Zeta Potential Profile Research Articles

Co-spray drying whey protein isolate with polysaccharides provides additional lubrication impacting the sensory profile of model beverages

For older adults, whey protein is associated with negative sensory attributes, including undesirable mouthfeel qualities, that limit consumption and acceptance. Previous work suggests that increased lubrication may have the ability to reduce whey protein-associated mouthdrying, a driver for disliking, by limiting interactions of whey protein with salivary proteins and mucin. This was investigated in the current study by co-spray drying whey protein with combinations of maltodextrin, xanthan gum and/or guar gum; the resulting powders were used to make 10% suspensions. The particle size, zeta potential, rheological and tribological profiles of these suspensions were measured. It was shown that co-spray drying whey protein with guar gum led to a reduction in instrumental friction, irrespective of changes in viscosity. These samples were perceived as significantly more mouthcoating and smooth when assessed by a trained sensory panel. Contrastingly, suspensions containing xanthan gum showed increased viscosity and enhanced shear thinning compared with whey protein, but no change in instrumental friction at higher sliding speeds. This may be a result of a larger particle size, representing increased aggregation in samples containing xanthan gum. There was no significant difference in mouthdrying or slipperiness perception between the suspensions. These findings suggest that the incorporation of guar gum has the capacity to reduce oral friction and impact mouthfeel in whey protein model beverages. This should be taken forward into temporal sensory trials to further investigate the effects of additional lubrication.

The role of carboxyl and cationic groups in low-level cationised cellulose fibres investigated by zeta potential and sorption studies

The anionic nature of both cellulose fibres and reactive dyes prevents substantial exhaustion of dye from the dyebath, which is at neutral pH before alkali is added to initiate dye fixation. Conventionally, salt is added to minimize the electrostatic repulsions that interfere with dye sorption, but that increases salt loads in effluents. An alternative is to affix cationic agents on the cellulose to overcome the inherent anionic charge, but that has generally been observed to result in uneven dye sorption. The focus of investigations in this work is to examine the influence of the ratio of charges on cellulose (of affixed cationic charges to inherent anionic charges) on the extents and evenness of dye sorption. The cationisation agent 3-chloro-2-hydroxypropyl-N,N,N-trimethylammonium chloride (CHPTAC) was grafted on loose viscose fibres to yield 12 to 185 mmol kg−1 cationic group content on the fibre that exhibited an inherent carboxyl group content of 68 mmol kg−1. Three different dyes (of varying molecular sizes and anionic group content) were employed for examination of sorption profiles. The results from both zeta potential measurements and dye sorption profiles showed evidence of limited dye uptake until the cationic group content in fibres exceeded that of the inherent carboxyl groups. Thereafter, an uptick in dye sorption was observed, with dye sorption levels increasing with rise in degree of cationisation. There were differences between the dyes in their degrees of sorption, which appear correlated with their molecular sizes.

Development and Assessment of Helicteres isora Extract Loaded Phospholipid Complex for Anti-Nociceptive Activity

Its primary objective is to assess the efficacy of a phospholipid complex formulation containing an extract of Helicteres isora in reducing inflammation, to determine its progress and evaluation. An Indian Screw Tree, also known as Helicteres isora, is an extremely healing plant. In addition to improving solubility and stability, the phospholipid complex formulation also increases bioavailability and efficacy. This formulation was created by combining Helicteres isora extract with phospholipids using a technique known as phospholipid complexation. Several parameters were evaluated to evaluate the formulation, including particle size, zeta potential, encapsulation efficiency, and drug release profile. Using both in vitro and in vivo models, the anti-inflammatory properties of a phospholipid complex formulation of Helicteres isora were assessed. The experiments were conducted using a rat model of carrageenan-induced paw edema. In this work, phospholipid complex formulations were shown to have improved physicochemical properties, including smaller particle sizes and higher encapsulation rates. According to the results of the in vivo evaluation, phospholipid complex formulations significantly reduced paw edema compared with plain extracts, indicating improved anti-inflammatory activity. The bioavailability, anti-inflammatory activity, and bioavailability of Helicteres isora extract are enhanced by the phospholipid complex formulation.

