High Encapsulation Efficiency Research Articles

Synthesis and characterization of a novel dual sensitive iron nanoparticles incorporated Schiff base composite hydrogel for diabetic wound healing therapy

Chronic wounds in diabetic patients deteriorate into multiple infections. A multifunctional transdermal material with high self-healing ability, remodeling capability, antibacterial and radicle scavenging activity, and an excellent multi-sensitive carrier was needed to promote wound healing. For that, Oxidized Cellulose (OC) and gelatin (GLN) are selected to construct a dual drug-loaded Schiff base hydrogel with iron nanoparticle (IONPS) incorporation for the controlled and sustained release of Insulin (INS) and Metfomin (MET), which synergistically promote wound repair. The INS/MET-IONPS-OC/GLN hydrogel drug payload was characterized using FT-IR, XRD, DLS, ZETA, TG, FE-SEM, TEM, and VSM analysis. The high drug loading and encapsulation efficiency were 93.20 % and 98.8 % for INS and 90.2 % and 95.1 % for MET, respectively. The temperature-sensitive drug release (92.0 % of INS and 90.0 % of MET) percentage is much better than the pH-sensitive drug release (83.5 % of INS and 80.2 % of MET). Above 90.0 % viability in MTT and apoptosis assay reveals the nontoxic nature of the INS/MET-IONPS-OC/GLN towards L929 normal cell lines. The zone of inhibition value of 12 and 15 mm in gram-negative bacteria reveals the anti-bacterial effect. The antioxidant activity of the carrier shields the cells against reactive oxygen species promotes healing rate ensures by DPPH assay.The cell proliferation and angiogenesis were confirmed by scratch assay on L929 cell lines in diabetic and non-diabetic conditions, showing the healing ability of the INS/MET-IONPS-OC/GLN hydrogel.

Combining Ultra-Turrax and ultrasonic homogenization to achieve higher vitamin E encapsulation efficiency in spray drying

Vitamin E, a soluble antioxidant widely used in the food and pharmaceutical industries, is rich in tocopherols and phytosterols. Since vitamin E molecules are highly sensitive to oxidation, encapsulation is a viable and effective technique for preservation of the properties of Vitamin E and improving its stability during storage, maintaining the nutritional value. In this work, the aim was to encapsulate concentrated vitamin E using a combination of Ultra-Turrax and ultrasonication to achieve higher encapsulation efficiency in spray drying. In the first stage, the vitamin E oil was encapsulated employing only Ultra-Turrax homogenization, with subsequent optimization of spray drying. The coating materials used were maltodextrin and whey protein isolate. Optimization of the spray drying step evaluated the effects of the drying air temperature (T) and the feed flow rate (Q), to obtain better yields and a high-quality product. In the second stage, the use of ultrasonication in an additional homogenization step was evaluated, aiming to further improve the encapsulation process. The results showed that the best drying conditions (first stage) were T = 180 °C and Q = 0.6 L/h, which provided the highest yield (67.73%) and high encapsulation efficiency (73.73%). The microspheres produced had similar properties, with mean diameters ranging from 0.64 to 12.99 μm. In the second stage of the investigation, the application of ultrasonication immediately after the Ultra-Turrax homogenization enabled the encapsulation efficiency to be increased to 94.05%, with a yield of 57.54%, using an ultrasonication time of only 7 min. This showed that addition of the ultrasonic homogenization step to the process greatly improved the encapsulation efficiency and could be used to produce vitamin E-enriched powder microcapsules by spray drying, with application in the food industry.

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.

PEGylated pH-Responsive Liposomes for Enhancing the Intracellular Uptake and Cytotoxicity of Paclitaxel in MCF-7 Breast Cancer Cells.

