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1.
In Silico Pharmacol ; 12(2): 81, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-39233909

RESUMEN

To evaluate the therapeutic potential of curcumin tagged cilostazol solid nano dispersion in wistar rat streptozotocin-nicotinamide-induced diabetic nephropathy. Cilostazol (CLT), a Phosphodiesterase (PDE) inhibitor has an inhibitory effect on reactive oxygen species (ROS), and Curcumin (Cur), an antioxidant, and anti-inflammatory, are water-soluble. Solid Nano dispersions were developed using the "Box-Behnken Design" and emulsion solvent evaporation procedure to improve the solubility and bioavailability. Streptozotocin (SPZ) and Nicotinamide (NA) caused diabetes in Wistar rats. DN developed 30-45 days after disease induction. All rat groups underwent histological, biochemical and pharmacokinetic evaluation. The optimized batch of Cilostazol Loaded Novel Curcumin Tagged Solid Nanodispersion (CLT-15 SND) estimated renal, lipid, and cytokine profiles better than the conventional batch. CLT-15 SND, given orally to diabetic rats for 45 days, significantly lowered fasting BGL and IL-6 levels and improved lipid and kidney-profile markers and body weight compared to plain Cilostazol Loaded Solid Nanodispersion (CLT-15 WC SND). CLT-15 SND treatment groups showed decreased blood glucose by 3.38 and 9.71 percent, increased body weight by 2.81 and 5.27 percent, improved Interleukin-6 (IL-6) by 21.36 and 18.36 percent, improved urine albumin levels by 5.67 and 14.19 percent and creatinine levels by 3.125 and 37.5 percent, improved serum urea by 30.48 percent, increased serum albumin by 2.59 and 11.18 percent, and decreased creatinine and 5.03 and 8.12 percent, respectively as compared to CLT-15 WC and MP treatment animal groups. CLT and Cur reduced IL-6, kidney, and lipid markers, demonstrating their renoprotective and pancreas-protective effects. CLT and Cur's inhibition may be the mechanism.

2.
Int J Biol Macromol ; 278(Pt 1): 134405, 2024 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-39116986

RESUMEN

The multibiocomponent hybrid alginate hydrogels based on brown and sea algae, containing 100 % ingredients of natural origin were prepared by ionic crosslinking reaction of a polymeric matrix with lipid nanodispersion. To the best of the Authors' knowledge such multicomponent biobased hydrogel of promising medical and cosmetical applications for the first time was obtained in the environment of flower water, received earlier as a waste by-product from various chemical processes. An innovative hybrid alginate hydrogel that is completely biodegradable and eco-friendly was obtained following waterless and upcycling trends that are in line with the principles of sustainable development. The optimal composition of the lipid nanodispersion and the polymeric matrix was selected using the statistical method of design of the experiment. Based on obtained results, multibiocomponent hybrid alginate hydrogels with various ratios of lipid nanodispersion were obtained. Subsequently, the porous structure and elasticity of the hybrid hydrogels were analyzed. Moreover, to confirm the safety of the multibiocomponent alginate hybrid hydrogels the cytotoxic tests were carried out using human fibroblasts and keratinocytes cell lines. As the final product hybrid of hydrolate-swollen alginate hydrogel and lipid nanodispersion containing several active ingredients (silymarin, bakuchiol, spirulina) was obtained.


Asunto(s)
Alginatos , Materiales Biocompatibles , Hidrogeles , Lípidos , Hidrogeles/química , Alginatos/química , Humanos , Lípidos/química , Materiales Biocompatibles/química , Cosméticos/química , Fibroblastos/efectos de los fármacos , Fibroblastos/citología , Queratinocitos/efectos de los fármacos , Queratinocitos/citología , Línea Celular
3.
Pestic Biochem Physiol ; 201: 105897, 2024 May.
Artículo en Inglés | MEDLINE | ID: mdl-38685223

