Table 2. Small molecules encapsulated in polymeric nanoparticles for ApoE-mediated brain targeting.
| Drug | Disease/Effect of drug | Nanoparticular formulation | Type of ApoE-functionalization | In Vivo | [Ref.] |
|---|---|---|---|---|---|
| Loperamide | Analgesia | PBCA | Indirect by PS80-coating | yes | [79b] |
| PBCA | Coating with ApoE | yes | [59] | ||
| HSA | Covalent linkage of ApoE | yes | [68, 71] | ||
| PLGA | Indirect by PS80- or poloxamer 188-coating | yes | [54] | ||
| PLGA-PEG-PLGA | Indirect by PS80- or poloxamer 188-coating | yes | [55] | ||
| Doxorubicin | Cerebral Cancer | PBCA | Indirect by PS80-coating | yes | [79c, 80, 82] |
| PLGA | Indirect by PS80- or poloxamer 188-coating | yes | [54, 85] | ||
| PDMA-PS | Coating with mApoE | no | [86a] | ||
| Doxorubicin | Brain metastases | PMA-PS80-starch | Indirect by PS80 | yes | [86b] |
| Methotrexate | Cerebral Cancer | PBCA | Indirect by PS80-coating | yes | [87] |
| Temozolomide | Cerebral Cancer | PBCA | Indirect by PS80-coating | yes | [88] |
| Cisplatin | Cerebral Cancer | PBCA | Indirect by PS80-coating | yes | [89] |
| Carboplatin | Cerebral Cancer | PLGA | Indirect by PS80-coating | yes | [123] |
| Docetaxel | Brain metastases | PMA-PS80-maltodextrin-dodecane | Indirect by PS80 | yes | [124] |
| Docetaxel | Cerebral Cancer | PLGA-PEG-DHA | Indirect by PEG and DHA | yes | [125] |
| Gemcitabine | Cerebral Cancer | PBCA | Indirect by PS80-coating | yes | [126] |
| Curcumin | Cerebral Cancer | PBCA | Coating with ApoE | no | [90a] |
| Curcumin | Alzheimer’s disease | PBCA | Coating with ApoE | no | [90b] |
| Tacrine | Alzheimer’s disease | PBCA | Indirect by PS80-coating | yes | [91a, 127] |
| PBCA-PEG | Indirect by PEG | yes | [127] | ||
| Rivastigmine | Alzheimer’s disease | PBCA | Indirect by PS80-coating | yes | [91b] |
| Estradiol | Alzheimer’s disease | PLGA | Indirect by PS80-coating | yes | [92] |
| Rosmarinic acid | Alzheimer’s disease | PAAM-CH-PLGA | Coating with ApoE | yes | [61] |
| Salvianolic Acid B | Neurodegenerative diseases | PECA | Indirect by PS80-coating | yes | [128] |
| Tubocurarine | Muscle relaxation | PBCA | Indirect by PS80-coating | yes | [79a] |
| Pentamidine | Human African Trypanosomiasis | PCL | Indirect by PS80-coating | no | [56] |
| Amitriptyline | Depression | PBCA | Indirect by PS80-coating | yes | [74] |
| MRZ 2/576 | Epilepsy | PBCA | Indirect by PS80-coating | yes | [129] |
| Valproic acid | Epilepsy | PBCA | Indirect by PS80-coating | yes | [130] |
| Breviscapine | Cerebrovascular diseases | PLA | Indirect by poloxamer 188-coating | yes | [131] |
| Puerarin | Stroke | PBCA | Indirect by PS80-coating | yes | [132] |
| Gatifloxacin | Central nervous system tuberculosis | PLGA | Indirect by PS80-coating | yes | [133] |
| Amphotericin B | Cryptococcal meningitis | PBCA | Indirect by PS80-coating | yes | [134] |
| PLA-PEG | Indirect by PS80-coating and PEG | yes | [135] | ||
| Quercetin | Antioxidant | PBCA | Indirect by PS80-coating | yes | [136] |
| Stavudine | Human immunodeficiency virus | PBCA | Indirect by PS80-coating | no | [137] |
| Delavirdine | Human immunodeficiency virus | PBCA | Indirect by PS80-coating | no | [137] |
| Saquinavir | Human immunodeficiency virus | PBCA | Indirect by PS80-coating | no | [137] |
| Obidoxime | Acetylcholinesterase reactivator | HSA | Covalent linkage of ApoE | no | [138] |
| Sumatriptan Succinate | Migraine | PBCA | Indirect by PS80-coating | yes | [139] |
| BSA | Covalent linkage of ApoE | yes | [139] |
a
Abbreviations: PS80 = polysorbate 80; PDMA = poly(dimethylacrylamide); PMA = poly(methacrylic acid); PECA = poly(ethylcyanoacrylate), BSA = bovine serum albumin.