Blog dedicated to answering technical questions in an open format relating to PolySciTech (A division of Akina, Inc.) products.
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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