RESUMEN

Solid nanodispersion (SND) is an important variety of nanopesticides which have been extensively studied in recent years. However, the key influencing factors for bioactivity enhancement of nanopesticides remain unclear, which not only limits the exploration of relevant mechanisms, but also hinders the precise design and development of nanopesticides. In this study, we explored the potential of SND in enhancing the bioactivity of nanopesticides, specifically focusing on abamectin SND prepared using a self-emulsifying-carrier solidifying technique combined with parameter optimization. Our formulation, consisting of 8% abamectin, 1% antioxidant BHT (2,6-di-tert-butyl-4-methylphenol), 12% complex surfactants, and 79% sodium benzoate, significantly increased the pseudo-solubility of abamectin by at least 3300 times and reduced its particle size to a mere 15 nm, much smaller than traditional emulsion in water (EW) and water-dispersible granule (WDG) forms. This reduction in particle size and increase in surface activity resulted in improved foliar adhesion and retention, enabling a more efficient application without the need for organic solvents. The inclusion of antioxidants also enhanced photostability compared to EW, and overall stability tests confirmed SND's resilience under various storage conditions. Bioactivity tests demonstrated a marked increase in toxicity against diamondback moths (Plutella xylostella L.) with abamectin SND, which exhibited 3.7 and 7.6 times greater efficacy compared to EW and WDG, respectively. These findings underscore the critical role of small particle size, high surface activity, and strong antioxidant properties in improving the performance and bioactivity of abamectin SND, highlighting its significance in the design and development of high-efficiency, eco-friendly nanopesticides and contributing valuably to sustainable agricultural practices.


Asunto(s)
Ivermectina , Ivermectina/análogos & derivados , Ivermectina/farmacología , Ivermectina/química , Animales , Insecticidas/farmacología , Insecticidas/química , Tamaño de la Partícula , Antioxidantes/farmacología , Antioxidantes/química , Nanopartículas/química , Mariposas Nocturnas/efectos de los fármacos , Tensoactivos/farmacología , Tensoactivos/química , Larva/efectos de los fármacos , Emulsiones
4.
Molecules ; 29(8)2024 Apr 18.
Artículo en Inglés | MEDLINE | ID: mdl-38675662

RESUMEN

Membrane materials with osmium nanoparticles have been recently reported for bulk membranes and supported composite membrane systems. In the present paper, a catalytic material based on osmium dispersed in n-decanol (nD) or n-dodecanol (nDD) is presented, which also works as an emulsion membrane. The hydrogenation of p-nitrophenol (PNP) is carried out in a reaction and separation column in which an emulsion in the acid-receiving phase is dispersed in an osmium nanodispersion in n-alcohols. The variables of the PNP conversion process and p-aminophenol (PAP) transport are as follows: the nature of the membrane alcohol, the flow regime, the pH difference between the source and receiving phases and the number of operating cycles. The conversion results are in all cases better for nD than nDD. The counter-current flow regime is superior to the co-current flow. Increasing the pH difference between the source and receiving phases amplifies the process. The number of operating cycles is limited to five, after which the regeneration of the membrane dispersion is required. The apparent catalytic rate constant (kapp) of the new catalytic material based on the emulsion membrane with the nanodispersion of osmium nanoparticles (0.1 × 10-3 s-1 for n-dodecanol and 0.9 × 10-3 s-1 for n-decanol) is lower by an order of magnitude compared to those based on adsorption on catalysts from the platinum metal group. The advantage of the tested membrane catalytic material is that it extracts p-aminophenol in the acid-receiving phase.

5.
BMC Chem ; 18(1): 62, 2024 Mar 30.
Artículo en Inglés | MEDLINE | ID: mdl-38555446

RESUMEN

Curcumin, a vital bioactive compound found naturally, has diverse biological applications. However, a major limitation of curcumin is its low bioavailability caused by its limited solubility in water. Hence, it is possible to overcome this problem through preparing oil in water nanodispersion of curcumin that emulsifier can play key role to produce nanodispersion. In the present study, the effect of three emulsifiers of Tween 80, Arabic Gum and Polyethylene glycol on preparing nanodispersions with desirable properties was investigated using subcritical water method and a mixture design. Zeta-potential and particle size of the achieved nanodispersions were taken into account as outcome factors. The optimum values for emulsifiers of Tween 80, Arabic Gum and Polyethylene glycol were obtained as 0.588 g, 0.639 g and 0.273 g, respectively, using the suggested model, so that obtained nanodispersion had minimum particle size (101.89 nm) and maximum zeta-potential (-24.99 mV). In fact, 102.5 nm and - 24.7 mV were obtained from experimental data at these values of emulsifiers. In addition, maximum loading potential (0.199 g/L), efficiency (99.5%), and minimum total curcumin loss (0.5%) were acquired at these optimum values. The results also show that the nanodispersion had a powerful antioxidant activity (65.27%) with extra antibacterial activity in facing with both E. coli and S. aureus strains. Moreover, curcumin nanodispersion was significantly taken up by HT-29 cells and resulted in the production of oxidative stress in the cells, leading to a decrease in the growth of cancer cells.

