Release Of Active Ingredients Research Articles

Antibacterial composite protein microneedle loaded with hypoxia-treated exosomes for oral ulcer healing

Oral ulcer treatment is challenging: various dressings have been developed, but they have poor efficacy. The efficacy of oral ulcer treatment depends on the local drug concentration; low drug concentrations result in slow wound healing. Therefore, the sustained release of active therapeutic ingredients from wound dressings with few administrations is promising. Hypoxic exosomes (Exos) can promote cell proliferation and angiogenesis. Further, silver nanoparticles (AgNPs) confer broad-spectrum antimicrobial effects. We prepared a light-cured composite microneedle (MN) patch based on bovine serum albumin methacryloyl (BSAMA) and methacrylic gelatin (GelMA) (the combination is denoted BG). Control, BG, BG@Exos, and BG@Exos&AgNPs were used to explore the therapeutic effects of hypoxic Exos and AgNPs on oral ulcers. In vitro experiments showed that BG@Exos&AgNPs MN patches effectively promoted cell migration, proliferation, and angiogenesis and significantly inhibited bacterial growth and expression of IL-2 and TNF-ɑ. We found that BG@Exos&AgNPs promoted the healing of oral ulcers in rats, demonstrated by rapid wound epithelial healing, downregulation of inflammatory factor expression, and increased macrophage polarization. Therefore, the designed BG@Exos&AgNPs MN patch is a valuable approach for treating oral ulcers.

Intelligent Systems Based on Cyclodextrins for the Treatment of Breast Cancer.

The incidence of breast cancer has been increasing over the last four decades, although the mortality rate has decreased. Endocrine therapy and chemotherapy are the most used options for cancer treatment but several obstacles are still attributed to these therapies. Smart materials, such as nanocarriers for targeting, delivery and release of active ingredients, sensitive to intrinsic-stimuli (pH-responsive, redox-responsive, enzyme- responsive, and thermo-responsive) and extrinsic-stimuli (ultrasound-responsive, magnetic-responsive, light-responsive) have been studied as a novel strategy in breast cancer therapy. Cyclodextrins (CDs) are used in the design of these stimuli-responsive drug carrier and delivery systems, either through inclusion complexes with hydrophobic molecules or covalent bonds with large structures to generate new materials. The present work aims to gather and integrate recent data from in vitro and in vivo preclinical studies of CD-based stimuli- responsive systems to contribute to the research in treating breast cancer. All drug carriers showed high in vitro release rates in the presence of a stimulus. The stimuli-responsive nanoplatforms presented biocompatibility and satisfactory results of IC50, inhibition of cell viability and antitumor activity against several breast cancer cell lines. Additionally, these systems led to a significant reduction in drug dosages, which encouraged possible clinical studies for better alternatives to traditional antitumor therapies.

Formulation and Evaluation of Tablets Using the Solvent Evaporation Method to Increase the Solubility of Lansoprazole

The inability to determine sufficient and repeatable bioavailability and/or desirable pharmacokinetic features in humans is one of the biggest obstacles to the oral administration of new medicines. The solubility and absorption of a medicine determine its bioavailability, which in turn determines its therapeutic efficacy. Achieving the target drug concentration in the systemic circulation and ensuring drug biological activity in humans are both affected by solubility. A stomach ulcer has the potential to rip through the stomach lining, the initial section of the small intestine, and possibly even the lower esophagus. Distinct ulcers form in different parts of the intestines; one forms in the duodenum and one in the stomach. Duodenal ulcers are most commonly characterized by upper abdominal pain at night that subsides after eating. Eating might exacerbate the discomfort from a stomach ulcer. Preparing and assessing the pills will yield optimal outcomes. The active component content is 99.90%, as is the active ingredient release rate. Compared to other formulations, solid dispersion tablets performed better in in-vitro tests (98.85%). The optimized formulation (lansoprazole solid dispersion tablets) outperformed the labeled formulation (conventional lansoprazole tablet) in terms of drug-releasing capacity within 6 hours, outperforming both formulations.

