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PloS One 2024This retrospective study aimed to evaluate the effects on the clinical signs of poisoning and adverse effects of intravenous lipid emulsion treatment in 82 animals (dogs...
This retrospective study aimed to evaluate the effects on the clinical signs of poisoning and adverse effects of intravenous lipid emulsion treatment in 82 animals (dogs and cats) with suspected poisonings over 18 months. Physical examination parameters and state of consciousness were documented every hour after the intravenous administration of a bolus of 2 ml/kg and 0.25 ml/kg/min over 60 minutes of a 20% intravenous lipid emulsion. The modified Glasgow coma scale and laboratory findings (blood gas analysis, triglyceride, lactate) were evaluated initially and three hours after discontinuing intravenous lipid emulsion administration. A statistical evaluation of the occurrence of adverse effects and the development of laboratory values was performed. A decrease in respiratory rate in the second control (8-12 hours) after ILE was observed. Three hours after completing of the intravenous lipid emulsion, triglyceride concentration increased about 10 times (p <0.001). Venous carbon dioxide partial pressure, bicarbonate, base excess, as well as the electrolytes sodium, potassium and ionized calcium decreased significantly (p <0.001). Patients who experienced a worsening of the modified Glasgow coma scale had a higher increase in triglyceride concentrations (p = 0.041) and plasma lactate (p = 0.034) and a larger decrease in bicarbonate concentrations (p = 0.053) compared to others. About 54% (n = 44) of the patients showed adverse effects which could be attributed to the administration of intravenous lipid emulsion and may be associated with a higher triglyceride increase. All of them were completely reversible within 33 hours. Adverse effects associated with intravenous lipid emulsion therapy were observed in half of the patients and were associated with a higher increase in triglycerides.
Topics: Animals; Fat Emulsions, Intravenous; Cats; Dogs; Retrospective Studies; Male; Female; Poisoning; Triglycerides; Glasgow Coma Scale; Cat Diseases; Dog Diseases; Blood Gas Analysis
PubMed: 38809887
DOI: 10.1371/journal.pone.0298828 -
International Journal of Environmental... Sep 2014Several obstacles are encountered in conventional chemotherapy, such as drug toxicity and poor stability. Nanotechnology is envisioned as a strategy to overcome these...
Several obstacles are encountered in conventional chemotherapy, such as drug toxicity and poor stability. Nanotechnology is envisioned as a strategy to overcome these effects and to improve anticancer therapy. Nanoemulsions comprise submicron emulsions composed of biocompatible lipids, and present a large surface area revealing interesting physical properties. Chalcones are flavonoid precursors, and have been studied as cytotoxic drugs for leukemia cells that induce cell death by different apoptosis pathways. In this study, we encapsulated chalcones in a nanoemulsion and compared their effect with the respective free compounds in leukemia and in non-tumoral cell lines, as well as in an in vivo model. Free and loaded-nanoemulsion chalcones induced a similar anti-leukemic effect. Free chalcones induced higher toxicity in VERO cells than chalcones-loaded nanoemulsions. Similar results were observed in vivo. Free chalcones induced a reduction in weight gain and liver injuries, evidenced by oxidative stress, as well as an inflammatory response. Considering the high toxicity and the side effects induced generally by all cancer chemotherapies, nanotechnology provides some options for improving patients' life quality and/or increasing survival rates.
Topics: Animals; Antineoplastic Agents; Chalcones; Chlorocebus aethiops; Drug Delivery Systems; Emulsions; In Vitro Techniques; Leukemia; Leukemia L1210; Liver; Male; Mice; Molecular Targeted Therapy; Nanoparticles; Oxidative Stress; Vero Cells
PubMed: 25264679
DOI: 10.3390/ijerph111010016 -
Biomaterials Science Feb 2021Emulsion electrospinning is a versatile technique used to create fibrous meshes for applications in drug delivery and tissue engineering. In this study, the effects of...
