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Gels (Basel, Switzerland) Apr 2024Biopolymeric nanoparticles (NPs) have gained significant attention in several areas as an alternative to synthetic polymeric NPs due to growing environmental and...
Biopolymeric nanoparticles (NPs) have gained significant attention in several areas as an alternative to synthetic polymeric NPs due to growing environmental and immunological concerns. Among the most promising biopolymers is poly(lactic acid) (PLA), with a reported high degree of biocompatibility and biodegradability. In this work, PLA NPs were synthesized according to a controlled gelation process using a combination of single-emulsion and nanoprecipitation methods. This study evaluated the influence of several experimental parameters for accurate control of the PLA NPs' size distribution and aggregation. Tip sonication (as the stirring method), a PLA concentration of 10 mg/mL, a PVA concentration of 2.5 mg/mL, and low-molecular-weight PLA (Mw = 5000) were established as the best experimental conditions to obtain monodisperse PLA NPs. After gelification process optimization, flutamide (FLU) was used as a model drug to evaluate the encapsulation capability of the PLA NPs. The results showed an encapsulation efficiency of 44% for this cytostatic compound. Furthermore, preliminary cell viability tests showed that the FLU@PLA NPs allowed cell viabilities above 90% up to a concentration of 20 mg/L. The comprehensive findings showcase that the PLA NPs fabricated using this straightforward gelification method hold promise for encapsulating cytostatic compounds, offering a novel avenue for precise drug delivery in cancer therapy.
PubMed: 38667693
DOI: 10.3390/gels10040274 -
Journal of Functional Biomaterials Apr 2024The present study aimed to formulate and characterize a hesperetin formulation to achieve adequate deposition and retention of hesperetin in the epidermis as a target...
The present study aimed to formulate and characterize a hesperetin formulation to achieve adequate deposition and retention of hesperetin in the epidermis as a target for some cosmetic/dermatological actions. To derive the final emulgel, various formulations incorporating different proportions of Polysorbate 80 and hyaluronic acid underwent testing through a Box-Behnken experimental design. Nine formulations were created until the targeted emulgel properties were achieved. This systematic approach, following the principles of a design of experiment (DoE) methodology, adheres to a quality-by-design (QbD) paradigm, ensuring a robust and purposeful formulation and highlighting the commitment to a quality-driven design approach. The emulsions were developed using the phase inversion method, optimizing the emulgel with the incorporation of hyaluronic acid. Physically stable optimized emulgels were evaluated for their globule size, surface charge, viscosity, pH, electrical conductivity, and hesperetin content. These assays, along with the temperature swing test, were used to select the optimal formulation. It was characterized by a droplet size, d[4,3], of 4.02 μm, a Z-potential of -27.8 mV, an O/W sign, a pH of 5.2, and a creamy texture and proved to be stable for at least 2 months at room temperature. Additionally, in vitro release kinetics from the selected emulgel exhibited a sustained release profile of hesperetin. Skin assays revealed adequate retention of hesperetin in the human epidermis with minimum permeation. Altogether, these results corroborate the promising future of the proposed emulgel in cosmetic or dermatological use on healthy or diseased skin.
PubMed: 38667546
DOI: 10.3390/jfb15040089 -
Antibiotics (Basel, Switzerland) Apr 2024Biofilm-associated infections caused by drug-resistant and persistent bacteria remain a significant clinical challenge. Here we report that farnesol, commercially...
Biofilm-associated infections caused by drug-resistant and persistent bacteria remain a significant clinical challenge. Here we report that farnesol, commercially available as a cosmetic and flavoring agent, shows significant anti-biofilm properties when dissolved in ethanol using a proprietary formulation emulsion technique. Farnesol in the new formulation inhibits biofilm formation and disrupts established biofilms for Gram-positive and Gram-negative , including their polymicrobial biofilms, and, moreover, kills persister cells that have developed tolerance to antibiotics. No resistance to farnesol was observed for after twenty continuous passages. Farnesol combats biofilms by direct killing, while also facilitating biofilm detachment. Furthermore, farnesol was safe and effective for preventing and treating biofilm-associated infections of both types of bacteria in an ex vivo burned human skin model. These data suggest that farnesol in the new formulation is an effective broad-spectrum anti-biofilm agent with promising clinical potential. Due to its established safety, low-cost, versatility, and excellent efficacy-including ability to reduce persistent and resistant microbial populations-farnesol in the proprietary formulation represents a compelling transformative, translational, and commercial platform for addressing many unsolved clinical challenges.