Formulation and Evaluation of Tablets Using the Solvent Evaporation Method to Increase the Solubility of Lansoprazole

The inability to determine sufficient and repeatable bioavailability and/or desirable pharmacokinetic features in humans is one of the biggest obstacles to the oral administration of new medicines. The solubility and absorption of a medicine determine its bioavailability, which in turn determines its therapeutic efficacy. Achieving the target drug concentration in the systemic circulation and ensuring drug biological activity in humans are both affected by solubility. A stomach ulcer has the potential to rip through the stomach lining, the initial section of the small intestine, and possibly even the lower esophagus. Distinct ulcers form in different parts of the intestines; one forms in the duodenum and one in the stomach. Duodenal ulcers are most commonly characterized by upper abdominal pain at night that subsides after eating. Eating might exacerbate the discomfort from a stomach ulcer. Preparing and assessing the pills will yield optimal outcomes. The active component content is 99.90%, as is the active ingredient release rate. Compared to other formulations, solid dispersion tablets performed better in in-vitro tests (98.85%). The optimized formulation (lansoprazole solid dispersion tablets) outperformed the labeled formulation (conventional lansoprazole tablet) in terms of drug-releasing capacity within 6 hours, outperforming both formulations.

Development of an innovative eugenol and borax-based orodispersible film for enhanced treatment of mouth ulcers

Orodispersible films (ODFs) have emerged as an advanced and patient-friendly delivery system due to ease of administration, improved patient compliance, quick release and taste-masking of active pharmaceutical ingredients. This research reports the preparation of the ODF containing eugenol and borax (EB-ODF) by a solvent casting technique for treating mouth ulcers. The EB-ODF consisted of vinyl pyrrolidone/vinyl acetate copolymer (Kollidon® VA64, VA64) and hydroxypropyl methylcellulose (HPMC-K250) as the film formers where eugenol and borax were loaded. The thickness of the EB-ODF obtained was 0.119 ± 0.001 mm and the tensile strength was 13.1 ± 1.1 N/mm2 (p > 0.05). The prepared films disintegrated in the oral cavity within 30 s and over 90% of the eugenol was released from the film in the first 5 min. Furthermore, the combined application of eugenol and borax, loaded in EB-ODF, displayed notable synergetic antibacterial property against both gram-negative and gram-positive bacteria. In an in-vivo study on a rat model with chemical burn-induced oral ulcers, the EB-ODF treatment group had a 100% reduction in ulcer area (p > 0.05) after 10 days of treatment and demonstrated a 38.7% higher reduction in oral ulcer area compared to the Dingpeng Cream treatment group (p < 0.0001). The EB-ODF treatment group showed minimal oral irritation, scoring only 1 point and a 65% preference in the taste tests (p < 0.0001). In summary, EB-ODF had successfully overcome the poor palatability of commercially available formulation and provided notable potential for further ulcer treatment product development.

Formation of Microcapsules of Pullulan by Emulsion Template Mechanism: Evaluation as Vitamin C Delivery Systems.

Pullulan is a polysaccharide that has attracted the attention of scientists in recent times as a former of edible films. On the other hand, its use for the preparation of hydrogels needs more study, as well as the formation of pullulan microcapsules as active ingredient release systems for the food industry. Due to the slow gelation kinetics of pullulan with sodium trimetaphosphate (STMP), capsules cannot be formed through the conventional method of dropping into a solution of the gelling agent, as with other polysaccharides, since the pullulan chains migrate to the medium before the capsules can form by gelation. Pullulan microcapsules have been obtained by using inverse water-in-oil emulsions as templates. The emulsion that acts as a template has been characterized by monitoring its stability and by optical microscopy, and the size of the emulsion droplets has been correlated with the size of the microcapsules obtained, demonstrating that it is a good technique for their production. Although some flocs of droplets form, these remain dispersed during the gelation process and two capsule size distributions are obtained: those of the non-flocculated droplets and the flocculated droplets. The microcapsules have been evaluated as vitamin C release systems, showing zero-order release kinetics for acidic pH and Fickian mechanism for neutral pH. On the other hand, the microcapsules offer good protection of vitamin C against oxidation during an evaluation period of 14 days.

