ABSTRACT

This chapter focuses on several key issues or dilemmas which make the study of lipoproteins as drug carriers challenging and directly applicable to other particles and vesicles introduced into biological fluids. An understanding of the regulatory controls over the transport processes is key in understanding both the pharmacokinetics and pharmacodynamics of site delivery for drugs using lipoproteins. Certain pharmacological agents taken by the oral route would by design naturally transport and incorporate into the lipoprotein assembly process much like cholesterol, triglycerides, vitamin E, and carotene. Reconstituted apoprotein-lipid-drug vesicular or micellar systems can be prepared by utilizing high ratios of tertiary butanol/water to solubilize the phospholipids, lipids, and amphipathic molecules followed by lyophilization then rehydration. Hydrophobic interactions play an important role in the interaction of apoproteins with the lipid domain of the lipoprotein. Fibroblast, endothelial, or epithelial cells are first cultured on coverslips then exposed to apo E-liposome complexes at different concentrations or time periods.