PubMed: 38667026
DOI: 10.3390/antibiotics13040350 -
RSC Advances Apr 2024Polymer nanoparticles (PNPs) have significantly advanced the field of biomedicine, showcasing the remarkable potential for precise drug delivery, administration of...
Polymer nanoparticles (PNPs) have significantly advanced the field of biomedicine, showcasing the remarkable potential for precise drug delivery, administration of nutraceuticals, diagnostics/imaging applications, and the fabrication of biocompatible materials, among other uses. Despite these promising developments, the invention faces notable challenges related to biodegradability, bioactivity, target-site specificity, particle size, carrier efficiency, and controlled release. Addressing these concerns is essential for optimizing the functionality and impact of PNPs in biomedical applications. Here, new poly cysteine methacrylate nanoparticles (PCMANPs), (200 nm) in size have been synthesized from the cysteine methacrylate (CysMA) monomer using different strategies, including emulsion and inverse emulsion polymerization techniques. The monomer was synthesized using the Michael addition reaction, involving the addition of 3-(acryloyloxy)-2-hydroxypropyl methacrylate to the sulfhydryl group (-SH) of the cysteine (Cys) active site, with the aid of dimethyl phenyl phosphine (DMPP) as a nucleophilic agent as previously reported. To enhance nano-polymerization, a thorough exploration of various initiators, including ammonium persulfate (APS) and 4,4'-azobis (4-cyanovaleric acid) (ACVA), alongside surfactants, such as polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), and sodium dodecyl sulfate (SDS), was conducted. Additionally, critical parameters, such as reaction time, temperature, and solvents, were systematically investigated due to their substantial influence on the shape, size, stability, and morphology of the synthesized polymer nanoparticles. This comprehensive approach aims to optimize the synthesis process, ensuring precise control over the key characteristics of the resulting nanoparticles for enhanced performance in diverse applications. Various characterization techniques, including field emission scanning electron microscopy (FESEM), transmission electron microscopy (TEM), nuclear magnetic resonance (NMR), Raman spectroscopy, Fourier-transform infrared spectroscopy (FTIR), zeta potential, and zeta sizer dynamic light scattering (DLS) analysis, were utilized to investigate purity, morphology, and particle size of the PNPs. As a result, a spherical, monodispersed (homogenized), and stable PCMANP with defined size and morphology was achieved. This may exhibit a remarkable achievement in the future of drug delivery systems and therapeutic index.
PubMed: 38665499
DOI: 10.1039/d4ra00067f -
Biomedicine & Pharmacotherapy =... Jun 2024To elucidate the therapeutic effects and mechanisms of Atractylodes macrocephala extract crystallize (BZEP) and BZEP self-microemulsion (BZEPWR) on metabolic...
The effects of Atractylodes macrocephala extract BZEP self-microemulsion based on gut-liver axis HDL/LPS signaling pathway to ameliorate metabolic dysfunction-associated fatty liver disease in rats.
OBJECTIVES
To elucidate the therapeutic effects and mechanisms of Atractylodes macrocephala extract crystallize (BZEP) and BZEP self-microemulsion (BZEPWR) on metabolic dysfunction-associated fatty liver disease (MAFLD) induced by "high sugar, high fat, and excessive alcohol consumption" based on the gut-liver axis HDL/LPS signaling pathway.