Comparative Evaluation of Dissolution Performance in a USP 2 Setup and Alternative Stirrers and Vessel Designs: A Systematic Computational Investigation.

The dissolution testing method described in the United States Pharmacopeia (USP) Chapter ⟨711⟩ is widely used for assessing the release of active pharmaceutical ingredients from solid dosage forms. However, extensive use over the years has revealed certain issues, including high experimental intervariability observed in specific formulations and the settling of particles in the dead zone of the vessel. To address these concerns and gain a comprehensive understanding of the hydrodynamic conditions within the USP 2 apparatus, computational fluid dynamic simulations have been employed in this study. The base design employed in this study is the 900 mL USP 2 vessel along with a paddle stirrer at a 50 rpm rotational speed. Additionally, alternative stirrer designs, including the hydrofoil, pitched blade, and Rushton impeller, are investigated. A comparison is also made between a flat-bottom tank and the USP round-bottom vessel of the same volume and diameter. Furthermore, this work examines the impact of various parameters, such as clearance distance (distance between the bottom of the impeller and bottom of the vessel), number of impeller blades, impeller diameter, and impeller attachment angle. The volume-average shear rate (Stv), fluid velocity (Utv), and energy dissipation rates (ϵtv) represent the key properties evaluated in this study. Comparing the USP2 design and systems with the same stirrer but flat-bottom vessel reveals more homogeneous mixing compared to the USP2 design. Analyzing fluid flow streamlines in different designs demonstrates that hydrofoil stirrers generate more suspension or upward movement of fluid compared to paddle stirrers. Therefore, when impellers are of a similar size, hydrofoil designs generate higher fluid velocities in the coning area. Furthermore, the angle of blade attachment to the hub influences the fluid velocity in the coning area in a way that the 60° angle design generates more suspension than the 45° angle design. The findings indicate that the paddle stirrer design leads to a heterogeneous shear rate and velocity distributions within the vessel compared with the other designs, suggesting suboptimal performance. These insights provide valuable guidance for the development of improved in vitro dissolution testing devices, emphasizing the importance of optimized design considerations to minimize hydrodynamic variability, enhance dissolution characterization, and reduce variability in dissolution test results. Ultimately, such advancements hold potential for improving in vitro-in vivo correlations in drug development.

Characterization and Performance Analysis of Hydrolyzed versus Non-Hydrolyzed Poly(NVF-co-HEA) Hydrogels for Cosmetic Applications.

This study explores the synthesis and modification of poly(N-vinylformamide-co-N-hydroxyethyl acrylamide) (poly(NVF-co-HEA)) hydrogels for cosmetic applications. Poly(NVF-co-HEA) hydrogels were produced followed by an acid hydrolysis reaction to produce poly(NVF-co-VAm-co-HEA) hydrogels, introducing poly(vinyl amine) (PVAm) into the structure. This modification considerably alters the hydrogels' properties, yielding materials with over 96% water content, predominantly in the form of non-freezing or free water, which is beneficial in the uptake and release of hydrophilic species. The primary amine groups from inclusion of VAm also improved the mechanical properties, as evidenced by an 8-fold increase in Young's modulus. The hydrogels also possessed pH-responsive behavior, which was particularly noticeable under acidic and basic conditions, where a large decrease in water content was observed (40% to 75% reduction). Characterizing the hydrogels' release capabilities involved using organic dyes of different functional groups and sizes to examine the pH impact on release. The results indicated that hydrolyzed hydrogels interacted more effectively with charged species, highlighting their suitability for pH-responsive delivery. The release of cosmetic active ingredients was also demonstrated through the controlled release of Liquid Azelaic™, specifically potassium azeloyl diglycinate (PAD). Our findings reveal that the hydrolyzed hydrogels exhibit superior burst release, especially under alkaline conditions, suggesting their suitability for cosmetic applications where controlled, pH-responsive delivery of active ingredients is desired. Overall, this investigation highlights the potential of hydrolyzed poly(NVF-co-HEA) hydrogels in cosmetic applications. Their ability to combine high water content with mechanical integrity, along with their pH-responsive release ability, allows for use in cosmetic formulations.

