-
Scientific Reports May 2024Hydatidosis causes a serious health hazard to humans and animals leading to significant economic and veterinary and public health concern worldwide. The present study...
Hydatidosis causes a serious health hazard to humans and animals leading to significant economic and veterinary and public health concern worldwide. The present study aimed to evaluate the in vitro and ex vivo protoscolicidal effects of synthesized poly(amidoamine), PAMAM, nanoemulsion. In this study, PAMAM was characterized through dynamic light scattering technique to investigate the particle size and zeta potential of nanoemulsified polymer. For the in vitro and ex vivo assays, we used eosin dye exclusion test and scanning electron microscope (SEM) to evaluate the effects of the prepared and characterized PAMAM nanoemulsion against protoscoleces from Echinococcus granulosus sensu lato G6 (GenBank: OQ443068.1) isolated from livers of naturally infected camels. Various concentrations (0.5, 1, 1.5 and 2 mg/mL) of PAMAM nanoemulsion at different exposure times (5, 10, 20 and 30 min) were tested against protoscolices. Our findings showed that PAMAM nanoemulsion had considerable concentration- and time-dependent protoscolicidal effect at both in vitro and ex vivo experiments. Regarding in vitro assay, PAMAM nanoemulsion had a potent protoscolicidal effect when compared with the control group with a highest protoscolicidal activity observed at the concentration of 2 mg/mL at all exposure times, such that 100% of protoscolices were killed after 20 min of exposure. Also, the mortality of protoscolices was 100% after 30 min of exposure to 1 and 1.5 mg/mL of PAMAM nanoemulsion, in vitro. Concerning ex vivo assay PAMAM nanoemulsion recorded the highest mortality rates at the concentration of 2 mg/mL (55, 99.4 and 100% at 10, 20, 30 min, respectively). Ultrastructure examination of examined protoscolices after 20 min of exposure to PAMAM nanoemulsion showed a complete loss of rostellar hooks, disruption of suckers with disorganization of hooks with partial or complete loss of them, and damage of protoscolices tegument with loss of their integrity in the form of holes and contraction of the soma region were observed in 1.5 and 2 mg/mL of PAMAM, in vitro and ex vivo, showing more damage in the in vitro conditions. It can be concluded that PAMAM nanoemulsion is a promising protoscolicidal agent offering a high protoscolicidal effect at a short exposure time. Further in vivo studies and preclinical animal trials are required to evaluate its efficacy and clinical applications against hydatid cysts.
Topics: Animals; Echinococcus granulosus; Emulsions; Echinococcosis; Polyamines; Nanoparticles; Particle Size; Camelus
PubMed: 38796499
DOI: 10.1038/s41598-024-62015-0 -
Pharmaceuticals (Basel, Switzerland) May 2024The use of medicinal substances in nanosized forms (nanoforms, nanoparticles) allows the therapeutic effectiveness of pharmaceutical preparations to be increased due to... (Review)
Review
The use of medicinal substances in nanosized forms (nanoforms, nanoparticles) allows the therapeutic effectiveness of pharmaceutical preparations to be increased due to several factors: (1) the high specific surface area of nanomaterials, and (2) the high concentration of surface-active centers interacting with biological objects. In the case of drug nanoforms, even low concentrations of a bioactive substance can have a significant therapeutic effect on living organisms. These effects allow pharmacists to use lower doses of active components, consequently lowering the toxic side effects of pharmaceutical nanoform preparations. It is known that many drug substances that are currently in development are poorly soluble in water, so they have insufficient bioavailability. Converting them into nanoforms will increase their rate of dissolution, and the increased saturation solubility of drug nanocrystals also makes a significant contribution to their high therapeutic efficiency. Some physical and chemical methods can contribute to the formation of both pure drug nanoparticles and their ligand or of polymer-covered nanoforms, which are characterized by higher stability. This review describes the most commonly used methods for the preparation of nanoforms (nanoparticles) of different medicinal substances, paying close attention to modern supercritical and cryogenic technologies and the advantages and disadvantages of the described methods and techniques; moreover, the improvements in the physico-chemical and biomedical properties of the obtained medicinal nanoforms are also discussed.
PubMed: 38794157
DOI: 10.3390/ph17050587 -
Medicina (Kaunas, Lithuania) May 2024Cellulite, or edemato-fibro-sclerotic panniculopathy (EFP), is characterized by dermal and hypodermal changes leading to adipose tissue accumulation and compromised... (Randomized Controlled Trial)
Randomized Controlled Trial
Clinical and Ultrasound Efficacy of Topical Hypertonic Cream (Jovita Osmocell) in the Treatment of Cellulite: A Prospective, Monocentric, Double-Blind, Placebo-Controlled Study.
