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Azo-polysiloxane micelles charged with nifedipine

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EN
Abstract One recent aspect of the research study on polymers is their capability to respond to external stimuli. Of importance are photosensitive polymers due to their application in drug delivery systems, sensors, therapeutic devices or optoelectronic switches. The present paper focuses on the azo-polysiloxane micelles capacity charged with hydrophobic drugs, such as nifedipine. Azo-polysiloxanes modified with quaternary ammonium groups and which are capable to generate photo-sensitive micelles were synthesized and characterized by 1H-NMR, UV-VIS and fluorescence spectroscopy. The critical concentration of the micellar aggregation (CCA) was evaluated as was the nifedipine embedding capacity. The CCA values were influenced only by the hydrophobic/hydrophilic balance and not by the chemical structure of the quaternary ammonium groups. The disaggregation capacity of the micelles under UV irradiation was investigated as well, and the best results were obtained for the samples with higher azobenzene content. The DLS measurements evidenced micelles diameters situated in the optimum range domain (70–130 nm). The capacity to incorporate nifedipine inside the micelles was demonstrated. The micelles proved to be stable in time, 21 days after preparation with the diameter having constant values. Graphical abstract [...]
EN
Amphiphilic macromolecular micelles are advantageous for drug delivery applications due to the decrease of side-effects, ease of screening drugs against degradation, long-term stability, targeted delivery and control of the amount of the released drug. A series of amphiphilic azo-polymers having a flexible or rigid main-chain were synthesized and characterized. The presence of chlorobenzyl side-groups allowed both the easy bonding of photo-sensitive or hydrophilic groups and good control of the degree of substitution. The chemical structure was confirmed by 1H-NMR. The critical concentration of aggregation (CCA) was calculated using the fluorescence emission spectrum of pyrene. The interest was focused on a preliminary study concerning the disaggregation capacity of micelles under UV irradiation. The presence of micellar aggregates was confirmed by DLS and SEM and different organization of the amphiphilic polymers was evidenced depending on polymers concentration and polymers structure. In low polymer concentrations in water predominantly globular aggregates were formed. The increase in concentration increased the polydispersity index due to the fusion of micelles and formation of associates of globular aggregates, inter-micellar associates (clusters) and vesicles. [...]
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