Cationic Nanoemulsion-Encapsulated Retinoic Acid as an Adjuvant to Promote OVA-Specific Systemic and Mucosal Responses.

Cationic nanostructures have emerged as an adjuvant and antigen delivery system that enhances dendritic cell maturation, ROS generation, and antigen uptake and then promotes antigen-specific immune responses. In recent years, retinoic acid (RA) has received increasing attention due to its effect in activating the mucosal immune response; however, in order to use RA as a mucosal adjuvant, it is necessary to solve the problem of its dissolution, loading, and delivery. Here, we describe a cationic nanoemulsion-encapsulated retinoic acid (CNE-RA) delivery system composed of the cationic lipid 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOTAP), retinoic acid, squalene as the oil phase, polysorbate 80 as surfactant, and sorbitan trioleate 85 as co-surfactant. Its physical and chemical properties were characterized using dynamic light scattering and a spectrophotometer. Immunization of mice with the mixture of antigen (ovalbumin, OVA) and CNE-RA significantly elevated the levels of anti-OVA secretory immunoglobulin A (sIgA) in vaginal lavage fluid and the small intestinal lavage fluid of mice compared with OVA alone. This protocol describes a detailed method for the preparation, characterization, and evaluation of the adjuvant effect of CNE-RA.

Effect of cationic surfactant on the physicochemical and antibacterial properties of colloidal systems (emulsions and microemulsions).

Colloidal systems have been used to encapsulate, protect and release essential oils in mouthwashes. In this study, we investigated the effect of cetylpyridinium chloride (CPC) on the physicochemical properties and antimicrobial activity of oil-in-water colloidal systems containing tea tree oil (TTO) and the nonionic surfactant polysorbate 80. Our main aim was to evaluate whether CPC could improve the antimicrobial activity of TTO, since this activity is impaired when this essential oil is encapsulated with polysorbate 80. These systems were prepared with different amounts of TTO (0-0.5% w/w) and CPC (0-0.5% w/w), at a final concentration of 2% (w/w) polysorbate 80. Dynamic light scattering (DLS) results revealed the formation of oil-swollen micelles and oil droplets as a function of TTO concentration. Increases in CPC concentrations led to a reduction of around 88% in the mean diameter of oil-swollen micelles. Although this variation was of only 20% for the oil droplets, the samples appearance changed from turbid to transparent. The surface charge of colloidal structures was also markedly affected by the CPC as demonstrated by the transition in zeta potential from slightly negative to highly positive values. Electron paramagnetic resonance (EPR) studies showed that this transition is followed by significant increases in the fluidity of surfactant monolayer of both colloidal structures. The antimicrobial activity of colloidal systems was tested against a Gram-negative (Escherichia coli) and Gram-positive (Staphylococcus aureaus) bacteria. Our results revealed that the inhibition of bacterial growth is observed for the same CPC concentration (0.05% w/w for E. coli and 0.3% w/w for S. aureus) regardless of TTO content. These findings suggest that TTO may not act as an active ingredient in polysorbate 80 containing mouthwashes.

Effect of salinity stress and surfactant treatment with zinc and boron on morpho-physiological and biochemical indices of fenugreek (Trigonella foenum-graecum).

Micronutrient application has a crucial role in mitigating salinity stress in crop plants. This study was carried out to investigate the effect of zinc (Zn) and boron (B) as foliar applications on fenugreek growth and physiology under salt stress (0 and 120 mM). After 35 days of salt treatments, three levels of zinc (0, 50, and 100 ppm) and two levels of boron (0 and 2 ppm) were applied as a foliar application. Salinity significantly reduced root length (72.7%) and shoot length (33.9%), plant height (36%), leaf area (37%), root fresh weight (48%) and shoot fresh weight (75%), root dry weight (80%) and shoot dry weight (67%), photosynthetic pigments (78%), number of branches (50%), and seeds per pod (56%). Fenugreek's growth and physiology were improved by foliar spray of zinc and boron, which increased the length of the shoot (6%) and root length (2%), fresh root weight (18%), and dry root weight (8%), and chlorophyll a (1%), chlorophyll b (25%), total soluble protein content (3%), shoot calcium (9%) and potassium (5%) contents by significantly decreasing sodium ion (11%) content. Moreover, 100 ppm of Zn and 2 ppm of B enhanced the growth and physiology of fenugreek by reducing the effect of salt stress. Overall, boron and zinc foliar spray is suggested for improvement in fenugreek growth under salinity stress.