Emulsion electrospinning is a versatile technique used to create fibrous meshes for applications in drug delivery and tissue engineering. In this study, the effects of surfactant and increasing internal phase volume fraction on emulsion electrospun fiber morphology were investigated. The fiber diameter, surface topography, internal architecture, mesh hydrophobicity, and fiber volume fraction were all characterized and the resulting effects on model drug release and cell response were determined. Surfactant relocation to the fiber surface resulted in alterations to fiber surface topography and internal morphology, increased rate of water adsorption into the mesh, and reduced burst effects of drug release. Increasing the internal phase volume fraction within the emulsion resulted in minimal change to fiber diameter, surface morphology, fiber volume fraction, and rate of water adsorption illustrating the ability to increase drug loading without affecting fiber properties. Lastly, all meshes promoted cell adhesion and good viability with a trend of increased MTT absorbance from cells on the surfactant and emulsion fibers possibly suggesting that an increase in surface area via smaller fiber diameter and fiber volume fraction increases metabolic activity. Overall, these studies indicate that fiber morphology and mesh hydrophobicity can be tuned by controlling surfactant location within fibers and internal phase volume fraction. Modulating fiber properties within the emulsion electrospun mesh is important to achieve controlled drug release and cell response for tissue engineering applications.
Topics: Cell Adhesion; Drug Liberation; Emulsions; Surface-Active Agents; Tissue Engineering
PubMed: 33393536
DOI: 10.1039/d0bm01751e -
Molecules (Basel, Switzerland) Oct 2022Cantharidin (CTD) is the major component of anticancer drugs obtained from and has a good inhibitory effect on several cancers, including hepatocellular carcinoma (HCC)...
Cantharidin (CTD) is the major component of anticancer drugs obtained from and has a good inhibitory effect on several cancers, including hepatocellular carcinoma (HCC) and breast cancer. However, due to its toxicity, oral administration can cause various adverse reactions, limiting its clinical application. The aim of this work was to design glycyrrhetinic acid (GA)- and/or folate (FA)-modified solid lipid nanoparticles (SLNs) for the encapsulation of CTD to target HCC. Four CTD-loaded SLNs (cantharidin solid lipid nanoparticles (CSLNs), glycyrrhetinic acid-modified cantharidin solid lipid nanoparticles (GA-CSLNs), folate-modified cantharidin solid lipid nanoparticles (FA-CSLNs), and glycyrrhetinic acid and folate-modified cantharidin solid lipid nanoparticles (GA-FA-CSLNs)) were prepared by the emulsion ultrasonic dispersion method, and their physicochemical parameters were determined (particle size and distribution, morphology, zeta-potential, entrapment efficiency, drug loading, and hemolysis). Additionally, the antitumor activities of the four SLNs were evaluated comprehensively by tests for cytotoxicity, cell migration, cell cycle, apoptosis, cellular uptake, competition suppression assay, and in vivo tumor suppression assay. Four SLNs showed spherical shapes and mean diameters in the range of 75-110 nm with size dispersion (PDI) within the range of 0.19-0.50 and zeta-potential approximately -10 mV. The entrapment efficiency of CTD in SLNs was higher than 95% for all tested formulations, and no hemolysis was observed. Compared to GA-CSLNs or CSLNs, GA-FA-CSLNs and FA-CSLNs showed stronger cytotoxicity on hepatocellular carcinoma cells (HepG2), and the cytotoxicity of GA-FA-CSLNs on hepatocyte cells (L-02) was remarkably reduced compared with other formulations. GA-FA-CSLNs and FA-CSLNs also increased the inhibition of HepG2 cell migration, and FA-CSLNs had the highest apoptosis rate. The cell cycle results indicated that HepG2 cells were arrested mainly in the S phase and G2/M phase. Analysis of competition inhibition experiments showed that GA and FA ligands had targeted effects on HepG2 cells. The in vivo tumor inhibition experiment showed that GA-FA-CSLNs and FA-CSLNs had excellent tumor inhibition ability-their tumor inhibition rates were 96.46% and 89.92%, respectively. Our results indicate that GA-FA-CSLNs and FA-CSLNs have a promising future in the therapeutic intervention of HCC.
