New: dPEG-Phospholipids for superior liposomes

Published on 17/06/2014

Novel liposomes built of dPEG-Phospholipids with defined PEG chain length provide prolonged blood-circulation time and improved cellular uptake as administration carriers for drugs, delivering active molecules to the desired target.

Liposomes made of conventional phospholipides have low bioavailability and blood-circulation time. Their performance can be improved significantly by the use of dPEG-Phospholipids (Poly(ethylene glycol)–distearoylphosphatidylethanolamine; PEG-DSPE). Those novel liposomes have clearly prolonged circulation time as administration carriers for drugs, delivering active molecules to the desired target^1,2. Due to PEG-DPSE’s amphiphilic characteristics and excellent biopcampatibility, it can as well be applied for polymeric nanoparticles, microemulsions, lipid polymer hybrid nanoparticles and solid lipid nanoparticles³.

Cellular uptake of PEG-DSPE liposomes can be improved significantly by using the right design elements such as the appropriate PEG-linker length in coordination with the appropriate liposomal PEG coating and optimal ligand density^4-6. Therefore we provide dPEG-Phospholipids with three different defined PEG lengths and additionally derivatives with MAL- or TFP-function for optimal drug loading.

Papahadjopoulos D, Allen T, Gabizon A, et al. Sterically stabilized liposomes: improvements in pharmacokinetics and antitumor therapeutic efficacy. Proc Natl Acad Sci U S A. 1991; 88(24): 11460–11464.
Allen TM, Hansen C, Martin F, Redemann C, Yau-Young A. Liposomes containing synthetic lipid derivatives of poly(ethylene glycol) show prolonged circulation half-lives in vivo. Biochim Biophys. 1991; 1066(1): 29–36.
Wang R, Xiao R, Zeng Z, Xu L, Wang J. Application of poly(ethylene glycol)–distearoylphosphatidylethanolamine (PEG-DSPE) block copolymers and their derivatives as nanomaterials in drug delivery. Int J Nanomedicine. 2012; 7: 4185-98. doi: 10.2147/IJN.S34489.
Jared F. Stefanick, Jonathan D. Ashley, and Basar Bilgicer, Enhanced Cellular Uptake of Peptide-Targeted Nanoparticles through IncreasedPeptide Hydrophilicity and Optimized Ethylene Glycol Peptide-Linker Length; ACSNano 2013; 7(9): 8115-8127; http://dx.doi.org/10.1021/nn4033954.
Jared F. Stefanick, Jonathan D. Ashley, Tanyel Kiziltepe, and Basar Bilgicer, ASystematic Analysis of Peptide Linker Length and Liposomal Polyethylene Glycol Coating on Cellular Uptake of Peptide-Targeted Liposomes; ACSNano 2013; 7(4): 2935-2947; http://dx.doi.org/10.1021/nn305663e.
Gavin T. Noble, Jared F. Stefanick, Jonathan D. Ashley, Tanyel Kiziltepe, and Basar Bilgicer, Ligand-targeted liposome design: challenges and fundamental considerations; Trends in Biotechnology 2014; 32(1): 32-45; http://dx.doi.org/10.1016/j.tibtech.2013.09.007.