PMID- 32548448
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20200928
IS  - 2470-1343 (Electronic)
IS  - 2470-1343 (Linking)
VI  - 5
IP  - 22
DP  - 2020 Jun 9
TI  - Electrostatic Interactions Enable Nanoparticle Delivery of the Flavonoid 
      Myricetin.
PG  - 12649-12659
LID - 10.1021/acsomega.9b04101 [doi]
AB  - Flavonoids are natural polyphenolic compounds with myriad biological activities 
      and potential as prophylactic and therapeutic agents. However, poor aqueous 
      solubility and low bioavailability have limited the clinical utility of 
      flavonoids, suggesting that drug delivery systems (DDSs) may improve their 
      clinical relevance. Therefore, loading of a representative flavonoid (i.e., 
      myricetin) into a diblock, polymeric nanoparticle carrier (NPC) DDS with a 
      cationic corona and hydrophobic core was investigated. Absorbance and 
      fluorescence spectroscopy results revealed association constants and standard 
      Gibbs free energy values that align with previously reported values (K (a) =  approximately 1-3 
      x 10(4) M(-1); DeltaG degrees  = -5.4 to -6.0 kcal mol(-1)), suggesting that NPCs load 
      myricetin via electrostatic interactions. The zeta potential and gel 
      electrophoresis analysis confirmed this loading mechanism and indicated that NPCs 
      improve myricetin solubility >25-fold compared to myricetin alone. Finally, the 
      dual-drug loading of NPCs was tested using a combination of myricetin and a 
      hydrophobic drug (i.e., farnesol). Electrostatic loading of NPCs with myricetin 
      at concentrations </=1.2 mM did not affect NPC core loading and release of 
      farnesol, thus demonstrating a novel formulation strategy for the 
      dual-drug-loaded NPC. These findings offer key insights into the NPC DDS design 
      that may enhance the clinical relevance of flavonoid-based therapeutic 
      approaches.
CI  - Copyright (c) 2020 American Chemical Society.
FAU - Sims, Kenneth R Jr
AU  - Sims KR Jr
AD  - Translational Biomedical Science, School of Medicine and Dentistry, University of 
      Rochester, Rochester, New York 14642, United States.
AD  - Department of Biomedical Engineering, University of Rochester, Rochester, New 
      York 14642, United States.
FAU - He, Brian
AU  - He B
AD  - Department of Statistics, University of Rochester, Rochester, New York 14642, 
      United States.
FAU - Koo, Hyun
AU  - Koo H
AD  - Department of Orthodontics, School of Dental Medicine, University of 
      Pennsylvania, Philadelphia, Pennsylvania 19104, United States.
AD  - Center for Innovation & Precision Dentistry, School of Dental Medicine, School of 
      Engineering and Applied Sciences, University of Pennsylvania, Philadelphia, 
      Pennsylvania 19104, United States.
FAU - Benoit, Danielle S W
AU  - Benoit DSW
AD  - Department of Biomedical Engineering, University of Rochester, Rochester, New 
      York 14642, United States.
AD  - Materials Science Program, University of Rochester, Rochester, New York 14642, 
      United States.
AD  - Department of Orthopaedics and Center for Musculoskeletal Research, School of 
      Medicine and Dentistry, University of Rochester, Rochester, New York 14642, 
      United States.
AD  - Center for Oral Biology, School of Medicine and Dentistry, University of 
      Rochester, Rochester, New York 14642, United States.
AD  - Department of Chemical Engineering, University of Rochester, Rochester, New York 
      14642, United States.
LA  - eng
PT  - Journal Article
DEP - 20200528
PL  - United States
TA  - ACS Omega
JT  - ACS omega
JID - 101691658
PMC - PMC7288370
COIS- The authors declare no competing financial interest.
EDAT- 2020/06/18 06:00
MHDA- 2020/06/18 06:01
PMCR- 2020/05/28
CRDT- 2020/06/18 06:00
PHST- 2019/12/02 00:00 [received]
PHST- 2020/05/15 00:00 [accepted]
PHST- 2020/06/18 06:00 [entrez]
PHST- 2020/06/18 06:00 [pubmed]
PHST- 2020/06/18 06:01 [medline]
PHST- 2020/05/28 00:00 [pmc-release]
AID - 10.1021/acsomega.9b04101 [doi]
PST - epublish
SO  - ACS Omega. 2020 May 28;5(22):12649-12659. doi: 10.1021/acsomega.9b04101. 
      eCollection 2020 Jun 9.