METHODS
In this study, BZEP and BZEPWR were obtained via isolation, purification, and microemulsification. Furthermore, an anthropomorphic MAFLD rat model of "high sugar, high fat, and excessive alcohol consumption" was established. The therapeutic effects of BZEPWR and BZEP on the model rats were evaluated in terms of liver function, lipid metabolism (especially HDL-C), serum antioxidant indexes, and liver and intestinal pathophysiology. To determine the lipoproteins in the serum sample, the amplitudes of a plurality of NMR spectra were derived via deconvolution of the composite methyl signal envelope to yield HDL-C subclass concentrations. The changes in intestinal flora were detected via 16 S rRNA gene sequencing. In addition, the gut-liver axis HDL/LPS signaling pathway was validated using immunohistochemistry, immunofluorescence, and western blot.
RESULTS
The findings established that BZEPWR and BZEP improved animal signs, serum levels of liver enzymes (ALT and AST), lipid metabolism (TC, TG, HDL-C, and LDL-C), and antioxidant indexes (GSH, SOD, and ROS). In addition, pathological damage to the liver, colon, and ileum was ameliorated, and the intestinal barrier function of the model rats was restored. At the genus level, BZEPWR and BZEP exerted positive effects on beneficial bacteria, such as Lactobacillus and norank_f__Muribaculaceae, and inhibitory effects on harmful bacteria, such as unclassified_f__Lachnospiraceae and Blautia. Twenty HDL-C subspecies were detected, and their levels were differentially increased in both BZEPWR and BZEP groups, with BZEPWR exhibiting a stronger elevating effect on specific HDL-C subspecies. Also, the gut-liver axis HDL/LPS signaling pathway was studied, which indicated that BZEPWR and BZEP significantly increased the expressions of ABCA1, LXR, occludin, and claudin-1 proteins in the gut and serum levels of HDL-C. Concomitantly, the levels of LPS in the serum and TLR4, Myd88, and NF-κB proteins in the liver were decreased.
CONCLUSION
BZEPWR and BZEP exert restorative and reversal effects on the pathophysiological damage to the gut-liver axis in MAFLD rats, and the therapeutic mechanism may be related to the regulation of the intestinal flora and the HDL/LPS signaling pathway.
Topics: Animals; Signal Transduction; Male; Emulsions; Rats; Liver; Atractylodes; Plant Extracts; Lipopolysaccharides; Gastrointestinal Microbiome; Rats, Sprague-Dawley; Lipoproteins, HDL; Disease Models, Animal; Lipid Metabolism; Fatty Liver; Non-alcoholic Fatty Liver Disease; Antioxidants
PubMed: 38663104
DOI: 10.1016/j.biopha.2024.116519 -
Saudi Pharmaceutical Journal : SPJ :... Jun 2024Isotretinoin (ITN) is a poorly water-soluble drug. The objective of this study was to design a successful liquid self-nanoemulsifying drug delivery system (L-SNEDDS) for...
PURPOSE
Isotretinoin (ITN) is a poorly water-soluble drug. The objective of this study was to design a successful liquid self-nanoemulsifying drug delivery system (L-SNEDDS) for ITN to improve its solubility, dissolution rate, and antibacterial activity.
METHODS
According to solubility and emulsification studies, castor oil, Cremophor EL, and Transcutol HP were selected as system excipients. A pseudo ternary phase diagram was constructed to reveal the self-emulsification area. The developed SNEDDS were visually assessed, and the droplet size was measured. In vitro release studies and stability studies were conducted. The antimicrobial effectiveness against multiple bacterial strains, including Staphylococcus aureus, methicillin-resistant Staphylococcus aureus (MRSA), and different accessory gene regulator (Agr) variants were investigated for the optimum ITN-loaded SNEDDS formulation.
RESULTS
Characterization studies showed emulsion homogeneity and stability (%T 95.40-99.20, A graded) with low droplet sizes (31.87 ± 1.23 nm-115.47 ± 0.36 nm). It was found that the developed ITN-SNEDDS provided significantly a higher release rate (>96 % in 1 h) as compared to the raw drug (<10 % in 1 h). The in vitro antimicrobial activities of pure ITN and ITN-loaded SNEDDS demonstrated a remarkable inhibitory effect on bacterial growth with statistically significant findings (p < 0.0001) for all tested strains when treated with ITN-SNEDDS as compared to the raw drug.
