High Loading Capacity Research Articles

Effect of poly(styrene sulfonate) treatment on the structural evolution and sonodynamic performance of PCN-224 nanoparticles

Porphyrin based nanosize metal-organic frameworks (MOFs), such as PCN-224, are promising sonosensitizers for the sonodynamic therapy (SDT) due to their high porphyrin loading capacity and excellent water dispersity. However, the limited pore size of PCN-224 and the close proximity between porphyrins may impede the generation and diffusion of reactive oxygen species (ROS). In this study, a facile ligand exchange method is developed to regulate the structure and the content of tetrakis(carboxyphenyl)-porphyrin (TCPP) in the treated PCN-224 nanoparticles (NPs). Through simple incubation of PCN-224 NPs in poly(styrene sulfonate) (PSS) solution, the ligand exchange between PSS and TCPP happens and a part of TCPP is released to the solution. The ligand exchange results in the transformation of the crystalline structure to amorphous structure of PCN-224, the formation of larger pores and the decrease of surface area. The increased pore size can enhance the generation ability of 1O2 due to the favorable diffusion of substances. This effect can compensate the decreased amount of TCPP in the NPs until the incubation time reaches 8 h in a 2 mg/mL PSS. After balancing the two factors of structure change and TCPP content in the treated PCN-224 NPs, one can achieve their optimal SDT performance. Through a ligand exchange process, this work provides a facile method to regulate the structure of MOFs-based sonosensitizers and their SDT performance.

Enhancing amorphous carbon wear resistance at high contact stresses through Ag incorporation

High load capacity is desirable in various industrial applications, such as gudgeon pins, cam followers, gears and bearings. Amorphous carbon (a-C) coatings, known for their minimal friction and low wear rates, have found extensive application in automotive components. However, the a-C films often fail at high contact stress (>2 GPa). Extensive efforts have been devoted for the application of a-C under high contact stress, and a few groups can prevent the sudden failure of a-C in high load condition up to now. Nevertheless, the wear rate is still high, which is in the range of ∼10−7 mm3/Nm, at least ten times greater than that of films under low stresses (<2 GPa). To tackle this issue, Ag-C supra-nano-dual-phase composite (SNDP) was fabricated using magnetron sputtering (‘supra-nano-dual-phase’ means the diameter of each phase is smaller than 10 nm). Various methods were employed to examine the structural features, mechanical attributes, and tribological performance of Ag-C SNDP. The research revealed that Ag nanocrystals, ranging in size from 2 to 4 nm, were uniformly incorporated within the amorphous carbon matrix. The Ag-C SNDP film with 4.0 at.% Ag shows an order of magnitude lower than amorphous carbon (a-C) at wear rate. It also pushes the load-bearing capacity as high as 4.0 GPa, which has rarely been reported before. The superior tribological behavior of Ag-C SNDP composite can be explained in three factors: (1) the ‘supra-nanometer-sized dual-phase’ structure provides adequate strength; (2) the surface graphitization within several nanometers from the surface enables low friction coefficient and prevents sudden failure; (3) incorporating Ag into the films resulted in a reduction in residual stress and an increase in film toughness.

Room temperature synthesis of β-cyclodextrin functionalized graphene oxide decorated MIL-100 (Fe): A sustainable drug cargo for anticancer drug delivery

