Polymeric micelles for drug delivery in oncology with an emphasis on siRNA conveyance

Marquet, Franck; Borchard, Gerrit

doi:10.1016/b978-0-323-89868-3.00014-8

Cited by 1 publication

(1 citation statement)

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“…With respect to polyplexes and/or micelleplexes, the most common stoichiometric determination is based on the N/P charge ratio or more precisely, on the ratio of positive charges of amino groups (N) to negative charges of phosphate groups (P) [ 8 ]. Usually, this ratio is greater than unity, which results in positive zeta-potential (ZP) values [ 9 ] that ensure a high loading capacity and an improved transfection capability. Although optimal complexation does not necessarily mean optimal transfection, complex stability remains a prerequisite to be observed through optimal loading at charge neutralization ratio.…”

Section: Introductionmentioning

confidence: 99%

Characterization of the Interaction of Polymeric Micelles with siRNA: A Combined Experimental and Molecular Dynamics Study

et al. 2022

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The simulation of large molecular systems remains a daunting challenge, which justifies the exploration of novel methodologies to keep computers as an ideal companion tool for everyday laboratory work. Whole micelles, bigger than 20 nm in size, formed by the self-assembly of hundreds of copolymers containing more than 50 repeating units, have until now rarely been simulated, due to a lack of computational power. Therefore, a flexible amphiphilic triblock copolymer (mPEG45-α-PLL10-PLA25) containing a total of 80 repeating units, has been emulated and synthesized to embody compactified nanoconstructs of over 900 assembled copolymers, sized between 80 and 100 nm, for siRNA complexing purposes. In this study, the tailored triblock copolymers containing a controlled number of amino groups, were used as a support model to address the binding behavior of STAT3-siRNA, in the formation of micelleplexes. Since increasingly complex drug delivery systems require an ever more optimized physicochemical characterization, a converging description has been implemented by a combination of experimentation and computational simulations. The computational data were advantageous in allowing for the assumption of an optimal N/P ratio favoring both conformational rigidifications of STAT3-siRNA with low competitive phenomena at the binding sites of the micellar carriers. These calculations were consistent with the experimental data showing that an N/P ratio of 1.5 resulted in a sufficient amount of complexed STAT3-siRNA with an electrical potential at the slipping plane of the nanopharmaceuticals, close to the charge neutralization.

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Section: Introductionmentioning

confidence: 99%