Topics: Humans; Carcinoma, Hepatocellular; Glycyrrhetinic Acid; Cantharidin; Folic Acid; Emulsions; Liver Neoplasms; Nanoparticles; Particle Size; Antineoplastic Agents; Drug Carriers
PubMed: 36296377
DOI: 10.3390/molecules27206786 -
Drug Delivery Dec 2023Intratympanic administration for the delivery of steroids has been extensively studied but limited because of low permeability of the drug through the row window...
Intratympanic administration for the delivery of steroids has been extensively studied but limited because of low permeability of the drug through the row window membrane. Here, to effectively deliver poorly soluble triamcinolone acetonide (TA), microemulsions (ME) were prepared from Capmul MCM (oil), Cremophor RH40 (surfactant), and tetraglycol (cosurfactant) based on solubility studies, emulsifying ability test, and pseudoternary phase diagrams. Microemulsion gel (MEG) was prepared by mixing TA-ME with a poloxamer hydrogel base. The physicochemical properties of ME and MEG formulations were characterized, and the toxicity and oto-protective effectiveness were evaluated in vitro and in vivo. The ME-3 formulation showed a small droplet size (16.5 ± 0.2 nm), narrow PDI (0.067 ± 0.041), and enhanced TA solubility (2619.7 ± 57.6 μg/g). The optimized MEG demonstrated temperature-dependent gelation with a gelation time of 208 ± 10 sec at 37 °C. Slow degradation of the gel matrix sustained release of TA from MEG compared to the ME formulation. Both TA-ME and TA-MEG were found to be nontoxic to NIH3T3 cells at the test concentrations (0 to 5 µg/mL), and biocompatible after intratympanic administration to mice. The incorporation of ME into thermosensitive hydrogels prolonged retention of TA at the site of administration until 6 days. As a consequence, the enhanced drug absorption into the cochlea in TA-MEG group (approximately 2 times higher than other groups) protected hair cells, spiral ganglion neurons, and stria vascular cells from cisplatin-induced damage. Therefore, this injectable TA-loaded MEG is an effective and safe vehicle for the sustained delivery of triamcinolone acetonide into the inner ear.
Topics: Mice; Animals; Triamcinolone Acetonide; NIH 3T3 Cells; Hydrogels; Surface-Active Agents; Hearing Loss, Sensorineural; Emulsions
PubMed: 37537864
DOI: 10.1080/10717544.2023.2242003 -
Food Research International (Ottawa,... Mar 2021Bioactive carrier systems produced from natural and biodegradable compounds offer diverse applications in the food and drug sector, whether for protection, controlled...
Bioactive carrier systems produced from natural and biodegradable compounds offer diverse applications in the food and drug sector, whether for protection, controlled delivery, texture modification or insertion of lipid compounds into aqueous systems. This study aimed to produce emulsion-filled hydrogels by sonication followed by ionic gelation, containing potato starch as the main compound (gelatinized or native), a low alginate concentration, and gelatin in the continuous phase. Emulsion-filled hydrogels were evaluated regarding chemical and physical structure, as well as morphology of hydrogels after simulated digestion. Slight intensity differences were observed between the FTIR spectra of hydrogels, reflecting water absorption, amorphous and crystalline structures. The chemical characteristics of hydrogels influenced the microstructure and stress at fracture. Hydrogel produced with gelatinized starch was harder than hydrogel with non-gelatinized starch. Regarding digestion assay, we postulated that alginate-gelatin network was degraded by swelling, while alginate-gelatin-starch gels were associated with an erosion mechanism, since its microstructure remained partially stable, only exposing the oil droplets at surface. These findings can provide different delivery and protection mechanisms, allowing varied applications.
Topics: Alginates; Emulsions; Gelatin; Hydrogels; Starch
PubMed: 33641959
DOI: 10.1016/j.foodres.2020.110059 -
Frontiers in Bioscience (Landmark... Dec 2023Among lipid-based formulations, self-nanoemulsifying drug delivery systems (SNEDDS) have captured a spotlight, captivating both academia and the pharmaceutical industry....
