Rapid yet Controlled Synthesis of 2D Covalent Organic Framework Nanocapsules as High-Performance Photocatalytic Carriers.

Synthesis and assembly of two-dimensional (2D) polymeric materials present a tricky trade-off between the high reaction rate and precise morphology control. Here we report a nanoconfined synthesis of imine-based 2D covalent organic frameworks (COFs) at the interface of oil-in-water (O/W) emulsion droplets stabilized by cationic surfactants. Highly uniform nanocapsules (NCs) could be prepared without adding extra catalysts at room temperature in just 4.5 h at a yield of 86%. The NCs have tunable average diameters and shell thicknesses, depending on the monomer and surfactant types/concentrations. Their BET-specific surface areas are up to 139.0 m2/g, mainly contributed by narrowly-distributed mesopores at ~5.0 nm and micropores at 1.4 nm. The surfactant plays the role of a catalyst during the reaction and interestingly, it also regulates the formation of mesopores and their sizes. Both theoretical and experimental studies confirm that the reaction has been accelerated by two orders of magnitude at the microdroplet interface, compared to that without emulsification. The resulting NCs could be well dispersed in water, and they have been demonstrated to be highly efficient nanocatalysts in application of water-based hydrogen evolution. Such microdroplet interface-confined synthesis may facilitate the future development of 2D polymeric materials for more advanced applications.

Phytochemicals and Nanotechnology: A Powerful Combination against Breast Cancer.

Considerable advancements have been made in breast cancer therapeutics in the past few decades. However, the advent of chemo-resistance and adverse drug reactions coupled with tumor metastasis and recurrence posed a serious threat to combat this lethal disease. Novel anti-cancer agents, as well as new therapeutic strategies, are needed to complement conventional breast cancer therapies. The quest for developing novel anti-cancer drugs caused an upsurge in exploring and harnessing natural compounds, especially phytochemicals. Various research groups have explored and documented the anti-cancer potential of wide variety of phytochemical groups including flavonoids (curcumin, kaempferol, myricetin, quercetin, naringenin, apigenin, genistein epigallocatechin gallate), stilbenes (resveratrol), carotenoids (crocin, lycopene, lutein), and anthraquinone (Emodin). However, low chemical stability, poor water solubility, and short systemic half-life impede their clinical utility. The implication of nano-technological approaches to decode the pharmacokinetic challenges associated with phytochemical usage, as well as selective drug targeting, have markedly enhanced the pre-clinical anti-cancer activity, thus aiding in their clinical translation. This review documented the recent advances in utilizing phytochemicals for breast cancer prevention and lipidbased nanotechnological approaches for circumventing their pharmacokinetic concerns to enhance their systemic availability, cytotoxicity, and targeted delivery against breast cancer alone as well as in combination with conventional therapeutic agents.

Preparation and structural characterization of chitosan­sodium alginate nanocapsules and their effects on the stability and antioxidant activity of blueberry anthocyanins.

This study prepared a nanocapsule (NPs) from chitosan (CS) and sodium alginate (ALG) and used them to enhance the stability of blueberry anthocyanins (BA) The optimal NPs was obtained at pH value of 3.25, BA concentration of 0.5 mg/mL and mixing ratio of CS to ALG of 1:1 (W/W). Further, the formation of composite NPs was confirmed by a series of characterization methods. The CS-BA-ALG NPs appeared spherical, smooth, and evenly distributed when observed under an optical microscope and transmission Electron Microscope. The X-ray Diffractometer and Fourier Transform Infrared spectroscopy data proved that electrostatic interaction and hydrogen bonding are dominant forces to form NPs. Thermogravimetric analysis and differential scanning calorimetry results demonstrated that the CS-BA-ALG NPs system significantly improved the thermal stability of anthocyanins. In addition, it was also proved that CS-BA-ALG NPs showed high antioxidant capacity and protection capacity.

Ultrasound-Assisted Preparation of Hyaluronic Acid-Based Nanocapsules with an Oil Core.