6.
Molecules ; 28(16)2023 Aug 08.
Artículo en Inglés | MEDLINE | ID: mdl-37630195

RESUMEN

Schistosomiasis is a tropical disease transmitted in an aqueous environment by cercariae from the Schistosoma genus. This disease affects 200 million people living in risk areas around the world. The control of schistosomiasis is realized by chemotherapy, wastewater sanitation, health education, and mollusk control using molluscicidal agents. This work evaluates the effects of a nanoemulsion containing essential oil from Myrciaria floribunda leaves as a molluscicidal and cercaricidal agent against Biomphalaria glabrata mollusks and Schistosoma mansoni cercariae. The Myrciaria floribunda essential oil from leaves showed nerolidol, ß-selinene, 1,8 cineol, and zonarene as major constituents. The formulation study suggested the F3 formulation as the most promising nanoemulsion with polysorbate 20 and sorbitan monooleate 80 (4:1) with 5% (w/w) essential oil as it showed a smaller droplet size of approximately 100 nm with a PDI lower than 0.3 and prominent bluish reflection. Furthermore, this nanoemulsion showed stability after 200 days under refrigeration. The Myrciaria floribunda nanoemulsion showed LC50 values of 48.11 µg/mL, 29.66 µg/mL, and 47.02 µg/mL in Biomphalaria glabrata embryos, juveniles, and adult mollusks, respectively, after 48 h and 83.88 µg/mL for Schistosoma mansoni cercariae after 2 h. In addition, a survival of 80% was observed in Danio rerio, and the in silico toxicity assay showed lower overall human toxicity potential to the major compounds in the essential oil compared to the reference molluscicide niclosamide. These results suggest that the nanoemulsion of Myrciaria floribunda leaves may be a promising alternative for schistosomiasis control.


Asunto(s)
Moluscocidas , Myrtaceae , Aceites Volátiles , Adulto , Humanos , Aceites Volátiles/farmacología , Moluscocidas/farmacología , Eucaliptol , Niclosamida , Alimentos
7.
ACS Appl Mater Interfaces ; 15(30): 37093-37106, 2023 Aug 02.
Artículo en Inglés | MEDLINE | ID: mdl-37488063

RESUMEN

Various strategies have been developed to improve the applicability of hydrophobic pesticides for better effectiveness in agriculture. However, existing formulations of hydrophobic pesticides still suffer from complicated processing, abused organic solvents, indispensable surfactants, or inescapable ecotoxicity, which strictly limit their applications. Herein, a dynamic covalent bond tailored pesticide (fipronil) amphiphile is constructed to address the above issues, which accomplishes the nanodispersion, full wetting, and precise delivery without organic solvents, surfactants, and materials simultaneously. By introducing a hydrophilic ligand on the hydrophobic fipronil through an imine bond, the cleavable fipronil amphiphile (FPP) exhibits superior water solubility and can even self-assemble into micelles at higher concentrations, which can be directly applied in powder form without organic solvents. Attributed to the suitable hydrophilic/hydrophobic ratio, FPP achieves full wetting and effective deposition on superhydrophobic rice leaves without surfactants. Moreover, benefiting from the unique dynamic nature of the imine bond, FPP maintains good storage stability while sensitively releasing back to fipronil under the humidity and pH trigger, consequently implementing the precise delivery for nontarget Apis cerana and target Chilo suppressalis without materials. To our knowledge, this dynamic covalent bond tailored amphiphile strategy is the first idea that simultaneously takes the dispersibility, wettability, and responsiveness of hydrophobic pesticides into account, providing a possibility to control the entire journey of field application and even promising to be incorporated into the synthesis process, thus paving the way for modern sustainable agriculture.

