Table 2.
Engineered liposomes with active ingredients for the effective treatment of AD
| Drug loaded in liposomes | Composition of liposomes | Therapeutic effect in AD | References |
|---|---|---|---|
| H102 peptide | Cholesterol, PEG, EPC, DSPE | Increase in spatial learning and memory, peptide stability and neuroprotective effect by elevated activities of acetylcholine esterase, (AchE), choline acetyltransferase (ChAT) and insulin degrading enzyme (IDE) in SD rats. | Zheng et al., 2015 |
| Rivastigmine | DPPC, cholesterol, methyl cellulose DDAB | Enhancement in amount of drug into the brain in BalBC mice. | Mutlu et al., 2011 |
| Aβ nano sweeper | Chitosan, pegylated Aβ sequence | Degradation of both soluble and insoluble Aβ, reduction in Aβ leading to decrease in Aβ toxicity, increased in neuronal survival in APPswe/PS1dE9 transgenic mice. The mice had fewer memory challenges. | Luo et al., 2018 |
| Quercetin | DPPC, PEG, stearylamine, cholesterol | Reduction in degeneration of cholinergic neurons in hippocampus of male wistar rat | Phachonpai et al., 2010 |
| DPPC, cardiolipin, DSPE-PEG2000-CA, SPC, stearylamine, cholesterol | The quercetin liposome RMP-7-Lf-liposome traversed BBB in SK-N-MC cells. Reduction in toxicity and damage to HBMECs and HA | Kuo and Tsao, 2017 | |
| Curcumin | Soyabean, cholesterol, phosphatidyl choline bonded with wheat germ agglutin and cardiolipin | Improved drug delivery to brain due to wheat germ agglutin. Curcumin inhibits aggregation of Aβ and also alters the activity of kinases involved in apoptosis pathway | Kuo and Lin, 2015; Kuo et al., 2017 |
| Poly(lactide-co-glycolic acid) (PLGA)-poly (ethylene glycol) (PEG) | Improvement in spatial learning and memory of APP/PS1 mice PLGA-PEG-B6/Cur reduced hippocampal Aβ formation and deposit and diminished tau hyperphosphorylation | Mourtas et al., 2011; Mourtas et al., 2014 | |
| PLGA-PEG | PLGA-PEG nanoparticles were loaded with Aβ generation inhibitorS1 CRT ((cyclic CRTIGPSVC peptide) that targets transferrin receptor to improve BBB transport of drugs. These multifunctional nanoliposomes decreased Aβ level, ROS, TNF- α and IL-6. Also improved spatial memory and recognition in transgenic mice AD mice. | Huang et al., 2017 | |
| NGF Nerve growth factor |
DPPC, cholesterol, DSPE- PEG | Liposome with surface lactoferrin (Lf) loaded with (NGF) improved the viability of neuron-like SK-N-MC cells with deposited β-amyloid peptide (Aβ). Increased drug delivery across BBB and had neuroprotective affect from Aβ-induced neurotoxicity. | Kuo and Chou, 2014 |
| (mApoE) a peptide obtained from the receptor-binding domain of apolipoprotein E | Phosphatidic acid Sphingomysine and cholesterol |
Bifunctionalized LIPs (mApoE-PA-LIP) administered in transgenic (Tg) AD mouse models destabilized Aβ aggregates and promoted peptide removal across the BBB. Reduction in amyloid burden and improvement in memory in transgenic mice was observed. | Balducci et al., 2014 |
| Procationic liposomes with lactoferrin | Lactoferrin | Uptake of PCL-LF liposomes in the brain was greater as compared to conventional liposomes | Chen et al., 2010 |
| Celecoxib, a COX-2 inhibitor | Erythrocyte membrane phospholipids | Liposome encapsulated with Celecoxib resulted in induction of neurogenesis. Allevation in cognitive decline. Reduction in cleared β-amyloid aggregates, apoptosis in mouse models of Alzheimer’s neurons. | Guo et al., 2017 |
| Donepzil | Cholesterol, PEG, DSPC | Intranasal drug delivery of Donepzil,acetyl cholinesterase inhibitor loaded liposome increased the bioavailability of the drug in wistar rat | Al Asmari et al., 2016 |
| Thiolated chitosan hydrogel | Intranasal drug delivery of Donepzil liposomal hydrogel had high encapsulation efficiency and demonstrated significant increase in donepezil in brain and plasma. | Al Harthi et al., 2019 | |
| α-Mangostin | DSPC and cholesterol, with transferrin conjugated to the PEG chains | IV administration of liposomes loaded with α-mangostin demonstrate neuroprotective affect in rats against Aβ-Oligomer toxicity. | Chen et al., 2010 |
| Methoxy-XO4 Brain permeable fluorescent probe | DPPC, cholesterol, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy (polyethylene glycol)-2000] (DSPE-mPEG-2000), and DSPE-PEG-3400-XO4 | A dual function Liposomes conjugated with Methoxy- X04 which targets Aβ Plaque administered IV in APP/PSEN1 transgenic mice. These particles cross blood brain barrier with high efficiency and binds selectively to Aβ plaques in labelling parenchymal and cerebral amyloid deposits | Tanifum et al., 2012 |
| Glutathione targeted pegylated liposomes | DMPC and egg-yolk phosphatidylcholine (EYPC) and PEG | An anti-amyloid single-domain antibody fragment (VHH-pa2H) was delivered using glutathione encapsulated liposomes to APPswe/PS1dE9 double transgenic mice. Significant increase in uptake of anti-amyloid antibody in the brain was shown | Rotman et al., 2015 |
| Resveratrol | Stearic acid based SLN poloxamer 188 coated | SLNs encapsulated Resveratrol coated with polaxmer were administered orally in Sprague-Dawley rats, increased oral bioavailability of resveratrol as compared to drug suspension | Pandita et al., 2014 |
DDAB: Dioctadecyl dimethyl ammonium bromide; DMPC: 1,2-dimyristoyl-sn-glycero-3-phosphocholine; DPPC: 1,2-dipalmitoyl-sn-glycero-3-phosphocholine; DPPC: dipalmitoyl phosphatidyl choline; DSPC: 1,2-distearoyl-sn-glycero-3-phosphocholine; DSPE: 1,2-distearoyl-sn-glycero-3-phosphoethanolamine; EPC: egg phosphatidylcholine; EYPC: egg-yolk phosphatidylcholine; HA: human astrocytes; HBMECs: human brain microvascular endothelial cells; NGF: nerve growth factor; PEG: poly ethylene glycol; PLGA: poly(lactic-co-glycolic acid); ROS: reactive oxygen species; SD rats: Sprague Dawley rats; SLN: solid lipid nanoparticles; SPC: soybean phosphatidylcholine.