NeuralCipher Research overview
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Entacapone is a catechol-O-methyltransferase (COMT) inhibitor, widely used for the symptomatic treatment of Parkinson's disease. However, it presents setbacks associated with a short half-life and a poor blood-brain barrier permeability. In order to surpass these limitations, entacapone was encapsulated in lipid-polymer hybrid nanoparticles (LPHNPs) functionalized with vitamin E (TPGS), using different liquid lipids as olive oil and coconut oil, and the co-surfactant and penetration enhancer Transcutol® HP. Depending on the system chosen, the nanoformulations presented differences in the hydrodynamic sizes (DDLS) after synthesis, and an increasing particle size in the following order: Transcutol® HP 80% after acute exposure to the nanoformulations in concentrations up to 40 μM in both wild-type (N2) and parkinson's disease model (WLZ3) strain, and antioxidant activity for HTT@Ent (40 μM) formulation in wlz3 strain. Overall, this work shows that the encapsulation of entacapone could be an interesting alternative in solving the drug performance by improving its physicochemical properties and permeability.
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