8.
Food Technol Biotechnol ; 61(1): 39-50, 2023 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-37200792

RESUMEN

Research background: Various approaches have been used to present functional lipids including lycopene in a palatable food form to consumers. However, being highly hydrophobic, lycopene is insoluble in aqueous systems and has a limited bioavailability in the body. Lycopene nanodispersion is expected to improve the properties of lycopene, but its stability and bioaccessibility are also affected by emulsifier type and environmental conditions such as pH, ionic strength and temperature. Experimental approach: The influence of soy lecithin, sodium caseinate and soy lecithin/sodium caseinate at 1:1 ratio on the physicochemical properties and stability of lycopene nanodispersion prepared using the emulsification-evaporation methods before and after treatment at different pH, ionic strength and temperature were investigated. The in vitro bioaccessibility of the nanodispersions was also studied. Results and conclusion: Under neutral pH conditions, nanodispersion stabilized with soy lecithin had the highest physical stability and the smallest particle size (78 nm), the lowest polydispersity index (PDI) value (0.180) and highest zeta potential (-64 mV) but the lowest lycopene concentration (1.826 mg/100 mL). Conversely, nanodispersion stabilized with sodium caseinate had the lowest physical stability. Combining the soy lecithin with sodium caseinate at 1:1 ratio resulted in a physically stable lycopene nanodispersion with the highest lycopene concentration (2.656 mg/100 mL). The lycopene nanodispersion produced by soy lecithin also had high physical stability under different pH range (pH=2-8) where the particle size, PDI and zeta potential remained fairly consistent. The nanodispersion containing sodium caseinate was unstable and droplet aggregation occurred when the pH was reduced close to the isoelectric point of sodium caseinate (pH=4-5). The particle size and PDI value of nanodispersion stabilized with soy lecithin and sodium caseinate mixture increased sharply when the NaCl concentration increased above 100 mM, while the soy lecithin and sodium caseinate counterparts were more stable. All of the nanodispersions showed good stability with respect to temperature changes (30-100 °C) except for the one stabilized by sodium caseinate, which exhibited an increased particle size when heated to above 60 °C. The combination of soy lecithin and sodium caseinate was found to increase the bioaccessibility of the lycopene nanodispersion. The physicochemical properties, stability and extent of the lycopene nanodispersion digestion highly depend on the emulsifier type. Novelty and scientific contribution: Producing a nanodispersion is considered one of the best ways to overcome the poor water solubility, stability and bioavailability issues of lycopene. Currently, studies related to lycopene-fortified delivery systems, particularly in the form of nanodispersion, are still limited. The information obtained on the physicochemical properties, stability and bioaccessibility of lycopene nanodispersion is useful for the development of an effective delivery system for various functional lipids.

9.
Inflammopharmacology ; 31(2): 877-886, 2023 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-36853419

RESUMEN

Bixa orellana L. is a plant popularly known as "ucurum", "annatto", and "achiote". It is native to South America, and its seeds are an abundant source of geranylgeraniol and tocotrienols. Nanoencapsulation is a valuable technique that can decrease the drug needed to achieve an effect, decreasing potential toxicity, side effects and potentiate the anti-inflammatory effect. This study aimed to evaluate the acute toxicity of an intramuscular application of a nanodispersion containing a standardized extract from the seeds of Bixa orellana (NBO) in Wistar rats. The chemical evaluation showed δ-tocotrienol at 0.725 ± 0.062 mg/mL (72.6 ± 0.9%). The stability study showed the nanoparticles had an average size from 53.15 ± 0.64 to 59.9 ± 3.63 nm, with a polydispersity index ranging from 0.574 ± 0.032 to 0.574 ± 0.32, Zeta potential from 18.26 ± 0.59 to 19.66 ± 1.45 mV. After testing the intramuscular application of NBO with doses from 1 to 5 mg/kg in animals, it was observed that the acute treatment did not elicit any toxic effects within this range. The dose of 10 mg/kg, although not affecting hematological and biochemical parameters (CPK, LDH, myoglobin, AST, ALT, TC, TG, glucose levels, creatinine, and urea), could induce some muscle tissue changes, including leukocyte infiltration, morphological chances, and potentially necrosis. In conclusion, the results showed that the treatments devoided toxicity between 1 and 5 mg/kg.


Asunto(s)
Bixaceae , Tocotrienoles , Ratas , Animales , Ratas Wistar , Tocotrienoles/farmacología , Tocotrienoles/uso terapéutico , Antiinflamatorios/toxicidad , Semillas , Extractos Vegetales/toxicidad , Extractos Vegetales/uso terapéutico
10.
J Environ Radioact ; 261: 107135, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-36773552

RESUMEN

A method of obtaining a nanodispersion of nickel-potassium ferrocyanides intended for purification of man-made polluted waters is proposed. It is applicable to purify effluent and floor drain water at nuclear power plants, which contains caesium, strontium, cobalt, manganese and other transition metals. The optimal conditions for the synthesis of nanodispersion have been determined, which is represented by clusters of nanoparticles associated with water molecules and nitrates dispersed in a dilute solution of nickel and potassium nitrates. On the surface of the formed nanocrystals there are fragments of structures of smaller formations. The mechanism of sorption of ions of alkali, alkaline earth and transition metals is investigated considering the ion charge density. The effect of competing ions (strontium, cobalt, manganese) on the sorption of caesium is taken into account. An integrated method of purification of multi-component man-made solutions including drainage waters of nuclear power plants is based on the use of nanodispersion of nickel-potassium ferrocyanides in combination with bentonite clay, which allows removing caesium from the drainage simulator with an efficiency of 96%, and strontium and transition metal ions (cobalt, manganese, copper, iron) with an efficiency of at least 98%.


