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Correlation between drug loading content and biological activity: the complexity demonstrated in paclitaxel-loaded glycopolymer micelle system.

Biomacromolecules 2019 Februrary 16
Drug delivery carriers are now widely established as they can increase the therapeutic efficiency of drugs. In general, the aim in this field is to create effective carriers that have large amounts of drugs loaded in order to minimize drug carrier material that needs to be disposed of. However, there was little attention so far in the literature on the effect of the amount of loaded drugs on the biological activity. In this paper, we are trying to answer the question how the drug loading content will affect the in vitro activity. Here, we use two methods to load paclitaxel (PTX) into micelles based on the glycopolymer, poly(1-O-methacryloyl-β-D-fructopyranose) -block-poly(methyl methacylate) (Poly(1-O-MAFru)35-b-PMMA145). In the one-step method, the drug is loaded into the particles during the self-assembly process. However, the size of nanoparticle increased with the PTX content from 26 nm to 50 nm triggering enhanced cellular uptake by MCF-7 and MDA-MB-231, which was caused by changes in diameter size and not by changes in drug concentration. To keep the nanoparticle size constant, preformed micelles were loaded with PTX (two-step process). The increasing amount of loaded drug led to decreased cellular uptake and reduced cytotoxicity by the cancer cell lines. Small angle neutron scattering (SANS) and small angle X-ray scattering (SAXS), supported by Transmission Electron Microscopy (TEM) and Dynamic light scattering (DLS) exposed the PTX location in the shell. This caused shrinkage of the shell and lower levels of shell hydration, resulting in the lower cellular uptake and lower cytotoxicity. Upon release of PTX, the shell regained its original level of hydration. We could show that since drug loading causes morphology changes, either in the shell or the size, it is impossible to separate the parameters that will influence the biological activity. Although the same phenomenon may not apply to every drug delivery system, it needs to be considered that except for the well-known parameters that affect cell uptake - size, shape, surface chemistry, type of nanoparticle and presence of bioactive groups - the amount of loaded drugs might change the physico-chemical parameters of the nanoparticle, thus the in vitro and potentially the in vivo outcomes.

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