Nanocapsule Formulations Research Articles

Formulation and characterization of nanocapsules loaded with roselle anthocyanins extract and enhancement of anthocyanins bioaccessibility

Hibiscus sabdariffa L. (roselle) is a medicinal and edible plant which rich in anthocyanins with potent antioxidant properties. To enhance the stability of roselle anthocyanins, they were encapsulated in nanocapsules composed of carboxymethyl chitosan (CMC), chitosan hydrochloride (CHC), and β-lactoglobulin (β-Lg). In vitro simulated digestion assays evaluated the impact of various core-to-wall ratios and β-Lg concentrations on the bioaccessibility of seven anthocyanins. Nanocapsules with a core-to-wall ratio of 1:2 and β-Lg at 10 mg/mL exhibited the highest encapsulation efficiency (EE). Cyanidin-3-glucoside had the highest EE, while cyanidin-3-sambubioside showed the outstanding retention rate. Furthermore, simulated digestion experiments combined with molecular docking revealed that peonidin-3-glucoside and petunidin-3-glucoside likely interact with and bind to the outer β-Lg layer of the nanocapsules, increasing their release during in vitro digestion. This study demonstrates that encapsulating roselle anthocyanins in CMC, CHC, and β-Lg nanocapsules significantly enhances their bioaccessibility.

Nanoemulsions and nanocapsules as carriers for the development of intranasal mRNA vaccines

The global emergency of coronavirus disease 2019 (COVID-19) has spurred extensive worldwide efforts to develop vaccines for protection against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Our contribution to this global endeavor involved the development of a diverse library of nanocarriers, as alternatives to lipid nanoparticles (LNPs), including nanoemulsions (NEs) and nanocapsules (NCs), with the aim of protecting and delivering messenger ribonucleic acid (mRNA) for nasal vaccination purposes. A wide range of prototypes underwent rigorous screening through a series of in vitro and in vivo experiments, encompassing assessments of cellular transfection, cytotoxicity, and intramuscular administration of a model mRNA for protein translation. As a result, two promising candidates were identified for nasal administration. One of them was a NE incorporating a combination of an ionizable lipid (C12-200) and cationic lipid (DOTAP), both intended to condense mRNA, along with DOPE, which is known to facilitate endosomal escape. This NE exhibited a size of 120 nm and a highly positive surface charge (+ 50 mV). Another candidate was an NC formulation comprising the same components and endowed with a dextran sulfate shell. This formulation showed a size of 130 nm and a moderate negative surface charge (-16 mV). Upon intranasal administration of mRNA encoding for ovalbumin (mOVA) associated with optimized versions of the said NE and NCs, a robust antigen-specific CD8 + T cell response was observed. These findings underscore the potential of NEs and polymeric NCs in advancing mRNA vaccine development for combating infectious diseases.Graphical

Elimination study of intact lipid nanocapsules afterintravenous ratadministration.

Aim: The present study investigated renal elimination after intravenous administration of four different formulations of lipid nanocapsules (LNCs) containing dyes adapted to Förster resonance energy transfer (FRET-LNCs).Materials & methods: FRET-LNCs of 85or 50nm with or withouta pegylated surface were injected and collected in the blood or urine of rats at different time points. Quantitative analysis was performed to measure intact FRET-LNCs.Results & conclusion: Nointact LNCs were found in urine (0particles/ml) for all formulations. The50-nm pegylated LNCs were eliminated faster from theblood, whereas 85-nm pegylated LNCS were eliminated slower than nonpegylated LNCs. Elimination of FRET-LNCs was mainly due to liver tissue interaction and not renal elimination.

Evaluation of the efficacy of different concentrations of nano-capsules containing Talaromyces flavus with two forms of powder and suspension in reducing the incidence of cotton Verticillium wilt.