Liquid-core nanocapsules (NCs) coated with amphiphilic hyaluronic acid (AmHA) have been proposed for the preparation of drug and food formulations. Herein, we focused on the use of ultrasound techniques to (i) optimize the polysaccharide chain length with respect to the properties of NCs stabilized with AmHAs and (ii) form oil-core nanocapsules with a coating composed of AmHAs. The results indicate that sonication is a convenient and effective method that allows for a controlled reduction in HA molecular weight. The initial (H-HA) and degraded (L-HA) polysaccharides were then reacted with dodecylamine to obtain hydrophobic HA derivatives (HA-C12s). Then, NCs were prepared based on HA-C12s using ultrasound-assisted emulsification of glyceryl triacetate oil. The nanocapsules coated with L-HA-C12 showed greater stability compared to the longer-chain polysaccharide. Molecular dynamics (MD) simulations revealed that HA-C12 readily adsorbs at the water-oil interphase, adopting a more compact conformation compared to that in the aqueous phase. The dodecyl groups are immersed in the oil droplet, while the main polysaccharide chain remaining in the aqueous phase forms hydrogen bonds or water bridges with the polar part of the triglycerides, thus increasing the stability of the NC. Our research underscores the usefulness of ultrasound technology in preparing suitable formulations of bioactive substances.

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.

Evaluation of the In-Vitro Effects of Albendazole, Mebendazole, and Praziquantel Nanocapsules against Protoscolices of Hydatid Cyst.

Cystic echinococcosis still remains a serious health and economic problem worldwide. The etiologic agent is Echinococcus granulosus sensu lato, giving origin to a fluid-filled cystic lesion. Therapy faces several challenges. Nanodrugs have shown promise as chemotherapeutics against hydatid cysts. The present study evaluated a highly safe lipid nano-polymeric capsule for its superior efficacy and ability to overcome drug resistance. Nanocapsule drugs were formulated into six groups: Albendazole, mebendazole, praziquantel, albendazole + mebendazole, albendazole + praziquantel, and praziquantel + mebendazole. The protoscolicidal effects of these six groups were assessed at 10, 60, and 120 min in three concentrations (1, 0.5, and 0.25 mg/mL). Drug formulations were evaluated via zeta potential, droplet size, solubility, particle size analyzer (PSA), and scanning electron microscopy. According to the PSA results, the mean size of the albendazole nanocapsules was 193.01 nm, mebendazole was 170.40 nm, and praziquantel was 180.44 nm. Albendazole + mebendazole showed the greatest protoscolicidal activity at a concentration of 1 mg/mL after 120 min. In contrast, each drug's 0.25 mg/mL single-dose times showed the least protoscolicidal activity after 120 min. With the right application of nanotechnology, it is possible to produce safe and effective drugs, such as the polymeric combination of albendazole and mebendazole, which has promising implications.

Lipid-Based Nanocarriers: Bridging Diagnosis and Cancer Therapy.

Theranostics is a growing field that matches diagnostics and therapeutics. In this approach, drugs and techniques are uniquely coupled to diagnose and treat medical conditions synergically or sequentially. By integrating diagnostic and treatment functions in a single platform, the aim of theranostics is to improve precision medicine by tailoring treatments based on real-time information. In this context, lipid-based nanocarriers have attracted great scientific attention due to their biodegradability, biocompatibility, and targeting capabilities. The present review highlights the latest research advances in the field of lipid-based nanocarriers for cancer theranostics, exploring several ways of improving in vivo performance and addressing associated challenges. These nanocarriers have significant potential to create new perspectives in the field of nanomedicine and offer promise for a significant step towards more personalized and precise medicine, reducing side effects and improving clinical outcomes for patients. This review also presents the actual barriers to and the possible challenges in the use of nanoparticles in the theranostic field, such as regulatory hurdles, high costs, and technological integration. Addressing these issues through a multidisciplinary and collaborative approach among institutions could be essential for advancing lipid nanocarriers in the theranostic field. Such collaborations can leverage diverse expertise and resources, fostering innovation and overcoming the complex challenges associated with clinical translation. This approach will be crucial for realizing the full potential of lipid-based nanocarriers in precision medicine.

