidence for prolonged systemic circulation and passive brain targeting

• FT-IR studies revealed that there is no potential chemical interaction between RSV and other liposomal components.
• DSC and XRD results confirmed that RSV is present as amorphous form in the liposomal bilayer membrane.
• Liposomal formulations showed sustained release (in vitro) all over the study period without any burst release.
• PEGylated (stealth) liposomal formulation improved the plasma half life of RSV up to 18 times.
• The brain distribution of PEGylated liposomes was found to be 9 times higher than that of pristine RSV solution.

Trans resveratrol (RSV) is a natural molecule proved for cardioprotective effects, vasodilation, anti-inflammatory, cancer preventive and therapeutic activities devoid of any potential side effects. Recently, anti cancer potential against glioma cells were also reported with proven molecular mechanisms. However, the therapeutic application of RSV in clinical disease management is restricted because of its rapid elimination from systemic circulation and thereby low biological half life in mammals. Therefore, the main objective of this study was to improve the systemic circulation and biological half life of RSV using DSPE PEG 2000 decorated (PEGylated) liposomes. Moreover, brain distribution of RSV loaded PEGylated liposomes (RSV-PEG-Lipo) and non-PEGylated liposomes (RSV-Lipo) was also evaluated for proving their passive brain targeting ability. In vitro drug release of both liposomes was found to be sustained up to 48 h. RSV-PEG-Lipo showed higher area under the curve, plasma half life and mean residence time and lower volume of distribution and clearance than that of pristine RSV solution and RSV-Lipo. Pharmaokinetics results clearly indicated that the RSV-PEG-Lipo will be promising tool for enhancing plasma half life and prolong the systemic circulation of RSV. Brain distribution studies revealed that the liposomal formulations can be applied as an effective tool for passive brain targeting useful in the treatment of glioma.

Figure optionsDownload as PowerPoint slide