Previous domestic and foreign studies have shown the significant effect of Talaromyces flavus on growth inhibition of some important plant pathogens including Verticillium dahliae, Fusarium oxysporum f. sp. lycopersici and Fusarium oxysporum f. sp. cucumerinum. In Iran, it is necessary to produce new formulations of this fungus based on modern technologies given the importance of attracting companies producing biological control agents and transferring the technical knowledge of mass production of formulations of these agents to them. In the present study, based on the method presented in the Pesticide Research Department of the Iranian Plant Protection Research Institute, two types of T. flavus formulations in the form of nano-capsules containing Talaromyces flavus with two forms of powder and suspension were prepared using nanotechnology. In the next step, during the greenhouse examination, the efficiency of each of these new formulations in concentrations of one to five per thousand for soil addition method and concentration of five per thousand for seed impregnation method (six treatments for each of the two new formulations) was compared with the registered formulation of Talaromin in two methods of seed impregnation and soil addition with healthy control and infected control to control cotton Verticillium wilt disease, in the form of a randomized complete block design with 16 treatments and 5 replications. After statistical analysis of the data obtained by Duncan's Multiple Range Test by MS TAT C software, the results showed that in terms of disease severity among treatments with the previous formulation (Talaromin) with each of the methods of soil addition and seed impregnation, there was no statistically significant difference between nano-suspension with each of the concentrations of one, four and five per thousand by the soil addition method and nano-powder with each of the concentrations of two and three per thousand by soil addition method, and the mentioned treatments were included in one statistical group in terms of disease severity with healthy control.

Enhancement of Liver Targetability through Statistical Optimization and Surface Modification of Biodegradable Nanocapsules Loaded with Lamivudine.

The intention of the current work was to develop and optimize the formulation of biodegradable polymeric nanocapsules for lamivudine (LMV) in order to obtain desired physical characteristics so as to have improved liver targetability. Nanocapsules were prepared in this study as aqueous-core nanocapsules (ACNs) with poly(lactide-co-glycolide) using a modified multiple emulsion technique. LMV was taken as a model drug to investigate the potential of ACNs developed in this work in achieving the liver targetability. Three formulations factors were chosen and 33 factorial design was adopted. The selected formulation factors were optimized statistically so as to have the anticipated characteristics of the ACNs viz. maximum entrapment efficiency, minimum particle size, and less drug release rate constant. The optimized LMV-ACNs were found to have 71.54 ± 1.93% of entrapment efficiency and 288.36 ± 2.53 nm of particle size with zeta potential of -24.7 ± 1.2 mV and 0.095 ± 0.006 h-1 of release rate constant. This optimized formulation was subjected to surface modification by treating with sodium lauryl sulphate (SLS), which increased the zeta potential to a maximum of -41.6 ± 1.3 mV at a 6 mM concentration of SLS. The results of in vivo pharmacokinetics from blood and liver tissues indicated that hepatic bioavailability of LMV was increased from 13.78 ± 3.48 μg/mL ∗ h for LMV solution to 32.94 ± 5.12 μg/mL ∗ h for the optimized LMV-ACNs and to 54.91 ± 6.68 μg/mL ∗ h for the surface-modified LMV-ACNs.

Ascendancy of pyraclostrobin nanocapsule formulation against Rhizoctonia solani: From a perspective of fungus

High-performance pesticide formulations are essential for sustainable agriculture. Among these, nano-pesticides exhibit great advantages in pest control because of their unique size effects. However, the direct effects of nano-formulation fungicides on fungal pathogens remain largely unexplored. In this study, three qualified formulations, suspension concentrate (SC), microcapsules (CS), and nanocapsules (NCS) of pyraclostrobin (PYR) were prepared and utilized to reveal their biocontrol activities against Rhizoctonia solani. Among these three formulations, NCS exhibited notable biocontrol efficacy against R. solani exemplified by an EC50 of 0.319 mg/L for mycelia, distortion of mycelia and abnormalities in cell ultrastructure. Moreover, NCS displayed excellent internalization within R. solani mycelia, contributing to severe damage to cell membrane permeability. Importantly, an equivalent quantity of NCS-PYR showed potent inhibitory effects on the target pathogen, as indicated by reduced adenosine triphosphate (ATP) content and mitochondrial Complex III activity. The NCS consistently exhibited superior in vivo protective and curative activities against R. solani compared to those of CS and SC in rice and faba bean. In summary, we uncovered the strength of rapid efficacy and biocontrol activity of NCS against R. solani and elucidated the advantages of NCS-PYR from the perspective of the target pathogen in agriculture.

Hydrogel Containing Silibinin-Loaded Pomegranate Oil-Based Nanocapsules for Cutaneous Application: In Vitro Safety Investigation and Human Skin Biometry and Permeation Studies.