This study aimed to develop paclitaxel (PTX)-loaded PEGylated (PEG)-pH-sensitive (SpH) liposomes to enhance drug delivery efficiency and cytotoxicity against MCF-7 breast cancer cells. PTX-loaded PEG-SpH liposomes were prepared using the thin film hydration method. ATR-FTIR compatibility studies revealed no significant interactions among liposome formulation components. TEM images confirmed spherical morphology, stability, and an ideal size range (180-200nm) for improved blood circulation. At pH 5.5, liposomes exhibited increased size and positive zeta potential, indicating pH-sensitive properties due to CHEMS response to the acidic tumor microenvironment. Conversely, at pH 7.4, liposomes showed a slightly larger size (199.25 ± 1.64nm) and a more negative zeta potential (-36.94 ± 0.32mV), suggesting successful PEG-SpH surface modification, enhancing stability, and reducing aggregation. PTX-loaded PEG-SpH liposomes demonstrated high encapsulation efficiency (84.57 ± 0.92% w/w) and drug loading capacity (4.12 ± 0.26% w/w). In-vitro drug release studies revealed accelerated first-order PTX release at pH 5.5 and a controlled zero-order release at pH 7.4. Cellular uptake studies on MCF-7 cells demonstrated enhanced PTX uptake, attributed to mPEG-PCL incorporation prolonging circulation time and CHEMS facilitating PTX release in the tumor microenvironment. Furthermore, PTX-loaded PEG-SpH liposomes exhibited significantly improved cytotoxicity with an IC50 value of 1.107µM after 72-h incubation, approximately 90% lower than plain PTX solution. Stability studies confirmed the robustness of the liposomal formulation under various storage conditions. These findings highlight the potential of PEGylated pH-responsive liposomes as effective nanocarriers for enhancing PTX therapy against breast cancer.

Zein nanoencapsulation enhances the antifungal activity of thymol for postharvest decay control in bananas

AbstractThe current work describes a nanoparticle system-based approach to enhance the antifungal activity of thymol, a ubiquitous natural antifungal phenolic compound, in postharvest control against banana anthracnose. Thymol was encapsulated within the amphiphilic protein zein by high-shear emulsification, yielding highly dispersible thymol-loaded zein nanoparticles with a high encapsulation efficiency (70%). These particles have an average diameter of 300 nm with spherical morphology, smooth interface, and matrix-type internal structure, as supported by comprehensive structural characterization (dynamic light scattering, transmission electron microscopy and atomic force microscopy). Based on a 40-d storage stability test, thymol was effectively retained within the nanoparticles at 4 °C and ambient room temperature (99% and 97% retention, respectively), despite thymol’s instability and volatility. Antifungal activity assessment against Colletotrichum musae, one of the predominant pathogens that cause banana anthracnose, showed a 200- to 300-fold improvement in the in vitro antifungal activity of thymol. Moreover, the application of thymol-loaded zein nanoparticles as a spray component for banana postharvest treatment demonstrated the efficacy of thymol-loaded zein nanoparticles in preventing and delaying the formation of initial symptoms of banana anthracnose. This appears to arise from the thymol-loaded zein nanoparticles depositing as a film on the banana epidermis, as revealed by atomic force microscopy. Overall, this nanoparticle system offers a new avenue for the design of effective antifungal materials with potential applications in combatting postharvest diseases. Graphical abstract

Cationic Amphiphilic Comb-Shaped Polymer Emulsifier for Fabricating Avermectin Nanoemulsion with Exceptional Leaf Behaviors and Multidimensional Controlled Release.