Chemotherapy remains an extensively used cancer treatment method with the accessibility of various chemotherapeutic agents. However, its effectiveness is limited by the inability to distinguish between precipitously propagating normal cells and cancer cells, leading to severe side effects. Targeted drug delivery systems (DDS), utilizing advanced nanomaterials such as nanocarriers and natural/green chemotherapeutic agents like caffeic acid (CA), offer a promising solution to overcome these challenges and improve the sustainable consumption of chemotherapeutic agents. The current study presents a self-assembled, sustainable, and straightforward method for synthesizing CA nanocarriers using β-cyclodextrin conjugated graphene oxide (β-CD-GO)-functionalized Fe-based metal-organic frameworks ((β-CD-GO@MIL-100(Fe)), herein denoted as BGw-MF, through a hydrofluoric acid (HF)-free approach. The structural, functional, and morphological attributes of obtained nanocarriers were inspected through respective characterization methods. Furthermore, the CA loading efficiency (LE) was evaluated for the obtained BGw-MF nanocarriers with fixed drug concentrations, varied CA: nanocarrier ratio (w/w), and pH of the media. The results showed that BG0.5-MF had the highest LE, reaching 56.44 ± 2.25% for a 2 w/w ratio of CA in an alkaline environment (pH 9). Moreover, the CA release pattern of BG0.5-MF-CA was more controlled, with nearly 57.07 ± 2.01% release at pH 5 and 48.04 ± 1.44% at pH 7.4 over 8 days, which might enhance the therapeutic efficiency with higher release at tumor sites. The kinetics studies were subsequently conducted to evaluate the CA release characteristics of the BG0.5-MF nanocarrier. The nanocarrier followed a pseudo-second-order kinetic model for CA release at pH 5. In-vitro cytotoxicity tests of BG0.5-MF-CA revealed significant toxicity to lung cancer cells (A549) and cell viability of 68 ± 2 %, with no evident toxicity induced to normal cells (HEK293) at 400 μg/mL dose. The findings of the present work emphasized the potential of BGw-MF nanocarriers obtained at room temperature for CA-based anticancer DDS. The high loading capacity of the nanocarriers combined with the sustainable release of the drug from the nanocomposite makes it suitable for drug delivery. Moreover, the cytotoxicity of the nanocomposite towards cancer cells establishes BG0.5-MF as a promising nanocarrier for anticancer DDS.

Construction, characterization and bioactivity evaluation of curcumin nanocrystals with extremely high solubility and dispersion prepared by ultrasound-assisted method

Curcumin (Cur) as a natural pigment and biological component, can be widely used in food and beverages. However, the water insolubility of Cur significantly limits its applications. In this study, we prepared a series of nanocrystals via ultrasound-assisted method to improve the solubility and availability of Cur. The results showed artemisia sphaerocephala krasch polysaccharide (ASKP), gum arabic (GA) and wheat protein (WP) were outstanding stabilizers for nanocryatals except traditional agent, poloxamer 188 (F68). The obtained curcumin nanocrystals (Cur-NC) displayed a rod-shaped, crystal- and nanosized structure, and extremely high loading capacity (more over 80 %, w/w). Compared with raw powder, Cur-NC greatly improved the water solubility and dispersibility, and the slow and complete release of Cur of Cur-NC also endowed them excellent antioxidant capacities even at 10 μg/mL. Importantly, as functional factor additive in beverages (e.g. water and emulsion), Cur-NC could increase the content of Cur to at least 600 μg/mL and retain a good stability. Overall, we provided an effective improvement method for the liposoluble active molecules (e.g. Cur) based on the nanocrystals, which not only tremendously enhanced its water solubility, but also strengthened its bioactivity. Notably, our findings broadened the application of water-insoluble compounds.

Caffeic Acid Phenethyl Ester Encapsulated in Self-Assemble Rice Peptides Nanoparticles: Storage Stability, In Vitro Release, and Their Interaction Mechanisms.

Caffeic acid phenethyl ester (CAPE) is an important active component of propolis with many bioactivities. However, its efficiency and practical application are restricted due to its poor aqueous solubility and storage stability. In this study, a nanocarrier was fabricated to encapsulate CAPE using self-assembled rice peptides obtained by controllable enzymolysis. The physicochemical properties, encapsulation efficiency, and loading capacity of rice peptides nanoparticles (RPNs) were characterized. The storage stability, in vitro release, and interaction mechanisms between CAPE and RPNs were investigated. The results showed that RPNs, mainly assembled by disulfide bonds and hydrogen bonds, possessed an effective diameter of around 210 nm and a high encapsulation efficiency (77.77%) and loading capacity (3.89%). Importantly, the water solubility of CAPE was increased by 45 times after RPNs encapsulation. Moreover, RPNs encapsulation also significantly increased CAPE stability, about 1.4-fold higher than that of unencapsulated CAPE after 18-day storage. An in vitro release study demonstrated that RPNs could delay the release of CAPE, implying a better CAPE protection against extreme environments during digestion. Hydrogen bond and van der Waals force are the predominant interaction forces between RPNs and CAPE. Therefore, the newly developed nanoparticle is a potential delivery system that could effectively improve the aqueous solubility and stability of CAPE.