Peptide-Coated Polycaprolactone-Benzalkonium Chloride Nanocapsules for Targeted Drug Delivery to the Pancreatic ß-Cell.

Targeting current therapies to treat or prevent the loss of pancreatic islet ß-cells in Type 1 Diabetes (T1D) may provide improved efficacy and reduce off-target effects. Current efforts to target the ß-cell are limited by a lack of ß-cell-specific targets and the inability to test multiple targeting moieties with the same delivery vehicle. Here, we fabricate a tailorable polycaprolactone nanocapsule (NC) in which multiple different targeting peptides can be interchangeably attached for ß-cell-specific delivery. Incorporation of a cationic surfactant in the NC shell allows for the attachment of Exendin-4 and an antibody for ectonucleoside triphosphate diphosphohydrolase 3 (ENTPD3) for ß-cell-specific targeting. The average NC size ranges from 250 to 300 nm with a polydispersity index under 0.2. The NCs are nontoxic, stable in media culture, and can be lyophilized and reconstituted. NCs coated with a targeting peptide were taken up by human cadaveric islet ß-cells and human stem cell-derived ß-like cells (sBC) in vitro with a high level of specificity. Furthermore, NCs successfully delivered both hydrophobic and hydrophilic cargo to human ß-cells. Additionally, Exendin-4-coated NCs were stable and targeted the mouse pancreatic islet ß-cell in vivo. Overall, our tailorable NCs have the potential to improve cell-targeted drug delivery and can be utilized as a screening platform to test the efficacy of cell-targeting peptides.

Polyvinyl alcohol-chitosan-polyethylene glycol-glycerol incorporated with Peganum harmala loaded in lipid nanocapsules as an elastic nanocomposite surgical sealant to control bleeding.

Uncontrolled hemorrhage remains a critical threat in trauma and surgery. This study developed a novel hemostatic composite by encapsulating Peganum harmala L. seed extract (PH) with known hemostatic properties into lipid nanocapsules (PH-LNCs) and then embedding them within a polyvinyl alcohol-chitosan-polyethylene glycol-glycerol (PVA-CS-PEG-G) matrix. The composite was physically crosslinked via the dual processes of freezing-thawing and thermal crosslinking and exhibited robust mechanical properties reaching 0.434 ± 0.014 MPa and elasticity of 40.685 % ± 4.04. It also demonstrated excellent biocompatibility, surface morphology, physical stability, and ex-vivo skin deposition/permeation were assessed. The characterization of PH-LNCs revealed optimal PH-LNC formation and successful integration into the composite with particle size, zeta potential, and PDI were approximately 45.45 ± 24 nm, -16.3 ± 1.4 mV, and 0.374 ± 0.1, respectively. In vitro studies highlighted enhanced blood clotting and platelet adhesion, while in vivo experiments confirmed superior hemostatic efficacy in a mouse tail amputation model. The composite's soft texture, conformability, and mechanical strength make it a promising candidate for effective traumatic wound management.

The influence of amphiphilic quaternary ammonium palmitoyl glycol chitosan (GCPQ) polymer composition on oil-loaded nanocapsule architecture.