Cellulite, or edemato-fibro-sclerotic panniculopathy (EFP), is characterized by dermal and hypodermal changes leading to adipose tissue accumulation and compromised venous circulation. This study investigates the efficacy of a hypertonic cream containing concentrated sodium chloride (Jovita Osmocell) in addressing water retention and structural alterations in adipose tissue, aiming to interrupt the cellulite formation process. A 12-week, prospective, monocentric, double-blind, placebo-controlled study enrolled 30 female subjects with grade II or III cellulite. Patients were randomized to receive hypertonic cream or a placebo. Thigh circumference, ultrasound evaluations, and standardized photographs were collected at baseline, intermediate, and endpoint visits. Adverse events were monitored. After 84 days, the hypertonic cream group exhibited a significant reduction in thigh circumference compared to the placebo group ( = 0.0037). B-mode ultrasound examinations revealed significant changes in the parameters studied, such as the thickness of the subcutaneous tissue. No statistically significant changes were noticed in the placebo group. Volunteers reported the investigational product's pleasantness and good anti-cellulite activity, with no reported adverse events. The hypertonic cream demonstrated efficacy in reducing thigh circumference, addressing water retention and structural alterations in adipose tissue. The proposed mechanism involves osmosis, releasing accumulated fluids between fat cells, supporting drainage, and reducing inflammation. This study supports the efficacy and safety of hypertonic sodium chloride emulsions in cellulite treatment and confirms safety and user satisfaction.
Topics: Humans; Female; Double-Blind Method; Prospective Studies; Cellulite; Adult; Middle Aged; Ultrasonography; Thigh; Treatment Outcome; Skin Cream; Administration, Topical
PubMed: 38792964
DOI: 10.3390/medicina60050781 -
International Journal of Molecular... May 2024Post-fermentation wastes are rich sources of various biologically active compounds with antimicrobial activity, whose potential is not being fully exploited. One of the...
Post-fermentation wastes are rich sources of various biologically active compounds with antimicrobial activity, whose potential is not being fully exploited. One of the possible applications of post-fermentation waste may be its use as a natural preservative that effectively combats pathogens found in formulations. The study aims included the following: (1) compare the antimicrobial and antioxidant activity of fermented vegetable extracts (FVEs), (2) examine the inhibition of cosmetic-borne pathogens by FVEs, and (3) estimate the preservative effectiveness of FVEs in o/w emulsions. It was found that fermented white cabbage, cucumber, celery, and the mixture of fermented white cabbage, cucumber, and celery (1:1:1) showed antibacterial and antifungal activity against all the tested reference microbial strains. The addition of fermented cucumber, celery, and the mixture of fermented white cabbage, cucumber, and celery (1:1:1) to the o/w emulsion fulfilled criterion A of the preservative effectiveness test for , , and , but did not fulfill the criterion for and . The tested FVEs have comparable activity to inhibit pathogens in o/w emulsion as sodium benzoate. The results of our study prove that FVEs can be valuable raw materials supporting the preservative system, which, in turn, can significantly reduce the concentration of preservatives used in o/w emulsion.
Topics: Fermentation; Vegetables; Emulsions; Food Preservatives; Antioxidants; Anti-Infective Agents; Plant Extracts; Microbial Sensitivity Tests; Staphylococcus aureus
PubMed: 38791548
DOI: 10.3390/ijms25105510 -
Biosensors Apr 2024Antimicrobial resistance (AMR) has become a crucial global health issue. Antibiotic-resistant bacteria can survive after antibiotic treatments, lowering drug efficacy...
Antimicrobial resistance (AMR) has become a crucial global health issue. Antibiotic-resistant bacteria can survive after antibiotic treatments, lowering drug efficacy and increasing lethal risks. A microfluidic water-in-oil emulsion droplet system can entrap microorganisms and antibiotics within the tiny bioreactor, separate from the surroundings, enabling independent assays that can be performed in a high-throughput manner. This study presents the development of a label-free dielectrophoresis (DEP)-based microfluidic platform to sort droplets that co-encapsulate () and ampicillin (Amp) and droplets that co-encapsulate Amp-resistant (AmpR) with Amp only based on the conductivity-dependent DEP force () without the assistance of optical analyses. The 9.4% low conductivity (LC) Luria-Bertani (LB) broth diluted with 170 mM mannitol can maintain and AmpR growth for 3 h and allow Amp to kill almost all , which can significantly increase the LCLB conductivity by about 100 μS/cm. Therefore, the AmpR /9.4%LCLB/Amp where no cells are killed and the /9.4%LCLB/Amp-containing droplets where most of the cells are killed can be sorted based on this conductivity difference at an applied electric field of 2 MHz and 100 V that generates positive . Moreover, the sorting ratio significantly decreased to about 50% when the population of AmpR was equal to or higher than 50% in droplets. The conductivity-dependent DEP-based sorting platform exhibits promising potential to probe the ratio of AmpR in an unknown bacterial sample by using the sorting ratio as an index.
