The self-assembly phenomenon of amphiphiles has attracted particular attention in recent years due to its wide range of applications. The formation of nanoassemblies able to solubilize sparingly water-soluble drugs was found to be a strategy to solve the problem of poor solubility of active pharmaceutical ingredients. Binary and ternary solid dispersions containing Biopharmaceutics Classification System (BCS) class II drug bicalutamide and either Poloxamer®188 or Poloxamer®407 as the surface active agents were obtained by either spray drying or solvent evaporation under reduced pressure. Both processes led to morphological changes and a reduction of particle size, as confirmed by scanning electron microscopy and laser diffraction measurements. The increase in powder wettability was confirmed by means of contact angle measurements. The effect of an alteration of the crystal structure was followed by powder X-ray diffractometry while thermal properties were determined using differential scanning calorimetry. Interestingly, bicalutamide exhibited a polymorph transition after spray drying with the poloxamer and polyvinylpyrrolidone (PVP), while the poloxamer underwent partial amorphization. Moreover, due to the surface activity of the carrier, the solid dispersions formed nanoaggregates in water, as confirmed using dynamic light scattering measurements. The aggregates measuring 200–300 nm in diameter were able to solubilize bicalutamide inside the hydrophobic inner parts. The self-assembly of binary systems was found to improve the amount of dissolved bicalutamide by 4- to 8-fold in comparison to untreated drug. The improvement in drug dissolution was correlated with the solubilization of poorly soluble molecules by macromolecules, as assessed using emission spectroscopy.
Recent developments in the fabrication of core-shell polymer nanocapsules, as well as their current and future applications, are reported here. Special attention is paid to the newly introduced surfactant-free fabrication method of aqueous dispersions of nanocapsules with hydrophobic liquid cores stabilized by amphiphilic copolymers. Various approaches to the efficient stabilization of such vehicles, tailoring their cores and shells for the fabrication of multifunctional, navigable nanocarriers and/or nanoreactors useful in various fields, are discussed. The emphasis is placed on biomedical applications of polymer nanocapsules, including the delivery of poorly soluble active compounds and contrast agents, as well as their use as theranostic platforms. Other methods of fabrication of polymer-based nanocapsules are briefly presented and compared in the context of their biomedical applications.
This paper reports the characterization of iron oxide magnetic nanoparticles obtained via the thermal decomposition of an organometallic precursor, which were then loaded into nanocapsules prepared via the emulsification process in the presence of an amphiphilic derivative of chitosan. The applied synthetic method led to the formation of a hydrophobic layer on the surface of nanoparticles that enabled their loading in the hydrophobic liquid inside of the polymer-based capsules. The average diameter of nanoparticles was determined to be equal to 15 nm, and they were thoroughly characterized using X-ray diffraction (XRD), magnetometry, and Mössbauer spectroscopy. A core–shell structure consisting of a wüstite core and maghemite-like shell was revealed, resulting in an exchange bias effect and a considerable magnetocrystalline anisotropy at low temperatures and a superparamagnetic behavior at room temperature. Importantly, superparamagnetic behavior was observed for the aqueous dispersion of the nanocapsules loaded with the superparamagnetic nanoparticles, and the dispersion was shown to be very stable (at least 48 weeks). The results were analyzed and discussed with respect to the potential future applications of these nanoparticles and nanocapsules based on biopolymers as platforms designed for the magnetically navigated transport of encapsulated hydrophobic substances.
1 December 2024 in Nanotechnology, Science and Applications
Introduction: Since the population of Europe is rapidly aging, the number of cases of neurodegenerative diseases sharply increases. One of the most significant limitations of current neurodegenerative disease treatment is the inefficient delivery of neuroprotective drugs to the affected part of the brain. One of the promising methods to improve the pharmacokinetic and pharmacodynamic properties of antioxidants is their encapsulation in nanocarriers. Materials and Methods: Encapsulation of carnosic acid into a chitosan-based nanoparticle system with ultrasound-assisted emulsification process was developed. The physicochemical properties (size, stability, concentration of nanoparticles) of obtained nanocapsules were analyzed. Also, the cytotoxicity and neuroprotective effect in SH-SY5Y cells exposed to toxic concentration of H2O2 of the obtained nanoparticles were evaluated in vitro. Results and Discussion: The capsules with diameters between 90 and 150 nm and long-term stability were obtained. Cytotoxicity tests of empty capsules indicate that observed toxic effects were concentration dependent and lower concentrations (dilution above 500×) can be considered as safe for tested cells. Our study also indicates that encapsulation of carnosic acid decreased the cytotoxicity of empty nanocapsules and can efficiently protect SH-SY5Y cells from factors causing cell destruction. In addition, the neuroprotective efficacy of carnosic acid loaded nanocapsules was also demonstrated in SH-SY5Y cells exposed to toxic concentration of H2O2. The designed nanoparticles appear to possess sufficient biocompatibility to deserve their further evaluation in in vivo models.