Abstract:Forward osmosis (FO) process has been extensively considered as a potential technology that could minimize the problems of traditional water desalination processes. Finding an appropriate osmotic agent is an important concern in the FO process. For the first time, a nonionic surfactant-based draw solution was introduced using self-assemblies of Tween 80 and choline chloride. The addition of choline chloride to Tween 80 led to micelles formation with an average diameter of 11.03 nm. The 1H NMR spectra exhibited… Show more
“…Considering that , where is the concentration of polysorbate 80, is the CMC value of polysorbate 80, is its aggregation number (experimentally reported values ranging between 22–350 [ 47 ]), and ( value is about 0.0014% w / w [ 48 ]), then Equations (3) and (4) can be combined: …”
This report presents a nanoparticulate platform for cannabidiol (CBD) for topical treatment of inflammatory conditions. We have previously shown that stabilizing lipids improve the encapsulation of CBD in ethyl cellulose nanoparticles. In this study, we examined CBD release, skin permeation, and the capability of lipid-stabilized nanoparticles (LSNs) to suppress the release of IL-6 and IL-8. The nanoparticles were stabilized with cetyl alcohol (CA), stearic acid (SA), lauric acid (LA), and an SA/LA eutectic combination (SALA). LSN size and concentration were measured and characterized by differential scanning calorimetry (DSC), in vitro release of loaded CBD, and skin permeability. IL-6 and IL-8 secretions from TNF-α-induced HaCaT cells were monitored following different LSN treatments. CBD released from the LSNs in dispersion at increasing concentrations of polysorbate 80 showed non-linear solubilization, which was explained by recurrent precipitation. A significant high release of CBD in a cell culture medium was shown from SALA-stabilized nanoparticles. Skin permeation was >30% lower from SA-stabilized nanoparticles compared to the other LSNs. Investigation of the CBD-loaded LSNs’ effect on the release of IL-6 and IL-8 from TNF-α-induced HaCaT cells showed that nanoparticles stabilized with CA, LA, or SALA were similarly effective in suppressing cytokine release. The applicability of the CBD-loaded LSNs to treat topical inflammatory conditions has been supported by their dermal permeation and release inhibition of pro-inflammatory cytokines.
“…Considering that , where is the concentration of polysorbate 80, is the CMC value of polysorbate 80, is its aggregation number (experimentally reported values ranging between 22–350 [ 47 ]), and ( value is about 0.0014% w / w [ 48 ]), then Equations (3) and (4) can be combined: …”
This report presents a nanoparticulate platform for cannabidiol (CBD) for topical treatment of inflammatory conditions. We have previously shown that stabilizing lipids improve the encapsulation of CBD in ethyl cellulose nanoparticles. In this study, we examined CBD release, skin permeation, and the capability of lipid-stabilized nanoparticles (LSNs) to suppress the release of IL-6 and IL-8. The nanoparticles were stabilized with cetyl alcohol (CA), stearic acid (SA), lauric acid (LA), and an SA/LA eutectic combination (SALA). LSN size and concentration were measured and characterized by differential scanning calorimetry (DSC), in vitro release of loaded CBD, and skin permeability. IL-6 and IL-8 secretions from TNF-α-induced HaCaT cells were monitored following different LSN treatments. CBD released from the LSNs in dispersion at increasing concentrations of polysorbate 80 showed non-linear solubilization, which was explained by recurrent precipitation. A significant high release of CBD in a cell culture medium was shown from SALA-stabilized nanoparticles. Skin permeation was >30% lower from SA-stabilized nanoparticles compared to the other LSNs. Investigation of the CBD-loaded LSNs’ effect on the release of IL-6 and IL-8 from TNF-α-induced HaCaT cells showed that nanoparticles stabilized with CA, LA, or SALA were similarly effective in suppressing cytokine release. The applicability of the CBD-loaded LSNs to treat topical inflammatory conditions has been supported by their dermal permeation and release inhibition of pro-inflammatory cytokines.