The development of intelligent multifunctional nanopesticides featuring enhanced foliage affinity and hierarchical target release is increasingly pivotal in modern agriculture. In this study, a novel cationic amphiphilic comb-shaped polymer, termed PEI-TA, was prepared via a one-step Michael addition between low-molecular-weight biodegradable polyethylenimine (PEI) and tetradecyl acrylate (TA), followed by neutralization with acetic acid. Using the emulsifier PEI-TA, a positively charged avermectin (AVM) nanoemulsion was prepared via a phase inversion emulsification process. Under optimal formulation, the obtained AVM nanoemulsion (defined as AVM@PEI-TA) demonstrated exceptional properties, including small size (as low as 67.6 nm), high encapsulation efficiency (up to 87.96%), and high stability toward shearing, storage, dilution, and UV irradiation. The emulsifier endowed AVM@PEI-TA with a pronounced thixotropy, so that the droplets exhibited no splash and bounce when they were sprayed on the cabbage leaf. Owing to the electrostatic attraction between the emulsifier and the leaf, AVM@PEI-TA showed improved leaf adhesion, better deposition, and higher washing resistance in contrast to both its negatively charged counterpart and AVM emulsifiable concentrate (AVM-EC). Compared to the large-sized particles, the small-sized particles of the AVM nanoemulsion more effectively traveled long distances through the vascular system of veins after entering the leaf apoplast. Moreover, the nanoparticles lost stability when exposed to multidimensional stimuli, including pH, temperature, esterase, and ursolic acid individually or simultaneously, thereby promoting the release of AVM. The release mechanisms were discussed for understanding the important role of the emulsifier in nanopesticides.

Interactions of human serum albumin with phosphate and Tris buffers: impact on paclitaxel binding and nanoparticles self-assembly

Aim To investigate the conformational changes in human serum albumin (HSA) caused by chemical (CD) and thermal denaturation (TD) at pH 7.4 and 9.9, crucial for designing controlled drug delivery systems with paclitaxel (PTX). Methods Experimental and computational methods, including differential scanning calorimetry (DSC), UV-Vis and intrinsic fluorescence spectroscopy, mean diameter, polydispersity index (PDI), ζ-potential, encapsulation efficiency (EE), in vitro release and protein docking studies were conducted to study the HSA denaturation and nanoparticles (NPs) preparation. Results TD at pH 7.4 produced smaller NPs (287.1 ± 12.9 nm) than CD at pH 7.4 with NPs (584.2 ± 47.7 nm). TD at pH 9.9 exhibited high EE (97.3 ± 0.2%w/w) with rapid PTX release (50% within 1h), whereas at pH 7.4 (96.4 ± 2.1%w/w), release only 40%. ζ-potentials were around −30 mV. Conclusion Buffer type and pH significantly influence NP properties. TD in PBS at pH 7.4, provided optimal conditions for a stable and efficient drug delivery system.

Preparation and photothermal properties of latent functional thermal fluid based on size-controllable phase change nanocapsules

To improve the solar heat utilization efficiency of working fluid in direct solar collector, a novel latent functional thermal fluid (LFTF) based on self-designed 1-octadecanol@silica phase change nanocapsules (NEPCMs) with excellent heat storage capacity and photothermal conversion efficiency were prepared. The NEPCMs prepared by sol–gel method were dispersed in water containing multi-walled carbon nanoparticles to prepare the LFTF. The prepared NEPCMs have high encapsulation efficiency (85.12 %) and melting phase change enthalpy (235.1 J/g), controllable particle size (27.13–167.30 nm), excellent thermal stability and cycle stability. The LFTF containing 10 wt% NEPCMs was considered the optimal choice for its excellent dispersion stability (zeta potential 35.63 mV), thermal storage capacity (peak specific heat capacity 5.11 J·g−1·K−1) and superior photothermal conversion efficiency (up to 98 %), which is roughly 3.29 times that of water. These results offer valuable insights for the future development of LFTF in the field of solar thermal applications.