A Ferroptosis‐Inducing Arsenene‐Iridium Nanoplatform for Synergistic Immunotherapy in Pancreatic Cancer

AbstractDue to multidrug resistance and the high risk of recurrence, effective and less toxic alternative pancreatic cancer treatments are urgently needed. Pancreatic cancer cells are highly resistant to apoptosis but sensitive to ferroptosis. In this study, an innovative nanoplatform (AsIr@PDA) was developed by electrostatic adsorption of a cationic iridium complex (IrFN) onto two‐dimensional (2D) arsenene nanosheets. This nanoplatform exhibits superior ferroptosis‐inducing effects with high drug loading capacity and, importantly, excellent anti‐cancer immune activation function, leading to efficient elimination of pancreatic tumors with no observable side effects. Interestingly, AsIr@PDA significantly prevents the recurrence of pancreatic cancer in vivo when compared with a cisplatin‐loaded nanoplatform. This designed nanoplatform demonstrated superior therapeutic efficacy by synergistic ferroptosis‐induced chemotherapy with immunotherapy via an all‐in‐one strategy, providing new insights for future pancreatic cancer therapy.

A Ferroptosis-Inducing Arsenene-Iridium Nanoplatform for Synergistic Immunotherapy in Pancreatic Cancer.

Due to multidrug resistance and the high risk of recurrence, effective and less toxic alternative pancreatic cancer treatments are urgently needed. Pancreatic cancer cells are highly resistant to apoptosis but sensitive to ferroptosis. In this study, an innovative nanoplatform (AsIr@PDA) was developed by electrostatic adsorption of a cationic iridium complex (IrFN) onto two-dimensional (2D) arsenene nanosheets. This nanoplatform exhibits superior ferroptosis-inducing effects with high drug loading capacity and, importantly, excellent anti-cancer immune activation function, leading to efficient elimination of pancreatic tumors with no observable side effects. Interestingly, AsIr@PDA significantly prevents the recurrence of pancreatic cancer in vivo when compared with a cisplatin-loaded nanoplatform. This designed nanoplatform demonstrated superior therapeutic efficacy by synergistic ferroptosis-induced chemotherapy with immunotherapy via an all-in-one strategy, providing new insights for future pancreatic cancer therapy.

Formulation development of methotrexate lipid-based nanogel for treatment of skin cancer

Skin cancer (SC) represents a prevalent malignancy worldwide, characterized by its high drug resistance and limited therapeutic efficacy with conventional treatments. Nanoparticles have emerged as promising vehicles for targeted drug delivery, aiming to overcome these challenges and enhance treatment outcomes. The solid lipid nanocarriers (SLNs) provide improved drug absorption, encapsulation, and controlled release. These SLNs can be customized to meet unique needs, allowing for enhanced targeting, distribution to specific sites, and profiles of sustained release. This study was focused on the development and optimization of methotrexate loaded solid lipid nanoparticles (MTX-SLNs) for improving the drug delivery to the skin cancer therapy. The optimized MTX-SLNs exhibited a particle size of 203 nm, a zeta potential of −8.93 mV, entrapment efficiency of 87%, and drug loading of 62.92%. Subsequently, the optimized MTX-SLNs was incorporated into a gel system containing 1% Carbopol 934, which was further underwent comprehensive characterization, encompassing analysis of rheological properties, texture profile analysis, extrudability and spreadability, as well as uniformity of content. Notably, the dermatokinetic and confocal microscopy evaluations revealed excellent uptake and deposition of MTX-SLNs within the epidermal and dermal layers of the skin. These observations were complemented by the computation of the area under the curve (AUC0–8hr), which demonstrated values of 245.035 and 702.59 for the epidermal and dermal layers, respectively. These findings underscore the tremendous potential of our MTX-SLNs gel formulation as a promising candidate for skin cancer treatment compared to the conventional topical gel therapies, exhibiting superior topical pharmacokinetics, nanometric size, high drug loading capacity, and enhanced efficacy.

The Effect of Polymer-Solvent Interaction on the Swelling of Polymer Matrix Tablets: A Magnetic Resonance Microscopy Study Complemented by Bond Fluctuation Model Simulations.

Polymer matrix tablets are an important drug-delivery system widely used for oral drug administration. Understanding the tablet hydration process, both experimentally and theoretically, is, thus, very important for the development of drug delivery systems that exhibit high drug loading capacity and controlled release potential. In this study, we used magnetic resonance microscopy (MRM) to nondestructively and dynamically analyze the water hydration process of xanthan-based tablets. The swelling process was characterized by well-resolved fronts of erosion, swelling, and penetration. The experimental results were complemented by numerical simulations of the polymer matrix hydration process. In the simulations, the polymer tablet matrix was modeled as an assembly of interacting chains with embedded drug particles, while its hydration process was mediated by interaction with solvent particles. The swelling dynamics were modeled within a Monte Carlo-based bond fluctuation model (BFM) that elegantly accounted for steric and nearest-neighbor interactions. This study provides an efficient experimental-theoretical approach for the study of polymer matrix swelling processes.