In previous studies, we developed a hydrogel formulation containing silibinin-loaded pomegranate oil nanocapsules (HG-NCSB) that had improved in vivo anti-inflammatory action in comparison to non-encapsulated silibinin. To determine skin safety and whether the nanoencapsulation influences silibinin skin permeation, NCSB skin cytotoxicity, HG-NCSB permeation in human skin, and a biometric study with healthy volunteers were conducted. The formulation of nanocapsules was prepared by the preformed polymer method while the HG-NCSB was obtained by thickening the suspension of nanocarriers with gellan gum. The cytotoxicity and phototoxicity of nanocapsules were assessed in Keratinocytes (HaCaT) and fibroblast (HFF-1) using the MTT assay. The hydrogels were characterized regarding the rheological, occlusive, and bioadhesive properties, and silibinin permeation profile in human skin. The clinical safety of HG-NCSB was determined by cutaneous biometry in healthy human volunteers. NCSB yielded better cytotoxicity results than the blank nanocapsules (NCPO). NCSB did not cause photocytotoxicity, while NCPO and the non-encapsulated substances (SB and pomegranate oil) were phototoxic. The semisolids presented non-Newtonian pseudoplastic flow, adequate bioadhesiveness, and low occlusive potential. The skin permeation demonstrated that HG-NCSB retained a higher SB amount in the outermost layers than HG-SB. In addition, HG-SB reached the receptor medium and had a superior concentration of SB in the dermis layer. In the biometry assay, there was no significant cutaneous alteration after the administration of any of the HGs. Nanoencapsulation promoted greater SB retention in the skin, averted percutaneous absorption, and made the topical use of SB and pomegranate oil safer.

In Vitro Cytotoxicity and In Vivo Antitumor Activity of Lipid Nanocapsules Loaded with Novel Pyridine Derivatives.

This study demonstrates high drug-loading of novel pyridine derivatives (S1-S4) in lipid- and polymer-based core-shell nanocapsules (LPNCs) for boosting the anticancer efficiency and alleviating toxicity of these novel pyridine derivatives. The nanocapsules were fabricated using a nanoprecipitation technique and characterized for particle size, surface morphology, and entrapment efficiency. The prepared nanocapsules exhibited a particle size ranging from 185.0 ± 17.4 to 223.0 ± 15.3 nm and a drug entrapment of >90%. The microscopic evaluation demonstrated spherical-shaped nanocapsules with distinct core-shell structures. The in vitro release study depicted a biphasic and sustained release pattern of test compounds from the nanocapsules. In addition, it was obvious from the cytotoxicity studies that the nanocapsules showed superior cytotoxicity against both MCF-7 and A549 cancer cell lines, as manifested by a significant decrease in the IC50 value compared to free test compounds. The in vivo antitumor efficacy of the optimized nanocapsule formulation (S4-loaded LPNCs) was investigated in an Ehrlich ascites carcinoma (EAC) solid tumor-bearing mice model. Interestingly, the entrapment of the test compound (S4) within LPNCs remarkably triggered superior tumor growth inhibition when compared with either free S4 or the standard anticancer drug 5-fluorouracil. Such enhanced in vivo antitumor activity was accompanied by a remarkable increase in animal life span. Furthermore, the S4-loaded LPNC formulation was tolerated well by treated animals, as evidenced by the absence of any signs of acute toxicity or alterations in biochemical markers of liver and kidney functions. Collectively, our findings clearly underscore the therapeutic potential of S4-loaded LPNCs over free S4 in conquering EAC solid tumors, presumably via granting efficient delivery of adequate concentrations of the entrapped drug to the target site.

Formulation of benznidazole-lipid nanocapsules: Drug release, permeability, biocompatibility, and stability studies

Benznidazole, a poorly soluble in water drug, is the first-line medication for the treatment of Chagas disease, but long treatment periods at high dosages cause several adverse effects with insufficient activity in the chronic phase. According to these facts, there is a serious need for novel benznidazole formulations for improving the chemotherapy of Chagas disease. Thus, this work aimed to incorporate benznidazole into lipid nanocapsules for improving its solubility, dissolution rate in different media, and permeability. Lipid nanocapsules were prepared by the phase inversion technique and were fully characterized. Three formulations were obtained with a diameter of 30, 50, and 100 nm and monomodal size distribution with a low polydispersity index and almost neutral zeta potential. Drug encapsulation efficiency was between 83 and 92 % and the drug loading was between 0.66 and 1.04 %. Loaded formulations were stable under storage for one year at 4 °C. Lipid nanocapsules were found to protect benznidazole in simulated gastric fluid and provide a sustained release platform for the drug in a simulated intestinal fluid containing pancreatic enzymes. The small size and the almost neutral surface charge of these lipid nanocarriers improved their penetration through mucus and such formulations showed a reduced chemical interaction with gastric mucin glycoproteins. LNCs. The incorporation of benznidazole in lipid nanocapsules improved the drug permeability across intestinal epithelium by 10-fold compared with the non-encapsulated drug while the exposure of the cell monolayers to these nanoformulations did not affect the integrity of the epithelium.

