Nanoemulsion Technology Research Articles

Development of Innovative Cosmetic Formulations to Help Fungal Treatment and Testing the Efficiency of Formulations

In the fungus of hands and toenails, the thickening of the nail and its yellow color are the first signs of attention. Fungus on the nails of the hands and feet is often caused by Trichophyton rubrum dermatophyte. They have antifungal properties due to the components found in lavender oil, geranium oil and tea tree oil structures. Oral antifungal agents used for treatment of nail fungi have serious side effects especially on liver. Therefore, topical applications have been given importance in recent years. However, in topical applications antifungal agents have difficulties in sending to the target area. For this reason, nanoemulsion technology was preferred in the study. Nanoemulsion formulations of essential oils were prepared using ultrasonication method. Centrifugal and thermal test were applied as preliminary stability to the formulations and the pH value, viscosity, droplet size and polidispersity index of the formulations passing this step were measured and organoleptic controls were performed. Antifungal efficacy and release studies were performed on the formulations F4P3-I (pelargonium), F4P3-L (lavender), F4P3-C (tea tree) and F4P3-K (mixture) which were successful as a result of all the tests. According to the study, it was concluded that F4P3-I, F4P3-L, F4P3-Ç, F4P3-K formulations may help in the treatment of fungi.

Arterial Elasticity: Linking of Cardiovascular Risks, Pulse Pressure, Dementia, Aging, and Drug Targeting

Cerebrovascular atherosclerosis, and several other cardiovascular (or "inflamm-aging" type) diseases, are more frequent and advanced in subjects with Alzheimer's disease compared with normal aging. In addition, the observed pathogenic link to dementia (and its associated cerebral microvascular damage) is readily explained by alterations of arterial elasticity. A therapeutic strategy to delay dementia could be based upon localized drug delivery, using lipid nanocarriers (i.e., biobased nanoemulsion technology), targeted toward a major serum amyloid A (SAA) receptor involved in certain proinflammatory, SAA-mediated, cell signaling events. Moreover, by incorporating drug molecules into such lipid nanocarriers, one can obtain a "combination therapeutic" capable of targeting simultaneously (via cell-surface scavenger receptors) a variety of cell types, each potentially implicated in Alzheimer's disease and/or dementia, for focused drug delivery in vivo.

Nanoemulsion and Solid Nanoemulsion for Improving Oral Delivery of a Breast Cancer Drug: Formulation, Evaluation, and a Comparison Study

Letrozole (LZ) is an aromatase inhibitor, which inhibits the formation of estrogens from androgens. Nanoemulsion is a liquid emulsion formulation utilized to increase solubility, bioavailability, and drug delivery to cancer cells. This study aims to improve LZ oral delivery through formulating solid nanoemulsion (SNE). Peppermint oil, tween 80, and transcutol P were used as an oil, surfactant, and co-surfactant, respectively. The optimized nanoemulsion (NE-3) was then incorporated into solid polyethylene glycol (PEG) to formulate (SNE). The optimized (NE-3), SNE-2, and the available marketed tablet have been compared. The optimized (NE-3) was selected according to specific parameters of optimum small nano-size 80 nm, PDI of 0.181, the zeta potential of-98.2, high transmittance (99.78%), optimum pH (5.6), a high percent of LZ content (99.03 ± 1.90), the relatively low viscosity of 60.2 mPa.s, and a rapid release of LZ within 30 min. NE-3 was selected to be formulated as SNE. LZ's best release rate was 80% in 5 min with a content homogeneity of 99.85 ± 0.04 for SNE-2. Zero-order kinetics is determined to have the greatest R2 values. Field emission scanning electron microscopy (FE-SEM) detected that SNE-2 was (36.75–96.64 nm) with a spherical form and no adhesion or aggregation. FT-IR showed no significant variations in position and shape of the absorption peaks between the pure drug and optimal formulation diagrams. This novel nanoemulsion technology aids in improving the solubility of poorly water-soluble drugs, particularly the SNE delivery method, which has a higher in-vitro release rate and expiration date of LZ than others.