The effect of caraway oil-loaded bio-nanoemulsions on the growth and performance of barnyard grass and maize.

A proper formulation is crucial to improve the herbicidal effects of essential oils and their selectivity. In this study, we investigated the physicochemical properties of bio-based nanoemulsions (CNs) containing several concentrations of caraway (Carum carvi) essential oil stabilized with Eco Tween 80, as a surfactant, maintaining 1:1 proportions. Detailed physicochemical characteristics of the CNs revealed that their properties were most desired at 2% of the oil and surfactant, i.e., the smallest droplet size, polydispersity index, and viscosity. The CNs caused biochemical changes in maize and barnyard grass (Echinochloa crus-galli) seedlings, however, to a different extent. Barnyard grass has overall metabolism (measured as a thermal power) decreased by 39-82% when exposed to the CNs. The CNs triggered changes in the content and composition of carbohydrates in the endosperm of both species' seedlings in a dose-response manner. The foliar application of CNs caused significant damage to tissues of young maize and barnyard grass plants. The effective dose of the CN (ED50, causing a 50% damage) was 5% and 17.5% oil in CN for barnyard grass and maize tissues, respectively. Spraying CNs also decreased relative water content in leaves and affected the efficiency of photosynthesis by disturbing the electron transport chain. We found that barnyard grass was significantly more susceptible to the foliar application of CNs than maize, which could be used to selectively control this species in maize crops. However, further studies are needed to verify this hypothesis under field conditions.

Vegetable oil-based surfactants are adjuvants that enhance the efficacy of neonicotinoid insecticides and can bias susceptibility testing in adult mosquitoes.

BACKGROUND: The standard operating procedure for testing the susceptibility of adult mosquitoes to neonicotinoid or butenolide insecticides recommends using a vegetable oil ester (Mero) as a surfactant. However, there is growing evidence that this adjuvant contains surfactants that can enhance insecticide activity, mask resistance and bias the bioassay. METHODOLOGY/PRINCIPAL FINDINGS: Using standard bioassays, we tested the effects of commercial formulations of vegetable oil-based surfactants similar to Mero on the activity of a spectrum of active ingredients including four neonicotinoids (acetamiprid, clothianidin, imidacloprid and thiamethoxam) and two pyrethroids (permethrin and deltamethrin). We found that three different brands of linseed oil soap used as cleaning products drastically enhanced neonicotinoid activity in Anopheles mosquitoes. At 1% (v/v), the surfactant reduced the median lethal concentration, LC50, of clothianidin more than 10-fold both in susceptible and in resistant populations of Anopheles gambiae. At 1% or 0.5% (v/v), linseed oil soap restored the susceptibility of adult mosquitoes fully to clothianidin, thiamethoxam and imidacloprid and partially to acetamiprid. By contrast, adding soap to the active ingredient did not significantly affect the level of resistance to permethrin or deltamethrin suggesting that vegetable oil-based surfactants specifically enhance the potency of some classes of insecticides. CONCLUSIONS/SIGNIFICANCE: Our findings indicate that surfactants are not inert ingredients, and their use in susceptibility testing may jeopardize the ability to detect resistance. Further research is needed to evaluate the potential, the limitations and the challenges of using some surfactants as adjuvants to enhance the potency of some chemicals applied in mosquito control.

Improved phyllosphere microbiome composition of tea plant with the application of small peptides in combination with rhamnolipid.

BACKGROUND: Small peptides play a crucial role in plant growth and adaptation to the environment. Exogenous small peptides are often applied together with surfactants as foliar fertilizers, but the impact of small peptides and surfactants on the tea phyllosphere microbiome remains unknown. RESULTS: In this study, we investigated the effects of small peptides and different surfactants on the tea phyllosphere microbiome using 16S and ITS sequencing. Our results showed that the use of small peptides reduced the bacterial diversity of the tea phyllosphere microbiome and increased the fungal diversity, while the use of surfactants influenced the diversity of bacteria and fungi. Furthermore, the addition of rhamnolipid to small peptides significantly improved the tea phyllosphere microbiome community structure, making beneficial microorganisms such as Pseudomonas, Chryseobacterium, Meyerozyma, and Vishniacozyma dominant populations. CONCLUSION: Our study suggests that the combined use of small peptides and surfactants can significantly modify the tea phyllosphere microbiome community structure, particularly for beneficial microorganisms closely related to tea plant health. Thus, this preliminary study offers initial insights that could guide the application of small peptides and surfactants in agricultural production, particularly with respect to their potential for modulating the phyllosphere microbiome community in tea plant management.

