Control-Release Polyethylenimine-Modified Fibroin Nanoparticles As A Potential Vehicle for the Oral Delivery of Quercetin

Phuong T.M. Ha; Thanh Lich Nguyen; Ngoc Yen Nguyen; Nguyen Trong Tuan; Manh Quan Nguyen; Tran Thi Bich Quyen; Duy Toan Pham

doi:10.35516/jjps.v18i3.3082

Authors

Phuong T.M. Ha Department of Chemistry, Faculty of Pharmacy and Nursing, Tay Do University, 68 Tran Chien Street, Can Tho 900000, Vietnam
Thanh Lich Nguyen Department of Health Sciences, College of Natural Sciences, Can Tho University, Campus II, 3/2 Street, Can Tho 900000, Vietnam
Ngoc Yen Nguyen Department of Health Sciences, College of Natural Sciences, Can Tho University, Campus II, 3/2 Street, Can Tho 900000, Vietnam
Nguyen Trong Tuan Department of Health Sciences, College of Natural Sciences, Can Tho University, Campus II, 3/2 Street, Can Tho 900000, Vietnam
Manh Quan Nguyen Department of Analytical Chemistry-Drug Quality Control, Faculty of Pharmacy, Can Tho University of Medicine and Pharmacy, 179 Nguyen Van Cu Street, Can Tho 900000, Vietnam.
Tran Thi Bich Quyen Faculty of Chemical Engineering, College of Engineering, Can Tho University, Campus II, 3/2 Street, Can Tho 900000, Vietnam
Duy Toan Pham Can Tho University

DOI:

https://doi.org/10.35516/jjps.v18i3.3082

Keywords:

Fibroin, Polyethylenimine, Nanoparticles, Quercetin, Oral delivery

Abstract

Polyphenolic compounds are a big class of chemicals employed in numerous biomedical applications. However, these compounds are susceptible to degradations, especially in the varied gastrointestinal pH, which hinders their use in oral administrations. Thus, this work developed fibroin nanoparticles (FNP) and polyethylenimine-modified FNP (PEI-FNP) to orally protect and deliver quercetin (QC), a model polyphenol. The particles were formulated using two distinct methods: adsorption and co-condensation. Both formulas showed appropriate physicochemical properties for oral administrations, including nano-sizes (~700 nm for FNP-QC and ~200 nm for PEI-FNP-QC), narrow size distribution (polydispersity index < 0.3), adjustable zeta potentials (~-20 mV for FNP-QC and ~+25 mV for PEI-FNP-QC), enhanced QC aqueous solubility to 2-3 times, and observable chemical interactions (hydrogen bonding and ionic interactions) between QC and fibroin/PEI. Moreover, depending on the formulation process and particle compositions, the particles possessed moderate QC entrapment efficiency (35-75%), smooth/rough surfaces, and rapid drug adsorption followed models including Langmuir and Dubinin-Radushkevich isotherms, as well as pseudo-second-order kinetics. Interestingly, in the mimicked oral condition, the particles can protect QC from the gastric condition at pH 1.2, with less than 20% QC release, while sustaining its release in the intestine at pH 6.8, with the release rates that could be favorably controlled by varying the formulation methods and/or PEI functionalization. In summary, the FNP and PEI-FNP demonstrated much potential as release-controllable delivery systems for oral administrations of polyphenolic compounds.

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