Considering a growing demand for medicinal/cosmetic products with natural actives, this study focuses on the low-energy nanoemulsions (LE-NEs) prepared via the Phase inversion composition (PIC) method at room temperature as potential carriers for natural oil. Four different red raspberry seed oils (ROs) were tested, as follows: cold-pressed vs. CO 2extracted, organic vs. non-organic, refined vs. unrefined. The oil phase was optimized with Tocopheryl acetate and Isostearyl isostearate, while water phase was adjusted with either glycerol or an antioxidant hydro-glycolic extract. This study has used a combined approach to formulation development, employing both conventional methods (pseudo-ternary phase diagram − PTPD, electrical conductivity, particle size measurements, microscopical analysis, and rheological measurements) and the methods novel to this area, such as textural analysis and Raman spectroscopy. Raman spectroscopy has detected fine differences in chemical composition among ROs, and it detected the interactions within nanoemulsions. It was shown that the cold-pressed, unrefined, organic grade oil (RO2) with 6.62% saturated fatty acids and 92.25% unsaturated fatty acids, was optimal for the LE-NEs. Textural analysis confirmed the existence of cubic gel-like phase as a crucial step in the formation of stable RO2-loaded LE-NEs, with droplets in the narrow nano-range (125 to 135 nm; PDI � 0.1). The DPPH test in methanol and ABTS in aqueous medium have revealed a synergistic free radical scavenging effect between lipophilic and hydrophilic antioxidants in LE-NEs. The nanoemulsion carrier has improved the biological effect of raw materials on HeLa cervical adenocarcinoma cells, while exhibiting good safety profile, as confirmed on MRC-5 normal
The main goal of this study was to develop a liposome formulation with sulfanilamide and to investigate the liposomes impact on its release and stability to the UV-A/UV-B and UV-C irradiation. Liposome dispersions with incorporated sulfanilamide were prepared by thin-film hydration method and liposomes role to the sulfanilamide release was investigated by using a dialysis method. Comparatively, sulfanilamide in phosphate buffer solution was subject to release study as well to the UV irradiation providing for the possibilities of kinetics analysis. drug release study demonstrated that 20% of sulfanilamide was released from liposomes within 1 h that is approximately twice as slower as in the case of dissolved sulfanilamide in phosphate buffer solution. The kinetic release process can be described by Korsmeyer-Peppas model and according to the value of diffusion release exponent it can be concluded that drug release mechanism is based on the phenomenon of diffusion. The sulfanilamide degradation in phosphate buffer solution and liposomes is related to the formation of UV-induced degradation products that are identified by UHPLC/MS analysis as: sulfanilic acid, aniline and benzidine. The UV-induced sulfanilamide degradation in the phosphate buffer solution and liposome vesicles fits the first- order kinetic model. The degradation rate constants are dependent on the involved UV photons energy input as well as sulfanilamide microenvironment. Liposome microenvironment provides better irradiation sulfanilamide stability. The obtained results suggest that liposomes might be promising carriers for delayed sulfanilamide delivery and may serve as a basis for further research.
The current study describes the experimental design guided development of PEGylated nanoemulsions as parenteral delivery systems for curcumin, a powerful antioxidant, as well as the evaluation of their physicochemical characteristics and antioxidant activity during the two years of storage. Experimental design setup helped development of nanoemulsion templates with critical quality attributes in line with parenteral application route. Curcumin-loaded nanoemulsions showed mean droplet size about 105 nm, polydispersity index <0.15, zeta potential of −40 mV, and acceptable osmolality of about 550 mOsm/kg. After two years of storage at room temperature, all formulations remained stable. Moreover, antioxidant activity remained intact, as demonstrated by DPPH (IC50 values 0.078–0.075 mg/mL after two years) and FRAPS assays. In vitro release testing proved that PEGylated phospholipids slowed down the curcumin release from nanoemulsions. The nanoemulsion carrier has been proven safe by the MTT test conducted with MRC-5 cell line, and effective on LS cell line. Results from the pharmacokinetic pilot study implied the PEGylated nanoemulsions improved plasma residence of curcumin 20 min after intravenous administration, compared to the non-PEGylated nanoemulsion (two-fold higher) or curcumin solution (three-fold higher). Overall, conclusion suggests that developed PEGylated nanoemulsions present an acceptable delivery system for parenteral administration of curcumin, being effective in preserving its stability and antioxidant capacity at the level highly comparable to the initial findings.
Objective The growing consumers’ preferences and concerns regarding healthy ageing, youthful skin appearance, environmental protection and sustainability have triggered an ever‐increasing trend towards natural, eco‐friendly and ethically sourced anti‐ageing products. Accordingly, this paper describes design and evaluation of novel, safe, effective and high‐quality emulsion serums, completely based on ingredients of natural origin, intended for improving facial fine lines and wrinkles. Methods Model formulations, stabilized by an innovative glycolipid mixed emulsifier (lauryl glucoside/myristyl glucoside/polyglyceryl‐6 laurate) and containing Acmella oleracea extract as a model anti‐ageing active, were prepared by cold process and fully assessed regarding their rheological behaviour (continuous rotational and oscillatory tests) and physical stability (dynamic‐mechanical thermoanalysis – DMTA test). To study and optimize the simultaneous influence of varied formulation factors (emollients and emulsifier concentrations) on critical rheological attributes of the developed serums, a central composite design within ‘design of experiments’ approach was employed. The general skin performance – preliminary safety and anti‐wrinkle efficacy of selected model serum, was evaluated in human volunteers, by employing several objective, non‐invasive bioengineering techniques. Results Rheological characterization revealed favourable shear‐thinning flow behaviour with yield point, and dominating elastic character (storage modulus G’ > loss modulus G") in both amplitude and frequency sweeps, which together with relatively small structural change obtained in DMTA test indicated overall satisfying rheological and stability properties of formulated serums. From the established design space, and taking into account formulation cost and carbon footprint, promising model serum (desired/optimal apparent viscosity, yield point and loss factor, rather small and constant structural change), containing 15% of emollients and 1% of emulsifier, was chosen for in vivo evaluations. Screening of skin irritation effects revealed the absence of potential irritancy of investigated serum, suggesting overall satisfying skin tolerability/preliminary safety. Silicone skin replica image analysis demonstrated noticeable reduction/improvement in all measured skin wrinkle parameters after only 2 weeks of test serum application in periorbital and perioral areas, indicating its rapid and beneficial effects on the facial expression lines and wrinkles. Conclusion Altogether, the results corroborate the promising potential of the developed Acmella oleracea extract‐loaded emulsion serum as safe, effective and non‐invasive natural anti‐wrinkle product.
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