Nanomaterials in Plant Protection against Parasitic Nemates

A review of current data on the effect of nanoparticles on phytoparasitic nematodes in the study in vitro and in planta and on plants infested with nematodes was carried out. Available data have shown that many nanoparticles of metals, metal oxides and non-metals have an effective nematicidal potential. According to the available data, NPs can have a direct toxic effect on nematodes, reduce the infection of plants during seed pretreatment or spraying, lead to inhibition of reproduction and development of the parasite in the roots, and their effectiveness may exceed known commercial nematicides. Some nanoparticles have an immunostimulatory effect on plants. Data on the mechanisms of action of NPs on nematodes are presented. An important mechanism for the toxicity of nanoparticles to nematodes may be the generation of reactive oxygen species (oxidative stress). Exposure to nanoparticles increased the expression of target genes involved in oxidative stress and DNA damage repair. A small number of works have dealt with nanonematicides, which in the form of nanocapsules have proven to be very effective against endoparasitic nematodes.

Ocular permeability, intraocular biodistribution of lipid nanocapsule formulation intended for retinal drug delivery

Recently, cGMP analogues have been investigated for the treatment of inherited retinal degenerations (IRD) using intravitreal injections. However, higher vitreous elimination rates limit the possibility to treat the retina with small molecule drugs. Here, we investigated the potential of lipid nanocapsules (LNCs) as vehicles to reduce clearance and prolong the delivery of cGMP analogue, CN03 to the retinal photoreceptors. Initially LNCs were investigated for both topical/periocular and intravitreal administration routes. While LNC-mediated drug permeation through the cornea proved to be too low for clinical applications, intravitreal application showed significant promise. Intravitreally administered LNCs containing fluorescent tracer in ex vivo porcine eyes showed complete intravitreal dispersal within 24 h. Ocular bio-distribution on histological sections showed that around 10 % of the LNCs had reached the retina, and 40 % accumulated in the ciliary body. For comparison, we used fluorescently labeled liposomes and these showed a different intraocular distribution with 48 % accumulated in the retina, and almost none were in the ciliary body. LNCs were then tested in retinal explants prepared from wild-type (WT) and rd1 mouse. In WT retina LNCs showed no significant toxic effects up to a concentration of 5 mg/mL. In rd1 retina, the LNC/CN03 formulation protected rd1 photoreceptors with similar efficacy to that of free CN03, demonstrating the usefulness of LNC/CN03 formulation in the treatment of IRD. Overall, our results indicate the suitability of LNCs for intraocular administration and drug delivery to both the retina and the ciliary body.

Ameliorating the antiparasitic activity of the multifaceted drug ivermectin through a polymer nanocapsule formulation

Ivermectin (IVM) is a potent antiparasitic widely used in human and veterinary medicine. However, the low oral bioavailability of IVM restricts its therapeutic potential in many parasitic infections, highlighting the need for novel formulation approaches. In this study, poly(ε-caprolactone) (PCL) nanocapsules containing IVM were successfully developed using the nanoprecipitation method. Pumpkin seed oil (PSO) was used as an oily core in the developed nanocapsules. Previously, PSO was chemically analyzed by headspace solid-phase microextraction coupled to gas chromatography/mass spectrometry (HS-SPME/GC–MS). The solubility of IVM in PSO was found to be 4266.5 ± 38.6 μg/mL. In addition, the partition coefficient of IVM in PSO/water presented a logP of 2.44. A number of nanocapsule batches were produced by factorial design resulting in an optimized formulation. Negatively charged nanocapsules measuring around 400 nm demonstrated unimodal size distribution, and presented regular spherical morphology under transmission electron microscopy. High encapsulation efficiency (98–100%) was determined by HPLC. IVM-loaded capsules were found to be stable in nanosuspensions at 4 °C and 25 °C, with no significant variations in particle size observed over a period of 150 days. Nanoencapsulated IVM (0.3 mM) presented reduced toxicity to J774 macrophages and L929 fibroblasts compared to free IVM. Moreover, IVM-loaded nanocapsules also demonstrated enhanced in vitro anthelmintic activity against Strongyloides venezuelensis in comparison to free IVM. Collectively, the present findings demonstrate the promising potential of PCL-PSO nanocapsules to improve the antiparasitic effects exerted by IVM.