Biophysical characterization of α-glucan nanoparticles encapsulating feruloylated soy glycerides (FSG)

Water insoluble α-glucans that were enzymatically synthesized using glucansucrase that was cloned from Leuconostoc mesenteroides NRRL B-1118 were previously shown to form nanoparticles via high pressure homogenization. These α-glucan nanoparticles were previously shown capable of encapsulating a small hydrophobic molecule. This work demonstrates that the same α-glucan can be formed into nanoparticles that encapsulate feruloylated soy glycerides from modified soybean oil, a product of interest to the cosmetic and skin care industries because of the UV absorbance and antioxidant properties of the feruloyl moiety. It is demonstrated that the feruloylated soy glyceride/α-glucan nanoparticles have distinct size, zeta potential and thermal profiles from that of nanoparticles made from α-glucan alone or feruloylated soy glyceride alone. Thermal analysis also demonstrates the release of feruloylated soy glycerides from the α-glucan nanoparticles.

Studying the Anti-Virulence Activity of Meta-Bromo-Thiolactone against Staphylococcus aureus and MRSA Phenotypes

Quorum-sensing inhibitors have recently garnered great interest, as they reduce bacterial virulence, lower the probability of resistance, and inhibit infections. In this work, meta-bromo-thiolactone (mBTL), a potent quorum and virulence inhibitor of Staphylococcus aureus (S. aureus) and methicillin-resistant S. aureus (MRSA), was formulated in chitosan nanoparticles (ChNPs) using the ionic gelation method. The mBTL-loaded-ChNPs were characterized by their particle size, polydispersity index, zeta potential, morphology, and drug release profile. The results show that the mBTL-loaded-CNPs comprised homogenized, spherical nanoparticles ranging from 158 ± 1.3 to 284 ± 5.6 nm with a sustainable release profile over 48 h at 37 °C. These findings confirm the successful preparation of mBTL-loaded-ChNPs. Confocal laser scanning microscopy showed a significant reduction in the number of viable cells, indicating the antibacterial efficacy of mBTL. Biofilms were observed by scanning electron microscopy, which showed that the bacterial cells in the control experiment were enclosed in thick biofilms. In the presence of mBTL, the bacterial cells remained disordered and did not form a biofilm. mBTL-loaded-ChNPs represent a potential approach to overcoming antimicrobial resistance in the treatment of MRSA infection.

Synthesis and evaluation of folate-mediated targeting and poly (β-amino ester)-mediated pH-responsive delivery system of riccardin D based on the O-carboxymethylated chitosan micelles

This study aimed to combine the active targeting function of folate (FA) receptor-mediated endocytosis with the pH-responsive drug delivery of poly (ethylene glycol)-grafted-poly (−amino ester) copolymers (PEG-PAE) in cancer targeting therapy. Herein, O-carboxymethylated chitosan (OCMC) was grafted with hydrophobic deoxycholic acid (DOCA). Further, PEG-PAE and FA-conjugated DOCA modified OCMC were synthesized to develop the potential cancer-targeted carrier (PEG-PAE-DOMC-FA), for which the structure was investigated by 1H NMR and FTIR. Then riccardin D (RD) was successfully loaded for tumor-targeted drug delivery. The particle size, zeta potential, encapsulating efficiencies, and loading content profiles of PEG-PAE-DOMC-FA/RD showed a strong dependence on the environmental pH values. The cumulative release of PEG-PAE-DOMC-FA/RD at pH 5.0 (90.63 %) was higher than pH 7.4 (51.12 %), which also indicated the pH sensitivity. Moreover, a lower IC50 and higher coumarin-6 uptake were found because of the folate-receptor-mediated endocytosis. In pharmacokinetic study, PEG-PAE-DOMC-FA/RD significantly improved the mean retention time (MRT) and AUC(0-∞) from 7.89 h and 36.1 mg/L·h of control group to 10.03 h and 123.8 mg/L·h. In the xenograft mice model, stronger antitumor efficacy and lower toxicity were confirmed. In conclusion, the multi-functional micelles could be considered as a promising vehicle for delivering hydrophobic drugs to tumors.

