Abstract
Doxorubicin (Dox) clinical use is limited by dose-related cardiomyopathy, becoming more prevalent with increasing cumulative doses. Previously, we developed Dox-loaded lipid-core nanocapsules (Dox-LNC) and, in this study, we hypothesized that self-assembling and interfacial reactions could be used to obtain arginylglycylaspartic acid (RGD)-surface-functionalized-Dox-LNC, which could target tumoral cells overexpressing αvβ3 integrin. Human breast adenocarcinoma cell line (MCF-7) and human glioblastoma astrocytoma (U87MG) expressing different levels of αvβ3 integrin were studied. RGD-functionalized Dox-LNC were prepared with Dox at 100 and 500 mg·mL−1 (RGD-MCMN (Dox100) and RGD-MCMN (Dox500)). Blank formulation (RGD-MCMN) had z-average diameter of 162 ± 6 nm, polydispersity index of 0.11 ± 0.04, zeta potential of +13.2 ± 1.9 mV and (6.2 ± 1.1) × 1011 particles mL−1, while RGD-MCMN (Dox100) and RGD-MCMN (Dox500) showed respectively 146 ± 20 and 215 ± 25 nm, 0.10 ± 0.01 and 0.09 ± 0.03, +13.8 ± 2.3 and +16.4 ± 1.5 mV and (6.9 ± 0.6) × 1011 and (6.1 ± 1.0) × 1011 particles mL−1. RGD complexation was 7.73 × 104 molecules per nanocapsule and Dox loading were 1.51 × 104 and 7.64 × 104 molecules per nanocapsule, respectively. RGD-functionalized nanocapsules had an improved uptake capacity by U87MG cells. Pareto chart showed that the cell viability was mainly affected by the Dox concentration and the period of treatment in both MCF-7 and U87MG. The influence of RGD-functionalization on cell viability was a determinant factor exclusively to U87MG.
Highlights
IntroductionSeveral nanoparticlebased drug delivery systems have obtained a great attention as promising approaches for tumor treatments [1,2,3,4]
Cancer is a major public health problem worldwide
Dox clinical use is limited by dose-related cardiomyopathy, which becomes more prevalent with increasing cumulative doses [7]
Summary
Several nanoparticlebased drug delivery systems have obtained a great attention as promising approaches for tumor treatments [1,2,3,4]. The use of nanotechnology in drug delivery systems opened new opportunities to Nanomaterials 2018, 8, 2; doi:10.3390/nano8010002 www.mdpi.com/journal/nanomaterials. Nanomaterials 2018, 8, 2 overcome limitations in therapeutics, such as low efficacy and high systemic toxicity of many drugs in clinical practice for cancer treatments [5]. Dox clinical use is limited by dose-related cardiomyopathy, which becomes more prevalent with increasing cumulative doses [7]. Poor penetration of antitumor drugs into the extravascular tumor tissue is often a major factor limiting the efficacy of treatments [8,9]
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