Shape-Controlled Nanoparticles from a Low-Energy Nanoemulsion.

Nanoemulsion technology enables the production of uniform nanoparticles for a wide range of applications. However, existing nanoemulsion strategies are limited to the production of spherical nanoparticles. Here, we describe a low-energy nanoemulsion method to produce nanoparticles with various morphologies. By selecting a macro-RAFT agent (poly(di(ethylene glycol) ethyl ether methacrylate-co-N-(2-hydroxypropyl) methacrylamide) (P(DEGMA-co-HPMA))) that dramatically lowers the interfacial tension between monomer droplets and water, we can easily produce nanoemulsions at room temperature by manual shaking for a few seconds. With the addition of a common ionic surfactant (SDS), these nanoscale droplets are robustly stabilized at both the formation and elevated temperatures. Upon polymerization, we produce well-defined block copolymers forming nanoparticles with a wide range of controlled morphologies, including spheres, worm balls, worms, and vesicles. Our nanoemulsion polymerization is robust and well-controlled even without stirring or external deoxygenation. This method significantly expands the toolbox and availability of nanoemulsions and their tailor-made polymeric nanomaterials.

Nanemulsions of foodstuffs and their nutritiological and valleological characteristics

Annotation. The use of nanotechnology in the medical, food, pharmaceutical, biotechnology industries today is an important scientific progress and valuable human heritage. Nanoemulsion technology is an ideal method for the manufacture of encapsulating systems for functional compounds, as it prevents their biotechnological biodegradation and improves their functional availability in the cells of the body. The aim of the article is a scientific-theoretical and practical review of the nutritional and valeological properties of nanoemulsions, their use for encapsulation of various nutraceuticals, namely fat-soluble vitamin D. The in vitro experiment was performed using Franz diffusion cells to study the release of bioactive compounds from nanocarriers. The cytotoxicity of nanoemulsions was investigated by analyzing the proliferation of thiazolyl blue tetrazolium bromide (TTB) cells and nasal epithelial cells as an “in vitro” model. The article provides to characterize the nutritional and valeological properties of nanoemulsions and to experimentally investigate hydrogels based on nanoemulsions as biocarriers of vitaminized compounds. During the study, low- and high-energy nanoemulsions were created, which were used for encapsulation of vitamin D3 and biologically active supplement - curcumin. Loaded nanoemulsions are added to homopolymer and copolymer hydrogels based on polysaccharides and their combinations. Both nanoemulsions and hydrogels are structurally characterized to evaluate the effect of the composition on the emulsification process by their properties. The cytotoxic effect of nanoemulsions "in vitro" on the epithelium of nasal cells, which had a positive therapeutic effect, was studied. In the future, further exploration and research will investigate the use of nanoemulsions as biocarriers for other vitamins and bioactive substances.

Water-in-Oil Nano-Emulsions Prepared by Spontaneous Emulsification: New Insights on the Formulation Process.

Nano-emulsions consist of stable suspensions of nano-scaled droplets that have huge loading capacities and are formulated with safe compounds. For these reasons, a large number of studies have described the potential uses of nano-emulsions, focusing on various aspects such as formulation processes, loading capabilities, and surface modifications. These studies typically concern direct nano-emulsions (i.e., oil-in-water), whereas studies on reverse nano-emulsions (i.e., water-in-oil) remain anecdotal. However, reverse nano-emulsion technology is very promising (e.g., as an alternative to liposome technology) for the development of drug delivery systems that encapsulate hydrophilic compounds within double droplets. The spontaneous emulsification process has the added advantages of optimization of the energetic yield, potential for industrial scale-up, improved loading capabilities, and preservation of fragile compounds targeted for encapsulation. In this study, we propose a detailed investigation of the processes and formulation parameters involved in the spontaneous nano-emulsification that produces water-in-oil nano-emulsions. The following details were addressed: (i) the order of mixing of the different compounds (method A and method B), (ii) mixing rates, (iii) amount of surfactants, (iv) type and mixture of surfactants, (v) amount of dispersed phase, and (vi) influence of the nature of the oil. The results emphasized the effects of the formulation parameters (e.g., the volume fraction of the dispersed phase, nature or concentration of surfactant, or nature of the oil) on the nature and properties of the nano-emulsions formed.