Chitosan-Coated Solid Lipid Nanoparticles as an Efficient Avenue for Boosted Biological Activities of Aloe perryi: Antioxidant, Antibacterial, and Anticancer Potential.

Aloe perryi (ALP) is an herb that has several biological activities such as antioxidant, antibacterial, and antitumor effects and is frequently used to treat a wide range of illnesses. The activity of many compounds is augmented by loading them in nanocarriers. In this study, ALP-loaded nanosystems were developed to improve their biological activity. Among different nanocarriers, solid lipid nanoparticles (ALP-SLNs), chitosan nanoparticles (ALP-CSNPs), and CS-coated SLNs (C-ALP-SLNs) were explored. The particle size, polydispersity index (PDI), zeta potential, encapsulation efficiency, and release profile were evaluated. Scanning electron microscopy was used to see the nanoparticles' morphology. Moreover, the possible biological properties of ALP were assessed and evaluated. ALP extract contained 187 mg GAE/g extract and 33 mg QE/g extract in terms of total phenolic and flavonoid content, respectively. The ALP-SLNs-F1 and ALP-SLNs-F2 showed particle sizes of 168.7 ± 3.1 and 138.4 ± 9.5 nm and the zeta potential values of -12.4 ± 0.6, and -15.8 ± 2.4 mV, respectively. However, C-ALP-SLNs-F1 and C-ALP-SLNs-F2 had particle sizes of 185.3 ± 5.5 and 173.6 ± 11.3 nm with zeta potential values of 11.3 ± 1.4 and 13.6 ± 1.1 mV, respectively. The particle size and zeta potential of ALP-CSNPs were 214.8 ± 6.6 nm and 27.8 ± 3.4 mV, respectively. All nanoparticles exhibited PDI < 0.3, indicating homogenous dispersions. The obtained formulations had EE% and DL% in the ranges of 65-82% and 2.8-5.2%, respectively. After 48 h, the in vitro ALP release rates from ALP-SLNs-F1, ALP-SLNs-F2, C-ALP-SLNs-F1, C-ALP-SLNs-F2, and ALP-CSNPs were 86%, 91%, 78%, 84%, and 74%, respectively. They were relatively stable with a minor particle size increase after one month of storage. C-ALP-SLNs-F2 exhibited the greatest antioxidant activity against DPPH radicals at 73.27%. C-ALP-SLNs-F2 demonstrated higher antibacterial activity based on MIC values of 25, 50, and 50 µg/mL for P. aeruginosa, S. aureus, and E. coli, respectively. In addition, C-ALP-SLNs-F2 showed potential anticancer activity against A549, LoVo, and MCF-7 cell lines with IC50 values of 11.42 ± 1.16, 16.97 ± 1.93, and 8.25 ± 0.44, respectively. The results indicate that C-ALP-SLNs-F2 may be promising nanocarriers for enhancing ALP-based medicines.

Sesame seed protein: Amino acid, functional, and physicochemical profiles

Sesame (Sesamum indicum L.) is an erect herbaceous annual plant with flat seeds. It is one of the oldest cultivated oilseed plants in the world, especially popular in Africa and Asia.&#x0D; The present research objective was to describe a sesame protein isolate, i.e., its amino acid profile, functional and physicochemical properties, zeta potential, and hydrodynamic diameter. The surface charge and hydrodynamic diameter in aqueous solutions were obtained for standard sesame seeds, defatted sesame seeds, and the sesame protein isolate.&#x0D; Defatted sesame seeds yielded the following optimal parameters: salt concentration – 0.6 M, pH – 7, iso-electric point (pI) – 4. The sesame protein isolate was rich in methionine content, which is rare in other plant proteins, but its lysine content was lower than in other isolates. The sesame protein isolate displayed almost identical zeta potential profiles with its pH. The decreasing pH increased the zeta values gradually from the lowest negative value to the highest positive value. The zeta potentials of standard and defatted sesame seeds at pH 7 were –23.53 and –17.30, respectively. The hydrodynamic diameter of the sesame protein isolate (0.33 μm) was smaller than that of sesame seeds (2.64 μm) and defatted sesame seeds (3.02 μm). The sesame protein isolate had a water holding capacity of 1.26 g/g and an oil holding capacity of 3.40 g/g. Its emulsifying properties looked as follows: emulsion capacity – 51.32%, emulsion stability – 49.50%, emulsion activity index – 12.86 m2/g, and emulsion stability index – 44.96 min, respectively. These values are suitable for the sesame protein isolate and are consistent with the literature.&#x0D; The sesame protein isolate was a good source of protein (88.98%). Using sesame proteins as functional components can be an important basis for better knowledge of the relationship between electrical charge interactions in food matrices and the structure, stability, shelf life, texture, structural and functional properties of food. Research prospects include the effects of sesame protein isolates on various food systems.

