Mean Hydrodynamic Diameter Research Articles

Development of a dry powder formulation for pulmonary delivery of azithromycin-loaded nanoparticles.

The COVID-19 pandemic has raised concern regarding respiratory system diseases and oral inhalation stands out as an attractive non-invasive route of administration for pulmonary diseases such as chronic bronchitis, cystic fibrosis, COVID-19 and community-acquired pneumonia. In this context, we encapsulated azithromycin in polycaprolactone nanoparticles functionalized with phospholipids rich in dipalmitoylphosphatidylcholine and further produced a fine powder formulation by spray drying with monohydrated lactose. Nanoparticles obtained by the emulsion/solvent diffusion-evaporation technique exhibited a mean hydrodynamic diameter around 195-228nm with a narrow monomodal size distribution (PdI < 0.2). Nanoparticle dispersions were spray-dried at different inlet temperatures, atomizing air-flow, aspirator air flow, and feed rate, using lactose as a drying aid, resulting in a maximal process yield of 63% and an encapsulation efficiency of 83%. Excipients and the dry powder formulations were characterized in terms of morphology, chemical structure, thermal analyses and particle size by SEM, FTIR, DSC/TGA and laser light diffraction. The results indicated spherical particles with 90% at 4.06µm or below, an adequate size for pulmonary delivery. Aerosolization performance in a NGI confirmed good aerodynamic properties. Microbiological assays showed that the formulation preserves AZM antimicrobial effect against Staphylococcus aureus and Streptococcus pneumoniae strains, with halos above 18mm. In addition, no formulation-related cytotoxicity was observed against the human cell lines BEAS-2B (lung epithelial), HUVEC (endothelial) and HFF1 (fibroblasts). Overall, the approach described here allows the production of AZM-PCL nanoparticles incorporated into inhalable microparticles, enabling more efficient pulmonary therapy of lung infections.

A Newly Validated HPLC-DAD Method for the Determination of Ricinoleic Acid (RA) in PLGA Nanocapsules.

The assessment of ricinoleic acid (RA) incorporated into polymeric nanoparticles is a challenge that has not yet been explored. This bioactive compound, the main component of castor oil, has attracted attention in the pharmaceutical field for its valuable anti-inflammatory, antifungal, and antimicrobial properties. This work aims to develop a new and simple analytical method using high-performance liquid chromatography with diode-array detection (HPLC-DAD) for the identification and quantification of ricinoleic acid, with potential applicability in several other complex systems. The method was validated through analytical parameters, such as linearity, limit of detection and quantification, accuracy, precision, selectivity, and robustness. The physicochemical properties of the nanocapsules were characterized by dynamic light scattering (DLS) to determine their hydrodynamic mean diameter, polydispersity index (PDI), and zeta potential (ZP), via transmission electron microscopy (TEM) and quantifying the encapsulation efficiency. The proposed analytical method utilized a mobile phase consisting of a 65:35 ratio of acetonitrile to water, acidified with 1.5% phosphoric acid. It successfully depicted a symmetric peak of ricinoleic acid (retention time of 7.5 min) for both the standard and the RA present in the polymeric nanoparticles, enabling the quantification of the drug loaded into the nanocapsules. The nanocapsules containing ricinoleic acid (RA) exhibited an approximate size ranging from 309 nm to 441 nm, a PDI lower than 0.2, ζ values of approximately -30 mV, and high encapsulation efficiency (~99%). Overall, the developed HPLC-DAD procedure provides adequate confidence for the identification and quantification of ricinoleic acid in PLGA nanocapsules and other complex matrices.

Advancing environmental remediation through tailored TiO2 nanomaterials in water and air purification