HYPOTHESIS: Predicting the exact nature of the self-assembly of amphiphilic molecules into supramolecular structures is of utmost importance for a variety of applications, but this is a challenge for nanotechnology. The amphiphilic drug delivery polymer-N-palmitoyl-N-monomethyl-N,N-dimethyl-N,N,N-trimethyl-6-O-glycolchitosan (GCPQ) self-assembles in aqueous media to form nanoparticles. EXPERIMENT: This work aimed to develop a systematic predictive mathematical model on the eventual nature of oil-loaded GCPQ-nanoparticles and to determine the main independent variables that affect their nanoarchitecture following self-assembly. GCPQ polymers were produced with varying degree of palmitoylation (DP, 5.7-23.8 mol%), degree of quaternization (DQ, 7.2-22.7 mol%), and molecular weight (MW, 11.2-44.2 kDa) and their critical hydrophilic-lipophilic balance (cHLB) optimized to produce oil-loaded nanocapsules. FINDINGS: Non-linear mathematical models (Particle size (nm) = 466.05 - 5.64DP - 6.52DQ + 0.13DQ2 - 0.03 MW2 - 14.48cHLB + 0.48cHLB2) were derived to predict the nanoparticle sizes (R2 = 0.998, R2adj = 0.995). Smaller nanoparticle sizes (148-157 nm) were obtained at high DP, DQ, and cHLB values, in which DP was the main independent variable responsible for nanoparticle size. Single or multiple-oil cores with small particles stabilizing polymer shells could be observed depending on the oil volume. Nanoparticle architectures, especially the nature of the oil-core(s), were driven by the DP, DQ, cHLB, and oil concentration. Here, we have developed a predictive model that may be applied to understand the nanoarchitecture of oil-loaded GCPQ-nanoparticles.

Diazepam nanocapsules as an alternative for sleep induction: Development study and toxicity assessment.

Diazepam (DZP) is a sedative medication prescribed to treat anxiety and as a sleep inducer, although its residual effects are unfavorable to patients. Nanotechnology represents a tool to improve the pharmacological characteristics of drugs, reducing their side effects. This study aimed to develop and characterize DZP nanocapsules and to evaluate their toxicity in alternative models and the hypnotic-sedative effect in mice. Nanocapsules were prepared by the nanoprecipitation method and properly characterized. Long-term and accelerated stability studies were performed. The in vitro release profile was determined by diffusion in Franz cells. The safety of the formulation was evaluated in the Caenorhabditis elegans (C. elegans) and the oral acute toxicity in mice. Pharmacological evaluation was performed using thiopental-induced sleeping time. DZP was successfully incorporated into Poly-(ɛ-caprolactone) (PCL) nanocapsules, with high entrapment efficiency. The nanocapsule did not affect the development or survival of C. elegans, different from the free drug, which affected the nematode development at the higher tested dose. No signs of toxicity, nor body mass or feed consumption changes were observed during the 14 days evaluated. Finally, this innovative formulation carrying DZP can produce a hypnotic-effect at a reduced dose compared to the free drug, with no toxicity in alternative models.

Comparative In Vitro Study between Biocompatible Chitosan-Based Magnetic Nanocapsules and Liposome Formulations with Potential Application in Anti-Inflammatory Therapy.

This study describes the comparison between the interaction of a series of peptide-functionalized chitosan-based nanocapsules and liposomes with two cell lines, i.e., mouse macrophages RAW 264.7 and human endothelial cells EA.hy926. Both types of nanocarriers are loaded with magnetic nanoparticles and designed for anti-inflammatory therapy. The choice of these magnetic nanostructures is argued based on their advantages in terms of size, morphology, chemical composition, and the multiple possibilities of modifying their surface. Moreover, active targeting might be ensured by using an external magnetic field. To explore the impact of chitosan-based nanocapsules and liposomes on cell cytophysiology, the cell viability, using the MTT assay, and cell morphology were investigated. The results revealed low to moderate cytotoxicity of free nanocapsules and significant cytotoxicity induced by chitosan-coated liposomes loaded with dexamethasone, confirming its release from the delivery system. Thus, after 48 h of treatment with nanocapsules, the viability of RAW 264.7 cells varied between 88.18% (OCNPM-1I, 3.125 µg/mL) and 76.37% (OCNPM-1, 25 µg/mL). In the same conditions, EA.hy926 cell viability was between 99.91% (OCNPM-3, 3.125 µg/mL) and 75.15% (OCNPM-3, 25 µg/mL) at the highest dose (25 µg/mL), the values being comparable for both cell lines. Referring to the cell reactivity after dexamethasone-loaded liposome application, the lowest viability of RAW 264.7 cells was 41.25% (CLDM5CP-1, 25 µg/mL) and 58.20% (CLDMM2CP-1 1.25 µg/mL) in the endothelial cell line, proving a selective character of action of nanocarriers. The cell morphology test, performed to support and confirm the results obtained by the MTT test, revealed a differentiated response for the two types of nano-carriers. As expected, an intense cytotoxic effect in the case of dexamethasone-loaded liposomes and a lack of cytotoxicity for drug-free nanocapsules were noticed. Therefore, our study demonstrated the biocompatible feature of the studied nanocarriers, which highlights them for future research as potential drug delivery systems for pharmacological applications, including anti-inflammatory therapy.