Development and in-vitro evaluation of chitosan and glyceryl monostearate based matrix lipid polymer hybrid nanoparticles (LPHNPs) for oral delivery of itraconazole

Itraconazole (ICZ) is a broad spectrum antifungal drug, but used as second or third line therapy due to its low and erratic oral bioavailability. This work was carried out to prepare and characterize matrix type lipid-polymer hybrid nanoparticles (LPHNPs) for dissolution enhancement of ICZ. LPHNPs were prepared using solvent diffusion/emulsification technique. Matrix LPHNPs were composed of chitosan (polymer), glyceryl monostearate (lipid) and poloxamer 188 (stabilizer). LPHNPs loaded with ICZ (LPHNPs-1, LPHNPs-2, LPHNPs-3 and LPHNPs-4) were developed using varying concentration of chitosan whereas LPHNPs (LPHNPs-5, LPHNPs-6, LPHNPs-7 and LPHNPs-8) were prepared using varying concentrations of poloxamer 188. LPHNPs loaded with ICZ were further evaluated for entrapment efficiency, particle size, polydispersity index (PDI), zeta potential and dissolution profiles at biorelevant pH conditions. The particle size (LPHNPs-1 to LPHNPs-4) was found to be in range of 421–588 nm with PDI values 0.34–0.41. The particles size of LPHNPs-5 to LPHNPs-8 was found to be in range of 489–725 nm with PDI 0.34–0.74. The entrapment efficiency of LPHNPs-1 to LPHNPs-4 was found to be in range of 85.21%–91.34%. The entrapment efficiency of LPHNPs-5 to LPHNPs-8 was found to be in range 78.32%–90.44%. . The scanning electron microscopy of optimized formulations LPHNPs-1 and LPHNPs-5 indicated formation of oval shaped nanoparticles. DSC thermogram of ICZ loaded LPHNPs also depicted the conversion of crystalline form of ICZ into amorphous form demonstrating the internalization and dissolution enhancement of drug in the hybrid matrix. The cumulative drug dissolved at acidic pH 1.2 was found to be 23.3% and 19.8% for LPHNPs-1 and LPHNPs-5 respectively. Similarly at basic pH values 7.4, cumulative amount of drug dissolved was 90.2% and 83.4% for LPHNPs-1 and LPHNPs-5 respectively. Drug dissolution kinetics exhibited fickian diffusion best described by Korse-meyer Peppas model. The results suggested that chitosan and glyceryl monostearate based matrix LPHNPs could be used as promising approach for dissolution enhancement of ICZ which could further increase its bioavailability.

NANOPARTÍCULAS DE SÍLICA (NPSiO2) UTILIZADAS PARA O TRATAMENTO DE DISTÚRBIOS ASSOCIADOS AO SISTEMA NERVOSO CENTRAL (SNC)

SILICA NANOPARTICLES (SiO2NP) USED FOR THE TREATMENT OF DISORDERS ASSOCIATED WITH THE CENTRAL NERVOUS SYSTEM (CNS). In the last decade, nanomedicine has investigated the potential use of silica nanoparticles for drug delivery due to the favorable physicochemical properties of these systems as carriers. Specifically, a few studies have focused on applying silica-based nanosystems to deliver drugs into the central nervous system to treat neurological disorders. The present review aimed to evaluate the properties of silica nanoparticles, such as size, zeta potential, surface area, entrapment efficiency, drug loading, and release profile, exclusively applied for the treatment of central nervous system disorders as well as to describe the correlation between biological outcomes and physicochemical properties. Furthermore, the main processes related to the development of silica nanoparticles, such as preparation and characterization methods, were covered in this review to aid the systematic development of silica-based nanoparticles. In the articles reviewed, silica nanocarriers used in neurological disorders did not exhibit physicochemical similarities. Thus, attempts to prospect relations between physicochemical properties and biological effects are still inefficient when silica nanoparticles are used as drug delivery systems in neurological disorders. Therefore, each silica-based nanocarrier must be fully physicochemical and biologically characterized to comprehend how the structural features of silica nanoparticles affect biological systems.

