Ellagic acid-loaded, tween 80-coated, chitosan nanoparticles as a promising therapeutic approach against breast cancer: In-vitro and in-vivo study

Aims

Among polyphenolic phytoconstituents with anticancer properties, Ellagic acid (EA) is widely reported for its translational potential in vitro but efficient in vivo delivery of EA has been a challenge. We, for the first time, used a tween 80 coated nano delivery of Ellagic acid to evaluate its preclinical efficacy in vitro and in vivo for breast cancer.

Highlights

We developed chitosan polymer nanoformulations of Ellagic acid (EA) with/without Tween 80 coating to increase in vivo efficacy

Tween 80 coated & uncoated EA nanoformulations shown higher cytotoxicity in MCF-7 and biocompatibility in Normal HEK293T cells

EAC tumor bearing mice: Higher efficacy by nanoformulations than EA without significant toxicity in vital organs

Tween 80 coating didn’t change particle size but shown better efficacy

Chitosan-EA synergistic efficacy interpreted with in silico simulation study

Main methods

To overcome the challenges of in vivo delivery, two batches of chitosan-based nanoformulations of EA (with and without tween 80 coating) were prepared by the ionotropic gelation method. The nanoformulations were characterized and further evaluated in vitro against breast cancer cells (MCF7) and in vivo with EAC tumor-bearing mice for establishing their anticancer efficacy compared to Ellagic acid alone. A quantitative simulation study was undertaken to understand if the observed antitumor efficacy is due to the synergistic efficacy of the Chitosan-Ellagic acid combination.

Key findings

Results revealed that nanoformulations consist of good nano-sized encapsulation of EA and showed good drug entrapment-release capacity. Nano-encapsulated EA is biocompatible and exhibited higher cytotoxicity in vitro compared to EA alone. Similarly, significantly higher tumor regression was observed in nano-EA treated mice compared to EA alone, and best efficacy was observed with the nanoformulation with tween 80 coating. Furthermore, nanoformulations showed higher apoptosis in tumor tissues with no significant tissue toxicity in vital organs.

Significance

We report synergism of Chitosan-Ellagic acid combination in the tween 80 coated nanoparticles of Ellagic acid resulting in enhanced anti-breast tumor efficacy that may be of translational value for other tumor types, too.

Read the article here

Article information: Harsheen Kaur, Sandip Ghosh, Pradeep Kumar, Biswarup Basu, Kalpana Nagpal, Ellagic acid-loaded, tween 80-coated, chitosan nanoparticles as a promising therapeutic approach against breast cancer: In-vitro and in-vivo study, Life Sciences, Volume 284, 2021. https://doi.org/10.1016/j.lfs.2021.119927.