CONCLUSION
These outcomes suggested that SNEDDS could be a potential approach for improving solubility, dissolution rates, and antibacterial activity of ITN.
PubMed: 38650911
DOI: 10.1016/j.jsps.2024.102063 -
Heliyon Apr 2024Thyme oil (TO) is a valuable essential oil believed to possess a variety of bioactivities, including antibacterial, anticancer, and antioxidant properties. These...
Thyme oil (TO) is a valuable essential oil believed to possess a variety of bioactivities, including antibacterial, anticancer, and antioxidant properties. These attributes grant TO the excellent capability to treat a wide range of diseases, particularly the effective eradication of infection in the stomach. However, its practical use is limited by its low stability under atmospheric conditions. Our current research aims to encapsulate TO in eudragit (EGT) microsponges to enhance its stability and improve its effectiveness against . The TO microsponges were prepared using EGT as a polymer, polysorbate 80 as a stabilizer, and dichloromethane (DCM) as a solvent via the quasi-emulsion solvent evaporation method. The product yield, particle size, surface morphology, entrapment efficiency, drug-polymer interaction, in-vitro floating, and in-vitro drug release of the microsponges were evaluated. The most promising microsponge was tested against ATCC 43504 strains. The results showed that the microsponges exhibited a high product yield (ranging from 41 % ± 0.75-81.27 % ± 1.13), excellent entrapment efficiency (ranging from 63.01 % ± 0.79-88.64 % ± 0.98), prolonged in-vitro floating time (more than 12 h) and sustained in-vitro drug release for 18 h (81.53 %). Scanning electron microscopy results indicated that the microsponges were spherical in shape with a spongy surface. The average particle size of the selected microsponges was determined to be 49.79 ± 1.4 μm, and their average pore size was measured to be 0.81 ± 0.14 μm. DSC study results revealed that TO was physically entrapped in the microsponges. In-vitro - activity studies demonstrated that TO in microsponge was more effective against than pure TO. In conclusion, the developed microsponges containing thyme oil provide a promising alternative for the efficient targeting and eradication of infection.
PubMed: 38638985
DOI: 10.1016/j.heliyon.2024.e29246 -
Journal of Ophthalmic & Vision Research 2024Recent studies have reported the promising effect of intravitreal propranolol on retinal neovascularization. However, rapid clearance and short half-life of the drug in...
PURPOSE
Recent studies have reported the promising effect of intravitreal propranolol on retinal neovascularization. However, rapid clearance and short half-life of the drug in the vitreous are the main drawbacks of this therapeutic approach. This study investigates the extension of the residence time of propranolol in the vitreous by polymeric nanoparticles (NPs) with the prospect of improving choroidal neovascularization treatment.
METHODS
The poly (lactic-co-glycolic) acid (PLGA) NPs were fabricated by a modified double emulsion solvent evaporation method and the obtained NPs were characterized for their size, poly dispersity index (PDI), and surface image. The release, cell cytotoxicity, and uptake of NPs were also evaluated. To investigate the effect of the vitreous pharmacokinetic drug loaded NPs versus that of the free propranolol, they were intravitreally injected into the rabbits' eyes and the drug vitreous concentrations in defined intervals were analyzed by high performance liquid chromatography (HPLC).
RESULTS
The spherical NPs with about 230 nm size, and almost 10% drug loading were obtained. Based on the 3-(4, 5-Dimethylthiazol-2-Yl)-2, 5-Diphenyltetrazolium Bromide (MTT) outcomes, 30 µg/ml of propranolol was considered as the guide dosage in the intravitreal injection. Confocal microscopy images verified the presence of labeled NPs in the posterior segment after five days of receiving the injection. assay revealed that the vanishing rate of propranolol in rabbits treated with propranolol NPs was reduced at twice the rate as compared to that of the vanishing rate experienced with only the free drug.
CONCLUSION
PLGA NPs can prolong the existence of propranolol in both vitreous and posterior ocular tissues, and thus, may provide an effective approach in treatment of posterior segment neovascularization.