“…6,7 On the other hand, surfactants are widely used to stabilize emulsions due to their capacity to reduce the water/oil interfacial tension. 8 Specifically, polysorbate 80 (Tween-80) is a nonionic surfactant with several applications: bioremediation of soils, 9,10 water desalinization, 11 nanoparticles stabilization with antibacterial purposes, 12 and hydrate formation. 13 Even so, the molecular structure of this surfactant is not univocal since ethylene oxide (EO) groups are randomly distributed in the multiple sites available for ethoxylation during its synthesis.…”
Surfactants are used in many fields of the chemical industry in a wide range of applications. Generally, surfactants on water/oil interfaces reduce interfacial tension, enabling the formation of emulsions or providing greater stability to the emulsion formed. Although molecular dynamics has been extensively used and has achieved remarkable success in describing thermodynamic and molecular properties of systems with surfaceactive compounds, the traditional molecular simulation force fields considerably constrain the system size and the time scale of simulations. Here, we propose a coarse-grained model of polysorbate 80, a nonionic surfactant commercially known as Tween-80. Based on the proposed coarse-grained model, we evaluate the influence of the more internal ethylene oxide chain on the properties of the water/Tween-80/decane system. We verify with the simulation results that the model can reproduce the expected decrease in interfacial tension as the surfactant quantity increases in the simulations. Furthermore, we observe changes in the surfactant orientation as their quantity in the interface increases, indicating a preferential orientation for these molecules in the adsorption layer. We also assessed the partition coefficient of the surfactant between the two bulk phases by performing free energy calculations, which showed a higher affinity of Tween-80 surfactants with the water phase.
“…P80 was added to phosphate-buffered saline to provide sufficient MTK water solubility by incorporating the hydrophobic compound into the micelle structure above the critical micelle concentration. 62 The equilibrated MTK solubility in 1 w/v% P80 phosphate-buffered saline was determined to 218 μg/mL (data not shown), which is adequate solubility to provide sink condition. Figure 5 In vitro dissolution profile of MTK from 200NS, 500NS, and 3MS under sink conditions.…”
Background: Montelukast (MTK), a representative leukotriene receptor antagonist, is currently being investigated as a potential candidate for treating Alzheimer's disease. For potent and effective dosing in elderly patients, a parenteral prolonged delivery system is favored, with improved medication adherence with reduced dosage frequency. Purpose: This study aimed to design a nanocrystalline suspension (NS)-based MTK prolonged delivery system and evaluate its pharmacokinetics profile and local tolerability following subcutaneous administration. Methods: To decelerate the dissolution rate, the amorphous MTK raw material was transformed into a crystalline state using a solvent-mediated transformation method and subsequently formulated into NS using a bead-milling technique. The MTK NSs were characterized by morphology, particle size, crystallinity, and in vitro dissolution profiles. The pharmacokinetic profile and local tolerability at the injection site following subcutaneous injection of MTK suspension were evaluated in rats. Results: Microscopic and physical characterization revealed that the amorphous MTK powder was lucratively transformed into a crystalline form in acidic media (pH 4). MTK crystalline suspensions with different diameters (200 nm, 500 nm, and 3 μm) were uniformly prepared using bead-milling technology, employing polysorbate 80 as suspending agent. Prepared crystalline suspensions exhibited analogous crystallinity (melting point, 150°C) and size-dependent in vitro dissolution profiles. MTK NSs with particle sizes of 200 nm and 500 nm provided a protracted pharmacokinetic profile for up to 4 weeks in rats, with a higher maximum drug concentration in plasma than the 3 μm-sized injectable suspensions. Histopathological examination revealed that MTK NS caused chronic granulomatous inflammation at the injection site, which resolved after 4 weeks.
Conclusion:The MTK parenteral NS delivery system is expected to be a valuable tool for treating Alzheimer's disease with extended dose intervals.
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