Improved bioavailability and antioxidation of β-carotene-loaded biopolymeric nanoparticles stabilized by glycosylated oat protein isolate

The limited bioavailability of β-carotene hinders its potential application in functional foods, despite its excellent antioxidant properties. Protein-based nanoparticles have been widely used for the delivery of β-carotene to overcome this limitation. However, these nanoparticles are susceptible to environmental stress. In this study, we utilized glycosylated oat protein isolate to prepare nanoparticles loaded with β-carotene through the emulsification-evaporation method, aiming to address this challenge. The results showed that β-carotene was embedded into the spherical nanoparticles, exhibiting relatively high encapsulation efficiency (86.21 %) and loading capacity (5.43 %). The stability of the nanoparticles loaded with β-carotene was enhanced in acidic environments and under high ionic strength. The nanoparticles offered protection to β-carotene against gastric digestion and facilitated its controlled release (95.76 % within 6 h) in the small intestine, thereby leading to an improved in vitro bioavailability (65.06 %) of β-carotene. This improvement conferred the benefits on β-carotene nanoparticles to alleviate tert-butyl hydroperoxide-induced oxidative stress through the upregulation of heme oxygenase-1 and NAD(P)H quinone dehydrogenase 1 expression, as well as the promotion of nuclear translocation of nuclear factor-erythroid 2-related factor 2. Our study suggests the potential for the industry application of nanoparticles based on glycosylated proteins to effectively deliver hydrophobic nutrients and enhance their application.

PH-Responsive Micellar Nanoparticles for the Delivery of a Self-Amplifying ROS-Activatable Prodrug.

The objective of this study is to enhance the therapeutic efficacy of the anticancer drug, camptothecin (CPT) via a nanoparticle (NP) formulation using a novel amphiphilic biopolymer. We have designed a dimeric prodrug of CPT with the ability to self-amplify and respond to reactive oxygen species (ROS). For this, we incorporated the intracellular ROS generator cinnamaldehyde into a ROS-cleavable thioacetal (TA) linker to obtain the dimeric prodrug of CPT (DCPT(TA)). For its efficient NP delivery, a pH-responsive block copolymer of acetalated dextran and poly(2-ethyl-2-oxazoline) (AcDex-b-PEOz) was synthesized. The amphiphilic feature of the block copolymer enables its self-assembly into micellar NPs and results in high prodrug loading capacity and a rapid release of the prodrug under acidic conditions. Upon cellular uptake by HeLa cells, DCPT(TA)-loaded micellar NPs induce intracellular ROS generation, resulting in accelerated prodrug activation and enhanced cytotoxicity. These results indicate that this system holds significant potential as an effective prodrug delivery strategy in anticancer treatment.

Simple thermal treatment to improve the MRI and magnetic hyperthermia performance of hybrid iron Oxide-Mesoporous silica nanocarriers

The design of multifunctional nanocomposites (NCs), incorporating a variety of controllable properties from nanostructured materials, spans their applicability as nanotools in biomedical applications. Santa Barbara Amorphous (SBA-15) mesoporous silica has showcased remarkable capabilities, ranging from bone regeneration to drug delivery. Its synergy with magnetic nanoparticles (MNPs) further broadens its scope as a theranostic agent, seamlessly integrating both therapeutic and diagnostic functions. However, efficiency issues arise due to MNP anchoring, necessitating novel solutions for optimization. This study focuses on enhancing the magnetic properties of hybrid iron oxide-SBA-15 mesoporous silica NCs through a simplified thermal procedure. The aim is to optimize their magnetic performance for dual functionality as contrast agents for magnetic resonance imaging (MRI) and as effective heaters in magnetic hyperthermia (MH) processes, while preserving the cylindrical mesoporous structure, high surface area, and high loading capacity compared to conventional ceramics. The investigation highlights that the impact of heat treatment on physicochemical properties varies depending on the compositions of the NCs. Specifically, the transversal relaxivity in MRI was doubled, accompanied by an enhanced Néel contribution in MH. This enhancement was achieved while maintaining the same biocompatibility as non-treated NCs, as demonstrated in evaluations with two cancer cell lines (HeLa and T-731 astrocytes), revealing low toxicity at concentrations up to 200 μg/mL.

