RESUMEN

In recent years, nanoparticles have gained significant importance due to their unique properties, such as pharmacological, electrical, optical, and magnetic abilities, contributing to the growth of the science and technology sector. Particular naturally derived biomolecules with beneficial effects on menopause disorder have been the subject of studies of pharmaceutical formulation to obtain alternative pharmaceutical forms with increased bioavailability and without side effects, as in nanostructured lipid carriers (NLCs) loaded with such active ingredients. In the present study, one stage of a broader project, we have performed pharmacotoxicology studies for six combinatory innovative nanocapsule pharmaceutical forms containing active natural biomolecules before considering them as oral formulas for (1) in vitro toxicity studies on culture cells and (2) in vivo preclinical studies on a surgically induced menopause model of Wistar female rats, and the influence of the NLCs on key biochemical parameters: lipid profile (TG, Chol, HDL), glycemic markers (Gli), bone markers (Pac, Palc, Ca, phosphorus), renal markers (Crea, urea, URAC), inflammation (TNF), oxidative stress (GSH, MDA), and estrogen-progesterone hormonal profile. The micronucleus test did not reveal the genotoxicity of the tested compounds; the menopause model showed no significant safety concerns for the six tested formulas evaluated using the blood biochemical parameters; and the results showed the potential hypoglycemic, hypolipidemic, hypouricemic, and antioxidant potential of one of the tested formulas containing nano diosgenin and glycyrrhizic acid.

Asunto(s)

Portadores de Fármacos , Nanopartículas , Ratas , Femenino , Animales , Composición de Medicamentos , Portadores de Fármacos/química , Lípidos/química , Ratas Wistar , Nanopartículas/química , Nanotecnología , Menopausia , Tamaño de la Partícula

RESUMEN

The use of bio-based reagents for silver nanoparticle (AgNP) production has gained much attention among researchers as it has paved the way for environmentally friendly approaches at low cost for synthesizing nanomaterials while maintaining their properties. In this study, Stellaria media aqueous extract was used for silver nanoparticle phyto-synthesis, and the resulting treatment was applied to textile fabrics to test its antimicrobial properties against bacteria and fungi strains. The chromatic effect was also established by determining the L*a*b* parameters. For optimizing the synthesis, different ratios of extract to silver precursor were tested using UV-Vis spectroscopy to observe the SPR-specific band. Moreover, the AgNP dispersions were tested for their antioxidant properties using chemiluminescence and TEAC methods, and the phenolic content was evaluated by the Folin-Ciocâlteu method. For the optimal ratio, values of average size, 50.11 ± 3.25 nm, zeta potential, -27.10 ± 2.16 mV, and polydispersity index, 0.209, were obtained via the DLS technique and zeta potential measurements. AgNPs were further characterized by EDX and XRD techniques to confirm their formation and by microscopic techniques to evaluate their morphology. TEM measurements revealed cvasi-spherical particles with sizes in the range of 10-30 nm, while SEM images confirmed their uniform distribution on the textile fiber surface.

RESUMEN

The main objective of this study was the testing of natural compounds, such as Polygonum cuspidatum (PgnC) loaded into nanostructured lipid carriers (NLC), which can act as a "double-edged sword" aimed at simultaneously combating dangerous free radicals and inhibiting pro-inflammatory cytokines. Resveratrol-rich PgnC extract was paired with another phytochemical, Diosgenin (DSG), in NLC. The lipid nanocarriers carrying both herbals (NLC-DSG-PgnC) had spherical diameters (100 ± 2 50 nm), a polydispersity index of ~0.15, and electrokinetic potentials greater than -46.5 mV. Entrapment efficiencies of 65% for PgnC and 87% for DSG were determined by chromatographic and UV-Vis spectroscopy assays. Cell cytotoxicity analysis proved that 50 µg/mL of NLC-PgnC and dual-NLC ensured a biocompatible effect like the untreated cells. The dual-NLC assured a much slower in vitro release of DSG and PgnC (67% PgnC and 48% DSG) than the individual-NLC (78% PgnC and 47% DSG) after 4 h of experiments. NLC encapsulating PgnC presented a superior ability to capture cationic radicals: 74.5 and 77.9%. The chemiluminescence results pointed out the non-involvement of DSG in stopping oxygenated free radicals, while the antioxidant activity was maintained at a level higher than 97% for dual-NLC. NLC-DSG-PgnC ensured a promising capacity for inhibition of pro-inflammatory cytokine IL-6, ranging from 91.9 to 94.9%.