Microencapsulation of star anise essential oil: Preparation, characterization, in vitro digestion, and biological activity

Star anise essential oil (SAEO) has garnered significant attention for its potent bioactivities. However, the instability and poor water solubility of SAEO limit its application in the food and pharmaceutical industries. To overcome these challenges and improve bioavailability, we encapsulated SAEO within β-cyclodextrin (β-CD) using a saturated aqueous solution method. Characterization techniques including Fourier transform infrared spectroscopy, Scanning electron microscopy, X-ray diffraction, and Thermogravimetric-differential scanning calorimetry confirmed the successful formation of SAEO and β-CD inclusion complex (SAEO-IC) with good thermal stability. The inclusion complex had a yield of 63.18 ± 3.18% and an oil content of 9.32 ± 0.36%. In vitro digestion studies revealed the stability of SAEO-IC in gastric conditions, with the primary release of active ingredients occurring in the intestine. Moreover, the encapsulation process preserved the antioxidant properties of SAEO and demonstrated enhanced antimicrobial and anti-tumor activity, suggesting that SAEO-IC has the potential to serve as a natural antimicrobial and anticancer agent.

Development of an emulsion composition with fennel and caraway essential oils for use in the combined therapy of ulcerative colitis

The aim of the study is to develop the composition of an emulsion containing essential oils of Fennel and Caraway seeds for use in the symptomatic complex therapy of ulcerative colitis with the aim of eliminating functional intestinal disorders. Materials and methods. The objects of the study were samples of emulsions containing active pharmaceutical ingredients (essential oils of Fennel and Caraway), purified water, oils (refined sunflower oil, refined olive oil, refined sesame oil), emulsifiers (polyethylene glycol 40 hydrogenated castor oil, polysorbate 80, polyethylene glycol 100 stearate, acacia gum, guar gum, xanthan gum, soya lecithin), viscosity regulator - apple pectin and flavouring agents (food additives with cherry and tarragon flavour). Organoleptic properties, stability, rheological parameters, pH, particle size determination by microscopy, and a taste test were carried out with model emulsion samples. Research to establish the optimal technological parameters was carried out in parallel. Results. The main parameters of the technological process have been established, which allow to obtain an emulsion with evenly distributed particles: 15 minutes at maximum speed. The concentration of emulsifiers at which the emulsions are stable was selected. It was found that the samples containing polyethylene glycol 100 stearate, gums, and soy lecithin have satisfactory organoleptic properties. The sample with soy lecithin emulsifier differs from the others in its ability to form microemulsions, but it has low viscosity. To improve the rheological properties, apple pectin was added to the emulsion. The taste test showed that among vegetable oils, refined sesame oil has a more neutral taste, and the flavouring additive "Tarkhun" balances the taste better. The release of active pharmaceutical ingredients (APIs) from the emulsion base was confirmed by thin-layer chromatography. Conclusions. A microemulsion with essential oils based on refined sesame oil, soy lecithin, with the addition of viscosity and flavour correctors was developed. The obtained emulsion has satisfactory organoleptic properties and conforms to the requirements for emulsion quality indicators

Self‐assembled nanoparticles based on pullulan‐g‐poly(Z‐L‐lysine) for controlled drug delivery: Synthesis, characterization and preliminary studies on the encapsulation of indomethacin

AbstractNovel biocompatible systems suitable for the controlled release of active ingredients are under the spotlight within the last few years. The present investigation focuses on the preparation of nanoparticles (NPs) based on the amphiphilic copolymer pullulan‐graft‐poly(Z‐L‐lysine) bearing different amounts of lysine (10, 20, and 30 wt%), and on the evaluation of their ensuing viability to encapsulate the hydrophobic nonsteroidal anti‐inflammatory drug indomethacin (INDO). The copolymers are synthesized by ring‐opening polymerization, characterized by NMR and FTIR, and their critical aggregation concentration is determined by fluorescence. The NPs are prepared with and without INDO using different copolymer/solvent ratios and INDO/copolymer ratios. The hydrodynamic diameter and polydispersity of the NP suspensions are monitored by dynamic light scattering for 30 days. Their sizes vary between 208 and 338 nm, and some reach the micrometric range (19–73 μm). INDO‐free NPs are identified as spherical‐shaped by atomic force microscopy. Two formulations are tested in terms of encapsulation efficiency (EE = 43%–89%), and the drug crystallinity (DC = 7%–27%) which is determined by differential scanning calorimetry, indicating a reduction with respect to pristine INDO. The results suggest that the copolymers prepared herewith have potential to be applied as carriers for new drug delivery systems of class II drugs.