Host-Guest Assembly-Crosslinked Nanoemulsions with Dual-Antimicrobial Mechanism for Treating Multidrug-Resistant Bacterial Biofilms.

Plant essential oils have good antimicrobial properties, but their poor stability and compatibility in aqueous solutions greatly limit their practical application. To address this issue, a dynamically crosslinked nanoemulsion based on host-guest assembly was developed in this study. First, a ß-cyclodextrin-functionalized quaternary ammonium surfactant (ß-CD-QA) and adamantane-terminated polyethylene glycol (APA) crosslinker were first synthesized. Then, the oil-in-water host-guest crosslinked nanoemulsions (HGCTNs) were formed by incorporating tea tree essential oils (TTO) as a natural antimicrobial agent. The results showed that HGCTNs significantly improved the stability of the essential oil nanoemulsions and extended their shelf life. Furthermore, HGCTNs demonstrated effective antimicrobial properties against both Gram-negative/positive bacterioplankton and bacterial biofilms. The results of antibacterial experiments showed that the dynamically crosslinked HGCTNs exhibit superior antibacterial efficacy, with a minimum inhibitory concentration (MIC) of 12.5 v/v % (0.13 µL/mL TTO) and could eradicate the biofilms. The electrical conductivity of the bacterial solution gradually increased within 5 h of treatment with the nanoemulsions, indicating that the HGCTNs have a slow-release effect of TTO and sustainable antibacterial ability. The antimicrobial mechanism can be attributed to the synergistic antibacterial action of the ß-CD-QA surfactant containing a quaternary ammonium moiety and TTO, which are stabilized by nanoemulsions.

Impact of Lipid Matrix Composition on Activity of Membranotropic Enzymes Galactonolactone Oxidase from Trypanosoma cruzi and L-Galactono-1,4-Lactone Dehydrogenase from Arabidopsis thaliana in the System of Reverse Micelles.

The study of many membrane enzymes in an aqueous medium is difficult due to the loss of their catalytic activity, which makes it necessary to use membrane-like systems, such as reverse micelles of surfactants in nonpolar organic solvents. However, it should be taken into account that the micelles are a simplified model of natural membranes, since membranes contain many different components, a significant part of which are phospholipids. In this work, we studied impact of the main phospholipids, phosphatidylcholine (PC) and phosphatidylethanolamine (PE), on activity of the membrane enzymes using galactonolactone oxidase from Trypanosoma cruzi (TcGAL) and L-galactono-1,4-lactone dehydrogenase from Arabidopsis thaliana (AtGALDH) as examples. Effect of the structure (and charge) of the micelle-forming surfactant itself on the activity of both enzymes has been studied using an anionic surfactant (AOT), a neutral surfactant (Brij-96), and a mixture of cationic and anionic surfactants (CTAB and AOT) as examples. The pronounced effect of addition of PC and PE lipids on the activity of AtGALDH and TcGAL has been detected, which manifests as increase in catalytic activity and significant change in the activity profile. This can be explained by formation of the tetrameric form of enzymes and/or protein-lipid complexes. By varying composition and structure of the micelle-forming surfactants (AOT, CTAB, and Brij-96) it has been possible to change catalytic properties of the enzyme due to effect of the surfactant on the micelle size, lipid mobility, charge, and rigidity of the matrix itself.

Characterization of biosurfactant produced in response to petroleum crude oil stress by Bacillus sp. WD22 in marine environment.

Bacillus sp. WD22, previously isolated from refinery effluent, degraded 71% of C8 hydrocarbons present in 1.0% v/v PCO in seawater (control medium), which reduced to 16.3%, on addition of yeast extract. The bacteria produced a biosurfactant in both media, whose surface was observed to be amorphous in nature under FESEM-EDAX analysis. The biosurfactant was characterized as a linear surfactin by LCMS and FT-IR analysis. The critical micelle concentration was observed as 50 mg/L and 60 mg/L at which the surface tension of water was reduced to 30 mN/m. Purified biosurfactant could emulsify petroleum-based oils and vegetable oils effectively and was stable at all tested conditions of pH, salinity and temperature up to 80 °C. The biosurfactant production was found to be mixed growth associated in control medium, while it was strictly growth associated in medium with yeast extract as studied by the Leudeking-Piret model.

