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. 2019 Aug 23;11(9):431. doi: 10.3390/pharmaceutics11090431

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© 2019 by the authors.

Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).

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Impact of cholesterol on biological efficacy of proteolipid-coated nanogels. Evaluation of (a) cellular uptake and (c) gene silencing potential in H1299_eGFP cells of siRNA-loaded nanogels (siNGs) coated with lipid mixtures containing physiological cholesterol (CHOL) levels (2.5, 5 to 10 wt%). Data show one representative (technical triplicate) of two independent experiments; formulations with different siRNA concentrations showed the same trend (data not shown). Evaluation of (b) cellular uptake and (d) gene silencing potential of siNGs coated with increased cholesterol fraction in the outer layer (~25 wt%) (n = 3). Cholesterol exceeding physiological levels partially hinder SP-B promoted siRNA delivery. All experiments were performed with a fixed NG concentration (30 µg/mL) and siRNA concentration (50 nM). LIP = DOPC:PG (85:15); LIP SP-B = DOPC:PG (85:15) + SP-B 0.4 wt%; LIP SP-B CHOL = DOPC:CHOL:PG (60:25:15) + SP-B 0.4 wt%. Data are represented as the mean ± SD and statistical significance is indicated (* p < 0.05, ** p < 0.01, *** p < 0.005, **** p < 0.0001, ns = not significant).