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Article

PLGA Microspheres with Alginate-Coated Large Pores for the Formulation of an Injectable Depot of Donepezil Hydrochloride

College of Pharmacy, Chung-Ang University, Seoul 06974, Korea
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2020, 12(4), 311; https://doi.org/10.3390/pharmaceutics12040311
Received: 12 March 2020 / Revised: 27 March 2020 / Accepted: 30 March 2020 / Published: 1 April 2020
As the main symptom of Alzheimer’s disease-related dementia is memory loss, patient compliance for donepezil hydrochloride (donepezil), administered as once-daily oral formulations, is poor. Thus, we aimed to design poly(lactic-co-glycolic acid) (PLGA) microspheres (MS) with alginate-coated large pores as an injectable depot of donepezil exhibiting sustained release over 2–3 weeks. The PLGA MS with large pores could provide large space for loading drugs with high loading capacity, and thereby sufficient amounts of drugs were considered to be delivered with minimal use of PLGA MS being injected. However, initial burst release of donepezil from the porous PLGA MS was observed. To reduce this initial burst release, the surface pores were closed with calcium alginate coating using a spray-ionotropic gelation method. The final pore-closed PLGA MS showed in vitro sustained release for approximately 3 weeks, and the initial burst release was remarkably decreased by the calcium alginate coating. In the prediction of plasma drug concentration profiles using convolution method, the mean residence time of the pore-closed PLGA MS was 2.7-fold longer than that of the porous PLGA MS. Therefore, our results reveal that our pore-closed PLGA MS formulation is a promising candidate for the treatment of dementia with high patient compliance. View Full-Text
Keywords: donepezil depot; sustained release; porous microsphere; pore size; porosity; drug loading; burst release; pore closing; convolution donepezil depot; sustained release; porous microsphere; pore size; porosity; drug loading; burst release; pore closing; convolution
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MDPI and ACS Style

Kim, D.; Han, T.H.; Hong, S.-C.; Park, S.J.; Lee, Y.H.; Kim, H.; Park, M.; Lee, J. PLGA Microspheres with Alginate-Coated Large Pores for the Formulation of an Injectable Depot of Donepezil Hydrochloride. Pharmaceutics 2020, 12, 311. https://doi.org/10.3390/pharmaceutics12040311

AMA Style

Kim D, Han TH, Hong S-C, Park SJ, Lee YH, Kim H, Park M, Lee J. PLGA Microspheres with Alginate-Coated Large Pores for the Formulation of an Injectable Depot of Donepezil Hydrochloride. Pharmaceutics. 2020; 12(4):311. https://doi.org/10.3390/pharmaceutics12040311

Chicago/Turabian Style

Kim, Dohyun, Tae H. Han, Seong-Chul Hong, Sun J. Park, Yong H. Lee, Hyeongmin Kim, Minwoo Park, and Jaehwi Lee. 2020. "PLGA Microspheres with Alginate-Coated Large Pores for the Formulation of an Injectable Depot of Donepezil Hydrochloride" Pharmaceutics 12, no. 4: 311. https://doi.org/10.3390/pharmaceutics12040311

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