This study investigates the green synthesis of TiO2 nanoparticles at varying concentrations (0 %, 0.1 %, 2.5 %, 5 %, and 10 %) using Viola betonicifolia plant extract, focusing on their application in environmental purification, specifically in water and air decontamination. X-ray diffraction (XRD) analysis confirmed the anatase crystal structure of TiO2 nanoparticles, with an average crystallite size of approximately 22 nm. Transmission electron microscopy (TEM) revealed a median diameter of around 22 nm, corroborating the findings from XRD. The effectiveness of these TiO2 nanomaterials was evaluated through bench-scale models simulating real-world conditions, targeting a broad range of pollutants, including heavy metals, organic dyes, volatile organic compounds (VOCs), and microbial pathogens. Advanced analytical techniques such as High-performance liquid chromatography (HPLC), Inductively coupled plasma mass spectrometry (ICP-MS), and microbial plate count methods quantified the pollutant removal efficiency, demonstrating the significant potential of the synthesized TiO2 nanoparticles. Dynamic light scattering (DLS) analysis showed a mean hydrodynamic diameter of 22 nm and a polydispersity index (PDI) below 0.1, indicating a uniform size distribution. The FTIR spectrum revealed a broad absorption band at 3400 cm−1, corresponding to O–H stretching vibrations, indicative of hydroxyl groups crucial for the photocatalytic activity of TiO2. The UV–visible spectroscopy indicated a maximum absorption at 642 nm, associated with the п-п* transition. Photocatalytic degradation of methylene blue under UV irradiation achieved a degradation efficiency of 94 % after 120 min, underscoring the superior efficiency of the green synthesis method.

Sodium-Alginate-Doped Lignin Nanoparticles for PBAT Composite Films to Dually Enhance Tensile Strength and Elongation Performance with Functionality.

It is a formidable challenge in thermoplastic/lignin composites to simultaneously boost tensile strength and elongation performance due to the rigidity of lignin. To address this issue, sodium-alginate-doped lignin nanoparticles (SLNPs) were prepared by combining solvent exchange and a coprecipitation method and used as an eco-friendly filler for poly(butylene adipate-co-terephthalate) (PBAT). The results indicated that the 1% polyanionic sodium alginate solution contributed to the formation of SLNP in lignin/THF solution. SLNP with a mean hydrodynamic diameter of ~500 nm and a Zeta potential value of -19.2 mV was obtained, indicating more hydrophobic lignin nanoparticles and a smaller number of agglomerates in SLNP suspension. Only 0.5 wt% SLNP addition improved the yield strength, tensile strength, and elongation at break by 32.4%, 31.8%, and 35.1% of the PBAT/SLNP composite films, respectively. The reinforcing effect resulted from the rigid aromatic structure of SLNP, whereas the enhanced elongation was attributed to the nanostructural feature of SLNP, which may promote boundary cracking. Additionally, the PBAT/SLNP composite films displayed excellent ultraviolet (UV) resistance with a UV shielding percentage near 100% for UVB and more than 75% for UVA, respectively. The addition of SLNP hindered water vapor, enhancing the moisture barrier properties. Overall, this study provides an effective strategy to eliminate the decrement in elongation performance for PBAT/lignin composites and suggest they are good candidates to be extensively utilized.

Facile synthesis of pH/reduction dual-triggered crosslinked polyprodrug nanoparticles for tumor specific doxorubicin delivery

Polyprodrugs have attracted more interest in tumor chemotherapy owing to their better on-demand controlled drug release than the conventional polymer prodrugs. Here, pH/reduction dual-triggered crosslinked polyprodrug nanoparticles were designed by the facile polycondensation of hexachlorocyclotriphosphazene (HCCP) and cystamine (Cys) modified DOX (DOX-Cys), with a higher DOX content of 53.41 % and mean hydrodynamic diameter (Dh) of 178.9 nm and narrow distribution. The in vitro drug release and cytotoxicity results indicated that introducing hydrophilic and flexible acid/GSH dual-triggered cleavable spacer in the crosslinked polyprodrug nanoparticles not only endowed the GSH-responsiveness with disulfide bond, but also modulated the acid-triggered drug release with Schiff base bond, making them a promising potential for tumor specific DOX delivery with minimized toxic/side effects, desired tumor selectivity and higher anti-tumor efficacy.

One-Step Preparation of Magnetic Lipid Bubbles: Magnetothermal Effect Induces the Simultaneous Formation of Gas Nuclei and Self-Assembly of Phospholipids.