Intravenous delivery of furosemide using lipid-based versus polymer-based nanocapsules: in vitro and in vivo studies.

OBJECTIVES: Furosemide (FSM), a potent loop diuretic, is used to treat edema due to hypertension, congestive heart failure, and liver and renal failures. FSM applications are limited by its low bioavailability. Our aim is to use different nanoencapsulation strategies to control the release of FSM and enhance its pharmacokinetic properties. METHODS: Two types of FSM-loaded nanocapsules, namely FSM-loaded lipid nanocapsules (LNCs) and polymeric nanocapsules (PNCs), were developed, physicochemically characterized, and subjected to pharmacokinetic and pharmacodynamic studies. Lipid nanocapsules were prepared by the simple phase inversion method using LabrafacTM lipid, while the polymeric nanocapsules were prepared by nanoprecipitation method using polycaprolactone polymer. RESULTS: Transmission electron microscopy ascertains spherical structures, corroborating the nanometric diameter of both types of nanocapsules. The particle size of the optimized FSM-loaded LNCs and FSM-loaded PNCs was 32.19 ± 0.72 nm and 230.7 ± 5.13 nm, respectively. The percent entrapment efficiency was 63.56 ± 1.40% of FSM for the optimized PNCs. The in vitro release study indicated prolonged drug release compared to drug solutions. The two loaded nanocapsules systems succeeded in enhancing the pharmacokinetic parameters in comparison to the marketed FSM solution with superior diuretic activity (p < 0.05). The results of the stability study and the terminal sterilization by autoclave indicated the superiority of LNCs over PNCs in maintaining the physical parameters under storage conditions and the drastic conditions of sterilization. CONCLUSIONS: LNCs and PNCs are considered promising nanosysems for improving the diuretic effect of FSM.

Stereoselective Interactions of Chiral Polyurea Nanocapsules with Albumins.

Exploiting the chirality of nanometric structures to modulate biological systems is an emerging and compelling area of research. In this study, we reveal that chiral polyurea nanocapsules exhibit significant stereoselective interactions with albumins from various sources despite their nearly neutral surface potential. Moreover, these interactions can be modulated by altering the nanocapsule surface composition, offering new opportunities to impact their distribution and, if used as a drug delivery system, the pharmacokinetics of the drug. Notably, these interactions promote preferential cellular internalization of only one chiral configuration. We synthesized chiral polyurea nanocapsules with reproducible sizes via interfacial polymerization between toluene 2,4-diisocyanate and d- or l-lysine enantiomers on a volatile oil-in-water emulsion interface, followed by solvent evaporation. Further synthesis optimization reduced the capsule size to a range compatible with in vivo administration, and capsules with alternating chiral patterns were also produced. The stereoselective interactions with albumins were assessed through capsule size changes, fluorescence quenching, and surface charge measurements. Biocompatibility, stability, and cellular internalization were evaluated. Additionally, scanning transmission electron and atomic force microscopy were carried out to assess the capsule shape, surface composition, and morphology. We discovered that d-nanocapsules exhibited 2.1-2.6 times greater albumin adsorption compared with their l-counterparts. This difference is attributed to the distinct morphology of d-nanocapsules, characterized by a more concave shape, central depression, and rougher surface. The extent of adsorption could be finely tuned by adjusting the d- and l-lysine monomer ratios during synthesis. Both chiral configurations demonstrated biocompatibility and stability with d-nanocapsules showing a 2.5-fold increase in cellular internalization.

