Monday, April 13, 2020

PLGA from PolySciTech used in development of donepezil-delivery system as treatment for Alzheimer’s disease


Donepezil is a drug often prescribed for treatment of Alzheimer’s disease however its oral administration in pill form is complicated by its gastric-irritation side effects and lack of patient compliance. For these reasons, a long-acting formulation would be preferable. Recently, researchers at Kangwon National University, Seoul National University (Korea), and UCLA used PLGA (AP059) as a donepezil-entrapment particle to be loaded into HA-Fe based hydrogel to provide for a long-lasting drug delivery system. This research holds promise to provide for improved therapies against Alzheimer’s disease. Read more: Lee, Song Yi, Ju-Hwan Park, Mingyu Yang, Min-Jun Baek, Min-Hwan Kim, Junmin Lee, Ali Khademhosseini, Dae-Duk Kim, and Hyun-Jong Cho. "Ferrous sulfate-directed dual-cross-linked hyaluronic acid hydrogels with long-term delivery of donepezil." International Journal of Pharmaceutics (2020): 119309. https://www.sciencedirect.com/science/article/pii/S0378517320302933

“Abstract: Ferrous sulfate (FeSO4)-directed dual-cross-linked hydrogels were designed for application in single-syringe injections. The use of FeSO4, rather than other iron salts, can modulate the gelation time and make it available for subcutaneous injection with a single syringe. These hydrogels are based on hyaluronic acid–dopamine (HA-dp) that contain donepezil (DPZ)-entrapping poly(lactic-co-glycolic acid) (PLGA) microsphere (MS). Although DPZ has been administered orally, its sustained release formulation via subcutaneous injection may reduce the dosing frequency for patients with Alzheimer’s disease. The HA-dp conjugate was synthesized via an amide bond reaction for coordination of dp with a metal ion (Fe2+ or Fe3+) and self-polymerization of dp. The HA-dp/DPZ-loaded PLGA MS (PD MS)/FeSO4 gel system was considerably hardened via both the coordination of the metal ion with HA-dp and covalent bonding of dp. In addition, a quick restoration of the collapsed gel structure and sustained DPZ release from the HA-dp/PD MS/FeSO4 structure were achieved. The pharmacokinetic parameters after its subcutaneous injection in a rat indicate the sustained release and absorption of DPZ from the HA-dp/PD MS/FeSO4 system. The proposed system can be prepared by a simple method and can be efficiently and safely used for the long-term delivery of DPZ after the subcutaneous injection.”

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