Nanoemulsion of Minthostachys verticillata essential oil. In-vitro evaluation of its antibacterial activity

Infectious diseases constitute a problem of great importance for animal and human health, as well as the increasing bacterial resistance to antibiotics. In this context, medicinal plants emerge as an effective alternative to replace the use antibiotics. The essential oil (EO) of Minthostachys verticillata (Griseb.) Epling (Lamiaceae) has demonstrated a strong antimicrobial activity. However, its instability and hydrophobicity under normal storage conditions are limitations to its use. Nanoemulsion technology is an excellent way to solubilize, microencapsulate, and protect this compound. This study aimed to obtain a nanoemulsion based on M. verticillata EO and evaluate its antibacterial activity against Staphylococcus aureus. The EO was obtained by steam distillation. Identification and quantification of their components were determined by GC-MS revealing that the dominated chemical group was oxygenated monoterpenes. Nanoemulsions (NE) were characterized by measuring pH, transmittance, separation percentage, release profile, and morphology. The effect of NE on the growth of S. aureus and cyto-compatibility was also evaluated. The results showed that NE containing a higher percentage of tween 20 exhibited higher stability with an approximated droplet size of 10 nm. The effect of encapsulation process was evaluated by GC-MS revealing that the volatile components in EO were no affected. After 24 h, 74.24 ± 0.75% of EO was released from NE and the antibacterial activity of EO was enhanced considerably by its encapsulation. The incubation of S. aureus with the NE and pure EO, show a bacterial growth inhibition of 58.87% ± 0.99 and 46.72% ± 3.32 (p < 0.05), respectively. In addition, nanoemulsión did not cause toxicity to porcine and equine red blood cells. The results obtained showed that NE could be a potential vehicle for M. verticillata EO with promissory properties to emerge as a tool for developing advanced therapies to control and combat infections.

Fabrication of nanoparticles for bone regeneration: new insight into applications of nanoemulsion technology.

Introducing synthetic bone substitutes into the clinic was a major breakthrough in the regenerative medicine of bone. Despite many advantages of currently available bone implant materials such as biocompatiblity and osteoconductivity, they still suffer from relatively poor bioactivity, osteoinductivity and osteointegration. These properties can be effectively enhanced by functionalization of implant materials with nanoparticles such as osteoinductive hydroxyapatite nanocrystals, resembling inorganic part of the bone, or bioactive polymer nanoparticles providing sustained delivery of pro-osteogenic agents directly at implantation site. One of the most widespread techniques for fabrication of nanoparticles for bone regeneration applications is nanoemulsification. It allows manufacturing of nanoscale particles (<100 nm) that are injectable, 3D-printable, offer high surface-area-to-volume-ratio and minimal mass transport limitations. Nanoparticles obtained by this technique are of particular interest for biomedical engineering due to fabrication procedures requiring low surfactant concentrations, which translates into reduced risk of surfactant-related in vivo adverse effects and improved biocompatibility of the product. This review discusses nanoemulsion technology and its current uses in manufacturing of nanoparticles for bone regeneration applications. In the first section, we introduce basic concepts of nanoemulsification including nanoemulsion formation, properties and preparation methods. In the next sections, we focus on applications of nanoemulsions in fabrication of nanoparticles used for delivery of drugs/biomolecules facilitating osteogenesis and functionalization of bone implants with special emphasis on biomimetic hydroxyapatite nanoparticles, synthetic polymer nanoparticles loaded with bioactive compounds and bone-targeting nanoparticles. We also highlight key challenges in formulation of nanoparticles via nanoemulsification and outline potential further improvements in this field.