Dual combination of resveratrol and pterostilbene aqueous core nanocapsules for integrated prostate cancer targeting.

Aim: Development and evaluation of aqueous core nanocapsules (ACNs) of BCS-II-class drug like resveratrol (RSV) and pterostilbene (PTE) for prostate cancer.Materials & methods: Identify synergistic effects of molar ratios of RSV and PTE against PC-3 cell. Selected ratio of drugs was added to ACNs by double-emulsification-method using Box-Behnken design. Further, assessed for physicochemical characterization, release kinetics, compatibility, in vitro cytotoxicity, in vivo pharmacokinetic and biodistribution studies.Results: Selected 1:1 ratio of RSV and PTE had greatest synergy potential have smaller particle-size (128.1 ± 3.21 nm), zeta-potential (-22.12 ± 0.2 mV), 0.53 PDI, improved encapsulation (87% for RSV, 72% for PTE), stable, no systemic toxicity, high biodistributed/accumulated in prostate cells.Conclusion: ACNs exhibited high t1/2 (12.42 ± 1.92 hs) and 8.20 ± 8.21 hs Mean Residence Time and lower clearance, proving the high effectiveness for prostate cancer.

[Box: see text].

Extracellular Vesicle-Inspired Minimalist Flexible Nanocapsules Assembled with Whole Active Ingredients for Highly Efficient Enhancement of DC-Mediated Tumor Immunotherapy.

The development of nanovaccines capable of eliciting tumor-specific immune responses holds significant promise for tumor immunotherapy. However, many nanovaccine designs rely heavily on incorporating multiple adjuvants and carriers, increasing the biological hazards associated with these additional components. Here, this work introduces novel flexible nanocapsules (OVAnano) designed to mimic extracellular vesicles, primarily using the ovalbumin antigen and minimal polyethylenimine adjuvant components. These results show that the biomimetic flexible structure of OVAnano facilitates enhanced antigen uptake by dendritic cells (DCs), leading to efficient antigen and adjuvant release into the cytosol via endosomal escape, and ultimately, successful antigen cross-presentation by DCs. Furthermore, OVAnano modulates the intracellular nuclear factor kappa-B (NF-κB) signaling pathway, promoting DC maturation. The highly purified antigens in OVAnano demonstrate remarkable antigen-specific immunogenicity, triggering strong antitumor immune responses mediated by DCs. Therapeutic tumor vaccination studies have also shown that OVAnano administration effectively suppresses tumor growth in mice by inducing immune responses from CD8+ and CD4+ T cells targeting specific antigens, reducing immunosuppression by regulatory T cells, and boosting the populations of effector memory T cells. These findings underscore that the simple yet potent strategy of employing minimal flexible nanocapsules markedly enhances DC-mediated antitumor immunotherapy, offering promising avenues for future clinical applications.

Lipidic Nanosystem as State-of-the-Art Nanovehicle for Biomedical Applications.

Lipids have tremendously transformed the biomedical field, especially in the last few decades. Nanosystems, especially Lipid nanocapsules (LNCs), have emerged as the most demanding nanovehicle systems for delivering drugs, genes, and other diagnostic agents. Unique attributes and characteristic features such as higher encapsulation efficiency, stealth effect, ability to solubilize a wide range of drugs, capability to inhibit P-gp efflux pumps, and higher stability play a vital role in engaging this nanosystem. LNCs are a lipid-based nano-drug delivery method that combines the most significant traits of liposomes with polymeric nanoparticles. Structurally, LNCs have an oily core consisting of medium and long triglycerides and an aqueous phase encased in an amphiphilic shell. This manuscript crosstalks LNCs for various biomedical applications. A detailed elaboration of the structural composition, methods of preparation, and quality control aspects has also been attained, with particular emphasis on application approaches, ongoing challenges, and their possible resolution. The manuscript also expounds the preclinical data and discusses the patents atlas of LNCs to assist biomedical scientists working in this area and foster additional research. Supplementary Information: The online version contains supplementary material available at 10.1007/s12088-024-01298-3.