Topics: Escherichia coli; Electrophoresis; Drug Resistance, Bacterial; Ampicillin; Anti-Bacterial Agents; Electric Conductivity; Microfluidic Analytical Techniques; Microbial Sensitivity Tests
PubMed: 38785691
DOI: 10.3390/bios14050218 -
International Journal of Nanomedicine 2024Therapeutic proteins and peptides offer great advantages compared to traditional synthetic molecular drugs. However, stable protein loading and precise control of...
BACKGROUND
Therapeutic proteins and peptides offer great advantages compared to traditional synthetic molecular drugs. However, stable protein loading and precise control of protein release pose significant challenges due to the extensive range of physicochemical properties inherent to proteins. The development of a comprehensive protein delivery strategy becomes imperative accounting for the diverse nature of therapeutic proteins.
METHODS
Biodynamers are amphiphilic proteoid dynamic polymers consisting of amino acid derivatives connected through pH-responsive dynamic covalent chemistry. Taking advantage of the amphiphilic nature of the biodynamers, PNCs and DEs were possible to be prepared and investigated to compare the delivery efficiency in drug loading, stability, and cell uptake.
RESULTS
As a result, the optimized PNCs showed 3-fold encapsulation (<90%) and 5-fold loading capacity (30%) compared to DE-NPs. PNCs enhanced the delivery efficiency into the cells but aggregated easily on the cell membrane due to the limited stability. Although DE-NPs were limited in loading capacity compared to PNCs, they exhibit superior adaptability in stability and capacity for delivering a wider range of proteins compared to PNCs.
CONCLUSION
Our study highlights the potential of formulating both PNCs and DE-NPs using the same biodynamers, providing a comparative view on protein delivery efficacy using formulation methods.
Topics: Peptides; Emulsions; Humans; Proteins; Drug Delivery Systems; Polymers; Nanoparticles; Hydrogen-Ion Concentration; Amino Acids; Drug Carriers; Drug Liberation; Cell Survival
PubMed: 38784761
DOI: 10.2147/IJN.S448578 -
Anais Da Academia Brasileira de Ciencias 2024The present study investigated mushroom by-products as a substitute for emulsifiers in the microencapsulation of apricot kernel oil. Mushroom by-product emulsions were...
The present study investigated mushroom by-products as a substitute for emulsifiers in the microencapsulation of apricot kernel oil. Mushroom by-product emulsions were more viscous and had higher centrifugal (85.88±1.19 %) and kinetic (90.52±0.98 %) stability than control emulsions (Tween 20 was used as emulsifier). Additionally, spray-drying mushroom by-product emulsions yielded a high product yield (62.56±1.11 %). Furthermore, the oxidative stability of powder products containing mushroom by-products was observed to be higher than that of the control samples. For an accelerated oxidation test, the samples were kept at various temperatures (20, 37, and 60 °C). TOTOX values were assessed as indicators of oxidation, with values exceeding 30 indicating oxidation of the samples. Of the samples stored at 60 °C, the non-microencapsulated apricot kernel oil oxidized by the fifth day (41.12±0.13 TOTOX value), whereas the powder samples containing the mushroom by-products remained unoxidized until the end of the tenth day (37.05±0.08 TOTOX value). This study revealed that mushroom by-products could be a viable alternative for synthetic emulsifiers in the microencapsulation of apricot kernel oil. It has been observed that using mushroom by-products instead of synthetic emulsifiers in oil microencapsulation can also delay oxidative degradation in microencapsulated powders.
Topics: Emulsions; Emulsifying Agents; Plant Oils; Prunus armeniaca; Drug Compounding; Agaricales; Oxidation-Reduction; Water
PubMed: 38775552
DOI: 10.1590/0001-3765202420220448 -
Brazilian Journal of Biology = Revista... 2024Munguba butter has bioactive compounds such as vitamin E and phytosterols, which has valued its application in the development of new products, with advantages in its...
Munguba butter has bioactive compounds such as vitamin E and phytosterols, which has valued its application in the development of new products, with advantages in its use in emulsified formulations. Therefore, the objective was to develop and evaluate the stability of a nanoemulsion containing munguba butter as the oily phase. Munguba butter was extracted by the ultrasound assisted method and its HLB (hydrophilic-lipophilic balance) was determined. Next, formulations varying the concentration of butter from 1-40% were developed and classified into liquid or solid emulsion and phase separation. Liquid emulsions were evaluated for hydrodynamic particle diameter, polydispersity index (PDI), Zeta potential (ζ), rheological characterization, and stability assays. The butter had an HLB of 6.98. The NE 1.0% formulation was selected and demonstrated to be unstable at high temperatures (45 ± 2 °C) and remained stable at room temperature, refrigeration and light radiation for 90 days. Munguba butter, because it has high amounts of saturated fatty acids, hinders its application in the development of new products. However, the success in the development of the NE 1.0% formulation is noteworthy, remaining stable when exposed to refrigeration, room temperature and light radiation.
