Abstract
With the aim to effectively deliver methotrexate (MTX) to breast cancer cells, we designed a nanocarrier system (DC) derived from the self-assembly of a dextran-curcumin conjugate prepared via enzyme chemistry with immobilized laccase acting as a solid biocatalyst. Nanoparticles consisted of homogeneously dispersed nanospheres with a mean diameter of 290 nm, as characterized by combined transmission electron microscopy and dynamic light scattering investigations. DC was able to control the MTX release overtime (t1/2 value of 310 min), with cell internalization studies proving its presence inside MCF-7 cytoplasm. Finally, improved MTX efficacy was obtained in viability assays, and attributed to the synergy of curcumin moieties and loaded MTX as underlined by a combination index (CI) < 1.
Highlights
Cancer is still one of the leading causes of death worldwide, resulting in a continuous increase in the economic and financial burden for cancer treatment and research [1,2]
Among the wide number of approaches reported in the literature [14], the use of polymeric materials for the synthesis of either polyphenol delivery vehicles for or synthesis of either polyphenol delivery vehicles or bioconjugates, has been proved to be effective bioconjugates, hasand been proved to be effective for their stabilization[15]
designed a nanocarrier system (DC) nanoparticles were prepared by a two-steps procedure, namely (i) the synthesis of DEX-CUR
Summary
Cancer is still one of the leading causes of death worldwide, resulting in a continuous increase in the economic and financial burden for cancer treatment and research [1,2]. Surgery and chemotherapy remain the first line cancer treatments, with chemotherapeutic protocols often consisting in a combination of two or more bioactive agents, each used at lower dosage [3,4,5] The advantages of such approach is the possibility to simultaneously target different cellular pathways [6,7], increasing the therapeutic efficiency, reducing the toxic side effects, and hindering the insurgence of multi-drug resistance [8]. With the aim to improve the therapeutic performance, great efforts have been made in both the fabrication of targeted nanocarriers [9] and the exploration of alternative anticancer agents [10,11] To this regard, polyphenols have been shown to possess strong anticancer activity in vitro, they suffering from some pharmacokinetic drawbacks, e.g., inefficient systemic delivery, poor bioavailability, and high required dosage, significantly hindering their use in the clinic [12]. Among the wide number of approaches reported in the literature [14], the use of polymeric materials for the Pharmaceuticals 2020, 13, 2; doi:10.3390/ph13010002 www.mdpi.com/journal/pharmaceuticals
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