Asunto(s)
Monitoreo de Radiación , Purificación del Agua , Humanos , Níquel/química , Ferrocianuros/química , Manganeso , Nitratos , Cesio , Cobre/química , Cobalto , Estroncio , Agua/química , Potasio
11.
Environ Res ; 223: 115485, 2023 04 15.
Artículo en Inglés | MEDLINE | ID: mdl-36775087

RESUMEN

Chromium (Cr) is reported to be hazardous to environmental components and surrounding biota when levels exceed allowable thresholds. As Cr is extensively utilized in different industries, thereby comprehensively studied for its toxicity. Along with Cr, the applications of nano-Cr or chromium oxide nanoparticles (Cr2O3-NPs) are also expanding; however, the literature is scarce or limited on their phytotoxicity. Thereby, the current work investigated the morpho-physiological insights of macro- and nanoparticles of Cr in Hordeum vulgare L. plants. The increased accumulation and translocation of Cr under the exposure of both forms disturbed the cellular metabolism that might have inhibited germination and growth as well as interfered with the photosynthesis of plants. The overall extent of toxicity was noticeably higher under nanoparticles' exposure than macroparticles of Cr. The potential cue for such phytotoxic consequences mediated by Cr nanoparticles could be an increased bioavailability of Cr ions which was also supported by their total content, mobility, and factor toxicity index. Besides, to support further these findings, synchrotron X-ray technique was used to reliably identify Cr-containing compounds in the plant tissues. The X-ray spectra of the near spectral region and the far region of the spectrum of K-edge of Cr were obtained, and it was established that the dominant crystalline phase corresponds to Cr2O3 (eskolaite) from the recorded observations. Thus, the obtained results would allow revealing the mechanism of macro- and nanoparticles of Cr induced impacts on plant at the tissue, cellular- and sub-cellular levels.


Asunto(s)
Hordeum , Nanopartículas , Cromo/química , Nanopartículas/toxicidad , Nanopartículas/química , Plantas , Raíces de Plantas/metabolismo
12.
Int J Pharm ; 633: 122612, 2023 Feb 25.
Artículo en Inglés | MEDLINE | ID: mdl-36642349

RESUMEN

This study evaluated the potential of monoolein (MO)-based nanodispersions to promote the cutaneous co-delivery of metformin (MET) and methylene blue (MB) for the treatment of non-melanoma skin cancer. MO-based nanodispersions were obtained using Kolliphor® P407 (KP) and/or sodium cholate (CH), and characterized concerning the structure, thermal stability, ability to disrupt the skin barrier, cutaneous permeation and retention of MB and MET. Additionally, the cytotoxic effect of MO nanodispersions-mediated combination therapy using MET and MB in A431 cells was evaluated. The nanodispersions exhibited nanometric size (<200 nm) and thermal and physical stability. Small angle X-ray scattering studies revealed multiple structures depending on composition. They were able to interact with stratum corneum lipid structure, increasing its fluidity. The effect of MO-nanodispersions on topical/transdermal delivery of MB and MET was composition-dependent. Nanodispersions with low MO content (5 %) and stabilized with KP and CH (0.05-0.10 %) were the most promising, enhancing the cutaneous delivery of MB and MET by 1.9 to 2.2-fold and 1.4 to 1.7-fold, respectively, compared to control. Cytotoxic studies revealed that the most promising MO nanodispersion-mediated combination therapy using MET and MB (1:1) reduced the IC50 by 24-fold, compared to MB solution, and a further reduction (1.5-fold) was observed by MB photoactivation.