In recent years, enveloped micro-nanobubbles have garnered significant attention in research due to their commendable stability, biocompatibility, and other notable properties. Currently, the preparation methods of enveloped micro-nanobubbles have limitations such as complicated preparation process, large bubble size, wide distribution range, low yield, etc. There exists an urgent demand to devise a simple and efficient method for the preparation of enveloped micro-nanobubbles, ensuring both high concentration and a uniform particle size distribution. Magnetic lipid bubbles (MLBs) are a multifunctional type of enveloped micro-nanobubble combining magnetic nanoparticles with lipid-coated bubbles. In this study, MLBs are prepared simply and efficiently by a magneto internal heat bubble generation process based on the interfacial self-assembly of iron oxide nanoparticles induced by the thermogenic effect in an alternating magnetic field. The mean hydrodynamic diameter of the MLBs obtained was 384.9 ± 8.5 nm, with a polydispersity index (PDI) of 0.248 ± 0.021, a zeta potential of -30.5 ± 1.0 mV, and a concentration of (7.92 ± 0.46) × 109 bubbles/mL. Electron microscopy results show that the MLBs have a regular spherical stable core-shell structure. The superparamagnetic iron oxide nanoparticles (SPIONs) and phospholipid layers adsorbed around the spherical gas nuclei of the MLBs, leading the particles to demonstrate commendable superparamagnetic and magnetic properties. In addition, the effects of process parameters on the morphology of MLBs, including phospholipid concentration, phospholipid proportiona, current intensity, magnetothermal time, and SPION concentration, were investigated and discussed to achieve controlled preparation of MLBs. In vitro imaging results reveal that the higher the concentration of MLBs loaded with iron oxide nanoparticles, the better the in vitro ultrasound (US) imaging and magnetic resonance imaging (MRI) results. This study proves that the magneto internal heat bubble generation process is a simple and efficient technique for preparing MLBs with high concentration, regular structure, and commendable properties. These findings lay a robust foundation for the mass production and application of enveloped micro-nanobubbles, particularly in biomedical fields and other related domains.

Biotoxicity and repellency of Vitex negundo (L.) oil nanoemulsion towards Rhyzopertha dominica (F.) on stored rice

Rhyzopertha dominica F. (lesser grain borer) is an important primary pest of stored rice that causes substantial economic loss. This pest developed resistance to a wide range of hazardous chemical pesticides due to its great degree of adaptability. This study proposed to prepare Vitex negundo oil nanoemulsion (VNO NE) to improve its efficacy against this target pest. Vitex negundo oil (VNO) contains key compounds such as Aromandendrene, ?-caryophyllene, Squalene, 3-octen-5-yne,2,7-dimethyl-,(E)-,5-(1-isopropenyl-4,5-dimethylbicyclo[4.3.0]nonan-5-yl)-3-methyl-2-pentenol acetate, Farnesyl bromide, 4-terpineol and Elemol. VNO NEs were prepared using a high-speed homogenizer from which nanoemulsion having 5% VNO mixed at a 1:2 (w/w) ratio with tween80 was found to be optimum considering different characterization parameters. The mean zeta potential, polydispersity index and hydrodynamic diameter of the nanoemulsion were -3.4 mV, 0.263 and 166.62 nm respectively. For contact toxicity lethal dose 50 (LD50) value of VNO NE was 0.517 ?L cm-2 against R. dominica which was 46.03% less, compared to bulk VNO. LD50 value of VNO NE for fumigant toxicity against R. dominica was 245.38 ?L L-1 which was 32.05% less than that of crude oil. The highest repellency increased by 30.14% than VNO, when treated with VNO NE in R. dominica. Significant inhibition of glutathione transferase enzyme was also detected in insects treated with VNO NE than VNO and control. These results indicated that VNO NE is an effective novel pesticide that can be recommended for the management of R. dominica in stored rice.

Synthesis of bio-stabilized silver nanoparticles using Roccella montagnei, their anticandidal capacities & potential to inhibit the virulence factors in fluconazole-resistant Candida albicans.

Candida species is the causative agent in approximately 80% of invasive mycoses and drug-resistant Candida albicans is among the four strains of 'critical priority group' framed by WHO. Lichens are endowed with some rare phytochemicals and a plethora of therapeutics viz. antifungal capacities of Roccella montagnei. Biosynthesis of silver nanoparticles (AgNPs) using lichen could offer an eco-friendly, and cost-effective alternative against emerging 'microbial resistance.' Therefore, the objective was to biosynthesize silver nanoparticles (Rm-AgNPs) using a Hydro-alcoholic (1:1) extract of R. montagnei to develop a potent anticandidal agent against Fluconazole-resistant C. albicans NBC099. UV-Spectroscopy identified AgNPs specific-peak of Rm-AgNPs at 420-440nm and FTIR revealed the presence of amines, alcohol, aromatic compounds, and acids. SEM and TEM analysis indicated that Rm-AgNPs are spherical shaped with a size range of 10-50nm. Zetasizer analysis indicated that particles are highly stable and have a mean hydrodynamic diameter of 116nm with a zeta potential charge of - 41mV. XRD analysis suggested face centered cubic crystal lattice structure. Results indicated that Rm-AgNPs strongly inhibited the growth of NBC099 at a minimum inhibitory concentration (IC50) of ≤ 15µg. C. albicans culture treated with Rm-AgNPs at concentrations below IC50, down-regulates the production of different virulence factors in NBC099, viz. hyphal formation (> 85%), biofilms production (> 80%), phospholipase, esterase, proteinase activity. The apoptosis assay demonstrated the Rm-AgNPs induced apoptosis in NBC099 cells via oxidative stress. Interestingly, Rm-AgNPs showed negligible cytotoxicity (< 6%) in murine RAW 246.7 macrophage cells at a concentration above 15µg/mL. Therefore, Rm-AgNPs have been offered as an anti-candida alternative that can be utilized to improve the efficacy of already available medications.

