Paclitaxel-loaded sodium deoxycholate-stabilized zein nanoparticles: characterization and in vitro cytotoxicity

Abstract

Paclitaxel (PTX) is one of the most successful antineoplastic drugs and is widely used for the treatment of many forms of advanced and refractory cancer. Unfortunately, various drawbacks including non-selective cytotoxicity, poor water solubility and low bioavailability limit its clinical use. The aim of this study was to characterize a novel colloidal system made up of the natural protein zein, that would be able to efficiently retain the anticancer compound and increase its in vitro pharmacological effects. In fact, zein has promising characteristics that render it a potential material to be used in drug delivery application. The influences of temperature, pH and serum incubation on the stability of these particles, entrapment efficiency of PTX and in vitro toxicity on different cancer cell lines were evaluated. The nanosystems containing PTX demonstrated suitable storage stability, and were not destabilized by temperatures of up to 50 °C, pH alterations, the freeze-drying process or serum proteins. The encapsulation of PTX did not destabilize the structure of the zein nanoparticles and a suitable drug entrapment efficiency resulted. PTX-loaded zein nanoparticles showed an increased toxicity on different cancer cell lines with respect to the free drug, confirming its potential application in preclinical and clinical investigations.

Nanoparticles Loaded with the BET Inhibitor JQ1 Block the Growth of Triple Negative Breast Cancer Cells In Vitro and In Vivo

“…The entrapment efficiency (EE%) of JQ1 was evaluated according to the following equation: EE% = De/Da × 100, where De is the amount of entrapped JQ1 and Da is the amount of active compound used during the preparation of the colloidal formulations. The release profile of JQ1 from the polymeric systems was investigated by the dialysis method [45].…”

Antitumor Features of Vegetal Protein-Based Nanotherapeutics

“…0.3 mg/mL of the drug added during the preparation steps of zein nanoparticles were efficiently retained by the protein structure (40%), confirming the peculiar properties of the nanosystems to entrap hydrophobic drugs as a consequence of the favorable interaction that comes about between the active compounds and the biopolymer [113]. PTX was gradually released by the nanostructures (70% after 5 days) and its nanoencapsulation permitted an increase in its cytotoxicity on various human cancer cells, such as K562 and MCF-7, with respect to its free form solubilized in ethanol [113] (Figure 3). A specific approach for contrasting the drug resistance of tumors is the employment of a combination of two active compounds aiming at different targets in order to obtain a synergistic anticancer effect [118].…”

“…The possibility of avoiding the use of organic solvents to solubilize paclitaxel (PTX), such as Cremophor EL, is an important target of pharmaceutical technology because these cause the most important side effects in patients treated with the conventional formulations [111]; therefore, albumin-based nanoparticles have been developed [112]. Other biomaterials are under investigation in order to modulate the biopharmaceutical properties of PTX after its encapsulation, and zein may represent an innovative therapeutic option to be used for the treatment of various tumors [113].…”

“…SD-stabilized zein nanoparticles were obtained by the nanoprecipitation method and were used to entrap PTX [113], a lipophilic antitumor compound that acts by binding the tubulin beta-subunit and avoiding the normal microtubular breakdown [114]. 0.3 mg/mL of the drug added during the preparation steps of zein nanoparticles were efficiently retained by the protein structure (40%), confirming the peculiar properties of the nanosystems to entrap hydrophobic drugs as a consequence of the favorable interaction that comes about between the active compounds and the biopolymer [113]. PTX was gradually released by the nanostructures (70% after 5 days) and its nanoencapsulation permitted an increase in its cytotoxicity on various human cancer cells, such as K562 and MCF-7, with respect to its free form solubilized in ethanol [113] (Figure 3).…”

Development and In Vivo Evaluation of Multidrug Ultradeformable Vesicles for the Treatment of Skin Inflammation

“…The various measurements were carried out in triplicate on three different batches (10 determinations for each batch). Results were expressed as the mean of three different experiments ± standard deviation [23].…”