BACKGROUND
Among lipid-based formulations, self-nanoemulsifying drug delivery systems (SNEDDS) have captured a spotlight, captivating both academia and the pharmaceutical industry. These remarkable formulations offer a valuable option, yet their liquid form presents certain challenges for delivering poorly soluble drugs. Ensuring compatibility with capsule shells, maintaining physical and chemical stability, and understanding their impact on lipolysis remain vital areas of exploration. Therefore, the incorporation of this liquid formulation into a solid dosage form (S-SNEDDS) is compelling and desirable. S-SNEDDSs, prepared by adsorption, enhances formulation stability but retards drug dissolution. This study aims to design drug-free solid S-SNEDDS + solid dispersion (SD) as a novel combination to enhance cinnarizine (CN) stability upon storage while maintaining enhanced drug dissolution.
METHODS
Drug-free liquid SNEDDSs were solidified using Neusilin® US2 at a 1:1 ratio. CN-SDs were prepared using freeze-drying technology. The SDs that were developed underwent characterization using various techniques, including scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), and Fourier transform infrared spectroscopy (FTIR). lipolysis studies were conducted to evaluate the effect of the combined system on the performance of the formulation upon exposure to enzymes within biorelevant media.
RESULTS
In agreement with the DSC and XRD results, FTIR confirmed the amorphization of CN within the freeze-dried solid dispersion (FD-SD) systems. The lipolysis studies showed that the drug-free S-SNEDDS + SD combination was able to maintain a significant portion of the initial CN in solution even in the presence of lipase for up to 30 min. The accelerated stability studies showed that the drug-free S-SNEDDS + SD combination maintained 96% intact CN in an amorphous state and more than 90% release at pH 1.2 for up to 6 months, while the dissolution profile at pH 6.8 showed a significant drop in CN release upon storage.
CONCLUSIONS
Overall, the developed formulation could be a potential technique to enhance the dissolution of weakly basic drugs that possess challenging stability limitations.
Topics: Solubility; Emulsions; Drug Delivery Systems; Drug Liberation; Microscopy, Electron, Scanning; Particle Size; Nanoparticles
PubMed: 38179768
DOI: 10.31083/j.fbl2812349 -
Translational Vision Science &... May 2022The aim of this study was to develop a nanogel emulsion as a minimally invasive, safe, and effective treatment alternative for posterior ocular diseases.
PURPOSE
The aim of this study was to develop a nanogel emulsion as a minimally invasive, safe, and effective treatment alternative for posterior ocular diseases.
METHODS
A gel-in-water (G/W) nanoemulsion was developed by ultrasonication using beeswax as an organogelator. Different physicochemical properties were evaluated along with particle size analysis by dynamic light scattering. In vitro biocompatibility of G/W nanoemulsion using rat hepatocytes and human umbilical vein endothelial cells (HUVECs) and in vivo corneal permeability as eye drops were investigated.
RESULTS
The nanogel emulsion was monodispersed with a polydispersity index and particle diameter of approximately 0.2 and 200 nm, respectively. The zeta potential value of -8.1 mV suggested enhanced stability and improved retinal permeability of nanoparticles. The prepared nanoemulsion was found to be biocompatible with hepatocytes and HUVECs in vitro. Moreover, in vivo study demonstrated high permeability of G/W nanoemulsion to the retinal layer with no ocular irritation.
CONCLUSIONS
G/W nanoemulsions have the potential for topical drug delivery in the posterior eye segment with maximum therapeutic efficacy.
TRANSLATIONAL RELEVANCE
Organogel nanodispersion is a new concept to deliver hydrophobic drugs to the posterior segment of eyes as a novel drug delivery system.
Topics: Animals; Drug Delivery Systems; Emulsions; Endothelial Cells; Nanogels; Rats; Water
PubMed: 35576213
DOI: 10.1167/tvst.11.5.16 -
Molecules (Basel, Switzerland) May 2022Emulsion electrospinning is a method of modifying a fibers' surface and functional properties by encapsulation of the bioactive molecules. In our studies, bovine serum...