Dual-responsive chondroitin sulfate self-assembling nanoparticles for combination therapy in metastatic cancer cells

In this study, we developed self-assembling nanoparticles (LCPs) able to trigger the release of Chlorambucil (Chl) and Doxorubicin (DOX) to MDA-MB-231 cells by exploiting the enzyme and redox signals. The DOX loaded LCPs was prepared by the self-assembly of two chondroitin sulphate (CS) derivatives, obtained by the covalent conjugation of Lipoic Acid (LA) and Chlorambucil (Chl) to the CS backbone. After the physic-chemical characterization of the conjugates by FT-IR, 1H NMR, and determination of the critical aggregation concentration, spherical nanoparticles with mean hydrodynamic diameter of 45 nm (P.D.I. 0.24) and Z-potential of - 44 mV were obtained by water addition/solvent evaporation method. In vitro experiments for the release of Chl and DOX were performed in healthy and cancer cells, using a cell culture media to maintain the physiological intracellular conditions (pH 7.4) (and concentration of esterase and GSH. The results allowed the selective release of the payloads to be detected: Chl release of 0 and 41% were obtained after 2 h incubation in normal and in cancer cells respectively, while values of 35 (in healthy cells) and 60% (in cancer cells) were recorded for DOX release after 96 h. Finally, viability studies proved the ability of the newly proposed nanosystem to enhance the cytotoxic activity of the two drugs against cancer cells.

Unlocking the potential of chitosan nanoparticle as a carrier for systemic acquired resistance (SAR)-inducing recombinant protein: A preliminary study

Dieback disease stemmed from a phytopathogenic bacteria named Erwinia mallotivora is disastrous to papaya plant. Disease management action plan occurred stagnantly across the continent, until the discovery of proteinaceous hairpin which may catalyse systemic-acquired resistance (SAR) as plants’ defence mechanism. However, hairpin utilization is seriously flawed by its instability and limited bioavailability in plant. In lieu of this matter, nanobiotechnology approach through the encapsulation of hairpin within chitosan nanoparticles may be a mediator towards enhancement of sustained delivery as well as synergistic effect during foliar application. In this preliminary work, hrpN, a hairpin functional as SAR elicitor from Erwinia mallotivora, was well-expressed and purified in Escherichia coli system at molecular weight and concentration; 30 kDa and 1 µg/µL, respectively. Optimization of ionic gelation simultaneously revealed that optimal chitosan (CS) to sodium tripolyphosphate (TPP) volume ratio was found to be 2.4:1 ratio, yielding nano-sized particles with mean hydrodynamic diameter 66.27 ± 1.77 nm, and homogenously distributed with polydispersity index 0.189 ± 0.027. Subsequently, encapsulation of purified hrpN within CNP was formulated at various hrpN concentration. Following that, encapsulation of 0.04 mg/mL hrpN within optimized CNP produced hrpN-encapsulated chitosan nanoparticles (CNP-hrpN) with small size (106.34 ± 2.053 nm), stable and well-dispersed (0.188 ± 0.011), as well as possessing excellent encapsulation efficiency (81.84 ± 3.43%). The outcome from current work portrayed the potential of chitosan nanoparticle to carry biomolecules with desired properties.

Liposome Encapsulation of the Palmitoyl-KTTKS Peptide: Structural and Functional Characterization.

