Tier 3 — preclinical

Preparation and optimization of poly (lactic acid) nanoparticles loaded with fisetin to improve anti-cancer therapy

Feng C, Yuan X, Chu K, Zhang H, Ji W, Rui M
International Journal of Biological Macromolecules 2019 125:700-10

Bibliography

PubMed
PMID 30521927
DOI
10.1016/j.ijbiomac.2018.12.003
Funding
Not stated in the reviewed abstract/metadata; conducted at the Department of Pharmaceutics, School of Pharmacy, Jiangsu University, Zhenjiang, China.
Competing interests
Not stated in the reviewed abstract/metadata.

Study snapshot

DesignFormulation and two-stage experimental optimisation (one-factor-at-a-time followed by a Taguchi orthogonal array design) of fisetin-loaded poly(lactic acid) (PLA) nanoparticles prepared by spontaneous emulsification solvent diffusion, followed by in vitro cytotoxicity testing in HCT116 colon cancer cells and in vivo antitumour efficacy testing in a 4T1 breast cancer xenograft mouse model, compared against free fisetin solution.
ModelHCT116 human colon cancer cells (in vitro) and BALB/c mice bearing 4T1 breast cancer xenografts (in vivo).
SampleStandard cell-culture replicate and mouse xenograft cohort sizes; exact n not stated in the reviewed abstract/metadata.
InterventionFisetin-loaded PLA nanoparticles (optimised formulation, approximately 227 nm particle size, 90.35% encapsulation efficiency) versus free fisetin solution, tested for cytotoxicity in HCT116 cells and antitumour efficacy in 4T1 xenograft mice.
DurationNot stated in the reviewed abstract/metadata.
EndpointsNanoparticle particle size, encapsulation efficiency and drug release (formulation optimisation); In vitro cytotoxicity in HCT116 colon cancer cells; In vivo antitumour efficacy in a 4T1 breast cancer xenograft model

What the study showed, in plain terms

Fisetin's anticancer promise is limited in practice because it barely dissolves in water, so researchers looked for a nanoparticle carrier that could get more of it where it needs to go.

A team in China packaged fisetin into poly(lactic acid) — a biodegradable polymer already used in medical devices — nanoparticles, fine-tuning the recipe over two rounds of experiments until they reached a small, stable particle that held onto about 90% of its fisetin payload.

Tested against colon cancer cells in a dish and in mice carrying breast cancer tumours, the nanoparticle-packaged fisetin was more effective at killing cancer cells and shrinking tumours than the same dose of plain fisetin.

Bottom line: another formulation-science result showing that a nanoparticle carrier can improve fisetin's anticancer performance compared with the unformulated compound — relevant background for why fisetin supplements use specialised delivery formats, though this study measured anticancer efficacy directly rather than oral bioavailability.

Key findings

Fisetin encapsulated in optimised poly(lactic acid) nanoparticles (about 227 nm, 90.35% encapsulation efficiency) showed greater cytotoxicity against HCT116 colon cancer cells and stronger antitumour activity in a 4T1 breast cancer xenograft mouse model than free fisetin solution at the same dose.

What this study can and cannot tell us

Preclinical only — HCT116 cell-line and mouse xenograft data, no human pharmacokinetic or clinical outcome data. The study measured anticancer efficacy directly rather than oral bioavailability or plasma concentration, so it doesn't by itself establish an absorption improvement the way a pharmacokinetic study would.

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Dr. Khaled Mahmoud, MBBChCritical Care Medicine, Longevity Science & Editorial Direction Dr. Amr Yasser, PhDCardiometabolic, Musculoskeletal, Gut & Bioavailability Dr. Abdulla Mostafa, PhDCellular Senescence, Neurological, Mitochondrial & Brain-Ageing Biology