An Update on the Routes for the Delivery of Donepezil

Zhao, Ze Qiang; Chen, Bo Zhi; Zhang, Xiao Peng; Zheng, Hui; Guo, Xin Dong

doi:10.1021/acs.molpharmaceut.1c00290

Cited by 16 publications

(8 citation statements)

References 94 publications

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“…As shown in Figure A, the prepared MNs consisted of an array of 10 × 10 needles with a height of 600 μm, a base diameter of 350 μm, and a spacing of 800 μm between the needles, and the surface of the needles was smooth without drug crystals precipitated. The height of the needle body of 600 μm was much more than the thickness of the human skin stratum corneum (50–100 μm), which ensures the delivery of drugs through the stratum corneum to the subcutis . The stratified structure of the upper and lower parts could be seen with the aid of rhodamine B as a simulated drug.…”

Section: Resultsmentioning

confidence: 99%

“…The height of the needle body of 600 μm was much more than the thickness of the human skin stratum corneum (50−100 μm), which ensures the delivery of drugs through the stratum corneum to the subcutis. 38 The stratified structure of the upper and lower parts could be seen with the aid of rhodamine B as a simulated drug. In the SEM image, the demarcation line between the two parts could be observed more microscopically.…”

Section: Characterization Of Mnsmentioning

confidence: 99%

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Subcutaneous Implantable Microneedle System for the Treatment of Alzheimer’s Disease by Delivering Donepezil

Zhao

Liang

et al. 2022

Biomacromolecules

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To alleviate the dilemma of drug administration in Alzheimer’s disease (AD) patients, it is of great significance to develop a new drug delivery system. In this study, a subcutaneously implanted microneedle (MN) device with a swellable gelatin methacryloyl (GelMA) needle body and a dissolvable polyvinyl alcohol (PVA) backing layer was designed. The backing layer quickly dissolved once the MN was introduced into the subcutaneous, and the hydrogel needles were implanted in the subcutaneous to enable prolonged drug release. Compared with oral administration, the MN system offers the benefits of a high administration rate, a fast onset of effect, and a longer duration of action. By detecting the concentration of acetylcholine (ACH) and Aβ 1–42, it was found that MN administration exhibited a stronger therapeutic effect. The biological safety of the MN system was also assessed, and no obvious signs of hemolysis, cytotoxicity, and inflammatory reaction were observed. Together, these findings suggested that the MN system is a convenient, efficient, and safe method of delivering donepezil hydrochloride (DPH) and may provide AD patients with a novel medicine administration option.

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Section: Resultsmentioning

confidence: 99%

Section: Characterization Of Mnsmentioning

confidence: 99%

Subcutaneous Implantable Microneedle System for the Treatment of Alzheimer’s Disease by Delivering Donepezil

Zhao

Liang

et al. 2022

Biomacromolecules

Self Cite

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“…Other drugs used to treat AD such as acetylcholine esterase (AChE) inhibitors and N-methyl-D-aspartic acid (NMDA) receptor antagonists are not disease-modifying and address only its symptoms. 13 Examples of these include donepezil (4), 14 memantine (5), 15 galanthamine (6) 16 and rivastigmine (7) 17 (Figure 4).…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Evaluation of Catechol-Based Amyloid Beta Aggregation Inhibitors

Konno¹,

Teruya²

2023

HETEROCYCLES

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The use of small molecules to inhibit amyloid β aggregation is one approach under investigation to prevent the onset of Alzheimer's disease (AD). One such small molecule is curcumin, but its utility is limited by poor water solubility and hence poor bioavailability. In this review, we summarize the findings of structure-activity relationship studies of curcumin and diaryl γ-dihydropyrone, undertaken to improve their inhibitory effect and physical properties. The key findings are: phenolic hydroxy groups can be introduced at the 2 and 3,4-positions of phenol rings, the C7 spacer of curcumin is essential for good anti-amyloid β aggregation activity; and the catechol moiety is important for both anti-aggregation activity and water solubility. The combination of the C5 spacer unit and mono ketone of curcumin analogues is more effective for water solubility with high antiamyloid β aggregation activity. Diaryl γ-dihydropyrone with hydroxy groups on phenol rings as cyclocurcumin mimetics also showed anti-amyloid β aggregation activity and high water solubility. Analogues of berberine, a benzylisoquinoline alkaloid also of interest to treat central nervous system diseases, are also reviewed.Finally, we review efforts to develop fluorescent curcumin analogues for use as diagnostic agents.

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“…This route of administration bypasses the BBB and allows the passage of molecules along the olfactory and trigeminal nerves, which are in direct contact with the CNS [14,15]. The efficacy of this system for CNS targeting has recently been validated in clinical trials for cerebral insulin delivery [16] and is being evaluated for other drugs such as acetylcholinesterase inhibitors [17]. The main advantages of the intranasal route of administration are (i) its accessibility, (ii) non-invasiveness, and (iii) its very low metabolic activity compared to the gastrointestinal wall, leading to high bioavailability [14,15].…”

Section: Introductionmentioning

confidence: 99%

Intranasal Administration of Nanovectorized Docosahexaenoic Acid (DHA) Improves Cognitive Function in Two Complementary Mouse Models of Alzheimer’s Disease

et al. 2022

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Polyunsaturated fatty acids (PUFAs) are a class of fatty acids that are closely associated with the development and function of the brain. The most abundant PUFA is docosahexaenoic acid (DHA, 22:6 n-3). In humans, low plasmatic concentrations of DHA have been associated with impaired cognitive function, low hippocampal volumes, and increased amyloid deposition in the brain. Several studies have reported reduced brain DHA concentrations in Alzheimer’s disease (AD) patients’ brains. Although a number of epidemiological studies suggest that dietary DHA consumption may protect the elderly from developing cognitive impairment or dementia including AD, several review articles report an inconclusive association between omega-3 PUFAs intake and cognitive decline. The source of these inconsistencies might be because DHA is highly oxidizable and its accessibility to the brain is limited by the blood–brain barrier. Thus, there is a pressing need for new strategies to improve DHA brain supply. In the present study, we show for the first time that the intranasal administration of nanovectorized DHA reduces Tau phosphorylation and restores cognitive functions in two complementary murine models of AD. These results pave the way for the development of a new approach to target the brain with DHA for the prevention or treatment of this devastating disease.

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An Update on the Routes for the Delivery of Donepezil

Cited by 16 publications

References 94 publications

Subcutaneous Implantable Microneedle System for the Treatment of Alzheimer’s Disease by Delivering Donepezil

Subcutaneous Implantable Microneedle System for the Treatment of Alzheimer’s Disease by Delivering Donepezil

Design, Synthesis and Evaluation of Catechol-Based Amyloid Beta Aggregation Inhibitors

Intranasal Administration of Nanovectorized Docosahexaenoic Acid (DHA) Improves Cognitive Function in Two Complementary Mouse Models of Alzheimer’s Disease

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