RESUMEN

A novel nanoscale approach was developed for the improved cellular internalization of hybrid bovine serum albumin-lipid nanocarriers loaded with piperine (NLC-Pip-BSA) in different tumor cells. The effect of the BSA-targeted-NLC-Pip and untargeted-NLC-Pip on the viability, proliferation, and levels of cell-cycle damage and apoptosis in the colon (LoVo), ovarian (SKOV3) and breast (MCF7) adenocarcinoma cell lines was comparatively discussed. NLCs were characterized concerning particle size, morphology, zeta potential, phytochemical encapsulation efficiency, ATR-FTIR, and fluorescence spectroscopy. The results showed that NLC-Pip-BSA showed a mean size below 140 nm, a zeta potential of -60 mV, and an entrapment efficiency of 81.94% for NLC-Pip and 80.45% for NLC-Pip-BSA. Fluorescence spectroscopy confirmed the coating of the NLC with the albumin. By MTS and RTCA assays, NLC-Pip-BSA showed a more pronounced response against the LoVo colon cell line and MCF-7 breast tumor cell lines than against the ovarian SKOV-3 cell line. Flow cytometry assay demonstrated that the targeted NLC-Pip had more cytotoxicity and improved apoptosis than the untargeted ones in MCF-7 tumor cells (p < 0.05). NLC-Pip caused a significant increase in MCF-7 breast tumor cell apoptosis of ~8X, while NLC-Pip-BSA has shown an 11-fold increase in apoptosis.

RESUMEN

The present study aims to bring an addition to biomass resources valorization for environmental-friendly synthesis of nanoparticles. Thus, the green synthesis of silver nanoparticles (AgNPs) was performed, using a novel and effective reducing agent, Primula officinalis extract. The synthesis was optimized by monitoring the characteristic absorption bands, using UV−Vis spectroscopy, and by evaluating the size and physical stability. The phenolic consumption was established using Folin-Ciocâlteu method (1.40 ± 0.42 mg, representing ~5% from the total amount of poly--phenols) and the antioxidant activity was evaluated using chemiluminescence and TEAC methods. The optimum ratio extract to Ag ions was 1:3, for which the AgNPs presented a zeta potential value of −29.3 ± 1.2 mV and particles size of 5−30 nm. For characterization, EDS and XRD techniques were used, along with microscopy techniques (TEM). The AgNPs dispersions were applied on natural textile samples (cotton and wool), as a novel antimicrobial treatment for textile preservation. The treated fabrics were further characterized in terms of chromatic parameters and antimicrobial effect against Escherichia coli, Staphylococcus aureus, Bacillus subtilis, and Penicillium hirsutum strains. The high percentages of bacterial reduction, >99%, revealed that the AgNPs produced are a good candidate for textiles preservation against microbial degradation.

RESUMEN

Conventional and herbal active principles can be combined in a beneficial harmony using their best features and compensating for the certain weaknesses of each. The study will answer the question, "how can willow bark extract (Wbe) or ivy leaf extract (Ile) influence the photoprotective, skin permeation and hydration properties of Bioactive Lipid Nanocarriers (BLN) loaded with UV-filters and selected herbals?". BLN-Wbe/Ile-UV-filters were characterized for particle size, zeta potential, thermal behavior, entrapment efficiency and drug loading. The formulated BLN-hydrogels (HG) were subjected to in vitro release and permeation experiments. The in vitro determination of sun protection factors, as well as comparative in vitro photostability tests, rheology behavior and in vivo hydration status have been also considered for hydrogels containing BLN-Ile/Wbe-UV-filters. Photoprotection of BLN-HG against UVA rays was more pronounced as compared with the UVB (UVA-PF reached values of 30, while the maximum SPF value was 13). The in vitro irradiation study demonstrated the photostability of BLN-HG under UV exposure. A noteworthy cosmetic efficacy was detected by in vivo skin test (hydration effect reached 97% for the BLN-Wbe-UV-filters prepared with pomegranate oil). The research novelty, represented by the first-time co-optation of the active herbal extracts (Wbe and Ile) together with two synthetic filters in the same nanostructured delivery system, will provide appropriate scientific support for the cosmetic industry to design novel marketed formulations with improved quality and health benefices.