Emulsion electrospinning is a method of modifying a fibers' surface and functional properties by encapsulation of the bioactive molecules. In our studies, bovine serum albumin (BSA) played the role of the modifier, and to protect the protein during the electrospinning process, the W/O (water-in-oil) emulsions were prepared, consisting of polymer and micelles formed from BSA and anionic (sodium dodecyl sulfate-S) or nonionic (Tween 80-T) surfactant. It was found that the micelle size distribution was strongly dependent on the nature and the amount of the surfactant, indicating that a higher concentration of the surfactant results in a higher tendency to form smaller micelles (4-9 µm for S and 8-13 µm for T). The appearance of anionic surfactant micelles reduced the diameter of the fiber (100-700 nm) and the wettability of the nonwoven surface (up to 77°) compared to un-modified PCL polymer fibers (100-900 nm and 130°). The use of a non-ionic surfactant resulted in better loading efficiency of micelles with albumin (about 90%), lower wettability of the nonwoven fabric (about 25°) and the formation of larger fibers (100-1100 nm). X-ray photoelectron spectroscopy (XPS) was used to detect the presence of the protein, and UV-Vis spectrophotometry was used to determine the loading efficiency and the nature of the release. The results showed that the location of the micelles influenced the release profiles of the protein, and the materials modified with micelles with the nonionic surfactant showed no burst release. The release kinetics was characteristic of the zero-order release model compared to anionic surfactants. The selected surfactant concentrations did not adversely affect the biological properties of fibrous substrates, such as high viability and low cytotoxicity of RAW macrophages 264.7.
Topics: Emulsions; Excipients; Lipoproteins; Micelles; Polymers; Pulmonary Surfactants; Serum Albumin, Bovine; Surface-Active Agents
PubMed: 35630708
DOI: 10.3390/molecules27103232 -
Contact Lens & Anterior Eye : the... Aug 2019To investigate the effects of a sea buckthorn oil and sodium hyaluronate-containing eyelid spray emulsion (SB spray) on dry eye. (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
To investigate the effects of a sea buckthorn oil and sodium hyaluronate-containing eyelid spray emulsion (SB spray) on dry eye.
METHODS
A randomized controlled study was carried out. Adults (25-70 years) with Ocular Surface Disease Index (OSDI) ≥20 and moderate or severe dryness, burning or grittiness of the eyes were included. In study part one (n = 2), SB spray was used on both closed eyelids four times in one day. In part two (n = 10), SB spray was used on one randomized eyelid, and a commercial reference spray on the other for nine days. In part three (n = 40), eyes were randomized to one eye receiving SB spray and an untreated control for 1.5 months. Dry eye tests were carried out at baseline, during, and at the end of each study section. Symptoms were recorded in questionnaires and daily logs.
RESULTS
In part one, the SB spray was well tolerated. In part two, OSDI decreased significantly (P = 0.022) in the SB spray eye compared to the reference spray, indicating a beneficial effect on symptoms. In part three, OSDI in the SB spray eye decreased significantly compared to the untreated control (P = 0.0007). The scores for dryness at the study end were lower in the SB spray eye compared to control (P = 0.0070). Symptom sums and frequencies of dryness (sum P = 0.0046, frequency P = 0.0016) and watering (sum P = 0.0003, frequency P = 0.013) in the daily logs were lower in the eye treated with SB spray.
CONCLUSIONS
SB spray on closed eyelids relieved the symptoms of dry eye.
Topics: Adult; Aerosols; Aged; Dry Eye Syndromes; Emulsions; Female; Hippophae; Humans; Hyaluronic Acid; Male; Middle Aged; Nebulizers and Vaporizers; Ophthalmic Solutions; Osmolar Concentration; Plant Oils; Seeds; Surveys and Questionnaires; Tears
PubMed: 30497904
DOI: 10.1016/j.clae.2018.11.011