Tanshinone IIA loaded bioactive nanoemulsion for alleviation of lipopolysaccharide induced acute lung injury via inhibition of endothelial glycocalyx shedding.

Acute lung injury (ALI) and its more serious form; acute respiratory distress syndrome are major causes of COVID-19 related mortality. Finding new therapeutic targets for ALI is thus of great interest. This work aimed to prepare a biocompatible nanoformulation for effective pulmonary delivery of the herbal drug; tanshinone-IIA (TSIIA) for ALI management. A nanoemulsion (NE) formulation based on bioactive natural ingredients; rhamnolipid biosurfactant and tea-tree oil, was developed using a simple ultrasonication technique, optimized by varying oil concentration and surfactant:oil ratio. The selected TSIIA-NE formulation showed 105.7 nm diameter and a PDI âˆ¼ 0.3. EE exceeded 98 % with biphasic sustained drug release and good stability over 3-months. In-vivo efficacy was evaluated in lipopolysaccharide (LPS)-induced ALI model. TSIIA-NE (30 µg/kg) was administered once intratracheally 2 h after LPS instillation. Evaluation was performed 7days post-treatment. Pulmonary function assessment, inflammatory, oxidative stress and glycocalyx shedding markers analysis in addition to histopathological examination of lung tissue were performed. When compared to untreated rats, in-vivo efficacy study demonstrated 1.4 and 1.9-fold increases in tidal volume and minute respiratory volume, respectively, with 32 % drop in wet/dry lung weight ratio and improved levels of arterial blood gases. Lung histopathology and biochemical analysis of different biomarkers in tissue homogenate and bronchoalveolar lavage fluid indicated that treatment may ameliorate LPS-induced ALI symptoms thorough anti-oxidative, anti-inflammatory effects and inhibition of glycocalyx degradation. TSIIA-NE efficacy was superior to free medication and blank-NE. The enhanced efficacy of TSIIA bioactive nanoemulsion significantly suggests the pharmacotherapeutic potential of bioactive TSIIA-NE as a promising nanoplatform for ALI.

Synthesis of N-acyl glycine surfactant from palm oil as green repellent and toxicant to termite (Microcerotermes diversus).

This study described for the first time, the synthesis of a greener, safer, and more effective termiticide using a bio-based surfactant, N-acyl glycine derived from palm oil for the control of Microcerotermes diversus. Laboratory findings showed that the highest repellent activity was observed in N-acyl glycine surfactant (83.33%) at 50 ppm. In addition, N-acyl glycine surfactant also exhibited substantial time and concentration-dependent anti-termiticidal activity in which the highest termite mortality was observed after 3 days of exposure at 50 ppm of the surfactant (100%). Furthermore, 32.49 ppm concentration of N-acyl glycine surfactant (LC50 = 32.49 ppm) attained 50% of termite lethality. The current innovated termiticide with the use of N-acyl glycine surfactant offers a better efficacy, lower cost, and prevents the use of dangerous termiticides that are critical in creating a more sustainable environment, and controls Microcerotermes diversus at the same time.

Production of new antimicrobial palm oil-derived sophorolipids by the yeast Starmerella riodocensis sp. nov. against Candida albicans hyphal and biofilm formation.