RESUMEN

There is ongoing research on various herbal bioactives and delivery systems which indicates that both lipid nanocarriers and herbal medicines will be fine tunned and integrated for future bio-medical applications. The current study was undertaken to systematically develop NLC-DSG-yam extract for the improved efficacy of herbal Diosgenin (DSG) in the management of anti-inflammatory disorders. NLCs were characterized regarding the mean size of the particles, morphological characteristics, physical stability in time, thermal behaviour, and entrapment efficiency of the herbal bioactive. Encapsulation efficiency and in vitro antioxidant activity measured the differences between the individual and dual co-loaded-NLC, the co-loaded one assuring a prolonged controlled release of DSG and a more emphasized ability of capturing short-life reactive oxygen species (ROS). NLCs safety properties were monitored following the in vitro MTS ((3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) tetrazolium reduction assay) and RTCA (Real-Time Cell Analysis) assays. Concentrations less than 50 µg/mL showed no cytotoxic effects during in vitro cytotoxicity assays. Besides, the NLC-DSG-yam extract revealed a great anti-inflammatory effect, as the production of pro-inflammatory cytokines (TNF-alpha, IL-6) was significantly inhibited at 50 µg/mL NLC (e.g., 98.2% ± 1.07 inhibition of TNF-α, while for IL-6 the inhibition percentage was of 62% ± 1.07). Concluding, using appropriate lipid nanocarriers, the most desirable properties of herbal bioactives could be improved.

RESUMEN

Although many phytochemicals have been used in traditional medicine, there is a great need to refresh the health benefits and adjust the shortcomings of herbal medicine. In this research, two herbal principles (Diosgenin and Glycyrrhiza glabra extract) coopted in the Nanostructured Lipid Carriers have been developed for improving the most desirable properties of herbal medicine-antioxidant and anti-inflammatory actions. The contribution of phytochemicals, vegetable oils and of lipid matrices has been highlighted by comparative study of size, stability, entrapment efficiency, morphological characteristics, and thermal behavior. According to the in vitro MTS and RTCA results, the dual herbal-NLCs were no cytotoxic toward endothelial cells at concentrations between 25 and 100 µg/mL. A rapid release of Glycyrrhiza glabra and a motivated delay of Diosgenin was detected by the in vitro release experiments. Dual herbal-NLCs showed an elevated ability to annihilate long-life cationic radicals (ABTS•+) and short-life oxygenated radicals (an inhibition of 63.4% ABTS•+, while the ability to capture radical oxygen species reached 96%). The production of pro-inflammatory cytokines was significantly inhibited by the newly herbals-NLC (up to 97.9% inhibition of TNF-α and 62.5% for IL-6). The study may open a new pharmacotherapy horizon; it provides a comprehensive basis for the use of herbal-NLC in the treatment of inflammatory diseases.

RESUMEN

In this study the conventional oils used for lipid nanocarriers (NLCs) synthesis were replaced by high concentration of fish oils (e.g., fish oil concentrated in omega-3 fatty acids, fish oil enriched in omega-3 and omega-6 fatty acids and salmon oil), in order to produce appropriate lipid based nanosystems able to entrap willow bark extract (WBE). Formulation factors such as the nature of the fish oil, glycerol content and WBE loading were evaluated to produce optimum lipid based nanosystems with suitable physical stability and enhanced antioxidant activity. The synthesized WBE-NLC showed spherical and homogeneous particles and average diameters in the range of 200-250 nm, as determined by TEM measurements. The electrokinetic potentials were negative for all free- and WBE-loaded NLCs, with values between -29.1 ÷ - 35.8 mV, which reveal an excellent physical stability. By scanning calorimetry measurements it has been shown that the lipid crystallization and melting behavior of NLCs before and after loading with WBE were no significantly influenced by the type of fish oil used and only in a few NLCs formulations an obvious perturbation of lipid network have been detected. The chemiluminescence technique has been used to assess the effect of fish oil type on the in vitro antioxidant activity of WBE-NLCs. Ability of WBE entrapped within NLCs to scavange the free radicals was greater than for native WBE and fish oils. The difference between the antioxidant activity of WBE-NLC (98%) and those of pure WBE (AA% = 77.2) and fish oil (AA% = 83.7), may be explained by the occurrence of a synergistic effect between the components of lipid nanocarriers.