Co-encapsulation of borage seed oil and peppermint oil blends within ultrasound-assisted soy protein isolate/purity gum ultra complex nanoparticles: Fabrication, structural interaction mechanisms, and in vitro digestion studies

This study aimed at co-encapsulating borage seed oil (BSO)- and peppermint oil (PO) blends in ultrasound-assisted complex nanoparticles stabilized by soy protein isolate (SPI) and purity gum ultra (PGU) in different ratios: SPI/PGU-1:0 (NP1), 0:1 (NP2), 1:1 (NP3), 1:3 (NP4), and 3:1 (NP5). The BSO- and PO-loaded SPI/PGU complex nanoparticles (BP-loaded SPNPs) coded as NP4 (SPI-PGU-1:3) revealed a zeta potential of −33.27 mV, a PDI of 0.14, and the highest encapsulation efficiency (81.38 %). The main interactions observed among SPI, PGU, BSO, PO, and a blend of BSO and PO, as determined by FTIR and molecular docking, involved hydrophobic effects, electrostatic attraction, and H-bonding. These interactions played crucial roles in the production of BP-loaded SPNPs. XRD results validated the alterations in the structure of BP-loaded SPNPs caused by varying proportions of SPI and PGU. The thermal capacity of BP-loaded SPNPs (NP4), as determined by TGA, exhibited the lowest amount of weight loss compared to other BP-loaded SPNPs. Morphological results revealed that NP4 and NP5 exhibited a spherical surface and two distinguishable layers, indicating successful coating of PGU onto the droplet surface. In addition, BP-loaded SPNPs (NP4) exhibited a higher antioxidant effect due to their improved progressive release and prolonged release of co-encapsulated BSO and PO during in vitro digestion. The comprehensive investigation of the co-encapsulation of BSO and PO in complex nanoparticles, dietary supplements, and double-layered emulsified systems provides valuable insights into the development of functional foods.

Preparation, Characterization and Sustained-release Study of Encapsulated Cinnamon Essential Oil Microcapsules

Aims: The aim of this study is to study preparation, characterization and sustained release of Encapsulated Cinnamon Essential Oil Microcapsules. Background: In this work, encapsulated cinnamon essential oil (CEO) microcapsules were prepared, characterized, and analyzed for their sustained-release properties. CEO microcapsules were encapsulated from an alginate polymer using homogenization and extrusion, and the encapsulation mechanism used was ionic gelation. The potent antibacterial properties of natural cinnamon oil extracts and their shelf-life activity can be reduced or eliminated as a result of deterioration caused by light, heat, and oxygen exposure during production. High-speed homogenization was utilized for the encapsulation, which encloses and protects the volatile compounds from degradation. Objective: The objective of this study is to synthesize sustained-release encapsulated cinnamon essential oil (CEO) microcapsules. Method: The preparation of encapsulated cinnamon oil was achieved through homogenization. The extrusion method was employed to obtain microcapsules encapsulating liquid active ingredients (AI) with alginate polymer to induce ionic gelation. Results: SEM and Optical images reveal that all microcapsules maintain their spherical shape with clearly defined membranes. XPS analysis indicates the presence of oxygen (O), carbon (C), and sodium (Na) on the surface, suggesting the presence of an alginate-based ionic gelation. Chromatographic studies demonstrate a high encapsulation efficiency of 99%. The average microcapsule size is 261.5 nm for the fresh sample and 278 nm after 3.5 months. The zeta potential is -29.8 mV for the fresh sample and -28.2 mV after 3.5 months. Notably, there is no evidence of microcapsule agglomeration during the 3.5-month storage period as observed in the study. TGA data reveals that only 7.5% of the adsorbed water and essential oil mixture is lost at 40°C over 4 hours, in contrast to 11.7% for the adsorbed water material, indicating a sustained release of the encapsulated CEO from the microcapsules. Conclusion: The microcapsules exhibited an impressive encapsulation efficiency of 99%, demonstrating stability over the 3.5-month investigation period and showcasing sustained-release properties.

