“…An exploration of the possible instability phenomena in the colloidal dispersion is presented in Figure 3. Phenomena such as flocculation, creaming, sedimentation, or coalescence induced by drug-loading or functionalization not were detected in this experiment [40,41]. There were no significant variations in either particle size or zeta potential over an interval of 6 weeks ( p > 0.05), which corroborated with the successful preparation of NPs able to improve the drug efficacy [42,43].…”
Cationic polymeric nanoparticles (NPs) have the ability to overcome biological membranes, leading to improved efficacy of anticancer drugs. The modulation of the particle-cell interaction is desired to control this effect and avoid toxicity to normal cells. In this study, we explored the surface functionalization of cationic polymethylmethacrylate (PMMA) NPs with two natural compounds, sialic acid (SA) and cholesterol (Chol). The performance of benznidazole (BNZ) was assessed in vitro in the normal renal cell line (HEK-293) and three human cancer cell lines, as follows: human colorectal cancer (HT-29), human cervical carcinoma (HeLa), and human hepatocyte carcinoma (HepG2). The structural properties and feasibility of NPs were evaluated and the changes induced by SA and Chol were determined by using multiple analytical approaches. Small (<200 nm) spherical NPs, with a narrow size distribution and high drug-loading efficiency were prepared by using a simple and reproducible emulsification solvent evaporation method. The drug interactions in the different self-assembled NPs were assessed by using Fourier transform-infrared spectroscopy. All formulations exhibited a slow drug-release profile and physical stability for more than 6 weeks. Both SA and Chol changed the kinetic properties of NPs and the anticancer efficacy. The feasibility and potential of SA/Chol-functionalized NPs has been demonstrated in vitro in the HEK-293, HepG2, HeLa, and HT-29 cell lines as a promising system for the delivery of BNZ.
“…An exploration of the possible instability phenomena in the colloidal dispersion is presented in Figure 3. Phenomena such as flocculation, creaming, sedimentation, or coalescence induced by drug-loading or functionalization not were detected in this experiment [40,41]. There were no significant variations in either particle size or zeta potential over an interval of 6 weeks ( p > 0.05), which corroborated with the successful preparation of NPs able to improve the drug efficacy [42,43].…”
Cationic polymeric nanoparticles (NPs) have the ability to overcome biological membranes, leading to improved efficacy of anticancer drugs. The modulation of the particle-cell interaction is desired to control this effect and avoid toxicity to normal cells. In this study, we explored the surface functionalization of cationic polymethylmethacrylate (PMMA) NPs with two natural compounds, sialic acid (SA) and cholesterol (Chol). The performance of benznidazole (BNZ) was assessed in vitro in the normal renal cell line (HEK-293) and three human cancer cell lines, as follows: human colorectal cancer (HT-29), human cervical carcinoma (HeLa), and human hepatocyte carcinoma (HepG2). The structural properties and feasibility of NPs were evaluated and the changes induced by SA and Chol were determined by using multiple analytical approaches. Small (<200 nm) spherical NPs, with a narrow size distribution and high drug-loading efficiency were prepared by using a simple and reproducible emulsification solvent evaporation method. The drug interactions in the different self-assembled NPs were assessed by using Fourier transform-infrared spectroscopy. All formulations exhibited a slow drug-release profile and physical stability for more than 6 weeks. Both SA and Chol changed the kinetic properties of NPs and the anticancer efficacy. The feasibility and potential of SA/Chol-functionalized NPs has been demonstrated in vitro in the HEK-293, HepG2, HeLa, and HT-29 cell lines as a promising system for the delivery of BNZ.
“…The reason for this is that the addition of salt confirmed the aggregation and dissociation of particles in the 2/1 and 1/2 suspensions, and that the zeta potential was maintained to some extent in the 1/1 suspension. It has been suggested that, owing to intermolecular interactions such as hydrogen bonding between DSPE-PEG2000 and Soluplus, an environment capable of holding a potential on the particle surface is created, and the resulting electrostatic repulsion force contributes to stabilization of the particles in the suspension [30,31]. Therefore, in order to investigate the intermolecular interaction in the suspension, we evaluated the particles with the use of TEM and 31 P-NMR.…”
The aim of this study was to evaluate the characterized hydration method to prepare nanoparticles using Soluplus, a block copolymer with amphipathic properties, and distearoyl phosphatidyl ethanolamine (DSPE)-PEG2000 owing to particle size distribution, zeta potential, particle stability, and transmission electron microscopy (TEM) observed and 31P-NMR spectra. The results showed that, in a suspension of DSPE-PEG2000 and Soluplus at a ratio of 1/1, the prepared microparticles were stable for five days in the dark and at 25 °C. It was also confirmed that the 1/1 suspension of DSPE-PEG2000/Soluplus was stable for five days under the same conditions with the magnesium chloride solution. TEM measurements confirmed the presence of micelle-like particles of 50 to 150 nm in the 1/1 ratio mix of DSPE-PEG2000/Soluplus. 31P-NMR spectral data confirmed that DPSE-PEG2000/Soluplus at mixing ratio of 1/1 has a strong intermolecular with the phosphate group, indicated by the fact that the peak shift and the full width at half maximum were the largest compared with DSPE-PEG2000 with the intermolecular interaction. On the basis of the findings of this study, we conclude that microparticles can be formed using DSPE-PEG2000 and Soluplus via the hydration method, and that the optimum weight ratio of DSPE-PEG2000 to Soluplus is 1/1.
“…Drug-PVP and Drug-PVP-SDS have been used to improve stability and dissolution properties of several hydrophobic drugs [22,23]. The combined use of a polymer and surfactant is known to contribute to enhanced rate of particle formation, and reduce the overall particle size by the sorption of a polymer-surfactant complex on the particle surface [24][25][26][27] drugs as they reduce surface tension and sterically inhibit waterinsoluble particles from aggregating. Studies with fluorometholone and indomethacin, poorly soluble ophthalmic active ingredients have shown that the surface tension could be decreased by using HPMC in suspensions.…”
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