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http://dx.doi.org/10.1111/j.1532-5415.2012.04182.xDOI Listing

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Article Synopsis
  • Alzheimer's disease leads to cognitive decline and increased care needs; Rivastigmine (RV) is a key treatment limited by the blood-brain barrier (BBB).
  • A new method using polymeric microneedles (PMN) and a solid lipid nanoparticle-RV-loaded thermosensitive gel (PMN-SLN-RV-TG) shows potential for better brain delivery compared to traditional methods.
  • The study found that PMN-SLN-RV-TG has improved penetration and pharmacokinetic parameters, yielding a higher brain-to-blood ratio and demonstrating safety for brain tissue, indicating a promising alternative for Alzheimer's treatment.
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Naphthyl-functionalized acetamide derivatives: Promising agents for cholinesterase inhibition and antioxidant therapy in Alzheimer's disease.

Bioorg Chem

December 2024

Departamento de Química Orgánica, Facultad de Ciencias Químicas, Universidad de Concepción, Concepción 4130000, Chile. Electronic address:

This study presents the synthesis and characterization of a series of 13 novel acetamides. These were subjected to Ellman's assay to determine the efficacy of the AChE and BChE inhibitors. Finally, we report their antioxidant activity as an alternative approach for the search for drugs to treat AD.

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Background And Objectives: Rivastigmine is a reversible cholinesterase inhibitor indicated for the treatment of all stages of Alzheimer's disease (AD). Transdermal patch formulation allows smooth and continuous drug delivery. Its tolerability, efficacy and convenience of use increase treatment compliance.

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The aim of the present study was to develop a topical liposomal formulation as a transdermal delivery of rivastigmine for the treatment of Alzheimer's disease as an alternative to the oral dosage form and to achieve smooth continuous drug delivery and maintain plasma levels within the therapeutic window. Rivastigmine-loaded liposomes were prepared by a thin layer hydration technique that was applied in - correlation study. Permeability parameters through rat skin in study and pharmacokinetic parameters in the study were evaluated.

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Prediction of Human Pharmacokinetic Profile After Transdermal Drug Application Using Excised Human Skin.

J Pharm Sci

September 2017

Drug Metabolism and Pharmacokinetics Research Laboratories, Takeda Pharmaceutical Company Ltd., 26-1, Muraoka-Higashi 2-chome, Fujisawa, Kanagawa, Japan.

Although several mathematical models have been reported for the estimation of human plasma concentration profiles of drug substances after dermal application, the successful cases that can predict human pharmacokinetic profiles are limited. Therefore, the aim of this study is to investigate the prediction of human plasma concentrations after dermal application using in vitro permeation parameters obtained from excised human skin. The in vitro skin permeability of 7 marketed drug products was evaluated.

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