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Table 3 Drugs with areas of opportunity for reformulation in NPs for PD

From: Repositioning of drugs for Parkinson’s disease and pharmaceutical nanotechnology tools for their optimization

Drug Clinical trial status Cross the BBB? Formulated in NPs? (Type/composition) Area of opportunity
Exenatide 3–Recruiting
2–Active
1–Terminated
1–Unknown
Yes Polymeric NPs/CSK-DEX-PLGA [128] Rapidly eliminated by glomerular filtration, reformulation in NPs could increase its half-life in plasma and avoid enzymatic degradation
Levetiracetam 3–Terminated
1–Suspended
1–Recruiting
1–Unknown
Yes Polymeric NPs/PLGA [129] Reformulation in NPs could reduce the dose and administration frequency, reducing side effects
Semaglutide 1–Not yet recruiting No Liposome/Phospholipid- cholesterol [130] NPs could improve stability, bioavailability, and passage through the BBB and avoid toxic accumulation due to its half-life of approximately one week
Vitamin B12 1–Terminated Yes Lipid-protein NPs/Barley protein-α-tocopherol-Phospholipids [131] Reformulate in NPs with surface functionalization allows their targeting to the brain
Pomalidomide N/I Restricted
(P-gp substrate)
N/I BCS class IV, reformulation in NPs could improve intestinal absorption and permeability through the BBB
Dabrafenib N/I Restricted
(P-gp substrate)
N/I Reformulation in NPs with anti-P-gp surface functionalization could allow passage through the BBB
Ketoconazole N/I Restricted
(P-gp substrate)
Polymeric NPs/PLGA [132] Low solubility. Reformulation in NPs could offer a controlled release, reduce toxic effects, and achieve greater bioavailability
Felodipine N/I Yes Polymeric NPs/PLGA [133]
SLN/Glyceryl behenate [134]
Variable bioavailability, poor solubility, and extensive liver metabolism. Reformulation in NPs could offer greater brain bioavailability
Raloxifene N/I Yes Polymeric NPs/CS [135]
SLN/Glyceryl behenate [136]
Low oral bioavailability, poor solubility, and extensive metabolism in the intestine (> 90%). Reformulation in NPs could improve oral bioavailability
Candesartan N/I Yes SLN/Trimyristin-Tripalmitin-Tristearin [137] Low oral bioavailability, poor solubility. Reformulation in NPs could improve oral bioavailability and target the brain
Telmisartan N/I Yes
(dose-dependent)
Polymeric NPs/PLA [138] Low oral bioavailability, poor solubility. NPs could allow greater penetration of the BBB and target the brain
Nitazoxanide N/I Low permeability SLN/Hydrogenated palm oil- Hydrogenated soybean lecithin [139] Reformulation in NPs could allow more passage through the BBB, greater control of the dosage, and avoid toxic effects
Metformin N/I Yes Polymeric NPs/Alginate [140] BCS class III, low absorption. Reformulation in NPs could facilitate absorption and control the dosage and release at the specific site of action
Nilotinib 1 – Active
2 – Terminated
Low permeability Polymeric micelles/Styrene-co-maleic acid [141] Low exposure to CSF limits its use in PD. Reformulation in functionalized NPs could allow vectorization towards the CNS
Exemestane N/I Yes Polymeric NPs/Alginate [142] Reformulating in NPs could improve solubility and bioavailability, control release, and decrease side effects
Salbutamol N/I Yes Polymeric NPs/PLGA, and poly(vinyl sulfonate-co-vinyl alcohol)-graft-PLGA [143] Low oral bioavailability. Reformulation in NPs could allow the targeting of the target neurons
Pentamidine N/I Low permeability Polymeric NPs/PLGA [144]
Liposome/Phosphatidylcholine
Polymeric NPs/PCL [145]
It can cause diabetes and other toxic effects. Reformulation in NPs could improve permeation through the BBB, greater control of the dosage, and avoiding toxic effects
Ceftriaxone 1 – Recruiting Yes Polymeric NPs/CS [146] It is administered parenterally. Only 1% oral bioavailability, reformulation in NPs could increase its bioavailability and allow a controlled release
Vilazodone N/I Restricted
(P-gp substrate)
Polymeric NPs/Copolymer Soluplus®-Polyvinylpyrrolidone [147] Low solubility. Reformulation in NPs could increase bioavailability and permeation through the BBB
Methylene blue N/I Yes Metallic NPs/Ag [148] Rapid distribution in tissues. Severe toxicity in high doses. Reformulation in NPs could allow controlled dosage and vectorization towards the CNS
Nalbuphine N/I Yes SLN/Phosphatidylcholine [149] They are limited to parenteral use. High concentrations can cause sedation. Reformulation of NPs could allow oral administration and greater dosage control
Ketamine N/I Yes Polymeric NPs/PEG-PLGA [150] Short half-life. Serious adverse effects. Reformulation in NPs could increase their bioavailability and specific release in target neurons
Dimethyl fumarate N/I Low permeability SLN/Tocopherol acetate [151] Short half-life. Reformulation in NPs could improve bioavailability, brain permeability and reduce adverse effects
Kanamycin N/I Low permeability Metallic NPs/Au [152] Relatively insoluble in lipids. Reformulation in NPs could allow greater oral bioavailability and permeation through the BBB
CMT-3 N/I Yes N/I Multi-target drug. Reformulation in NPs could allow targeting of target neurons
Doxycycline N/I Yes Polymeric NPs/PLGA-PCL (153) Reformulation in NPs would allow the sustained administration of the drug, minimizing adverse effects
  1. Ag Silver, Au Gold, BBB Blood–brain barrier, BCS Biopharmaceutical classification system, CMT-3 Tetracycline 3 modified chemically, CNS Central nervous system, CS Chitosan, CSF Cerebrospinal fluid, CSK CSKSSDYQC peptide, DEX Dextran, N/I No information, NPs Nanoparticles, PCL Poly ɛ‐caprolactone, PD Parkinson’s disease, PEG Polyethylene glycol, P-gp P-glycoprotein, PLA Polylactic acid, PLGA Poly lactic-co-glycolic acid, SiO2 Silicon dioxide, SLN Solid lipid nanoparticles