Colistin sulfate-sodium deoxycholate sulfate micelle formulations; molecular interactions, cell nephrotoxicity and bioactivity

This study aimed to develop a micelle formulation of colistin with several mole ratios of sodium deoxycholate sulfate (SDCS) carrier to reduce its nephrotoxicity. The molar ratio and surface properties of colistin and SDCS were determined. Colistin was incorporated into SDCS micelles followed by lyophilisation. The formulated micelles were evaluated in terms of particle size, zeta potential, morphology, thermal properties, encapsulation efficiency (EE) and release profile. The interactions were analysed with FTIR, NMR and also in-silico studies using molecular docking. The MIC and MBC were calculated, while time-kill kinetics were observed. Furthermore, a cytotoxicity study of the formulations against kidney cells was carried out and data were analysed. Particle sizes were in the range of 140.9–162.6 nm with spherical shapes, and the zeta potential values were between −35.3 and −22.8 mV. The EE of colistin was between 17.73 and 40.15%. FTIR and DSC data indicated an interaction between the colistin and SDCS, and the NMR analysis revealed hydrogen bonding and electrostatic interaction as the main interaction. Molecular docking simulation showed that multiple hydrogen bonds were present between the hydrophilic ring of colistin and SDCS. The formulations showed good safety profiles with non-cytotoxic effects against the kidney cell while maintaining antibacterial activity. The overall results indicated that micelle formulations with SDCS can be a good option for the delivery of colistin to reduce its nephrotoxicity with better antibacterial activity, while further studies in the animal model are important.

Lentil protein: impact of different extraction methods on structural and functional properties

Plant proteins with improved solubility, foaming, and emulsifying properties are required to meet the demand for plant-based foods. This study evaluated the influence of alkaline extraction combined with enzyme- and ultrasound-assisted extraction on lentil protein structure and functionality. Enzyme- and ultrasound-assisted extractions were not capable of increasing the protein yield compared to alkaline extraction alone. However, the purity of isolated protein was dependent on the extraction process, ranging from 82.7% to 90%. Although the molecular mass, zeta potential profiles, and denaturation temperature were not dependent on the extraction method, the enthalpy of denaturation for protein obtained solely by alkaline extraction was significantly lower than that for assisted processes, indicating that protein denaturation is caused by an alkaline process. Changes in protein structure were also suggested by solubility analyses that showed that lentil proteins obtained by enzyme-assisted and ultrasound-assisted extraction have better solubility at pH 7 when compared to alkaline extraction alone. The surface activity of lentil protein was evidenced by interfacial and surface analysis, and it was influenced by the extraction process applied. We demonstrated that combining alkaline extraction with assisted processes, especially ultrasound technology, results in concentrates/isolates with higher solubility as compared to ones obtained solely by the traditional alkaline method, even though the choice of extraction method should depend on the desired functionality.

In vitro and in vivo evaluation of a novel lidocaine-loaded cubosomal gel for prolonged local anesthesia.