PubMed: 38638633
DOI: 10.18502/jovr.v19i1.15436 -
Open Veterinary Journal Jan 2024and are implicated in foodborne diseases that have major effects on human health; therefore, it is considered universal public health disorders. Essential oils and...
BACKGROUND
and are implicated in foodborne diseases that have major effects on human health; therefore, it is considered universal public health disorders. Essential oils and essential oils nano emulsions have a sufficient antibacterial performance against a variety of bacteria, especially multi-drug resistant bacteria. Probiotics showed several health benefits via moderating the GIT microbiota and their metabolites.
AIM
The study was designed to evaluate the biocontrol ability of cinnamon essential oil (CEO) nano emulsion and probiotics as natural antibacterial additives and reveal their bactericidal mechanism.
METHODS
250 random samples (50 raw milk, 50 rice pudding, 50 kariesh cheese, 50 yogurt, and 50 ice cream) were purchased separately from different areas in Mansoura city, Egypt, and exposed to bacteriological analysis.
RESULTS
was found with the highest mean value of 66 × 10 ± 1.3 × 10 CFU/g in raw milk and the lowest mean value of 28 × 10 ± 2.6 × 10 CFU/g in kariesh cheese while was found in 64% of the total inspected samples with the highest incidence (84%) in yogurt. The toxinogenic potential of the tested pathogens has been evaluated by multiplex PCR pointing and genes for isolates while targeting in , and gene. Different concentrations (0.17%, 0.25%, 0.5%, 0.8%, 1%, 1.5%, and 2%) of cinnamon oil nano emulsion were employed in this study. CEO nano emulsion had the highest reduction rate at a concentration of 1.5% in the case of and 2% in the case of . Among different types of probiotics, the best one which showed inhibitory potential against and was
CONCLUSION
and CEO nano emulsion at a concentration of 2% have the highest reduction rate against , while and CEO nano emulsion at a concentration of 1.5% has the best antibacterial effect against . In conclusion, more attention is required for both safety and quality in dairy products through the application of natural additives such as essential oils and probiotics.
Topics: Animals; Humans; Milk; Oils, Volatile; Food Microbiology; RNA, Ribosomal, 16S; Probiotics; Bacillus cereus; Anti-Bacterial Agents
PubMed: 38633175
DOI: 10.5455/OVJ.2024.v14.i1.43 -
Scientific Reports Apr 2024Self-nanoemulsifying drug delivery systems (SNEDDS) have been used to improve the oral bioavailability of various drugs. In the current study, apigenin was developed as...
Self-nanoemulsifying drug delivery systems (SNEDDS) have been used to improve the oral bioavailability of various drugs. In the current study, apigenin was developed as SNEDDS to solve its dissolution problem and enhance oral bioavailability and antioxidant potential. SNEDDS were prepared by mixing Gelucire 44/14, Tween 80, and PEG 400 under controlled conditions. The droplet of diluted SNEDDS demonstrated a spherical shape with a size of less than 100 nm and a neutral charge. The very fast self-emulsification was obtained within 32 s, and the transmittance values exceeded 99%. The highest drug loading was 90.10 ± 0.24% of the initial load with the highest %encapsulation efficiency of 84.20 ± 0.03%. FT-IR and DSC spectra showed no interaction between components. The dissolution in buffer pH 1.2, 4.5, and 6.8 showed significantly higher dissolved apigenin than the apigenin coarse powder. The dissolution profiles were fitted to the Korsmeyer-Peppas kinetics. The cellular antioxidant activities in Caco-2 cells were approximately 52.25-54.64% compared to no treatment and were higher than the apigenin coarse powder (12.70%). Our work highlights the potential of SNEDDS to enhance the dissolution and permeability of apigenin and promote antioxidant efficacy, which has a strong chance of being developed as a bioactive compound for nutraceuticals.
Topics: Humans; Antioxidants; Apigenin; Caco-2 Cells; Powders; Spectroscopy, Fourier Transform Infrared; Solubility; Emulsions; Drug Delivery Systems; Administration, Oral; Nanoparticles; Particle Size; Biological Availability; Drug Liberation
PubMed: 38632321
DOI: 10.1038/s41598-024-59617-z