Comparison of nano-capsulated thyme essential oils on intestinal microbial population and anti-oxidation status of broilers

This study was conducted to evaluate the effects of non and nano-capsulated thyme essential oils with saturated and unsaturated lipids (tallow and canola oil) and two levels of diet crude protein (standard and low than standard) on intestinal microbial population and anti-oxidation status of broilers. In this study, 384 Ross-308 broiler chickens in a factorial engagement of 2×2×2 (2 medicinal plant essential oils, two sources of vegetable oils, and 2 levels of diet crude protein) were used in a completely randomized design with 8 treatments, 4 replicates, and 12 bird in each replicate for 42 days. Experimental periods included starter (1-10 days), grower (11-24 days), and finisher (25-42 days). Canola oil significantly reduced the intestinal coliforms population. In contrast, tallow increased them (P<0.05), a similar effect was observed with thyme forms, so the lowest coliform population blogged to the nano-capsulated form of thyme. In contrast, the highest coliform population resulted in non-capsulated thyme essential oil (P<0.05). In an interaction between thyme essential oil form and diet crude protein level, the lowest coliform population was observed with diet contained nano-capsulated thyme essential oil and low level of diet crude protein (P<0.05). Regarding antioxidant status, reducing the diet crude protein increased MDA and GPX (P<0.05). In an interaction between diet crude protein and thyme form, a diet with low crude protein and capsulated thyme increased the level of SOD (P<0.05). In general, results of the current experiment indicated that in Ross-308, broiler chickens using capsulated thyme essential oil with canola oil and low crude protein improves intestine microbial population and antioxidant status of broilers.

Pharmacokinetic profiles, cytotoxicity, and redox metabolism of free and nanoencapsulated curcumin

To analyze the biodistribution, pharmacokinetics, and toxicity of curcumin, we made in silico predictions and performed in vitro tests to demonstrate the differences in the behavior of two cells types (peripheral blood mononuclear cells, PBMCs, and fibroblasts, HFF-1 cell line) treated with curcumin nanocapsule formulations and curcumin solution with respect to cytotoxic effects and redox metabolism. We generated in silico, ADME/Tox profile predictions of curcumin using computational tools. We produced and characterized Eudragit® L-100 and PCL nanocapsules containing curcumin using interfacial deposition of preformed polymer, evaluation of hemolytic potential in erythrocytes, cytotoxic capacity (MTT and dsDNA PicoGreen® assay), and influence on redox metabolism (nitric oxide and DCF production) of PBMCs and HFF-1 treated with curcumin nanoformulations and solution response curves. Computational results showed low biodistribution, no permeation at of the blood-brain barrier (BBB), discreet gastrointestinal absorption, a potential inhibitor of cytochrome P450 isoforms (CYP2C9 and CYP3A4), toxicity class IV, and immunomodulatory action. In vitro tests showed that cell type influenced curcumin behavior. For cytotoxicity, PBMCs showed a concentration-dependent standard, while HFF-1 cells showed that incubation time was an important variable. Redox interactions showed that nanocapsules induced NO production, and all treatments reduced DCF levels. We highlight the pleiotropic biological activities of curcumin and drug release models so that the therapeutic properties of this polyphenol might be better used. Finally, we emphasize that pharmacological safety must always be evaluated in drug delivery systems and, especially, for substances with multiple interaction pathways.