Topics: Emulsions; Vigna; Butter; Particle Size; Drug Stability; Rheology
PubMed: 38775525
DOI: 10.1590/1519-6984.281236 -
International Journal of Nanomedicine 2024Cannabidiol (CBD) is a promising therapeutic drug with low addictive potential and a favorable safety profile. However, CBD did face certain challenges, including poor...
PURPOSE
Cannabidiol (CBD) is a promising therapeutic drug with low addictive potential and a favorable safety profile. However, CBD did face certain challenges, including poor solubility in water and low oral bioavailability. To harness the potential of CBD by combining it with a transdermal drug delivery system (TDDS). This innovative approach sought to develop a transdermal patch dosage form with micellar vesicular nanocarriers to enhance the bioavailability of CBD, leading to improved therapeutic outcomes.
METHODS
A skin-penetrating micellar vesicular nanocarriers, prepared using nano emulsion method, cannabidiol loaded transdermal nanocarriers-12 (CTD-12) was presented with a small particle size, high encapsulation efficiency, and a drug-loaded ratio for CBD. The skin permeation ability used Strat-M™ membrane with a transdermal diffusion system to evaluate the CTD and patch of CTD-12 (PCTD-12) within 24 hrs. PCTD-12 was used in a preliminary pharmacokinetic study in rats to demonstrate the potential of the developed transdermal nanocarrier drug patch for future applications.
RESULTS
In the transdermal application of CTD-12, the relative bioavailability of the formulation was 3.68 ± 0.17-fold greater than in the free CBD application. Moreover, PCTD-12 indicated 2.46 ± 0.18-fold higher relative bioavailability comparing with free CBD patch in the ex vivo evaluation. Most importantly, in the pharmacokinetics of PCTD-12, the relative bioavailability of PCTD-12 was 9.47 ± 0.88-fold higher than in the oral application.
CONCLUSION
CTD-12, a transdermal nanocarrier, represents a promising approach for CBD delivery, suggesting its potential as an effective transdermal dosage form.
Topics: Cannabidiol; Animals; Skin Absorption; Transdermal Patch; Biological Availability; Drug Carriers; Administration, Cutaneous; Male; Nanoparticles; Rats; Rats, Sprague-Dawley; Particle Size; Skin; Micelles
PubMed: 38770103
DOI: 10.2147/IJN.S455032 -
Food Research International (Ottawa,... Jul 2024The antioxidant activity of the natural phenolic extracts is limited in particular food systems due to the existence of phenolic compounds in glycoside form. Acid...
The antioxidant activity of the natural phenolic extracts is limited in particular food systems due to the existence of phenolic compounds in glycoside form. Acid hydrolysis post-treatment could be a tool to convert the glycosidic polyphenols in the extracts to aglycones. Therefore, this research investigated the effects of an acid hydrolysis post-treatment on the composition and antioxidant activity of parsley extracts obtained by an ultrasound-assisted extraction method to delay lipid oxidation in a real food system (i.e., soybean oil-in-water emulsion). Acid hydrolysis conditions were varied to maximize total phenolic content (TPC) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity. When extracts were exposed to 0.6 M HCl for 2 h at 80 ℃, TPC was 716.92 ± 24.43 µmol gallic acid equivalent (GAE)/L, and DPPH radical scavenging activity was 66.89 ± 1.63 %. Not only did acid hydrolysis increase the concentrations of individual polyphenols, but it also resulted in the release of new phenolics such as myricetin and gallic acid. The extract's metal chelating and ferric-reducing activity increased significantly after acid hydrolysis. In soybean oil-in-water emulsion containing a TPC of 400 µmol GAE/L, the acid-hydrolyzed extract had an 11-day lag phase for headspace hexanal compared to the 6-day lag phase of unhydrolyzed extract. The findings indicated that the conversion of glycosidic polyphenols to aglycones in phenolic extracts can help extend the shelf-life of emulsion-based foods.
Topics: Emulsions; Plant Extracts; Soybean Oil; Phenols; Hydrolysis; Antioxidants; Petroselinum; Plant Leaves; Oxidation-Reduction; Water; Lipid Peroxidation; Biphenyl Compounds; Picrates; Polyphenols
PubMed: 38763687
DOI: 10.1016/j.foodres.2024.114452