Asunto(s)

Antioxidantes/química , Portadores de Fármacos/química , Aceites de Pescado/química , Nanopartículas/química , Extractos Vegetales/química , Salix/química , Estabilidad de Medicamentos , Tamaño de la Partícula , Corteza de la Planta/química

RESUMEN

Basal cell carcinoma (BCC) is one of the commonest malignancies occurred on sun-exposed skin, mainly by UV-B radiation, of lighter-skinned individuals. The aim of the present study was to develop advanced drug delivery formulations used in BCC therapy that overcomes chemotherapy-induced side-effects of skin photosensitivity by an integrative approach of nanoencapsulation in conjunction with combination therapy that uses chemotherapeutic, chemoprotective and sunscreen agents. The combination of anticancer drug together with sunscreen agent is very useful in therapy, especially for individuals who are more exposed to the sun without using a sunscreen. Nanostructured lipid carriers (NLCs) employed as drug delivery systems were co-loaded with 5-fluorouracil (5-FU), a hydrophilic chemotherapeutic drug, and ethylhexyl salicylate (EHS), a lipophilic UV-B sunscreen agent. The NLCs were developed using bioactive squalene (50.8% w/w) from amaranth seed oil as chemoprotective agent. By varying the concentrations of 5-FU and EHS, the co-loaded NLCs presented particle sizes of about 100nm, acceptable physical stability with values smaller than -25mV and appropriate entrapment efficiency that reaches values over 65% for both types of drugs. The UV-B blocking ability of EHS loaded into NLCs were influenced by the concentration of 5-FU. The amaranth oil offered a capacity of 70% in scavenging the free radicals. In vitro drug release showed that NLCs presented sustained release of 5-FU that followed the Fick's law of diffusion.

Asunto(s)

Portadores de Fármacos/farmacología , Lípidos/administración & dosificación , Nanopartículas/administración & dosificación , Protectores Solares/administración & dosificación , Amaranthus/química , Antioxidantes/administración & dosificación , Antioxidantes/farmacología , Rastreo Diferencial de Calorimetría , Carcinoma Basocelular/tratamiento farmacológico , Carcinoma Basocelular/prevención & control , Portadores de Fármacos/administración & dosificación , Fluorouracilo/administración & dosificación , Fluorouracilo/farmacocinética , Humanos , Lípidos/química , Lípidos/farmacología , Nanopartículas/química , Tamaño de la Partícula , Aceites de Plantas/administración & dosificación , Aceites de Plantas/farmacología , Salicilatos/administración & dosificación , Salicilatos/química , Salicilatos/farmacología , Neoplasias Cutáneas/tratamiento farmacológico , Neoplasias Cutáneas/prevención & control , Escualeno/administración & dosificación , Escualeno/farmacología , Protectores Solares/química , Protectores Solares/farmacología , Rayos Ultravioleta