BACKGROUND: Microbial derived-surfactants display low eco-toxicity, diverse functionality, high biodegradability, high specificity, and stability under extreme conditions. Sophorolipids are emerging as key biosurfactants of yeast origins, used in various industrial sectors to lower surface tension. Recently, sophorolipid complexes have been applied in biomedicals and agriculture to eradicate infectious problems related to human and plant fungal pathogens. This study aimed to characterize the functional properties and antifungal activities of sophorolipids produced by a newly characterized Starmerella riodocensis GT-SL1R sp. nov. strain. RESULTS: Starmerella riodocensis GT-SL1R sp. nov. strain was belonged to Starmerella clade with 93.12% sequence similarity using the ITS technique for strain identification. Sophorolipids production was examined, using co-carbon substrates glucose and palm oil, with a yield on the substrate between 30 and 46%. Using shake-flasks, the S. riodocensis GT-SL1R strain produced biosurfactants with an emulsification activity of 54.59% against kerosene compared to the S. bombicola BCC5426 strain with an activity of 60.22%. Maximum productivities of GT-SL1R and the major sophorolipid-producer S. bombicola were similar at 0.8 gl-1 h-1. S. riodocensis GT-SL1R produced mixed forms of lactonic and acidic sophorolipids, shown by TCL, FTIR, and HPLC. Importantly, the complex sophorolipid mixture displayed antifungal activity against an opportunistic yeast pathogen Candida albicans by effectively reducing hyphal and biofilm formation. CONCLUSIONS: Sophorolipids derived from S. riodocensis demonstrate potential industrial and biomedical applications as green surfactant and antifungal agent. Since numerous renewable bioresources and industrial wastes could be used by microbial cell factories in the biosynthesis of biosurfactants to reduce the production cost, sophorolipids hold a promising alternative to current antimicrobials in treatments against infectious diseases in humans, animals, and plants.

Application of a biosurfactant from Pseudomonas cepacia CCT 6659 in bioremediation and metallic corrosion inhibition processes.

Biosurfactants are capable of meeting the challenges of the oil industry by reducing its social, economic, and environmental impacts. The aim of the present study was to produce a biosurfactant from Pseudomonas cepacia CCT6659 in 2.0-L and 5.0-L bioreactors and evaluate its long-term stability over 120 days of storage. Ecotoxicological tests were performed with Artemia salina larvae during the use of the biosurfactant to increase in solubilisation of heavy oil in seawater compared to the use of a chemical surfactant. The biosurfactant was also applied as a bioremediation agent for sand contaminated with a petroleum product and as an inhibitor of corrosion on metallic surfaces. A concentration of 35.0 g/L of the biosurfactant was achieved in the 5.0-L reactor and low toxicity to the bioindicator was found, with an approximate 40% reduction in the mortality rate compared to the chemical surfactant. The stability of the biosurfactant was demonstrated by the maintenance of its tensioactive properties throughout the entire storage period. Besides its advantageous bioremediating capacity, with the removal of 94.5% of oil from sand, the biosurfactant proved to be an effective inhibitor of both metallic corrosion and microbial biofilm, with minimal loss of mass (15.7%) compared to the control condition, demonstrating its potential for industrial applications.

Ultrasound-assisted nanoemulsion of Trachyspermum ammi essential oil and its constituent thymol on toxicity and biochemical aspect of Aedes aegypti.

Aedes aegypti is the main vector of yellow fever, chikungunya, Zika, and dengue worldwide and is managed by using chemical insecticides. Though effective, their indiscriminate use brings in associated problems on safety to non-target and the environment. This supports the use of plant-based essential oil (EO) formulations as they are safe to use with limited effect on non-target organisms. Quick volatility and degradation of EO are a hurdle in its use; the present study attempts to develop nanoemulsions (NE) of Trachyspermum ammi EO and its constituent thymol using Tween 80 as surfactant by ultrasonication method. The NE of EO had droplet size ranging from 65 ± 0.7 to 83 ± 0.09 nm and a poly dispersity index (PDI) value of 0.18 ± 0.003 to 0.20 ± 0.07 from 1 to 60 days of storage. The NE of thymol showed a droplet size ranging from 167 ± 1 to 230 ± 1 nm and PDI value of 0.30 ± 0.03 to 0.40 ± 0.008 from 1 to 60 days of storage. The droplet shape of both NEs appeared spherical under a transmission electron microscope (TEM). The larvicidal effect of NEs of EO and thymol was better than BEs (Bulk emulsion) of EO and thymol against Ae. aegypti. Among the NEs, thymol (LC50 34.89 ppm) had better larvicidal action than EO (LC50 46.73 ppm). Exposure to NEs of EO and thymol causes the shrinkage of the larval cuticle and inhibited the acetylcholinesterase (AChE) activity in Ae. aegypti. Our findings show the enhanced effect of NEs over BEs which facilitate its use as an alternative control measure for Ae. aegypti.

Staphylococcus aureus-targeting peptide/surfactant assemblies for antibacterial therapy.