BIOBASED NANOEMULSION FOR BLOCKING COVID-19 FROM ACCELERATING ALZHEIMER'S DISEASE

An effective therapeutic strategy to delay dementia could be based upon nanotargeting drug(s), using lipid nanocarriers (&lt;i&gt;i.e.&lt;/i&gt;, biobased nanoemulsion technology), toward a major serum amyloid A (SAA) receptor responsible for certain proinflammatory, SAA-mediated, cell signaling events. For example, other investigators have already confirmed that SR-BI receptors (or its human ortholog CLA-1) function as proinflammatory cell-surface SAA receptors, and additionally report that various ligands for CLA-1/SR-BI "efficiently compete" with SAA for CLA-1/SR-BI binding. A similar benefit (of "competitive binding") may well accompany the clinical intravenous use of the ("HDL-like") lipid nanocarriers (&lt;i&gt;i.e.&lt;/i&gt;, biobased nanoemulsion [see above]), which have already been repeatedly described in the peer-reviewed literature as a targeted (and SR-BI mediated) drug-delivery agent. To conclude, the above-proposed "competitive binding", between SAA and such biobased nanoemulsion(s), could assist/enhance the protective (ordinarily anti-inflammatory) role of HDL - as well as provide targeted drug-delivery to the (human) brain cells bearing CLA-1/SR-BI receptors. The first resulting advantage is that this (intravenous) colloidal-nanocarrier therapeutic makes it possible for various cell types, all potentially implicated in Alzheimer's disease and/or (late-onset) dementia, to be simultaneously sought out and better reached for localized drug treatment of brain tissue &lt;i&gt;in vivo&lt;/i&gt;. A second major advantage is that this therapeutic-target approach has particular relevance to the current COVID-19 human pandemic; namely, immune response and excessive inflammation in COVID-19 infection may accelerate the progression of brain inflammatory neurodegeneration which, if effectively halted, might play a major role in reducing Alzheimer's disease pathology.

Formulation and characterization of nanoemulsion from Alhagi maurorum essential oil and study of its antimicrobial, antibiofilm, and plasmid curing activity against antibiotic-resistant pathogenic bacteria.

Nanoemulsion technology is an alternative candidate to overcome antibiotic resistance in pathogenic bacteria. The aim of this research was nanoemulsion production from the essential oil of Alhagi maurorum and the characterization of this nanostructure. Nanoemulsion of essential oil from A. maurorum was prepared using the ionotropic gelation method and chitosan as a nano-carrier. Scanning Electron Microscopy (SEM) was used to characterize the synthesized nanoparticles. The effect of nanoemulsion on the antibacterial, antibiofilm, and plasmid curing of six antibiotic-resistant pathogenic bacteria (P. aeruginosa, E. coli, S. aureus, K. pneumonia, A. baumannii, B. cereus) was evaluated. The results of this study showed that nanoparticles had a spherical shape and smooth topology. The mean size were 172 ± 4nm and Zeta potentials was +28.6 mv. The results of antibacterial activity confirmed that nanoemulsion of essential oil had higher inhibition against bacteria compared to free essential oil. Also, this nanoemulsion had antibiofilm activity. Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration for Biofilm (MBCB) were determined for nanoemulsion against the biofilm of pathogenic bacteria. The results have shown that the MIC value for A. baumannii is 12.5mgml -1 and for E. coli this value is 1.75mgml -1. This finding means that MIC values were highest for A. baumannii and lowest for E. coli. Statistical analysis demonstrated that the inhibitory effect of nanoemulsion against bacterial biofilm was significant (P < 0.05). This nanoemulsion also had a remarkable effect the curing of R-plasmid of three antibiotic-resistant bacteria. According to GC-MS analysis of A. maurorum essential oil, the main compounds were oxygenated sesquiterpenes and hydrocarbons. Nanoemulsion of A. maurorum had the potential to use as suitable antimicrobial agents against antibiotic-resistant bacteria.