Asunto(s)
Metformina , Azul de Metileno , Administración Cutánea , Azul de Metileno/farmacología , Piel , Humanos , Línea Celular Tumoral
13.
Nat Prod Res ; 37(10): 1719-1724, 2023 May.
Artículo en Inglés | MEDLINE | ID: mdl-35921497

RESUMEN

Fruits of Citrus sinensis L. Osbeck var. Valencia contain hesperidin as a major flavanone glycoside. Hesperidin (H) was isolated from the peels of Valencia orange and formulated as hexosomal nanodispersions (F1) adopting the hot emulsification method. The antimycobacterial activity(anti-TB) was evaluated through a microplate Alamar blue (MABA) assay where F1 showed significant activity with MIC = 0.19 µM. To unravel the potential mechanism of the anti-TB, a molecular docking study of H using the Mycobacterial Dihydrofolate reductase (Mtb. DHFR) enzyme was performed. Hesperidin exhibited significant interactions with Mtb. DHFR active site. Sulforhodamine B assay was applied to evaluate cytotoxic activity against the lung cancer cell line (A-549). F1 showed a cytotoxic effect at IC50= 33 µM. It also has potent antiviral activity against Human Coronavirus 229E with IC50= 258.8 µM utilising crystal violet assay. Peels of Valencia orange could be a source of bioactive metabolites to control significant diseases.


Asunto(s)
Antineoplásicos , Citrus sinensis , Hesperidina , Mycobacterium , Humanos , Hesperidina/farmacología , Hesperidina/química , Simulación del Acoplamiento Molecular , Glicósidos/química , Citrus sinensis/química
14.
Int J Nanomedicine ; 17: 6447-6465, 2022.
Artículo en Inglés | MEDLINE | ID: mdl-36573206

RESUMEN

Purpose: Vitamin E (VitE) may be classified in "the first line of defense" against the formation of reactive oxygen species. Its inclusion in nanoemulsions (NEs) is a promising alternative to increase its bioavailability. The aim of this study was to compare O/W NEs including VitE based on Almond or Neem oil, showing themselves antioxidant properties. The potential synergy of the antioxidant activities of oils and vitamin E, co-formulated in NEs, was explored. Patients and Methods: NEs have been prepared by sonication and deeply characterized evaluating size, ζ-potential, morphology (TEM and SAXS analyses), oil nanodroplet feature, and stability. Antioxidant activity has been evaluated in vitro, in non-tumorigenic HaCaT keratinocytes, and in vivo through fluorescence analysis of C. elegans transgenic strain. Moreover, on healthy human volunteers, skin tolerability and anti-inflammatory activity were evaluated by measuring the reduction of the skin erythema induced by the application of a skin chemical irritant (methyl-nicotinate). Results: Results confirm that Vitamin E can be formulated in highly stable NEs showing good antioxidant activity on keratinocyte and on C. elegans. Interestingly, only Neem oil NEs showed some anti-inflammatory activity on healthy volunteers. Conclusion: From the obtained results, Neem over Almond oil is a more appropriate candidate for further studies on this application.


Asunto(s)
Antioxidantes , Vitamina E , Animales , Humanos , Antioxidantes/farmacología , Antioxidantes/química , Vitamina E/farmacología , Caenorhabditis elegans , Dispersión del Ángulo Pequeño , Difracción de Rayos X , Emulsiones/química
15.
Int J Pharm ; 620: 121770, 2022 May 25.
Artículo en Inglés | MEDLINE | ID: mdl-35483618

RESUMEN

Natural aglycones, a major ingredient accompanied by glycosides in plants, have played an important role in the treatment of various diseases. However, their bioavailability is limited by their poor water solubility. In contrast to previous efforts that required the use of new exotic materials which may raise concerns about biocompatibility, we report the first case of excipient-free nanodispersions in which an insoluble glycyrrhetinic acid (GA) assembled with its amphiphilic parent drug diammonium glycyrrhizinate (DG) into water-dispersible nanodispersions (130.8 nm for particle size and 91.74% for encapsulation efficiency). This strategy largely increased GA's water apparent solubility by hundreds of times to 549.0 µg/mL with a high cumulative dissolution percentage in vitro greater than 80% in 5 min. The study on the formation mechanism showed that the OH, C-O and C=O group stretching peaks shifted in the FTIR spectra of GA-DG nanodispersions, while the COOH peak (δ COOH 12.19 ppm) disappeared in the 1H NMR spectrum of GA-DG nanodispersions, indicating that carboxyl groups on GA may interact with the hydroxyl groups of DG in solution. Molecular dynamics simulations suggested that both hydrophobic interactions and hydrogen-bond interactions contribute to the coassembly of GA and DG molecules in aqueous solution. Oral pharmacokinetic studies in rats demonstrated that such nanodispersions have a significant increase in Cmax and AUC0-t of 2.45- and 3.45-fold compared with those for GA, respectively. Therefore, this strategy, employing amphiphilic glycosides as excipients to prepare nanodispersions, not using new materials, paves the way for the further application of hydrophobic aglycone drugs.