Lyophilized tablets of felodipine-loaded polymeric nanocapsules to enhance aqueous solubility: Formulation and optimization

The aim of this study was to enhance the physicochemical properties of felodipine through the formulation of lyophilized polymeric nanocapsule tablets. Felodipine was loaded into polymeric nanocapsules composed of Labrafac™ PG (oil solubilizer) and Eudragit® EPO (cationic coating polymer) using the sonoprecipitation technique. The effect of changing quantities of Labrafac™ PG (X1) and Eudragit® EPO (X2) on the mean particle size (Y1), zeta potential (Y2) and entrapment efficiency (Y3) were studied via 32 full factorial design. Both factors X1 and X2 had a significant effect on the mean particle size, while the zeta potential was affected by X2. The entrapment efficiency was affected significantly by X2 and by the interaction between both factors (X1X2). After purification by filtration and ultracentrifugation, the optimized formulation was incorporated into lyophilized tablets using poly (vinyl alcohol) as binder and stabilizer and either of two types of cryoprotectant (mannitol or sucrose). Different characterizations were performed on both types of lyophilized polymeric nanocapsule tablets, showing that each type exhibited porous structure, high-level drug content, rapid disintegration, and fast dissolution rate. Moreover, the saturation solubility for each type was vastly increased. The present study provides a unique formulation of high-level drug-loaded polymeric nanocapsules that could be efficiently incorporated in lyophilized tablets to remarkably enhance its stability and to improve the physicochemical properties of felodipine.

Development and Characterization of Innovative Polymeric Oil-core Nanocarriers for Nisin Delivery

Nisin is an antimicrobial peptide broadly used as a preservative in the food industry. In this study, oil-core polymeric nanocapsules encapsulating nisin were prepared by a nanoprecipitation technique using three different synthetic biodegradable polymers, namely poly(butylene adipate-co-terephthalate) (PBAT), Eudragit RS-100® (EUD), and poly(ε-caprolactone) (PCL), and their physical characteristics, thermal resistance and antimicrobial activity against Listeria monocytogenes were investigated. All nanocapsule formulations showed entrapment efficiency superior to 96%. EUD and PCL nanocapsules showed average diameters ranging from 145 to 303 nm, while PBAT-nisin nanocapsules showed larger size and PDI index (556.2 nm and 0.51, respectively), possibly due to changes in the organic phase equilibrium during preparation. The thermogravimetric analysis indicates lower decomposition temperatures in the PCL and EUD nanocapsules containing nisin compared with the unload nanocapsule and the contrary effect in the PBAT. Moreover, all nisin-containing polymeric nanocapsules exhibited antimicrobial activity against L. monocytogenes in both agar diffusion tests and determination of antimicrobial units (AU/mL) in liquid media. Oil-core polymeric nanocapsules have not been previously described as carriers for nisin, and the results suggested that PBAT, EUD, and PCL could be suitable polymers for nisin delivery systems.

Itraconazole for Topical Treatment of Skin Carcinogenesis: Efficacy Enhancement by Lipid Nanocapsule Formulations.

Itraconazole (ITC), an antifungal drug with anticancer activity, shows potential for oral treatment of skin cancer. There is clinical need for topical ITC for treating low-risk skin carcinogenesis. Our objective was to develop ITC nanoformulations with enhanced anticancer efficacy. Lipid nanocapsules (LNC), either unmodified (ITC/LNC) or modified with the amphiphiles miltefosine (ITC/MF-LNC) or the lipopeptide biosurfactant surfactin (ITC/SF-LNC) as bioactive additives were developed. LNC formulations showed high ITC entrapment efficiency (>98%), small diameter (42-45 nm) and sustained ITC release. Cytotoxicity studies using malignant SCC 9 cells and normal human fibroblasts (NHF) demonstrated significant enhancement of ITC anticancer activity and selectivity for cancer cells by the LNC formulations and a synergistic ITC-amphiphile interaction improving the combination performance. Treatment of intradermal tumor-bearing mice with the ITC nanoformulation gels compared with ITC and 5-FU gels achieved significant tumor growth inhibition that was remarkably enhanced by ITC/MF-LNC and ITC/SF-LNC as well as recovery of skin architecture. Molecularly, tumoral expression of Ki-67 and cytokeratin proliferative proteins was significantly suppressed by LNC formulations, the suppressive effect on cytokeratins was superior to that of 5-FU. These findings provide new evidence for effective topical treatment of low-risk skin carcinogenesis utilizing multiple approaches that involve drug repurposing, nanotechnology, and bioactive amphiphiles as formulation enhancing additives.

Nanoencapsulation of Mandarin Essential Oil: Fabrication, Characterization, and Storage Stability.