Encapsulation of Lipid-Soluble Bioactives by Nanoemulsions

Lipid-soluble bioactives are important nutrients in foods. However, their addition in food formulations, is often limited by limited solubility and high tendency for oxidation. Lipid-soluble bioactives, such as vitamins A, E, D and K, carotenoids, polyunsaturated fatty acids (PUFA) and essential oils are generally dispersed in water-based solutions by homogenization. Among the different homogenization technologies available, nanoemulsions are one of the most promising. Accordingly, this review aims to summarize the most recent advances in nanoemulsion technology for the encapsulation of lipid-soluble bioactives. Modern approaches for producing nanoemulsion systems will be discussed. In addition, the challenges on the encapsulation of common food ingredients, including the physical and chemical stability of the nanoemulsion systems, will be also critically examined.

Protective Effects of Anethum graveolens Seed's Oil Nanoemulsion Against Cadmium-Induced Oxidative Stress in Mice.

The cadmium (Cd) is a toxic heavy metal that induces oxidative stress in both humans and animals. The plant phenolic compounds are capable of alleviating the toxicity of heavy metals. The encapsulation of plant bioactive compounds using nanoemulsion technology could enhance their bioefficacy. In this study, the protective effects of Anethum graveolens seed's oil nanoemulsion (AGN) against cadmium-induced oxidative stress in mice were studied. The results showed that the major bioactive compounds of essential oil were carvone and limonene. The result of particle size analysis revealed the pseudo-spherical droplets with nanometer size (148.8 ± 9.48nm), homogenous dispersion, and physical colloidal stability. The Cd intoxication in mice (5mg/kg BW for 30days) reduced the body weight gain; however, treatment of the mice with different concentration of AGN (0.125, 0.25, and 0.5mg/L, 30days) through drinking water improved the body weight loss, liver Cd deposition, lipid peroxidation, cellular antioxidant redox potential, and inflammation in the liver, kidney, and brain of the mice challenged by cadmium-induced oxidative stress. The results of the present study revealed that drinking the essential oil of Anethum graveolens nanoemulsion containing carvone and limonene could be a promising strategy to protect the tissues against cadmium-induced oxidative damage.

Formulation and Characterization of Nanoemulsion of Tread leave Ethanol Extract (Catharanthus roseus (L.) G. Don) as Antihyperglycemic

Nanoemulsion technology has been widely developed and applied on natural extract to enhance bioavailability and drug effects. The tread plant (Catharanthus roseus (L.) G. Don) is commonly known in traditional medicine for lowering blood sugar levels. This study aimed to make and characterize nanoemulsion of tread leaf extract as antihyperglycemic using sesame oil and olive oil as carriers. Nanoemulsion formulations were made using ethanol extract of tread leaves, and additives such as Tween 80, isopropyl myristate in varying ratios and some of vegetable oils. The nanoemulsion was physically evaluated tests including the pH, the type of emulsion, homogeneity and size distribution which measured by the Particle Size Analyzer (PSA). Antihyperglycemic testing was carried out on 4 groups of male mice (5 mice/ group) induced with glucose and treated with extract, nanoemulsion, and distilled water. The results showed that the nanoemulsion preparation had a pH of 6.4 to 6.5; o/w type of emulsion and it was stable on storage for 1 month. The particle size distribution of the nanoemulsion was 85.8% with size &lt;500 nm. Nanoemulsion could reduce the blood glucose levels in mice to normal level after 60 minutes. It also showed the decreae for 43-46% of the blood glucose level after 2 hours. The Nanoemulsion of tread leaf extract has a faster ability and a greater percentage in reducing blood glucose levels compared to extract and control.&#x0D; Keywords: Nanoemulsion, Catharanthus roseus, sesame oil, olive oil, Antihyperglikemic