Marketed lidocaine dosage forms (such as ointment, gels, and injections) used to manage acute and chronic pain showed a short duration of action (<2 h). In this study, a lidocaine-loaded cubosomal gel was prepared to sustain the release of lidocaine to prolong the local anesthetic effect (high drug retention in the skin). Lidocaine-loaded cubosomal gels were prepared by melt emulsification and sonication using Pluronic F127 and DL-α-monoolein (at different levels). The cubosomal gels were characterized by morphology, size, zeta potential, entrapment efficacy, assay, viscosity, pH, and texture profiles. Ex vivo lidocaine permeation and retention studies were performed using Sprague-Dawley rat skin. Transmission electron microscopy images confirmed the bi-continuous liquid crystalline phase with a honeycomb cubosome structure. The cubosomal particle size (103-227nm), viscosity (13,524-15,627cp), and entrapment efficacy (78.4-94.7%) increase with the level of monoolein. The ex-vivo permeation study showed a biphasic release pattern, with lidocaine cleared from ointment within 4h (97.9% cumulative release), while cubosomal gels showed sustained release up to 24h (53.33-98.86% cumulative release). A skin retention study demonstrated that cubosomes can increase (up to 28-fold) the lidocaine content in the skin (4.56mg) compared to ointment (0.19mg). A rabbit skin irritation study showed no sign of irritation after the application of cubosomal gel. In the radiant heat tail-flick study, the local anesthetic effect of lidocaine from the cubosomal gel was sustained for up to 16h with 1.43-fold higher efficacy than marketed ointment. In conclusion, the study demonstrated the potential of cubosomal nanoparticle-laden gel to sustain the release of lidocaine for prolonging local anesthetic effects for pain management.

Sustained delivery of salbutamol from cubosomal gel for management of paediatric asthma: in vitro and in vivo evaluation

Aim In the current study, efforts are being made to formulate transdermal salbutamol-cubosomal gel to manage paediatric asthma. Methods Salbutamol-loaded cubosomal gels were prepared by melt emulsification and sonication. The cubosomal gels were characterised by morphology, particle size, zeta potential, entrapment efficacy, assay, viscosity, and texture profiles. Ex vivo permeation and pharmacokinetic studies were performed using rats. Results The mean cubosomal particle size (208–361 ± 12.5–32.5 nm), PDI (0.06–0.11 ± 0.01–0.02), viscosity (8527–9019 cp), and entrapment efficacy (76.3–91.0% w/w) increase with the level of monoolein. The ex vivo permeation study showed a biphasic release pattern, with salbutamol cleared from control gel within 8 h, while cubosomal gels showed sustained release up to 72 h. The pharmacokinetic profiles in the rat model showed 8.62-fold higher bioavailability with cubosomal gel. Conclusion The study demonstrated the potential of cubosomal nanoparticle-laden gel to sustain the release of salbutamol to treat paediatric asthma.

Development of Biodegradable Delivery Systems Containing Novel 1,2,4-Trioxolane Based on Bacterial Polyhydroxyalkanoates

In this work, delivery systems in the form of microparticles and films containing 1,2,4-trioxolane (ozonide, OZ) based on polyhydroxyalkanoates (PHAs) were developed. Main systems’ characteristics were investigated: the particle yield, average diameter, zeta potential, surface morphology, loading capacity, and drug release profile of microparticles, as well as surface morphology and release profiles of OZ-containing films. PHA-based OZ-loaded microparticles have been found to have satisfactory size, zeta potential, and ozonide loading-release behavior. It was noted that OZ content influenced the surface morphology of obtained systems.

Development, Characterization, Optimization, and In Vivo Evaluation of Methacrylic Acid-Ethyl Acrylate Copolymer Nanoparticles Loaded with Glibenclamide in Diabetic Rats for Oral Administration.

The methacrylic acid–ethyl acrylate copolymer nanoparticles were prepared using the solvent displacement method. The independent variables were the drug/polymer ratio, surfactant concentration, Polioxyl 40 hydrogenated castor oil, the added water volume, time, and stirring speed, while size, PDI, zeta potential, and encapsulation efficiency were the response variables analyzed. A design of screening experiments was carried out to subsequently perform the optimization of the nanoparticle preparation process. The optimal formulation was characterized through the dependent variables size, PDI, zeta potential, encapsulation efficiency and drug release profiles. In vivo tests were performed in Wistar rats previously induced with diabetes by administration of streptozotocin. Once hyperglycemia was determined in rats, a suspension of nanoparticles loaded with glibenclamide was administered to them while the other group was administered with tablets of glibenclamide. The optimal nanoparticle formulation obtained a size of 18.98 +/− 9.14 nm with a PDI of 0.37085 +/− 0.014 and a zeta potential of −13.7125 +/− 1.82 mV; the encapsulation efficiency was of 44.5%. The in vivo model demonstrated a significant effect (p < 0.05) between the group administered with nanoparticles loaded with glibenclamide and the group administered with tablets compared to the group of untreated individuals.