This study evaluates the combined efficiency of whey protein isolate (WPI) with maltodextrin (MD) and gum arabic (GA), as a delivery system for encapsulating Citrus reticulata essential oil (CEO). The wall materials blended at different rates were produced to obtain seven formulations of nanocapsules (NCEO), namely NCEO-GA, NCEO-MD, NCEO-WPI, NCEO-GA/MD, NCEO-GA/WPI, NCEO-MD/WPI, and NCEO-GA/MD/WPI. The interaction between CEO and WPI was simulated by molecular docking. Findings showed that the physicochemical characteristics and storage stability of formulations containing WPI were considerably improved. The NCEO-GA/MD/WPI formulation demonstrated the optimum values of encapsulation efficiency (92.08%), highest glass transition temperature (79.11 °C), high crystallinity (45.58%), high thermal stability (mass loss at 100 °C < 5%), and also had the highest antioxidant activity and lowest peroxide value after storage. This study demonstrated that combining WPI with MD and GA, as wall material encapsulation, can produce nanocapsules with superior properties to those created using polysaccharides individually.

Chitosan/cyclodextrin surface-adsorbed naringenin-loaded nanocapsules enhance bacterial quorum quenching and anti-biofilm activities

Pathogenic bacteria use quorum sensing (QS), a cell-to-cell communication process that relies on small signaling molecules, to regulate the genetic expression that leads to several essential virulence factors such as bioluminescence, biofilm formation, bacterial motility, among other. Naringenin (NAR), a bitter and colorless flavanone ubiquitous in herbs and fruits, has been shown to inhibit QS activity in P. aeruginosa by decreasing the production of pyocyanin and elastase. In this study, to evaluate the anti-QS activity of naringenin against an E. coli Top 10 biosensor, we developed a novel core-corona nanocapsule formulation comprising surface co-adsorbed β-cyclodextrin (Captisol®) and chitosan loaded with NAR. The results showed that both the nanocapsule (NC) and nanoemulsion (NE) formulations, NAR payload associated with high efficiency , namely ~ 92.88 and ~ 67.98%, respectively. These formulations remained stable for 24 h and showed a biphasic controlled release profile in bacterial M9 medium. Captisol® was effectively immobilized on the NC’s surface, resulting in a surface charge inversion from positive (~ + 42 mV) to negative (~ −32 mV) ζ-potential. The biosensor assay revealed that NC outperformed NE in quenching the QS response and the incorporation of naringenin at the NC’s multifunctional surface enhanced this bioactivity. Cytotoxicity assays showed that when NAR was associated in NC (188 µM) it was not cytotoxic to Caco2 cells, by contrast with its free form, thus highlighting the cytoprotective effect of the developed formulation. Biofilm formation was inhibited up to ~ 60% in NAR-loaded NC (188 μM), indicating the synergistic effect of positively charged chitosan with the bioactivity of NAR while harnessing the NC's high surface area-to-volume ratio.

Characterization, Cytotoxicity and Anti-Inflammatory Effect Evaluation of Nanocapsules Containing Nicotine.

(1) Background: Nanotechnology is an emerging field that can be applied in the biomedical area. In this study, Eudragit nanocapsules (NCs) containing nicotine were produced. Nicotine is the main alkaloid found in tobacco and has anti-inflammatory properties. NCs containing nicotine may be used as an adjuvant therapy in the treatment of inflammation in the central nervous system. (2) Methods: Nanocapsules were prepared by the interfacial deposition of the pre-formed polymer method and characterized in terms of zeta potential, diameter, polydispersity index, pH, encapsulation efficiency (EE), stability and sustained release profile. In vitro tests with the PC12 cell line were performed, such as MTT, LIVE/DEAD and ELISA assays, to verify their cytotoxic and anti-inflammatory effects. (3) Results: The nanocapsules presented satisfactory values of the characterization parameters; however, poor encapsulation was obtained for nicotine (8.17% ± 0.47). The in vitro tests showed that the treatment with nanocapsules reduced cell viability, which suggests that the Eudragit or the amount of polymer on top of the cells may be detrimental to them, as the cells were able to survive when treated with bulk nicotine. ELISA showed an increment in the expression of IL-6 and IL-1β, corroborating the hypothesis that NCs were toxic to the cells because of the increase in the levels of these pro-inflammatory cytokines. (4) Conclusions: This study demonstrates that NCs of Eudragit present toxicity. It is therefore necessary to improve NC formulation to obtain better values for the encapsulation efficiency and reduce toxicity of these nanodevices.