Evaluation of Kemiri Sunan (Reutealis trisperma Blanco) Seed Oil Nanoemulsion as insecticide against Planococcus minor (Hemiptera: Pseudococcidae)

Estate commodities and flowering plants are mostly attacked by Planoccocus minor. Nowadays, botanical pesticide nanoemulsion technology is developing to be used to control insect pests. To evaluate the kemiri sunan seed oil nanoemulsion as insecticide against P.minor was the objective of this study. Completely Randomized Design (CRD) with four replication was used on the kemiri sunan evaluation test. Each replication consist of seven concentration (0,2%; 0,39%; 0,78%; 1,56%; 3,13%; 6%; and water as control). Analysis of variance (ANOVA) at α 95% followed by Duncan multiple test at α 5% was carried out. The evaluation result showed an increase in the insecticidal effect of kemiri sunan seed oil nanoemulsion against the insect species when formulated as a nano-emulsion. The application of kemiri sunan seed oil nanoemulsion for five day after treatment was able to cause the mortality of P. minor as much as 90%. Within 5 days after treatment, LC50 was 0.09 % and LT50 was 3,7 days. It is implies that the kemiri sunan seed oil nanoemulsion when to be sprayed may kill directly to the target pest and it is needed around 3,7 days to kill 50% population of pest. The results obtained indicate that kemiri sunan seed oil based nanoemulsion formulations can be used as toxicants for the control of P. minor. The kemiri sunan seed oil based nanoemulsion can be developed into botanical pesticides. Low chemical residues, safe for natural enemies and can be used as component in integrated pest management are the advantages of The kemiri sunan seed oil based nanoemulsion.

ENHANCE SOLUBILITY AND PROLONG RELEASE OF PROCHLORPERAZINE MALEATE USING FLOATING NANOEMULSION IN SITU GEL

Objective: The objective of this study was to prepare floating gastric in situ gel of prochlorperazine maleate (PM) using nanoemulsion technology to improve drug solubility, bioavailability, reduce dosing frequency, and patient compliance.Methods: Eight nanoemulsion formulas (F1–F8) of PM were prepared by ultrasonication method using oil, surfactants: cosurfactants (Smix) with different types, concentrations, and ratios, and deionized distilled water. The nanoemulsion formulas were characterized to select the optimum recipe from which six floating in situ gel formulas (floating nanoemulsion in situ [FNI] 1-FNI 6) were prepared using sodium alginate as gelling agent, hydroxypropyl methylcellulose (HPMCK) 4M as rate retarding polymer, calcium chloride as cross-linking agent, calcium carbonate as floating agent, and sodium citrate as buffering and neutralizing gastric acid. All FNI formulas were subjected for the evaluation to assess the formulations suitability concerning the dosage form and intended therapeutic purpose.Results: Formulation variables such as the concentration of sodium alginate, HPMCK 4M, calcium carbonate, and calcium chloride affected the gelling properties, formulation viscosity, floating behavior, and in vitro drug release. Formulation FNI 6 showed acceptable floating lag time (55±2.3 s) and &gt;12 h floating duration time, and observe prolong release of the drug in in-situ gelling preparation.Conclusion: The prepared FNI formulas of PM could float in the gastric conditions and released the drug in a sustained manner. The present formulation was enhanced drug solubility with good retention properties and better patient compliance.