Effect of maltodextrin and Persian gum as wall materials and tannic acid as copigment on some properties of encapsulated sour cherry anthocyanin microcapsules

Due to the instability of anthocyanins, their application as natural colorants is limited. To improve their stability, anthocyanins extracted from sour cherry were copigmented with tannic acid at varying molar ratios. The optimal anthocyanin:copigment molar ratio was determined to be 1:0.25. Subsequently, both non-copigmented and copigmented anthocyanins (using the optimal tannic acid molarity) were spray-dried with either maltodextrin alone (T1 and T2) or a combination of maltodextrin and Persian gum (T3 and T4). The anthocyanin retention in T2 and T4 was approximately 53 % and 38 %, respectively, which were higher than in the non-copigmented samples. All powders demonstrated high encapsulation efficiency (>90.37 %). Stability tests on the anthocyanins conducted over 28 days indicated that light exposure had no effect on the reduction of anthocyanin content when maltodextrin was used. Thus, the copigmentation of anthocyanins with tannic acid, combined with encapsulation in maltodextrin, presents a promising method for producing a stable natural colorant.

Decorating Delivery Vehicles Using Hyaluronic Acid Oligosaccharides Enables Active Targeting Toward Cancer and Minimizes Adverse Effect of Chemotherapeutics.

The major drawback of conventional chemotherapeutic treatment is the non-specificity or inability to ascertain and target cancerous cells directly. In this study, an active targeting strategy that is poised to carry the anticancer agents to the desired sites for therapeutic action while avoiding toxicity to normal organs is provided. The active targeting of delivery vehicles is achieved by ligand-receptor interactions, in particular the specific binding between hyaluronic acid oligosaccharides (oHAs) and CD44 receptors. This study first prepares oHAs by the size-exclusion chromatography and utilizes them to decorate chitosan (CTS) as basic materials (oHAs-CTS) for drug delivery, then fabricates oHAs-CTS into micro/nanoscale carriers to encapsulate agents for cancer chemotherapy. The oHAs-CTS micro/nanocarriers exhibit high drug encapsulation efficiency (58-87%), and the drug releases present a sustained behavior. Notably, oHAs-CTS delivery vehicles display an enhanced active targeting toward cancers and alleviate the cytotoxic effects on normal cells. Additionally, in vivo results show that drug-laden oHAs-CTS nanocarriers demonstrate a significant inhibitory effect on 4 T1 tumors without any toxicity to the major organs. Taken together, the findings highlight the potential of oHAs-CTS micro/nanospheres as delivery vehicles with enhanced active targeted capability toward cancers and minimized adverse effects of chemotherapeutic agents for cancer treatment.

Characterization of orange peel extract-cross linking whey protein nanoparticles and their influences on the physical and sensory properties of orange juice

This work explores the characterization of orange peel extract (OPE)-cross-linked whey-protein nanoparticles for enhancing the physical and sensory properties of orange juice. Three methods were employed to cross-link particle-forming peptides with citric acid, i.e., OPE charging–cross-linking–desolvation (A), cross-linking–OPE charging–desolvation (B), and OPE charging–desolvation–cross-linking (C). B method produced smaller particles (229 ± 11.53 nm) with higher encapsulation efficiency (67.16 ± 1.75%). Kinetic studies indicated predominantly diffusion-based release of OPE from the particles, B express the lowest diffusion rate with 10.20 ± 1.23% after 6 h incubation in NaCl. Using citric acid as a cross-linking agent enhanced the encapsulation efficiency. Moreover, functional orange juices were formulated using OPE and B capsules (500 mg/L). Under simulated in-vitro gastrointestinal conditions, the antioxidant activity was higher in B capsule supplemented juice comparing to OPE supplemented juice at oral, gastric, and intestinal phase which recorded of 69.43 ± 0.750, 85.66 ± 1.12 and 94.53 ± 2.00 mg ascorbic acid/100g respectively by DPPH and 80.91 ± 1.37, 132.01 ± 0.50 and 153.47 ± 2.63 mg ascorbic acid/100g respectively by ABTS. Sensory evaluation demonstrated the acceptability of OPE and cross-linked nanoparticles by the panelists. Cross-linking–OPE charging–desolvation provides high encapsulation efficiency with palatable physico-sensorial attributes in orange juice and offers a promising strategy for creating a nutritious beverage.