Alloy nanozyme-reinforced hyaluronic acid-based hydrogel with wound environment-responsive properties for synergistically accelerating infectious wound healing

The recovery of infectious wound tissues presents a significant global health challenge due to the impediments posed by the harsh healing microenvironment, which includes ongoing bacterial invasion, high oxidative stress, inflammatory response, and impaired angiogenesis. To overcome the above issues, we propose a composite hydrogel based on the multiple-crosslinked mechanism involving the covalent network of CC bonds within catechol and maleic-modified HA (CMHA), the self-assembly network of glycyrrhizic acid (GA), and the metal-polyphenol coordination induced by ZHMCe for accelerating infectious wound healing. The resulting CMHA/GA/ZHMCe hydrogels demonstrate enhanced mechanical, adhesive, antioxidative, and antibacterial properties. Importantly, the hydrogel system possesses wound environment-responsive properties that allow it to adapt to the specific therapeutic requirements of different stages by regulating various enzyme activities in the healing of infected wounds. Furthermore, the biocompatible CMHA/GA/ZHMCe shows the ability to promote cell migration and angiogenesis in vitro while reprogramming macrophages toward an anti-inflammatory phenotype due to the effective release of active ingredients. In vivo experiments confirm that the CMHA/GA/ZHMCe hydrogel significantly enhances infectious wound healing by accelerating re-epithelialization, promoting collagen deposition, regulating inflammation, and contributing to vascularization. These findings underscore the therapeutic potential of our hydrogel dressings for the treatment of bacterially infected cutaneous wound healing.

Plant-based delivery systems for controlled release of hydrophilic and hydrophobic active ingredients: Pea protein-alginate bigel beads

Oral delivery systems for nutrients and nutraceuticals are required for personalized nutrition applications. In some applications, these delivery systems need to encapsulate both hydrophilic and hydrophobic bioactive agents. In this study, bigel beads (2 mm) were prepared using pea protein (PP) and sodium alginate (SA) to form the hydrogel phase, and glyceryl monostearate and soybean oil to form the oleogel phase. The hydrogel phase was crosslinked by using Ca2+ ions to form electrostatic bridges between the alginate molecules. The bigel beads had an oil-in-water type structure consisting of an oleogel dispersed phase within a hydrogel continuous phase. These beads were used to encapsulate and control the release of model hydrophobic (curcumin) and hydrophilic (epigallocatechin gallate) nutraceuticals. The textural and microstructural characteristics of the bigel beads were evaluated by dynamic shear rheology, textural profile analysis, cryo-electron microscopy, and fluorescence confocal microscopy. As the concentration of SA increasing from 0.2 to 1.0%, the hardness of bigel beads increased from 306.75 g to 792.40 g. In vitro digestion experiments showed that most of the nutraceuticals were released in the small intestine, rather than the stomach. Nutraceutical release could be controlled by manipulating bead composition, with the extent of nutraceutical release decreasing with increasing alginate concentration. The bigel beads developed in this study could be used as easy-to-swallow carriers for the controlled release of hydrophilic and hydrophobic bioactive ingredients. These kinds of products may be especially useful for people with dysphagia.

A bio-degradable, triboelectric self-stimulated herbal transdermal therapeutic dressing for healing massive chronic wound

Homogeneous controlled release of active ingredients, avoiding secondary damage of dressing changes would be considerable advance for transcutaneous drug delivery treatment. Here, a bio-degradable, self-stimulated herbal transdermal therapeutic dressing (irritability) driven by multi-ball nimble-rolling triboelectric nanogenerator (mbnr-TENG) is proposed that provided a stable and adjustable triboelectric field for controlling drug release. The mbnr-TENG deliver a periodic triboelectric field of 140 V for herbal dressings by collecting human mechanical energy to enhance transdermal properties of total flavonoids and chlorogenic acid in ss-HTTD by 310% and 147%. Following a therapeutic cycle using ss-HTTD, the secretion of inflammatory factors decreased by 50.35%, and wound healing rate increased by 24.98%, then completely degraded after 10 days. As a new drug delivery system, this work holds great potential in healing massive chronic wound, ss-HTTD is advantageous in controlling drug release, enhancing the activity and the long-term stability of herbal medicines.