To address the challenge from microbial resistance, this work developed a surfactant with 18-carbon single hydrocarbon chain and multi-amine head groups (C18N3). After assembling with Staphylococcus aureus-targeting peptide (CARG), the obtained C18N3/CARG assemblies exhibited excellent antimicrobial activities against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus in vitro and in vivo, in which the targeting peptide CARG bonded specifically to Staphylococcus aureus and C18N3 killed bacteria with a mechanism of membrane disruption. Importantly, C18N3 could also work as a ß-lactamase inhibitor to overcome the bacterial resistance to ß-lactam antibiotics through noncompetitive inhibition. The combination of ß-lactam antibiotic and C18N3/CARG assemblies more effectively suppressed methicillin-resistant Staphylococcus aureus in vitro and in vivo relative to equivalent dose of free antibiotic or C18N3. Thus, the antibacterial platform of antibiotic-carrying surfactant assemblies bearing bacteria-targeted peptides, in which C18N3 performed dual function, antibacterial agent and ß-lactamase inhibitor, may help fight against the difficult-to-treat infections.

Structurally Related Liposomes Containing N-Oxide Surfactants: Physicochemical Properties and Evaluation of Antimicrobial Activity in Combination with Therapeutically Available Antibiotics.

Although liposomes are largely investigated as drug delivery systems, they can also exert a pharmacological activity if devoid of an active principle as a function of their composition. Specifically, charged liposomes can electrostatically interact with bacterial cells and, in some cases, induce bacterial cell death. Moreover, they also show a high affinity toward bacterial biofilms. We investigated the physicochemical and antimicrobial properties of liposomes formulated with a natural phospholipid and four synthetic l-prolinol-derived surfactants at 9/1 and 8/2 molar ratios. The synthetic components differ in the nature of the polar headgroup (quaternary ammonium salt or N-oxide) and/or the length of the alkyl chain (14 or 16 methylenes). These differences allowed us to investigate the effect of the molecular structure of liposome components on the properties of the aggregates and their ability to interact with bacterial cells. The antimicrobial properties of the different formulations were assessed against Gram-negative and Gram-positive bacteria and fungi. Drug-drug interactions with four classes of available clinical antibiotics were evaluated against Staphylococcus spp. The target of each class of antibiotics plays a pivotal role in exerting a synergistic effect. Our results highlight that the liposomal formulations with an N-oxide moiety are required for the antibacterial activity against Gram-positive bacteria. In particular, we observed a synergism between oxacillin and liposomes containing 20 molar percentage of N-oxide surfactants onStaphylococcus haemolyticus, Staphylococcus epidermidis, andStaphylococcus aureus. In the case of liposomes containing 20 molar percentage of the N-oxide surfactant with 14 carbon atoms in the alkyl chain for S. epidermidis, the minimum inhibitory concentration was 0.125 µg/mL, well below the breakpoint value of the antibiotic.

Compatibility and efficiency of preservatives in emulsive cosmetics containing high surfactant content

Abstract The objective of this study was to determine the influence of nonionic surfactants on the effectiveness of preservatives used in emulsions containing high surfactant content. Mixtures of different concentrations were prepared between polyethoxylated (40) hydrogenated castor oil (PHCO) and polyoxyethylene sorbitan monooleate (PSO), with methylparaben, phenoxyethanol, methylparaben, ethylparaben, propylparaben, and isobutylparaben (PMEPBI) blend, phenoxyethanol and benzoic acid (BP) blend, and phenoxyethanol and caprylyl glycol (PC) blend. Subsequently, the compatibility of the formulation ingredients and the effectiveness of the preservatives were evaluated by the challenge test. It was found that PHCO and PSO inactivated the antimicrobial action of methylparaben and PMEPBI. Paraben-free preservatives BP and PC had less influence on surfactants than systems containing parabens. When incorporated into microemulsions and nanoemulsions containing 40% and 20% surfactants, methylparaben and BP 0.2% and 0.5% were only effective against Aspergillus niger. The PMEPBI 0.2% was effective as a preservative in nanoemulsified formulations against A. niger, Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus. The results demonstrate that the efficacy of the preservative system in formulations containing nonionic surfactant excipients depends on the type of excipient, the components of the formulation, the preservative systems composition, the excipient to preservative ratio, and the availability in the formulation.