Hybrid Liposome-MSN System with Co-Delivering Potential Effective Against Multidrug-Resistant Tumor Targets in Mice Model.

RNA interference (RNAi) stands as a widely employed gene interference technology, with small interfering RNA (siRNA) emerging as a promising tool for cancer treatment. However, the inherent limitations of siRNA, such as easy degradation and low bioavailability, hamper its efficacy in cancer therapy. To address these challenges, this study focused on the development of a nanocarrier system (HLM-N@DOX/R) capable of delivering both siRNA and doxorubicin for the treatment of breast cancer. The study involved a comprehensive investigation into various characteristics of the nanocarrier, including shape, diameter, Fourier transform infrared (FT-IR) spectroscopy, X-ray photoelectron spectroscopy (XPS), encapsulation efficiency, and drug loading. Subsequently, in vitro and in vivo studies were conducted on cytotoxicity, cellular uptake, cellular immunofluorescence, lysosome escape, and mouse tumor models to evaluate the efficacy of the nanocarrier in reversing tumor multidrug resistance and anti-tumor effects. The results showed that HLM-N@DOX/R had a high encapsulation efficiency and drug loading capacity, and exhibited pH/redox dual responsive drug release characteristics. In vitro and in vivo studies showed that HLM-N@DOX/R inhibited the expression of P-gp by 80%, inhibited MDR tumor growth by 71% and eliminated P protein mediated multidrug resistance. In summary, HLM-N holds tremendous potential as an effective and targeted co-delivery system for DOX and P-gp siRNA, offering a promising strategy for overcoming MDR in breast cancer.

Optimisation of the Encapsulation of Grape Pomace Extract by Spray Drying Using Goat Whey Protein as a Coating Material

The aim of this research was to determine the optimal conditions for the process of the microencapsulation of phenol-rich grape pomace extract (GPE) using spray drying and goat whey protein (GW) as a coating. The encapsulation was carried out with the aim of protecting the original bioactive components extracted from grape pomace to ensure their stability and protection from external agents, as well as antioxidant activity, during the conversion of the liquid extract into powder and during storage. Using the response surface methodology, an inlet air temperature of 173.5 °C, a GW ratio of 2.5 and a flow rate of 7 mL/min were determined as optimum process parameters. Under these conditions, a high yield (85.2%) and encapsulation efficiency (95.5%) were achieved with a satisfactorily low moisture content in the product (<5%). The amount of coating had the greatest influence on the MC properties. GW showed a more pronounced stabilising effect on the phenolic compounds in GPE during a longer storage period compared to anthocyanins. The results obtained indicate the potential of GW as a coating and are an example of the possible upcycling of GPE and GW, which can lead to a high-quality product that can be a functional ingredient.

Improved viability of probiotics by co-encapsulation of wheat germ oil under storage and gastrointestinal conditions: Effects of drying methods and wall composition

To improve the viability of probiotics during food storage and gastrointestinal digestion, this study developed solid microcapsules co-loaded with probiotics and wheat germ oil using W1/O/W2 emulsion pre-encapsulation, followed by spray drying (SD), freeze drying (FD) and spray freeze drying (SFD), respectively. The effects of drying methods and wall materials on the microstructure, physicochemical properties, storage stability, and gastrointestinal tolerability were highlighted. Firstly, all samples showed high encapsulation efficiency for probiotics (86%–99.2%) and wheat germ oil (72%–85%), low moisture content (2.8%–5.3%) and hygroscopicity (6.3%–11.6%), and wall materials exhibited structural stability during the drying process. The results of viable cell counts indicated that SFD caused more damage to bacterial cells than the other two drying methods, as evidenced by the total death of encapsulated probiotics within 90 days. In contrast, SD and FD encapsulated probiotics remained at 8.8–9.9 log CFU/g after 150 days of storage at 4 °C and 25 °C. Furthermore, the viability of probiotics in the co-encapsulated and pectin-added microcapsules was significantly enhanced in storage stability and simulated gastrointestinal digestion tests. Based on the above results, it was suggested that the co-encapsulation strategy of combining the W1/O/W2 structure and SD or FD to prepare microencapsulated powders can obtain probiotic products with high activity and high stability. Meanwhile, composite wall material (whey protein isolate and pectin) could enhance probiotics' protective effect and colonic targeted release behavior. In conclusion, the current research provides a valuable reference for the application of probiotics and functional oils in the food industry.