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.

PH-responsive and folate-coated liposomes encapsulating irinotecan as an alternative to improve efficacy of colorectal cancer treatment

Irinotecan (IRN) is a semisynthetic derivative of camptothecin that acts as a topoisomerase I inhibitor. IRN is used worldwide for the treatment of several types of cancer, including colorectal cancer, however its use can lead to serious adverse effects, as diarrhea and myelosuppression. Liposomes are widely used as drug delivery systems that can improve chemotherapeutic activity and decrease side effects. Liposomes can also be pH-sensitive to release its content preferentially in acidic environments, like tumors, and be surface-functionalized for targeting purposes. Herein, we developed a folate-coated pH-sensitive liposome as a drug delivery system for IRN to reach improved tumor therapy without potential adverse events. Liposomes were prepared containing IRN and characterized for particle size, polydispersity index, zeta potential, concentration, encapsulation, cellular uptake, and release profile. Antitumor activity was investigated in a murine model of colorectal cancer, and its toxicity was evaluated by hematological/biochemical tests and histological analysis of main organs. The results showed vesicles smaller than 200 nm with little dispersion, a surface charge close to neutral, and high encapsulation rate of over 90%. The system demonstrated prolonged and sustained release in pH-dependent manner with high intracellular drug delivery capacity. Importantly, the folate-coated pH-sensitive formulation had significantly better antitumor activity than the pH-dependent system only or the free drug. Tumor tissue of IRN-containing groups presented large areas of necrosis. Furthermore, no evidence of systemic toxicity was found for the groups investigated. Thus, our developed nanodrug IRN delivery system can potentially be an alternative to conventional colorectal cancer treatment.

Preparation and characterization of PANI: α borophene electrode for supercapacitors

In this study, α Borophene as a two-dimensional nanomaterial was prepared via a facile and low-cost ultrasonic exfoliation. Zeta potential profile showed that the prepared α borophene has sufficient electrostatic repulsion to achieve good physical stability. Randomly grown Polyaniline (PANI): α borophene nano network electrode was prepared on Ni foam substrate. Electrochemical performance of PANI: α borophene was investigated. The electrochemical measurements reveal that the specific capacitance of the PANI: α borophene electrode was 960 Fg -1 with the capacitance retention of 95% after 1000 cycles. α Borophene enhanced the capacitive performance of PANI. PANI: α borophene is a promising material with high specific capacity and good stability for supercapacitors. • α Borophene was prepared via ultrasonic exfoliation. • Polyaniline (PANI): α borophene nano network electrode was prepared. • The specific capacitance of the electrode was 960 Fg -1 with the capacitance retention of 95%

A Screening Study for the Development of Simvastatin-Doxorubicin Liposomes, a Co-Formulation with Future Perspectives in Colon Cancer Therapy

An increasing number of studies published so far have evidenced the benefits of Simvastatin (SIM) and Doxorubicin (DOX) co-treatment in colorectal cancer. In view of this, the current study aimed to investigate the pharmaceutical development of liposomes co-encapsulating SIM and DOX, by implementing the Quality by Design (QbD) concept, as a means to enhance the antiproliferative effect of the co-formulation on C26 murine colon cancer cells co-cultured with macrophages. It is known that the quality profile of liposomes is dependent on the critical quality attributes (CQAs) of liposomes (drug entrapped concentration, encapsulation efficiency, size, zeta potential, and drug release profile), which are, in turn, directly influenced by various formulation factors and processing parameters. By using the design of experiments, it was possible to outline the increased variability of CQAs in relation to formulation factors and identify by means of statistical analysis the material attributes that are critical (phospholipids, DOX and SIM concentration) for the quality of the co-formulation. The in vitro studies performed on a murine colon cancer cell line highlighted the importance of delivering the optimal drug ratio at the target site, since the balance antiproliferative vs. pro-proliferative effects can easily be shifted when the molar ratio between DOX and SIM changes.