Nanoemulsions containing Garcinia mangostana L. pericarp extract for topical applications: Development, characterization, and in vitro percutaneous penetration assay.

A highly stable oil-in-water nanoemulsion for topical applications, containing mangostins extracted from the pericarp of mangosteen (Garcinia mangostana L.), is a promising strategy to protect mangostins as well as to improve penetration of these important antioxidants through the skins. Nanoemulsions consisted of virgin coconut oil as the oil phase, Tween-80 and Span-80 as surfactants, and xanthan gum as the thickening agent, were prepared using the high-energy and low-energy emulsification methods. The nanoemulsions that were stable up to 28 days had oil droplet diameter of 220 nm to 353 nm and zeta potential of -46.9 mV to -63.7 mV. The accelerated stability test showed that the most stable nanoemulsions were those prepared using the low-energy emulsification method with an estimated shelf life of eleven months, composed of 11% oil phase, 17% surfactant, and 72% aqueous phase. The in vitro percutaneous penetration test for the nanoemulsion with added xanthan gum provided high cumulative skin penetration of mangostins of up to 114 µg/cm2. The results of this study indicate that virgin coconut oil-based nanoemulsions containing mangostins, prepared using the low-energy emulsification method, stabilized by xanthan gum and mixed at 40°C can prospectively be used for topical applications.

Investigation on the surface-active and antimicrobial properties of a natural glycolipid product.

Glycolipids are a group of sugar-containing lipids with versatile functions. In this study, a natural glycolipid product was obtained from soy lecithin, and its emulsifying, oil-gelling, antibacterial and antiviral properties were investigated. A silica-based extraction method on a preparative scale was used to recover the glycolipid product (GLP) from soy lecithin. The GLP consisted of three different glycolipid classes: acylated sterol glucoside (64.16%), sterol glucoside (25.57%) and cerebroside (6.71%). As an emulsifier, the GLP was able to form a stable water-in-oil emulsion. The GLP exhibited a good oil-gelling property, capable of gelling rapeseed oil at a concentration of 6%. For the investigated microorganisms (Escherichia coli, Pseudomonas aeruginosa and Staphylococcus aureus), the GLP did not show any antibacterial effects. The GLP exerted antiviral activity against lentivirus, but not adenovirus. The results of this study help in enriching the knowledge on the properties of naturally occurring glycolipids, which may find potential applications in the food, pharmaceutical and related industries.

Elucidating the anticancer activities of guanidinium-functionalized amphiphilic random copolymers by varying the structure and composition in the hydrophobic monomer.

Rationale: Use of traditional anticancer chemotherapeutics has been hindered by the multifactorial nature of multi-drug resistance (MDR) development and metastasis. Recently, cationic polycarbonates were reported as novel unconventional anticancer agents that mitigated MDR and inhibited metastasis. The aim of this study is to explore structure-anticancer activity relationship. Specifically, a series of cationic guanidinium-based random copolymers of varying hydrophobicity was synthesized with a narrow polydispersity (Ð = 1.12-1.27) via organocatalytic ring-opening polymerization (OROP) of functional cyclic carbonate monomers, and evaluated for anticancer activity, killing kinetics, degradability and functional mechanism. Methods: Linear, branched and aromatic hydrophobic side chain units, such as ethyl, benzyl, butyl, isobutyl and hexyl moieties were explored as comonomer units for modulating anticancer activity. As hydrophobicity/hydrophilicity balance of the polymers determines their anticancer efficacy, the feed ratio between the two monomers was varied to tune their hydrophobicity. Results: Notably, incorporating the hexyl moiety greatly enhanced anticancer efficiency and killing kinetics on cancer cells. Degradation studies showed that the polymers degraded completely within 4-6 days. Flow cytometry and lactate dehydrogenase (LDH) release analyses demonstrated that anticancer mechanism of the copolymers containing a hydrophobic co-monomer was concentration dependent, apoptosis at IC50, and both apoptosis and necrosis at 2 × IC50. In contrast, the homopolymer without a hydrophobic comonomer killed cancer cells predominantly via apoptotic mechanism. Conclusion: The hydrophobicity of the polymers played an important role in anticancer efficacy, killing kinetics and anticancer mechanism. This study provides valuable insights into designing novel anticancer agents utilizing polymers.