Investigation on the structure and properties of nanostructured lipid carriers loaded with different contents of phytosterols and their impact on lipid oxidation

In this study, nanostructured lipid carriers (NLCs) were prepared using walnut oil as a liquid lipid to load phytosterols (PS). The effects of different ratios of PS to lipids on the structural and functional properties of these carriers and lipid oxidation of PS-loaded carriers were investigated. The XRD, FTIR, and DSC results indicated that NLCs formulated with walnut oil as the liquid lipid were successful in incorporating PS. These NLCs exhibited a smaller average particle size (<300 nm) and a lower PDI (<0.3), along with a higher zeta potential. Furthermore, transmission electron microscopy (TEM) revealed that PS5-NLC displayed the most uniform particle size distribution and excellent dispersion. Notably, NLCs demonstrate high encapsulation efficiency and antioxidant capacity. Importantly, the bioaccessibility of PS in the carriers significantly increased from 23.5% to 86.8% compared with that of pure PS. Following a storage period of 21 days, the NLCs loaded with PS showed a lipid hydroperoxide (LH) value of 32.4 mmol/L and a malondialdehyde (MDA) content of 9.9 μmol/L, which were 13.6% and 33.3% lower, respectively, than those of the carriers without PS, indicating an effective reduction in lipid oxidation. This study is first to introduce the innovative use of walnut oil as a liquid lipid for preparing NLCs. It was observed that incorporating PS not only enhanced the bioaccessibility of these compounds but also effectively mitigated lipid oxidation. Overall, this study offers valuable insights into the development of PS delivery systems and broadens the potential applications of walnut oil.

Development and characterization of a zeolite based drug delivery system: Application to cannabidiol oral delivery

The growing interest in the therapeutic potential of cannabidiol (CBD) has led to the need for effective and reliable delivery methods that overcome its low oral absorption. Zeolites, a class of porous nanoparticles, offer unique advantages as drug carriers due to their high surface area and adjustable pore size. In this study, a zeolite-based drug delivery system was developed for the encapsulation of CBD. The zeolite particles were characterized using various techniques such as Scanning Electron Microscopy (SEM), N2 adsorption analysis, Solid-state Fourier Transform Infrared (FTIR), Direct Light Scattering (DLS), X-ray diffraction (XRD) and thermogravimetric analysis (TGA) before and after the loading. The drug encapsulation efficiency, and the release profile of CBD from the zeolite matrix were evaluated in addition to in vitro dissolution experiments in the intestinal and gastric simulated fluids. The results showed that the loaded zeolite particles exhibited high encapsulation efficiency of 73.5 %. XRD analysis proved that the USY structure remained intact after loading with CBD. DLS and N2 adsorption analysis indicated that CBD was successfully loaded into the zeolite matrix. When compared to CBD containing particles in a commercialized capsule, the in-vitro dissolution rate of CBD loaded zeolite was significantly higher after 30 min in the simulated stomach (pH 1.8) and the intestinal (pH 6.8) fluids, 67.8 % versus 43.6 % and 62.6 % vs 38.4 % respectively. Our findings open new avenues for the use of zeolites as an efficient drug delivery system for drugs with low bioavailability like CBD.