Fabrication of pH-responsive nanoparticles for co-delivery of fungicide and salicylic acid with synergistic antifungal activity

Stimuli-responsive co-delivery nanopesticides with different action mechanisms have received widespread attention due to the improved bioactivity, long effective duration, and reduced risks to the environment. Herein, fungicide tebuconazole (TEB) and plant immune inducer poly(salicylic acid) (PSA) co-assembled nanoparticles (TP NPs) are fabricated through non-covalent interactions without the use of any adjuvants. The results show that the obtained TP NPs have excellent physicochemical properties, displaying uniform morphology with an average particle size of 152 nm, low PDI (0.064), and high surface activity. The TP NPs exhibit acid-responsive behaviors, enabling the intelligent release of active ingredients in the specific acidic microenvironment caused by the invasion of plant pathogens. In vitro fungicidal activities of TP NPs are 1.9 and 1.6 times higher than TEB technical against Sclerotinia sclerotiorum and Fusarium graminearum respectively. Additionally, the stimuli-responsive co-delivery fungicidal nanosystem not only has a longer effective duration compared to both TEB technical and TP Mix but also significantly reduces the genetic toxicity of TEB to the plants. Therefore, this fungicide and plant immune inducer co-delivery nanosystem provides a novel strategy for development of multimode synergetic nanopesticide and sustainable plant disease management.

Photothermal controlled antibacterial Ta4C3Tx-AgNPs/nanocellulose bioplastic food packaging

Uncontrolled antibacterial, insufficient barrier and low strength are the bottlenecks of food packaging applications. Herein, Ta4C3Tx nanosheet as a template was used to prepare Ta4C3Tx immobilized silver nanoparticles (Ta4C3Tx-AgNPs), which was compounded with nanocellulose to obtain high-strength and high barrier controllable bactericidal nanocellulose-based bioplastic packaging (CTa-Ag). The results indicated that due to the hydrogen bonding between nanocellulose and Ta4C3Tx, the bridging effect of QCS (quaternized chitosan) and the filling of Ta4C3Tx-AgNPs, the CTa-Ag had tightly stacked microstructure, which endowed them with excellent mechanical properties (4.0 GPa), ultra-low oxygen permeability (0.009 cm3/m2·d·atm) and stable photothermal conversion efficiency. Importantly, the packaging exhibits the ability to control the release of antibacterial active ingredients. Moreover, the synergistic effects of controllable release of nano active factors, photothermal and photocatalysis in CTa-Ag gave it long-lasting antibacterial properties. This study brings new insights into the design and manufacture of multifunctional, controllable and long-lasting antibacterial bioplastic food packaging.

Unraveling the Therapeutic Prospects of Solid Lipid Nanoparticles for the Treatment of Parasitic Diseases

Parasites induce a spectrum of illnesses, ranging from mild to severe, often causing significant global outbreaks. Existing antiparasitic drugs exhibit toxicity and notable side effects. Nanocarriers offer a promising solution by mitigating these issues through reduced side effects, enhanced target delivery, and additionally regulated prolonged active ingredient release. Solid lipid nanoparticles (SLNs), a subset of lipid nanoparticles (LNPs), have gained prominence for their favorable attributes. SLNs present themselves as a feasible option among colloidal carriers, offering an optimal release rate, stability, and precise target delivery. Their potential to deliver natural antiparasitic products is particularly noteworthy. Recent advancements in utilizing nanoparticles to enhance SLN stability and loading capacity are also explored in this review. The narrative encompasses SLN development, preparation methods, characterization, and the incorporation of drugs for combating parasitic diseases, offering insights into the evolving landscape of antiprotozoal SLN-saturated medications

Co-Assembly of Cancer Drugs with Cyclo-HH Peptides: Insights from Simulations and Experiments.