ENHANCE SOLUBILITY AND PROLONG RELEASE OF PROCHLORPERAZINE MALEATE USING FLOATING NANOEMULSION IN SITU GEL

Objective: The objective of this study was to prepare floating gastric in situ gel of prochlorperazine maleate (PM) using nanoemulsion technology to improve drug solubility, bioavailability, reduce dosing frequency, and patient compliance.Methods: Eight nanoemulsion formulas (F1–F8) of PM were prepared by ultrasonication method using oil, surfactants: cosurfactants (Smix) with different types, concentrations, and ratios, and deionized distilled water. The nanoemulsion formulas were characterized to select the optimum recipe from which six floating in situ gel formulas (floating nanoemulsion in situ [FNI] 1-FNI 6) were prepared using sodium alginate as gelling agent, hydroxypropyl methylcellulose (HPMCK) 4M as rate retarding polymer, calcium chloride as cross-linking agent, calcium carbonate as floating agent, and sodium citrate as buffering and neutralizing gastric acid. All FNI formulas were subjected for the evaluation to assess the formulations suitability concerning the dosage form and intended therapeutic purpose.Results: Formulation variables such as the concentration of sodium alginate, HPMCK 4M, calcium carbonate, and calcium chloride affected the gelling properties, formulation viscosity, floating behavior, and in vitro drug release. Formulation FNI 6 showed acceptable floating lag time (55±2.3 s) and &gt;12 h floating duration time, and observe prolong release of the drug in in-situ gelling preparation.Conclusion: The prepared FNI formulas of PM could float in the gastric conditions and released the drug in a sustained manner. The present formulation was enhanced drug solubility with good retention properties and better patient compliance.

Preparation, Characterization, and Pharmacokinetic Evaluation of Imperatorin Lipid Microspheres and Their Effect on the Proliferation of MDA-MB-231 Cells.

Imperatorin is a chemical compound belonging to the linear furanocoumarins. Imperatorin is attracting considerable attention because of its antitumor, antibacterial, anti-inflammatory, and anticoagulant activities, inhibition of myocardial hypertrophy, and other pharmacological efficacies. However, imperatorin has limited water solubility and has better lipid solubility; thus, we decided to design and synthesize imperatorin lipid microspheres to optimize the preparation conditions. The aim was to develop and formulate imperatorin lipid microspheres through nanoemulsion technology and apply the response surface–central composite design to optimize the imperatorin lipid microsphere formulation. The influence of the amounts of egg lecithin, poloxamer 188, and soybean oil for injection on the total percentage of the oil phase was investigated. The integrated effect of dependent variables, including particle size, polydispersity index, zeta potentials, drug loading, and encapsulation efficiency, was investigated. Data of overall desirabilities were fitted to a second-order polynomial equation, through which three-dimensional response surface graphs were described. Optimum experimental conditions were calculated by Design-Expert 8.06. Results indicated that the optimum preparation conditions were as follows: 1.39 g of egg lecithin, 0.21 g of poloxamer 188, and 10.57% soybean oil for injection. Preparation of imperatorin lipid microspheres according to the optimum experimental conditions resulted in an overall desirability of 0.7286, with the particle size of 168 ± 0.54 nm, polydispersity index (PDI) of 0.138 ± 0.02, zeta potentials of −43.5 ± 0.5 mV, drug loading of 0.833 ± 0.27 mg·mL−1, and encapsulation efficiency of 90 ± 1.27%. The difference between the observed and predicted values of the overall desirability of the optimum formulation was in the range from 2.4% to 4.3%. Subsequently, scanning electron microscopy was used to observe the micromorphology of the imperatorin lipid microspheres, showing round globules of relatively uniform shape and sizes within 200 nm. The effect of imperatorin lipid microspheres on MDA-MB-231 proliferation was investigated by the MTT method. Furthermore, pharmacokinetics in Sprague-Dawley rats was evaluated using orbital bleeding. A sensitive and reliable liquid chromatography with the high-performance liquid chromatography (HPLC) method was established and validated for the quantification of imperatorin in rat plasma samples. The data were calculated by DAS (drug and statistics) Pharmacokinetic Software version 3.3.0 (Version 3.3.0, Shanghai, China). Results demonstrated that imperatorin lipid microspheres can significantly enhance the bioavailability of imperatorin and can significantly inhibit MDA-MB-231 cell proliferation. In conclusion, our results suggested that the response surface–central composite design is suitable for achieving an optimized lipid microsphere formulation. Imperatorin lipid microspheres can improve the bioavailability of imperatorin and better inhibit the proliferation of MDA-MB-231 cells as compared to imperatorin alone.