In this study, the amphiphilic N-palmitoyl-KTTKS peptide was integrated in the bilayer of egg-derived phosphatidylcholine (PC) vesicles using two different preparation methods, namely thin-film evaporation (TLE) and reverse-phase evaporation (REV). Both the REV and TLE methods allowed for the formation of homogeneous liposome dispersions (PdI < 0.20) with mean hydrodynamic diameters of <100 nm and <200 nm, respectively, a net negative surface charge and a percentage of structured phospholipids higher than 90%. The inclusion of the amphiphilic N-palmitoyl-KTTKS peptide within phospholipid-based vesicles could improve peptide stability and skin delivery. Therefore, the obtained liposomes were evaluated via experiments assessing the synthesis of collagen and the ECM in 3T3-NIH fibroblasts. The obtained results showed that, when delivered with PC liposomes, pal-KTTKS stimulated collagen production more than free pentapeptide and 1 mM ascorbic acid, used as a positive control.

Chitosan film of thiolated TPGS-modified Au-Ag nanoparticles for combating multidrug-resistant bacteria

The widely used vitamin-E based amphiphilic material, tocopheryl polyethylene glycol succinate (TPGS) was further improvised to redox-sensitive thiolated TPGS (TPGS-SH), which has been achieved by attaching 4-aminothiophenol. Further, TPGS and TPGS-SH-coated bimetallic gold-silver nanoparticles (TPGS-Au-Ag-NP and TPGS-SH-Au-Ag-NP) were formulated to explore their antibacterial and wound healing abilities. The prepared NP were monodisperse with a mean hydrodynamic diameter of 69.5±3.23 nm, 59.65±3.23 nm, PDI of 0.3±0.05, 0.2±0.03 and a zeta potential of +29.2±2.71 mV and +35.28±1.53 mV, respectively. The TPGS and TPGS-SH modified Au-Ag-NP were tested for their antibacterial efficacy against methicillin-resistant Staphylococcus aureus (MRSA) and E. coli; minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) results showed that TPGS Au-Ag-NP, TPGS-SH-Au-Ag-NP displayed significantly stronger antibacterial activity than their coating material alone. The anti-efflux pump activity of the most potent antibacterial agent TPGS-SH-Au-Ag-NP was evaluated against MRSA. Toxicity assessment of TPGS-SH-Au-Ag-NP in human dermal fibroblasts showed 88% viability up to 125 µg/mL. The TPGS-SH-Au-Ag-NP, after incorporation in chitosan film (TPGS-SH-Au-Ag-NP-CS), exhibited sustained release and prolonged in vivo residence characteristics, which were evaluated by IVIS. Results also revealed that treatment with TPGS-SH-Au-Ag-NP showed a significant 87% wound healing rate after 12 days of application in the rat model. Hence, we concluded that TPGS-SH-Au-Ag-NP was safe and effective against test bacteria MRSA and capable of efficient wound healing when incorporated in chitosan film.

Polystyrene nanoplastics alter the ecotoxicological effects of diclofenac on freshwater microalgae Scenedesmus obliquus.

Due to the escalating risk of plastic pollution, nanoplastics have attracted considerable attention in the recent past. They can co-exist and interact with other contaminants like pharmaceuticals in the aquatic environment. Therefore, it is pertinent to understand how these pollutants interact with one another in the ecosystem. The current study examined the individual and combined effects of fluorescent polystyrene nanoplastics (FNPs) and diclofenac (DCF) on Scenedesmus obliquus using a full factorial design. The toxicity of S. obliquus significantly increased in a dose-dependent manner upon exposure to pristine forms of DCF and FNPs. The major cause of individual toxicity of DCF and FNPs in S. obliquus was oxidative stress. In the combined toxicity tests when FNPs (0.01, 0.1, and 1 mg L-1) and DCF (1 mg L-1) were mixed, a synergistic effect was noted compared to the respective pristine FNPs. However, when the DCF concentration in the mixture was decreased to 0.25 mg L-1, the combined toxicity with FNPs (0.01, 0.1, and 1 mg L-1) reduced indicating an antagonistic effect. The independent action model also showed an antagonistic effect for low-dose combinations of DCF and a synergistic effect for high-dose combinations. The estimation of oxidative stress parameters, antioxidant enzyme activity, and photosynthetic pigment content in the algae further validated the cytotoxicity data. The mean hydrodynamic diameter and surface charge analyses further indicated that the colloidal stability of the FNPs in the medium was affected when they were combined with DCF. The key reason for differences in the cytotoxicity of combinations could be observed variations in the aggregation of FNPs and differential adsorption patterns of DCF on the FNPs. These factors efficiently altered cell-particle interactions in the mixture demonstrating a hormesis effect. Thus, this current study highlighted the hazardous nature of the nanoplastics and their co-exposure risks with pharmaceuticals on microalgae in freshwater environments.