Peptide-based nanomaterials can serve as promising drug delivery agents, facilitating the release of active pharmaceutical ingredients while reducing the risk of adverse reactions. We previously demonstrated that Cyclo-Histidine-Histidine (Cyclo-HH), co-assembled with cancer drug Epirubicin, zinc, and nitrate ions, can constitute an attractive drug delivery system, combining drug self-encapsulation, enhanced fluorescence, and the ability to transport the drug into cells. Here, we investigated both computationally and experimentally whether Cyclo-HH could co-assemble, in the presence of zinc and nitrate ions, with other cancer drugs with different physicochemical properties. Our studies indicated that Methotrexate, in addition to Epirubicin and its epimer Doxorubicin, and to a lesser extent Mitomycin-C and 5-Fluorouracil, have the capacity to co-assemble with Cyclo-HH, zinc, and nitrate ions, while a significantly lower propensity was observed for Cisplatin. Epirubicin, Doxorubicin, and Methorexate showed improved drug encapsulation and drug release properties, compared to Mitomycin-C and 5-Fluorouracil. We demonstrated the biocompatibility of the co-assembled systems, as well as their ability to intracellularly release the drugs, particularly for Epirubicin, Doxorubicin, and Methorexate. Zinc and nitrate were shown to be important in the co-assembly, coordinating with drugs and/or Cyclo-HH, thereby enabling drug-peptide as well as drug-drug interactions in successfully formed nanocarriers. The insights could be used in the future design of advanced cancer therapeutic systems with improved properties.

O-nitrobenzyl Caged Molecule Enables Photo-controlled Release of Thiabendazole.

Pesticides are essential in agricultural development. Controlled-release pesticides have attracted great attentions. Base on a principle of spatiotemporal selectivity, we extended the photoremovable protective group (PRPG) into agrochemical agents to achieve controllable release of active ingredients. Herein, we obtained NP-TBZ by covalently linking o-nitrobenzyl (NP) with thiabendazole (TBZ). Compound NP-TBZ can be controlled to release TBZ in dependent to light. The irradiated and unirradiated NP-TBZ showed significant differences on fungicidal activities both in vitro and in vivo. In addition, the irradiated NP-TBZ displayed similar antifungal activities to the directly-used TBZ, indicating a factual applicability in controllable release of TBZ. Furthermore, we explored the action mode and microcosmic variations by SEM analysis, and demonstrated that the irradiated NP-TBZ retained a same action mode with TBZ against mycelia growth.

Influence of Amitraz-Based Product Characteristics on Varroa Mite Population Control

The presence of the Varroa destructor mite requires the use of acaricide treatments for honeybee colonies. Amitraz is one of the most common acaricide-active ingredients used by beekeepers. Certain Varroa mite populations have developed resistance to amitraz, thereby leading to a loss in the efficacy of amitraz-based treatments. Two products, Apivar and Supatraz, were applied in the same apiary in France to evaluate their efficacy. Both treatments are amitraz-based but have different galenics. Thanks to field data, a dynamic model was used to simulate the actions of Apivar and Supatraz on the mite population. We considered two parameters to compare the products as follows: the daily mortality rate and the treatment duration. In the field, the percentage of the efficacy of the two products was not significantly different, but Supatraz kills mites faster and decreases 90% of the mite infestation in 28.4 days compared with 50.9 days when using Apivar. Through modeling, we showed the daily impact of the two different products on mite population. Supatraz has a higher daily mortality rate during the first two weeks than Apivar. Supatraz requires a lower efficacy (% of varroa mites killed during all the treatment) to stabilize the varroa mite population due to its faster release of active ingredients than Apivar, thereby needing a shorter period to achieve the same result. Depending on the model, Supatraz conserves effective efficacy when used against moderately resistant mites (with mite mortality being 40–70% at the LC90) but not against highly resistant mites (with mite mortality being &lt;40% at the LC90). These results show that the comparison of the efficacy of the two products with different characteristics (duration of treatment and daily mortality rate) should be analyzed with caution.