Improved Physicochemical Properties of Yogurt Fortified with Fish Oil/γ-Oryzanol by Nanoemulsion Technology.

Fish oil has several dietary benefits, but its application in food formulations is limited because of its poor water-solubility, easy oxidation and strong odor. The purposes of this study were to produce a fish oil/γ-oryzanol nanoemulsion and to evaluate the effect of adding this nanoemulsion on the physicochemical and sensory characteristics of yogurts. Adding fish oil/γ-oryzanol nanoemulsion resulted in a significant reduction in the acidity and syneresis of yogurt. Yogurt with the nanoemulsion had significantly lower peroxide value (0.28 mmol/L after 21 days) and higher retention of eicosapentaenoic acid and docosahexaenoic acid contents (decreased to 95% and 94% of its initial value, respectively) than yogurt with fish oil/γ-oryzanol (peroxide value = 0.65 mmol/L; eicosapentaenoic acid and docosahexaenoic acid contents decreased to 72% and 53% of its initial value, respectively). Fish oil/γ-oryzanol nanoemulsion incorporated into yogurt had closer sensory attributes scores to plain yogurt. This study may have important implications for the application of fish oil/γ-oryzanol nanoemulsion in yogurt.

Protective effects of a nanoemulsion adjuvant vaccine (2C-Staph/NE) administered intranasally against invasive Staphylococcus aureus pneumonia.

No licensed Staphylococcus aureus (S. aureus) vaccine is currently available. To develop an effective S. aureus vaccine, we selected the recombinant proteins staphylococcal enterotoxin B (rSEB) and manganese transport protein C (rMntC) as vaccine candidates and formulated a 2C-Staph vaccine. Based on the optimised formation of nanoemulsion (NE) technology, we constructed a novel NE adjuvant vaccine, 2C-Staph/NE. The 2C-Staph/NE particles showed a suitable diameter (24.9 ± 0.14 nm), a good protein structure of integrity and specificity, and high thermodynamic stability. 2C-Staph formulated with an NE adjuvant induced higher survival rates than a 2C-Staph/MF59 vaccine in sepsis and pneumonia models. Moreover, intramuscular vaccination with 2C-Staph/NE yielded protection efficacy in a sepsis model, and the intranasal vaccination route induced a potent protective effect in a pneumonia model. Intranasal vaccination with 2C-Staph/NE induced a strong mucosal response with high levels of IgA and IL-17A in bronchoalveolar lavage fluid (BALF), and the IgG levels in the BALF were comparable to those induced by the intramuscular vaccination route. Furthermore, the serum and BALF induced by intranasal administration showed potent opsonophagocytic activity against S. aureus. And, the IL-17A played a protective role in the pneumonia model demonstrated by a cytokine neutralization test. Taken together, our results showed that intranasal administration of 2C-Staph formulated with an NE adjuvant yielded ideal protection in a murine S. aureus pneumonia model.

Preparation, characterization, and antimicrobial activity of nanoemulsions incorporating citral essential oil

Citral is a typical essential oil used in the food, cosmetic, and drug industries and has shown antimicrobial activity against microorganisms. Citral is unstable and hydrophobic under normal storage conditions, so it can easily lose its bactericide activity. Nanoemulsion technology is an excellent way to hydrophilize, microencapsulate, and protect this compound. In our studies, we used a mixed surfactant to form citral-in-water nanoemulsions, and attempted to optimize the formula for preparing nanoemulsions. Citral-in-water nanoemulsions formed at So 0.4 to 0.6 and ultrasonic power of 18 W for 120 seconds resulted in a droplet size of < 100 nm for nanoemulsions. The observed antimicrobial activities were significantly affected by the formulation of the nanoemulsions. The observed relationship between the formulation and activity can lead to the rational design of nanoemulsion-based delivery systems for essential oils, based on the desired function of antimicrobials in the food, cosmetics, and agrochemical industries.