Asunto(s)
Excipientes , Ácido Glicirretínico , Animales , Disponibilidad Biológica , Excipientes/química , Glicósidos , Ácido Glicirrínico , Interacciones Hidrofóbicas e Hidrofílicas , Ratas , Agua
16.
Food Chem ; 382: 132300, 2022 Jul 15.
Artículo en Inglés | MEDLINE | ID: mdl-35134726

RESUMEN

Concentrated γ-Oryzanol nanodispersions were fabricated using milli-Q water (no emulsifier) or 0.1% (w/w) polysorbate 80 (T80), modified lecithin (ML) or sodium caseinate (SC) as emulsifiers. The freshly prepared nanodispersions had comparable particle diameter (118 to 157 nm), γ-Oryzanol concentration (1.75 to 1.92 mg mL-1) and free-radical scavenging activity (59 to 62%) and had negative ζ-potentials (-22 to -59 mV), indicating that both γ-Oryzanol and emulsifier coexisted on the particles' interface. The nanoparticles had superior physicochemical stability up to 30 days of storage at 5 °C and were successfully autoclaved without excessive growth or aggregation. Nevertheless, they showed distinct physical stability upon storage at specific environmental conditions, which affected their In-vitro gastrointestinal digestion. Comprehensively, emulsifier-free nanodispersions were sensitive to acidic pH, NaCl and CaCl2 addition. ML and SC coated nanoparticles were sensitive to Ca2+ ions, while T80 stabilized nanodispersions resisted to all environmental stresses, resulting in optimal simulated intestinal absorption.


Asunto(s)
Emulsionantes , Fenilpropionatos , Emulsiones , Tamaño de la Partícula , Solventes
17.
Braz. J. Pharm. Sci. (Online) ; 58: e191093, 2022. tab, graf
Artículo en Inglés | LILACS | ID: biblio-1383999

RESUMEN

Abstract In recent years, improvements have been made, through biotechnological processes, in the production and development of peptides capable of increasing collagen and elastin synthesis for anti-aging skin care. However, proteins have many limitations due to their structural, chemical and physical fragility to external aggressions, which may cause conformational changes, leading to loss of biological activity. Therefore, it is important to create delivery systems that protect these biomolecules from damage, allowing them to reach their target. This work aimed to develop a system able to carry bovine serum albumin (BSA), used as a model of a protein, and to incorporate this system in a semisolid formulation suitable for skin application. A microemulgel based on a solid-in-oil-in-water (S/O/W) microemulsion was prepared. Firstly, the association efficiency (AE) of lyophilized BSA-sucrose ester complex and the size of S/O nanodispersion were assessed; then, the characterization and stability evaluation of the final semisolid formulation through evaluation of pH, texture and rheological behavior were performed. The average value of AE was 54.74% ± 2.17. It was possible to develop an S/O/W microemulsion, which allowed the subsequent development of an S/O/W microemulgel that assured suitable pH, texture and rheological characteristics for skin application.


Asunto(s)
Albúmina Sérica Bovina , Proteínas/efectos adversos , Colágeno , Péptidos/agonistas , Piel/efectos de los fármacos , Productos Biológicos , Envejecimiento , Concentración de Iones de Hidrógeno
18.
Polymers (Basel) ; 13(22)2021 Nov 17.
Artículo en Inglés | MEDLINE | ID: mdl-34833265

RESUMEN

The influence of a nanodispersion of TiO2 in water (nanoparticle size: 40 nm, polydispersity index: 0.25), brushed on a Paraloid film and subjected to UV-Vis irradiation was evaluated. The TiO2 nanodispersions showed a tendency to reduce the molecular weight of Paraloid due to its photocatalytic properties. FTIR and GPC analyses and SEM images suggested the degradation of the polymer, while chromatic variations of the films were scarcely detected. This study is very remarkable in the perspective of using this material for the removal of polymeric films used in conservation.