Imidazo-Pyrazole-Loaded Palmitic Acid and Polystyrene-Based Nanoparticles: Synthesis, Characterization and Antiproliferative Activity on Chemo-Resistant Human Neuroblastoma Cells.

Neuroblastoma (NB) is a childhood cancer, commonly treated with drugs, such as etoposide (ETO), whose efficacy is limited by the onset of resistance. Here, aiming at identifying new treatments for chemo-resistant NB, the effects of two synthesized imidazo-pyrazoles (IMPs) (4G and 4I) were investigated on ETO-sensitive (HTLA-230) and ETO-resistant (HTLA-ER) NB cells, detecting 4I as the more promising compound, that demonstrated IC50 values lower than those of ETO on HTLA ER. Therefore, to further improve the activity of 4I, we developed 4I-loaded palmitic acid (PA) and polystyrene-based (P5) cationic nanoparticles (P5PA-4I NPs) with high drug loading (21%) and encapsulation efficiency (97%), by a single oil-in-water emulsification technique. Biocompatible PA was adopted as an emulsion stabilizer, while synthesized P5 acted as an encapsulating agent, solubilizer and hydrophilic-lipophilic balance (HLB) improver. Optic microscopy and cytofluorimetric analyses were performed to investigate the micromorphology, size and complexity distributions of P5PA-4I NPs, which were also structurally characterized by chemometric-assisted Fourier transform infrared spectroscopy (FTIR). Potentiometric titrations allowed us to estimate the milliequivalents of PA and basic nitrogen atoms present in NPs. P5PA-4I NPs afforded dispersions in water with excellent buffer capacity, essential to escape lysosomal degradation and promote long residence time inside cells. They were chemically stable in an aqueous medium for at least 40 days, while in dynamic light scattering (DLS) analyses, P5PA-4I showed a mean hydrodynamic diameter of 541 nm, small polydispersity (0.194), and low positive zeta potentials (+8.39 mV), assuring low haemolytic toxicity. Biological experiments on NB cells, demonstrated that P5PA-4I NPs induced ROS-dependent cytotoxic effects significantly higher than those of pristine 4I, showing a major efficacy compared to ETO in reducing cell viability in HTLA-ER cells. Collectively, this 4I-based nano-formulation could represent a new promising macromolecular platform to develop a new delivery system able to increase the cytotoxicity of the anticancer drugs.

Investigating the Correlation Between Drug Physical Properties and Physical Characteristics and Drug Entrapment Efficiencies of Chitosan-TPP Nanoparticles

Chitosan nanoparticles (NPs) have been the subject of intensive research. This study aimed to determine how different drug characteristics such as molecular weights, drug solubility in the processing medium, and drug ionization/charge state affected chitosan NPs particularly their percentage entrapment efficiency (% EE) and mean hydrodynamic diameters (MHDs). Drugs with varying molecular weights but of similar aqueous solubilities were chosen and were dissolved in a 2% chitosan-acetic acid solution. Chitosan NPs were formed using by ionic gelation technique using sodium tripolyphosphate (TPP) at specific concentration and volume ratios of chitosan to TPP. NPs containing Enalapril and Paracetamol displayed better short-term stability in terms of MHDs. A direct relationship between MHDs of NPs and chitosan concentrations was found. In comparison, at both low and high admixed drug concentrations and at high chitosan concentration, larger NPs sizes were associated with the lower molecular weight drug (Paracetamol). However, the study did not demonstrate a direct relationship between NPs characteristics such as MHDs and drugs molecular weights. The ZP of Paracetamol-loaded NPs was lowest at high drug concentrations at all chitosan concentrations compared to other drugs-loaded NPs. When compared to drugs with high and low molecular weights, medium molecular weight Atenolol showed the highest % EE. This clearly indicated that there was no direct correlation between drug molecular weight and % EE, but rather other factors influenced on % EE. Nevertheless, an inverse linear relationship with high correlation coefficients was only found when % EE was plotted against each drug molecular weight divided by the ratio of drugs solubilities in acetic acid to their employed concentrations, however the correlation was inconsistent between drugs of varying molecular weights.