Spontaneous Fusion of Core-Shell Nanocapsules with Oil Cores and Oppositely Charged Polysaccharide Shells.

Polymer nanocapsules with hydrophobic cores are promising candidates for nanoreactors to carry out (bio)chemical reactions mimicking the performance of natural cellular systems. Their architecture allows reagents to be encapsulated in the cores enabling reactions to proceed in confined environments in a controlled, and efficient manner. Polysaccharide-shell oil-core nanocapsules are proposed here as facile mergeable nanoreactors. Spontaneous fusion of oppositely charged polysaccharide capsules is demonstrated for the first time. Such capsules are formed and easily loaded with reagents by nanoemulsification of an aqueous solution of hydrophobically modified polysaccharides (chitosan, hyaluronate) and oleic acid with dissolved desired hydrophobic compounds. Efficient fusion of the formed nanocapsules dispersed in an aqueous medium at optimized conditions (pH, ionic strength) is followed using fluorescence microscopy by labeling both their cores and shells with fluorescent dyes. As a proof of concept, a model fluorogenic synthesis is also realized by fusing the capsules containing separated reagents and the catalyst. The nanocapsules and fusion process developed here establish a platform for realization of versatile reactions in a confined environment including model studies on biologically relevant processes taking place in natural systems.

Curcumin Nanocapsules based on carbon dots for photodynamic sterilization towards Listeria monocytogenes and Staphylococcus aureus.

Curcumin (Cur) as a natural food additive and photosensitizer has been widely applied on photodynamic sterilization and preservation for food, but the poor aqueous solubility and light stability restrict its extensive application. In this study, we report a Cur nanocapsules (Cur-CDs) made by carbon dots (CDs). Attributing to the hydrogen bonds formed between Cur and CDs, Cur-CDs exhibits excellent Cur aqueous solubility each to 9286.98 ng/mL (enhanced by 246.27 times) and light stability (enhanced by 1.51 times). The photogenerated electron transmission from Cur to CDs in addition resulted in >1.23 and 1.60 times generation of •O2- and •OH, compared to that of bare Cur. Accordingly, 5.73 × 103 CFU L. monocytogenes, and 5.43 × 103 CFU S. aureus were killed by 0.06 mg/mL Cur-CDs within 20 mins of blue light, showing the promising potential in the development and application of safe and environmentally friendly non-thermal sterilization technology based on Cur-CDs.

Bioactive baicalin rhamno-nanocapsules as phytotherapeutic platform for treatment of acute myeloid leukemia.

Leukemia, particularly acute myeloid leukemia (AML) is considered a serious health condition with high prevalence among adults. Accordingly, finding new therapeutic modalities for AML is urgently needed. This study aimed to develop a biocompatible nanoformulation for effective oral delivery of the phytomedicine; baicalin (BAC) for AML treatment. Lipid nanocapsules (LNCs) based on bioactive natural components; rhamnolipids (RL) as a biosurfactant and the essential oil linalool (LIN), were prepared using a simple phase-inversion method. The elaborated BAC-LNCs displayed 61.1 nm diameter and 0.2 PDI. Entrapment efficiency exceeded 98 % with slow drug release and high storage-stability over 3 months. Moreover, BAC-LNCs enhanced BAC oral bioavailability by 2.3-fold compared to BAC suspension in rats with higher half-life and mean residence-time. In vitro anticancer studies confirmed the prominent cytotoxicity of BAC-LNCs on the human leukemia monocytes (THP-1). BAC-LNCs exerted higher cellular association, apoptotic capability and antiproliferative activity with DNA synthesis-phase arrest. Finally, a mechanistic study performed through evaluation of various tumor biomarkers revealed that BAC-LNCs downregulated the angiogenic marker, vascular endothelial growth-factor (VEGF) and the anti-apoptotic marker (BCl-2) and upregulated the apoptotic markers (Caspase-3 and BAX). The improved efficacy of BAC bioactive-LNCs substantially recommends their pharmacotherapeutic potential as a promising nanoplatform for AML treatment.