19.
Pharmaceutics ; 13(11)2021 Nov 18.
Artículo en Inglés | MEDLINE | ID: mdl-34834368

RESUMEN

Natural polyelectrolytes, including in the form of complexes with colloidal particles, are increasingly used in pharmacy due to the possibility of regulated attachment of medicinal substances and their targeted delivery to the target organ. However, the formation, stability, and molecular-mass characteristics of polyelectrolyte nanodispersions (ND) vary depending on the nature and composition of the medium of their origin. This is due to the lack of standardized approaches to quality control and regulatory documentation for most natural ND. In this paper, we first introduced the isolation, followed by investigations into their physico-chemical properties and bioactivity. Using the dried droplet method, we were able to detect the "coffee ring effect". Fractographic studies of the surface structure of EHA and FA dried samples using SEM showed its heterogeneity and the presence of submicron particles encapsulated in the internal molecular cavities of polyelectrolyte. FTIR spectroscopy revealed the ND chemical structure of benzo-α-pyron and benzo-γ-pyron, consisting of nanoparticles and a branched frame part. The main elements detected by X-ray fluorescence in humic substance extract and fulvic acid include Si, P, S, K, Ca, Mn, Fe, Cu, Zn, whereas Fe is in high concentrations. The UV-spectra and fluorescent radiation demonstrated the possibility of studying the effect of the fulvate chromone structure on its optical properties. It is shown that dilution of the initial solutions of polyelectrolytes 1:10 contributes to the detection of smaller nanoparticles and an increase in the absolute value of the negative ζ-potential as a factor of ND stability. A study of the EHS effect on the SARS-CoV-2 virus infectious titer in the Vero E6 cell showed the effective against virus both in the virucidal scheme (the SI is 11.90-22.43) and treatment/prevention scheme (the SI is 34.85-57.33). We assume that polyelectrolyte ND prevent the binding of the coronavirus spike glycoprotein to the receptor. Taking into account the results obtained, we expect that the developed approach can become unified for the standardization of the ND natural polyelectrolytes complex, which has great prospects for use in pharmacy and medicine as a drug with antiviral activity.

20.
Curr Top Med Chem ; 21(2): 140-150, 2021.
Artículo en Inglés | MEDLINE | ID: mdl-32888268

RESUMEN

AIMS: The present work aimed to develop MT loaded solid Nano dispersion by improving its solubility, half-life and bioavailability in biological system thereby this formulation may be afforded economically. BACKGROUND: Small cell lung carcinoma is a type of malignant tumor characterized by uncontrolled cell growth at lung tissues. The potent anti-cancer drug methotrexate (MT) chosen for the present work is poorly soluble in water (BCS type IV class) with short half-life and hepatotoxic effect. OBJECTIVE: With the concept of polymeric surfactant to improve the solubility along with wettability of drugs, the present work has been hypothesized to improve its solubility using polyvinyl pyrollidone (PVP K30) polymer and α- tocopheryl polyethylene glycol 1000 succinate (TPGS) surfactant, thereby the bioavailability is expected to get enhanced. By varying the PVP K30 and TPGS ratios different formulations were developed using emulsification process. METHODS: The developed MT loaded solid nanodispersion was further characterized for its particle size, charge, morphology, encapsulation efficiency and in-vitro release behavior etc. Results: The results of FT-IR spectrometric analysis indicated the compatibility nature of MTX, PVPK30 and TPGS. The developed formulations showed spherical morphology, particle size ranging from 59.28±24.2 nm to 169.33±10.85 nm with a surface charge ranging from -10.33 ± 2.81mV to -9.57 ± 1.2 mV. The in vitro release studies as performed by dialysis bag method showed a sustained release pattern as checked by UV Spectrophotometer. Residual solvent analysis for MTXNDs performed by HPLC indicates there is no residual DMSO in the formulation. Transmission electron microscopic image of MTXNDs revealed that the particles are spherical shaped with a solid core structure. Haemolytic assay indicates that the developed formulation is safe for intravenous administration. Cell culture studies in A549 cells indicates the enhanced cytotoxic effect for the developed formulation. CONCLUSION: This proof of study indicates that the developed formulation may have anticancer potential for SCLC treatment.


Asunto(s)
Antimetabolitos Antineoplásicos/farmacología , Neoplasias Pulmonares/tratamiento farmacológico , Metotrexato/farmacología , Polímeros/química , Carcinoma Pulmonar de Células Pequeñas/tratamiento farmacológico , Tensoactivos/química , Células A549 , Antimetabolitos Antineoplásicos/química , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Humanos , Neoplasias Pulmonares/patología , Metotrexato/química , Nanomedicina , Nanopartículas/química , Tamaño de la Partícula , Carcinoma Pulmonar de Células Pequeñas/patología , Solubilidad , Agua/química
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