Synthesis and self-assembly of H-shaped amphiphilic block copolymer based on polyoxyethylene, polyoxybutylene, and poly(ε-caprolactone) units

In this research, a new amphiphilic copolymer with an H-shaped macromolecular structure consisting of three hydrophobic blocks and two hydrophilic blocks were synthesized by a combination of ring-opening polymerization and click chemistry. The central chain and two of the side arms of the H-shaped structure were made of oxybutylene and hexanoate repeating units, respectively (hydrophobic segments). The remaining two side arms are made of oxyethylene repeating units (hydrophilic segments) that are connected to the rest of the structure through disulfide bonds. The prepared H-shaped macromolecules were characterized by elemental analysis (CHNS), FT-IR, and 1H-NMR techniques. Based on transmission electron microscopy (TEM) images, the amphiphilic nature of the H-shaped polymer allowed it to form spherical molecular assemblies with a mean diameter of about 80 nm. The critical micelle concentration (CMC) in an aqueous solution was determined using the fluorometric method (CMC = 4.76 × 10−3 mg/mL). According to the profiles obtained from dynamic light scattering (DLS), the resulting spherical micelles had a mean hydrodynamic diameter ( H ) of ∼95 nm with a low polydispersity index (PDI = 0.26).

Zeolite Nanoparticles Loaded with 2-Methoxystradiol as a Novel Drug Delivery System for the Prostate Cancer Therapy.

The estrogen metabolite 2-methoxyestradiol (2ME) is a promissory anticancer drug mainly because of its pro-apoptotic properties in cancer cells. However, the therapeutic use of 2ME has been hampered due to its low solubility and bioavailability. Thus, it is necessary to find new ways of administration for 2ME. Zeolites are inorganic aluminosilicates with a porous structure and are considered good adsorbents and sieves in the pharmaceutical field. Here, mordenite-type zeolite nanoparticles were loaded with 2ME to assess its efficiency as a delivery system for prostate cancer treatment. The 2ME-loaded zeolite nanoparticles showed an irregular morphology with a mean hydrodynamic diameter of 250.9 ± 11.4 nm, polydispersity index of 0.36 ± 0.04, and a net negative surface charge of -34 ± 1.73 meV. Spectroscopy with UV-vis and Attenuated Total Reflectance Infrared Fourier-Transform was used to elucidate the interaction between the 2ME molecules and the zeolite framework showing the formation of a 2ME-zeolite conjugate in the nanocomposite. The studies of adsorption and liberation determined that zeolite nanoparticles incorporated 40% of 2ME while the liberation of 2ME reached 90% at pH 7.4 after 7 days. The 2ME-loaded zeolite nanoparticles also decreased the viability and increased the mRNA of the 2ME-target gene F-spondin, encoded by SPON1, in the human prostate cancer cell line LNCaP. Finally, the 2ME-loaded nanoparticles also decreased the viability of primary cultures from mouse prostate cancer. These results show the development of 2ME-loaded zeolite nanoparticles with physicochemical and biological properties compatible with anticancer activity on the human prostate and highlight that zeolite nanoparticles can be a good carrier system for 2ME.

Green Synthesis of Silver Nanoparticles from Solenostemma argel Leaf Extract: Characterization and Wound Healing Activity

Green synthesis or biosynthesis of nanoparticles (NPs) has recently emerged as a significant approach to producing metallic NPs due to its rapid, affordable and ease of fabrication. Silver nanoparticles (AgNPs) are particularly impressive due to their antimicrobial, bacteriostatic, and low in vivo toxicity. Wound healing is a complex procedure involving the activity of various tissues and cell lineages that have long been the topic of intense research. A faster and more efficient recovery with the minimum side effects is one of the key goals in wound healing. The current study aims to perform a green synthesis of AgNPs mediated by Solenostemma argel leaf extract, combine it with chitosan (CS) gel, and evaluate its effectiveness as a wound healing agent in a rat model. The biosynthesized AgNPs were characterized by UV-visible spectroscopy, FTIR, XRD, DLS analysis and SEM imaging. The developed AgNPs were spherical, with sizes ranging from 60–90 nm. Analysis of the UV-visible spectrum revealed a strong peak at 418.02 nm; this was the first indication of the biosynthesis of AgNPs. X-Ray diffraction analysis indicated the crystallinity phase of biosynthesized AgNPs. The mean hydrodynamic diameter and PDI of the biosynthesized AgNPs were 71.38±2.73 nm and 0.208±0.01, respectively. A high negative zeta potential (30.95±0.58 mV) indicates that the nanomaterial is highly stabilized. The developed AgNPs were uniformly dispersed with 2% w/v CS solution to form AgNPs/CS gel. The in-vivo animal experiment and histopathological analysis outcomes revealed that groups of wounded animals receiving the topical application of AgNPs/CS-gel experienced quicker and better wound healing. Based on this outcome, it can be concluded that biosynthesized AgNPs developed into AgNPs/CS-gel have great potential to be established as wound healing agents.

