Background: Native lipoproteins as nanoparticulate drug delivery systems have gained considerable attention in recent years. This is due to their biocompatibility, being endogenous, no triggering the immunological responses, relatively long half-life in the circulation, simple diffusion from vascular to extravascular compartments due to their nanometric particle size, potentially targeting capability to cellular receptors, simple preparative processes in the reconstituted forms, easy functionalization and high capacity for drug loading. Clinical application of many therapeutic agents like anticancer drugs and genes is hampered due to their susceptibility to degradation and difficult delivery into cells. Several nanoparticle platforms for siRNA delivery have been developed to overcome the major limitations facing the therapeutic uses of bioactive therapeutic agents.
Methods: This review covers a broad spectrum of lipoproteins as non-viral drug and gene delivery systems. These nanoparticles are developed for enhanced cellular uptake and specially targeted gene silencing in vitro and in vivo and their characteristics and opportunities for clinical applications of therapeutic agents are discussed in this article. Various types of lipoprotein nanovectors including: natural and modified lipoproteins used to deliver drugs, bioactive and genetic materials are introduced and the development of theranostics and combinational treatments are also discussed.
Results: The unique physicochemical properties of lipoproteins as natural nanostructures in biological systems and their structural diversity, including chylomicrons, VLDL, LDL and HDL, has caused their utility as potent pharmaceutical carriers.
Conclusion: According to the literatures, different lipoproteins especially the artificial lipoproteins, reconstituted and modified ones have potential to be used in targeted delivery of therapeutic agents to the tumors and effective delivery of the corresponding genetic and other bioactive components involving in diseases.
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