Vesicular Phospholipid Gels: A Technology Platform

Abstract

Vesicular phospholipid gels (VPGs) represent semi-solid phospholipid dispersions. Their morphology is truly vesicular with aqueous compartments both within the core of the vesicles and in-between the vesicles. VPGs are suited to carry both hydrophilic, amphiphilic and lipophilic drugs. Their drug load is stable since there is no concentration gradient between the vesicles' core and the surrounding water phase. VPGs are suited to release drugs in a controlled manner, and thus may serve as depot implants. When blended with excess aqueous medium VPGs are easily converted into small-sized liposome (SUV) dispersions showing high encapsulation efficiencies for all kinds of drugs. VPG-formulations with various cytostatic drugs have been tested successfully in human xenografts. Obviously, the vesicles protect the drugs from premature metabolic inactivation and/or elimination and guide them to solid tumors with enhanced vascular permeability (passive targeting).

Furthermore, when mounted on a filter support, VPGs represent a tight diffusion barrier suitable for screening of oral drug permeability, as demonstrated by a set of 21 drug compounds. Permeability values were shown to fit well with human absorption in vivo, indicating that the model is suited for rapid screening of passive transport properties of new chemical entities.

Keywords: :

• small unilamellar vesicle (SUV)
• vesicle morphology
• depot
• sustained release
• liposome loading
• encapsulation efficiency
• particle size distribution
• permeability

Notes

Bender, J. (2000). Vesikuläre Phospholipidgele: Herstellungsmethoden, Dispergierverhalten, Lagerstabilität und physikalische Charakterisierung. Diss. rer. nat. Freiburg, Albert-Ludwigs-Universität: 117.