Synthesis of modified tannic acid hydrogel for the transdermal delivery of curcumin

The search for new materials with a wide range of qualities and uses in the field of anti-cancer drug delivery is on the rise. The field of medication delivery is likewise at its pinnacle, with high-acceptability materials such as hydrogels, liposomes, and nanoparticles being reported daily. Even while strong delivery candidates are present, maintaining their size while preserving biocompatibility is difficult. A solution is phytochemicals with reducing characteristics, which might be further improved by grafting with appropriate monomers. As a matter of fact, the goal of this research was to synthesize a new chemically modified oleic acid-silver nanoparticle conjugated poly vinyl alcohol-tannic acid nanohydrogel for the transdermal delivery of curcumin for cancer therapy. It is believed to increase percutaneous absorption, reduce side effects, target breast carcinoma cells, and maximize the drug's cytocompatibility. Fourier transform infrared (FTIR) spectroscopy, ultraviolet–visible (UV-Vis) spectroscopy, scanning electron microscopy (SEM), dynamic light scattering (DLS), and zeta potential analysis were used to characterize the synthesized material. Drug release investigations were also carried out. The prepared hydrogel had porous surface morphology and a three-dimensional network structure in cross-section with a mean hydrodynamic diameter of 5.0 nm. The drug loading and encapsulation efficiency were found to be 77.0% and 87.5%, respectively with a pH stimulated maximum swelling percentage of 380.0%. Further investigations proved increased percutaneous absorption and anti-bacterial activity along with reduced side effects. The produced transdermal hydrogel was found to be an excellent option for pH-controlled administration of anticancer medication curcumin to target breast carcinoma cells, and maximize the drug's cytocompatibility.

Synthesis and characterization of pH-responsive PCL-PVA polymersome for dual delivery to breast cancer cells

pH-sensitive polymersomes have shown promising potential in drug delivery to cancer cells in past decades. Having various structural characteristics would make them suitable for dual drug delivery applications. In this study, aldehyde-modified PCL and hydrazine-modified PVA were synthesized and were used to form PCL-PVA copolymer through Schiff base reaction mechanism. The obtained structures were characterized by the H-NMR analysis, and it was determined that PCL and PVA are attached by a pH-sensitive hydrazone bond. According to H NMR spectra, PCL-PVA copolymer degree of substitution (DS) was determined 84% and it consists of 38% PVA and 62% PCL as the hydrophile and hydrophobe part, respectively. The solvent switch method was used to synthesize the polymersomes. Drug-free polymersomes which were synthesized with the order of aqueous solvent addition to organic solvent had the lowest size of 136 nm while, the ones synthesized with the order of organic solvent addition to aqueous solvent had the highest loading efficiency for curcumin (92%) and methotrexate (60%). The mean hydrodynamic diameter of drug-loaded polymersomes was obtained 220 nm by DLS and their spherical morphology was confirmed by TEM and SEM. Curcumin and Methotrexate release was evaluated at pH 5.5 and 7.4 and it was demonstrated that the drug release was higher in the acidic environment, confirming the system is pH-sensitive. Also, the cumulative release of CUR and MTX at pH 5.5 after 48 h achieved 91% and 63% respectively. Cytotoxicity assay was also performed and it showed that the dual drug-loaded polymersomes are more toxic than the single drug-loaded carrier and individual free drugs against MCF7 cells. Moreover, no toxicity was shown when the drug-free polymersomes were exposed to MCF7 cells after 48 h. It was also observed that the dual drug-loaded polymersomes were correctly targeted and have high cellular uptake. In general, the results show that this novel pH-sensitive system could be a promising system for breast cancer treatment by approaching co-delivery concept in future investigations.