RESUMEN

The aim of this research was to develop advanced lipid nanocarriers based on renewable vegetable resources (rice bran oil and raspberry seed oil) that possess self-antioxidative properties, having advantages in terms of minimal side effects and exhibiting the ability to simultaneously co-encapsulate and co-release two active compounds. The focus has been oriented towards developing safe cosmetic formulations with broad-spectrum photoprotection based on these new lipid nanocarriers that contain large amounts of vegetable oils and low concentrations of synthetic UVA and UVB filters (butyl-methoxydibenzoylmethane - BMDBM and octocrylene - OCT). The lipid nanocarriers have a spherical shape and show good physical stability, with a zeta potential in the range of -25.5 to -32.4 mV. Both vegetable oils play a key role in the preparation of efficient nanocarriers, leading to a less ordered arrangement of the lipid core that offers many spaces for the entrapment of large amounts of BMDBM (79%) and OCT (90%), as wells as improved antioxidant activity and UV absorption properties, particularly for the lipid nanocarriers prepared from rice bran oil. By formulating the lipid nanocarriers into creams containing only 3.5% of the UV filters and 10.5% of the vegetable oils, the resulting sunscreens exhibited improved photoprotection, reflecting up to 91% and 93% of UVA and UVB rays, respectively. A new direction of research achieved by this study is the multiple release strategy of both UV filters from the same lipid nanocarrier. After 24 hours, a slow release of BMDBM (less than 4%) and OCT (17.5%) was obtained through a Fick diffusion process. This study demonstrates a significant advance in the areas of both nanotechnology and cosmetics, developing safer cosmetic formulations that possess broad antioxidant, photoprotective and co-release effectiveness due to the existence of a high content of nanostructured vegetable oils combined with a low amount of synthetic UV filters in the same carrier system.

Asunto(s)

Frutas/química , Nanocápsulas/química , Oryza/química , Aceites de Plantas/química , Semillas/química , Protectores Solares/química , Absorción de Radiación , Acrilatos/química , Alcanos/química , Antioxidantes/química , Chalconas/química , Química Farmacéutica , Cosméticos/química , Cristalización , Difusión , Estabilidad de Medicamentos , Cinética , Lípidos/química , Tamaño de la Partícula , Procesos Fotoquímicos , Propiofenonas , Rayos Ultravioleta

RESUMEN

The coencapsulation of two UV filters, butyl-methoxydibenzoylmethane (BMDBM) and octocrylene (OCT), into lipid nanocarriers was explored to develop stable cosmetic formulations with broad-spectrum photoprotection and slow release properties. Different types of nanocarriers in various concentrations of the two UV filters were tested to find the combination with the best absorption and release properties. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) have been the two types of lipid nanocarriers used. The NLCs were based on either medium chain triglycerides (MCT) or squalene (Sq). The following physicochemical properties of the nanocarriers have been evaluated: particle size, morphology, zeta potential (ZP), entrapment efficiency, loading capacity, and thermal behavior. The nanocarriers have been formulated into creams containing low amounts of UV filters (2.5% BMDBM and 1% OCT). The best photoprotection results were obtained with the cream based on NLCs prepared with MCT, having a sun protection factor (SPF) of 17.2 and an erythemal UVA protection factor (EUVA-PF) of 50.8. The photostability of the encapsulated BMDBM filter was confirmed by subjecting the nanocarriers-based creams to in vitro irradiation. The prolonged UV-protection efficacy was coupled with a slow in vitro release of the synthetic UV filters, which followed the Higuchi release model.

Asunto(s)

Acrilatos/química , Alcanos/química , Chalconas/química , Portadores de Fármacos/química , Composición de Medicamentos , Lípidos/química , Nanopartículas/química , Protectores Solares/química , Rayos Ultravioleta , Técnicas In Vitro , Procesos Fotoquímicos , Propiofenonas

RESUMEN

The efficiency of a cosmetic product depends not only on the active ingredients, but also on the carrier system devoted to improve its bioavailability. This article aims to encapsulate two couples of UV molecular absorbers, with a blocking action on both UV-A and UV-B domains, into efficient lipid nanoparticles. The effect of encapsulation on the specific properties such as sun protection factor and photostability behaviour has been demonstrated. The lipid nanoparticles with size range 30-350 nm and a polydispersity index between 0.217 and 0.244 are obtained using a modified high shear homogenisation method. The nanoparticles had spherical shapes with a single crystallisation form of lipid matrices characteristic for the least ordered crystal structure (α-form). The in vitro determination of photoprotection has led to high SPF ratings, with values of about 20, which assure a good photoprotection and filtering about 95% of UV radiation. The photoprotection effect after irradiation stage was observed to be increased more than twice compared to initial samples as a result of isomerisation phenomena. All the results have shown that good photoprotection effect and improved photostability could be obtained using such sunscreen couples, thus demonstrating that UV absorbers-solid lipid nanoparticles are promising carriers for cosmetic formulations.