Piperine-Loaded Glycyrrhizic Acid- and PLGA-Based Nanoparticles Modified with Transferrin for Antitumor
- 29 September 2021
- journal article
- research article
- Published by Springer Science and Business Media LLC in AAPS PharmSciTech
- Vol. 22 (7), 1-17
- https://doi.org/10.1208/s12249-021-02123-6
Abstract
The purpose of this study was to enhance the antitumor effect of piperine by constructing the nanoparticles modified with transferrin (Tf-PIP-NPs) and evaluating their efficacy in vitro and in vivo. The Tf-PIP-NPs were prepared by the solvent evaporation method, and their properties were characterized. The effects of Tf-PIP-NPs on cytotoxicity, cell uptake, apoptosis, and mitochondrial membrane potential were evaluated in HepG2 cells, MDA-MB-231 cells, and 4T1 cells. In a 4T1 tumor-bearing mouse model, the antitumor efficacy of Tf-PIP-NPs was assessed in terms of tumor volumes, changes in body weight, HE staining, and immunohistochemical analysis. With a mean particle size of 112.2 ± 1.27 nm, the zeta potential of (− 28.0 ± 1.6 mV) Tf-PIP-NPs were rapidly internalized by tumor cells after 1 h through the transferrin receptor (TfR)-mediated endocytosis pathway, significantly inducing cellular apoptosis and mitochondrial membrane potential loss. Although Tf-PIP-NPs had no significant difference with PIP-NPs in tumor volume inhibition due to the presence of tumor microenvironment, it could significantly upregulate the expression of related pro-apoptotic proteins and induce tumor necrosis. We used the self-assembly properties of glycyrrhizic acid (GL) and polymer-PLGA to encapsulate piperine and modified with the transferrin, which provided a promising approach to improve the antitumor efficacy for anticarcinogen.Keywords
This publication has 57 references indexed in Scilit:
- Piperine inhibits the growth and motility of triple-negative breast cancer cellsCancer Letters, 2015
- Nano-extrusion: A promising tool for continuous manufacturing of solid nano-formulationsInternational Journal of Pharmaceutics, 2014
- Non-Invasive In Vivo Imaging of Near Infrared-labeled Transferrin in Breast Cancer Cells and Tumors Using Fluorescence Lifetime FRETPLOS ONE, 2013
- Preparation of 10-hydroxycamptothecin-loaded glycyrrhizic acid-conjugated bovine serum albumin nanoparticles for hepatocellular carcinoma-targeted drug deliveryInternational Journal of Nanomedicine, 2013
- Piperine, a dietary phytochemical, inhibits angiogenesisThe Journal of Nutritional Biochemistry, 2013
- Aerosolized Antimicrobial Agents Based on Degradable Dextran Nanoparticles Loaded with Silver Carbene ComplexesMolecular Pharmaceutics, 2012
- The Effect of Nanoparticle Size, Shape, and Surface Chemistry on Biological SystemsAnnual Review of Biomedical Engineering, 2012
- Fas-mediated neutrophil apoptosis is accelerated by Bid, Bak, and Bax and inhibited by Bcl-2 and Mcl-1Proceedings of the National Academy of Sciences of the United States of America, 2011
- Black Pepper and its Pungent Principle-Piperine: A Review of Diverse Physiological EffectsCritical Reviews in Food Science and Nutrition, 2007
- How porosity and size affect the drug release mechanisms from PLGA-based microparticlesInternational Journal of Pharmaceutics, 2006