The corporation's nanoemulsion formulations, which are especially useful for "actively targeted" chemotherapy, comprise several key lipid components that can be adjusted for specific applications. [ For a detailed review of the relevant scientific and patent literature, associated know-how, advantages over competing technologies, etc., see recent book: D'Arrigo, J.S. (2011) Stable Nanoemulsions: Self-Assembly in Nature and Nanomedicine, 436 pp., Elsevier Science, Amsterdam and Oxford.] Briefly, the above 2011 book reviews and analyzes much experimental (in vivo) data which collectively demonstrate that this type of stable lipid nanoemulsion, upon intravenous injection, is capable of "active targeting" of various lipophilic drugs to hyperproliferative-disease sites (such as tumors, neuro-injury scar tissue, atherosclerotic lesions, etc.) -- which commonly overexpress certain cell-surface receptors. These overexpressed receptors fall within the category known as "lipoprotein receptors", which includes notably the (class B) scavenger receptor referred to as SR-BI.
This "active" targeting behavior of the FilmixTM lipid nanoemulsion vehicle (via the process of receptor-mediated endocytosis), involving SR-BI receptors, has direct relevance to the (rapidly targeted) chemotherapy of atherosclerotic plaques. This nontoxic Filmix nanoemulsion drug-delivery vehicle, a stable mixed-lipid carrier of lipophilic drugs, is readily adaptable for enhanced (local) delivery to the site of vascular lesions in coronary and/or peripheral arteries. For example, Van Eck et al. [Curr. Opin. Lipidol. 16:307-315 (2005)] point out that (the human version of) SR-BI is expressed in macrophage-rich areas of human atherosclerotic lesions [Hirano et al., Circ. Res. 85:108-116 (1999)], indicating that this scavenger receptor plays an important role locally in atherosclerotic lesion development in the arterial wall in humans [see also D'Arrigo (2011) reference above]. In addition, Nakagawa-Toyama et al. reported in human aorta and coronary arteries, SR-BI was highly expressed in atherosclerotic plaques, but not in non-atherosclerotic lesions. Double immunostaining demonstrated that SR-BI was expressed in a subpopulation of macrophages [Atherosclerosis 183:75-83 (2005)]. Chinette et al. further explain that human SR-BI (i.e., CLA-1) is undetectable in human monocytes but the expression of this receptor is induced upon cellular differentiation into macrophages. These authors similarly conclude, from their independent experimental results and immunohistological analysis, that human atherosclerotic lesions displayed high expression of CLA-1 in macrophages of the lipid core [Circulation 101:2411-2417 (2000)]. Hence, as summarized by Van Eck et al., the development of initial fatty-streak lesions is induced by macrophage SR-BI/CLA-1 facilitating the uptake of atherogenic lipoproteins like VLDL and oxidized LDL by macrophages -- which transform into foam cells [Curr. Opin. Lipidol. 16:307-315 (2005) ]. (However, Van Eck et al. also point out that the macrophage SR-BI/CLA-1 receptor has a unique dual role in atherogenesis, depending on the stage of lesion development. Initially, this receptor induces formation of foam cells and early fatty-streak lesions; in contrast, at later stages of atherosclerotic lesion development, the function of this SR-BI/CLA-1 receptor, which includes cholesterol efflux to HDL, protects the arterial wall from extensive lipid accumulation [Curr. Opin. Lipidol. 16:307-315 (2005)].) Therefore, the ultimate objective of "targeted chemotherapy" of atherosclerotic plaques, utilizing "active targeting" behavior to the site of vascular lesions, is particularly well suited to the Filmix nanoemulsion drug-delivery vehicle -- since SR-BI/CLA-1 has emerged as the lipoprotein receptor primarily involved in ligand-receptor binding of this lipid nanoemulsion vehicle at target cells [D'Arrigo (2011) reference above].