Poly (β-amino esters)/Mobil Composition of Matter 41-mediated delivery of siIL-1β alleviates deep vein thrombosis in rat hind limbs.

Introduction: Deep vein thrombosis (DVT) is a major cause of cardiovascular disease-related deaths worldwide and is considered a thrombotic inflammatory disorder. IL-1β, as a key promoter of venous thrombus inflammation, is a potential target for DVT treatment. Constructing a nanocarrier system for intracellular delivery of siIL-1β to silence IL-1β may be an effective strategy for alleviating DVT. Methods: ELISA was used to detect the expression levels of IL-1β and t-PA in the serum of DVT patients and healthy individuals. In vitro, HUVEC cells were treated with IL-1β, and changes in VWF and t-PA expression levels were assessed. PBAE/MCM-41@siIL-1β (PM@siIL-1β) nano-complexes were synthesized, the characterization and biocompatibility of PM@siIL-1β were evaluated. A rat hind limb DVT model was established, and PM@siIL-1β was used to treat DVT rats. Morphology of the inferior vena cava, endothelial cell count, IL-1β, vWF, and t-PA levels, as well as changes in the p38 MAPK and NF-κB pathways, were examined in the different groups. Results: IL-1β and t-PA were highly expressed in DVT patients, and IL-1β treatment induced a decrease in VWF levels and an increase in t-PA levels in HUVEC cells. The synthesized PM@siIL-1β exhibited spherical shape, good stability, high encapsulation efficiency, and high drug loading capacity, with excellent biocompatibility. In the DVT model rats, the inferior vena cava was filled with blood clots, endothelial cells increased, IL-1β and VWF levels significantly increased, while t-PA levels were significantly downregulated. Treatment with PM@siIL-1β resulted in reduced thrombus formation, decreased endothelial cell count, and reversal of IL-1β, VWF, and t-PA levels. Furthermore, PM@siIL-1β treatment significantly inhibited p38 phosphorylation and upregulation of NF-κB expression in the DVT model group. Conclusion: IL-1β can be considered a therapeutic target for suppressing DVT inflammation. The synthesized PM@siIL-1β achieved efficient delivery and gene silencing of siIL-1β, demonstrating good therapeutic effects on rat hind limb DVT, including anti-thrombotic and anti-inflammatory effects, potentially mediated through the p38 MAPK and NF-κB pathways.

Synthesis of Ganoderic Acids Loaded Zein-Chitosan Nanoparticles and Evaluation of Their Hepatoprotective Effect on Mice Given Excessive Alcohol.

Ganoderma lucidum, used in East Asia for its health benefits, contains ganoderic acids (GA) which have various pharmacological activities but are limited by poor water solubility and low oral bioaccessibility. This study synthesized and characterized ganoderic acids loaded zein-chitosan nanoparticles (GA-NPs), and investigated its advantages in alleviating alcoholic liver injury (ALI) in mice model. The GA-NPs demonstrated high encapsulation efficiency (92.68%), small particle size (177.20 nm), and a +29.53 mV zeta potential. The experimental results of alcohol-induced liver injury mouse model showed that GA-NPs significantly improved liver metabolic function, reduced alcohol-induced liver oxidative stress in liver by decreasing lactate dehydrogenase activity and malondialdehyde level, while increasing the activities of liver antioxidant enzymes and alcohol dehydrogenase. Moreover, GA-NPs were favorable to ameliorate intestinal microbiota dysbiosis in mice exposed to alcohol by increasing the proportion of probiotics such as Romboutsia, Faecalibaculum, Bifidobacterium and Turicibacter, etc., which were highly correlated with the improvement of liver function. Furthermore, GA-NPs modulated the mRNA expression related to ethanol metabolism, oxidative stress and lipid metabolism. Conclusively, this study revealed that GA-NPs have stronger hepatoprotective effects than non-encapsulated ganoderic acids on alleviating ALI by regulating intestinal microbiota and liver metabolism.