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. Author manuscript; available in PMC: 2021 Aug 11.
Published in final edited form as: Adv Drug Deliv Rev. 2020 Aug 11;159:377–390. doi: 10.1016/j.addr.2020.08.003

Table 2.

Lipoprotein-based drug delivery systems.

Chemotherapy
Molecule Lipoprotein subclass Pathology Experiments Ref
5-fluorouracil, 5-iododeoxyuridine, doxorubicin, and vindesine Natural VLDLs, LDLs, and HDLs Cervical cancer and breast cancer In vitro Human cervical cancer (HeLa) and breast cancer (MCF-7) [58]
Paclitaxel oleate sLDLs GBM In vitro Human cervical cancer (HeLa) and GBM (SF-767, U-251, SF-763) [42]
Paclitaxel-alpha linolenic acid sLDLs GBM and hepatocarcinoma In vitro Human GBM (U-87 MG) and hepatocarcinoma (HepG2)
In vivo BALB/c nude mice bearing subcutaneous tumors (U-87 MG)
[64]
Paclitaxel sHDLs Breast cancer, prostate cancer, and ovarian cancer In vitro Human breast cancer (MCF7), prostate cancer (DU145), and ovarian cancer (OVCAR-3 OV1063)
In vivo C57BL6 mice
[65]
Withalongolide A 4,19,27-triacetate sHDLs Adrenocortical carcinoma In vitro Human adrenocortical carcinoma (H295R, SW13).
In vivo Athymic nude mice Foxn1nu bearing subcutaneous tumors (H295R).
[66]
Sorafenib and dihydroartemisinin sLDLs Liver cancer In vitro Human liver cancer (HepG2)
In vivoBALB/c nude mice bearing subcutaneous tumors (HepG2)
[67]
Toll-like receptor 9 agonist and tumor-specific neoantigens sHDLs Gliomas In vivo C57BL/6 mice bearing subcutaneous tumors (GL261) and CD4−/− and CD8−/− knockout (KO) mice bearing orthotopic tumors (GL261) [68]
Antigen peptides and CpG sHDLs Colon adenocarcinoma In vivo C57BL/6 mice bearing subcutaneous tumors (MC-38) [69]
Nucleic acids
Molecule Lipoprotein subclass Pathology Experiments Ref #
Androgen receptor siRNA sHDLs Prostate cancer In vivo Human prostate cancer (LNCaP), melanoma (A375), breast cancer (MDA-MB-231), and ovarian cancer (OvCar3)
In vivo Athymic nude mice bearing subcutaneous tumors (LNCaP)
[70]
ApoB siRN sHDLs sLDLs Atherosclerosis In vitro Mouse primary hepatocytes
In vivo C57BL6 double transgenic mice expressing human apoB and cholesterol ester transfer protein
[71]
Activating transcription factor-5 siRNA sHDLs Glioblastoma In vitro Rat glioblastoma cells (C6)
In vivo NOD/SCID mice bearing subcutaneous tumors (C6)
[72]
Atherosclerosis treatments
Molecule Lipoprotein subclass Pathology Experiments Ref #
Anti-inflammatory liver X receptor agonist sHDLs Atherosclerotic plaques In vitro Mouse macrophages (J774A.1)
In vivo C57BL/6 J mice and apoE-deficient mice (B6.129P2-Apoetm1Unc/J)
[73]
Lovastatin sHDLs Hypercholesterole mia In vitro Mouse macrophages (RAW 264.7)
In vivo ApoE knockout mice (B6.129P2-Apoetm1Unc/J)
[74]
Simvastatin Hyaluronan-anchored core-shell sHDL Atherosclerotic plaques In vitro Human umbilical vein endothelial cells (HUVECs) and mouse macrophages (RAW 264.7)
In vivo Atherosclerotic New Zealand White (NZW) rabbits
[75]
Simvastatin sHDL Atherosclerotic plaques In vitro Mouse macrophages (J774A.1), mouse endothelial cells (MS1), mouse aortic smooth muscle cells (MOVAS) and mouse liver cells (Hepa-1c1c7)
In vivo ApoE-knockout mice (B6.129P2-Apoetm1Unc/J)
[76]
β-cyclodextrin and simvastatin sHDL Atherosclerotic plaques In vitro Mouse macrophages (RAW 264.7) [77]
Imaging molecules
Molecule Lipoprotein subclass Pathology Experiments Ref #
Amphiphilic gadolinium-diethylenetriaminepenta acetic acid chelates LDLs Liver cancer In vitro Human liver cancer (HepG2) and Chinese hamster ovary cells (ldlA7).
In vivo Nude mice bearing subcutaneous tumors (HepG2)
[78]
Silicon tetra-tert-butyl-phthalocyanine sLDLs Liver cancer In vitro Human liver cancer (HepG2) [79]
Nanocrystals as imaging molecules sHDLs Atherosclerosis In vivo Wild type and apoE knockout mice [80]
Valrubicin sHDLs Prostate cancer In vitro Human prostate cancer (PC3) [81]
99mTc- hydrazinonicotinic acid -N-dodecylamide sHDLs Prostate cancer In vitro Human prostate cancer (PC3)
In vivo In vivo subcutaneous tumor (PC3)
[82]
Triphenylphosphonium cations and quantum dots sHDLs Atherosclerotic plaques In vitro Mouse macrophages (RAW 264.7)
In vivo Sprague Dawley rats
[83]
Anti-virals
Molecule Lipoprotein subclass Pathology Experiments Ref #
Lopinavir and Ritonavir sChylomicrons Human immunodeficiency virus In vitro Human colorectal adenocarcinoma cells (Caco-2).
In vivo Sprague Dawley rats
[62]
Hepatitis B antigens sChylomicrons Hepatitis B In vitro Human bone marrow-derived dendritic cells and monocyte-derived dendritic cells
In vivo Sprague Dawley rats
[84]
His-tagged West Nile virus envelope protein Nickel-chelating nanolipoprotein particles West Nile encephalitis In vivo Swiss Webster mice [85]
Alzheimer’s disease
ApoE3 sHDL Alzheimer’s disease In vivo Senescence-accelerated prone mouse (SAMP8) and senescence-accelerated mouse resistant R1 (SAMR1) [86]
Tissue regeneration
Rapamycin sHDL Tissue regeneration In vitro Human monocyte cell line (THP-1)
In vivo Zebrafish larvae
[87]

Apo, apolipoprotein; DHL, dihydroartemisinin; Foxn1, forkhead Box N1; GBM, glioblastoma multiforme; HDL, high-density lipoprotein; LDL, low-density lipoprotein; NOD, non-obese diabetic; nu, nude; Ref, reference; s, synthetic; SCID, severe combined immune deficiency; siRNA, small interfering RNA; VLDL, very low-density lipoprotein.