Journal
NANOMEDICINE
Volume 12, Issue 21, Pages 2581-2596Publisher
FUTURE MEDICINE LTD
DOI: 10.2217/nnm-2017-0219
Keywords
antiproliferative effect; benzazulene; carboxylated lignin nanoparticles; drug loading; pH-responsive release; targeting functionalization
Funding
- Fundacao para a Ciencia e a Technologia-Ministerio da Ciencia, Tecnologia e Ensino Superior (FCT-MCTES), Portugal [UTAP-ICDT/DTP-FTO/0016/2014, SAICTPAC/0019/2015, UID/DTP/04138/2013]
- Academy of Finland [108376]
- University of Helsinki Research Funds
- Sigrid Juselius Foundation [4704580]
- European Research Council under the European Union's Seventh Framework Programme (FP) [310892]
- Fundação para a Ciência e a Tecnologia [UTAP-ICDT/DTP-FTO/0016/2014] Funding Source: FCT
- Academy of Finland (AKA) [108376, 108376] Funding Source: Academy of Finland (AKA)
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Aim: To carboxylate kraft lignin toward the functionalization of carboxylated lignin nanoparticles (CLNPs) with a block copolymer made of PEG, poly(histidine) and a cell-penetrating peptide and then evaluate the chemotherapeutic potential of the innovative nanoparticles. Materials & methods: The produced nanoparticles were characterized and evaluated in vitro for stability and biocompatibility and the drug release profiles and antiproliferative effect were also assessed. Results: The prepared CLNPs showed spherical shape and good size distribution, good stability in physiological media and low cytotoxicity in all the tested cell lines. A poorly water-soluble cytotoxic agent was successfully loaded into the CLNPs, improving its release profiles in a pH-sensitive manner and showing an enhanced antiproliferative effect in the different cancer cells compared with a normal endothelial cell line. Conclusion: The resulting CLNPs are promising candidates for anticancer therapy.
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