Progress of Drug Nanocrystal Self-Stabilized Pickering Emulsions: Construction, Characteristics In Vitro, and Fate In Vivo.

A drug nanocrystal self-stabilized Pickering emulsion (DNSPE) is a novel Pickering emulsion with drug nanocrystals as the stabilizer. As a promising drug delivery system, DNSPEs have attracted increasing attention in recent years due to their high drug loading capacity and ability to reduce potential safety hazards posed by surfactants or specific solid particles. This paper comprehensively reviews the progress of research on DNSPEs, with an emphasis on the main factors influencing their construction, characteristics and measurement methods in vitro, and fate in vivo, and puts forward issues that need to be studied further. The review contributes to the advancement of DNSPE research and the promotion of their application in the field of drug delivery.

"One-Pot" Method Preparation of Dendritic Mesoporous Silica-Loaded Matrine Nanopesticide for Noninvasive Administration Control of Monochamus alternatus: The Vector Insect of Bursapherenchus xylophophilus.

Monochamus alternatus is an important stem-boring pest in forestry. However, the complex living environment of Monochamus alternatus creates a natural barrier to chemical control, resulting in a very limited control effect by traditional insecticidal pesticides. In this study, a stable pesticide dendritic mesoporous silica-loaded matrine nanopesticide (MAT@DMSNs) was designed by encapsulating the plant-derived pesticide matrine (MAT) in dendritic mesoporous silica nanoparticles (DMSNs). The results showed that MAT@DMSNs, sustainable nanobiopesticides with high drug loading capacity (80%) were successfully constructed. The release efficiency of DMSNs at alkaline pH was slightly higher than that at acidic pH, and the cumulative release rate of MAT was about 60% within 25 days. In addition, the study on the toxicity mechanism of MAT@DMSNs showed MAT@DMSNs were more effective than MAT and MAT (0.3% aqueous solutions) in touch and stomach toxicity, which might be closely related to their good dispersibility and permeability. Furthermore, MAT@DMSNs are also involved in water transport in trees, which can further transport the plant-derived insecticides to the target site and improve its insecticidal effect. Meanwhile, in addition, the use of essential oil bark penetrants in combination with MAT@DMSNs effectively avoids the physical damage to pines caused by traditional trunk injections and the development of new pests and diseases induced by the traditional trunk injection method, which provides a new idea for the application of biopesticides in the control of stem-boring pests in forestry.

Convergence of Nanotechnology and Bacteriotherapy for Biomedical Applications.

Bacteria have distinctive properties that make them ideal for biomedical applications. They can self-propel, sense their surroundings, and be externally detected. Using bacteria as medical therapeutic agents or delivery platforms opens new possibilities for advanced diagnosis and therapies. Nano-drug delivery platforms have numerous advantages over traditional ones, such as high loading capacity, controlled drug release, and adaptable functionalities. Combining bacteria and nanotechnologies to create therapeutic agents or delivery platforms has gained increasing attention in recent years and shows promise for improved diagnosis and treatment of diseases. In this review, design principles of integrating nanoparticles with bacteria, bacteria-derived nano-sized vesicles, and their applications and future in advanced diagnosis and therapeutics are summarized.

Alginate-coated pomelo pith cellulose matrix for probiotic encapsulation and controlled release

A novel carrier comprised of ethanol- and alkali-modified cellulosic pomelo pith matrix coated with alginate was developed to improve viability while enabling gastrointestinal release of probiotics. Scanning electron microscopy imaging revealed the agricultural byproduct had a honeycomb-structured cellulose framework, enabling high loading capacity of the probiotic Lactobacillus plantarum up to 9 log CFU/g. Ethanol treatment opened up pores with an average diameter of 97 μm, while alkali treatment increased swelling and porosity, with an average pore size of 51 μm. The survival rate through the stomach was increased from 89.76 % to 91.08 % and 91.24 % after ethanol and alkali modification, respectively. The control group displayed minimal release in the first 4 h followed by a burst release. Both ethanol modification and alkali modification resulted in constant linear release over time. The release time was prolonged when decreasing the width of the pomelo peel rolls from 10 mm to 5 mm while keeping the volume of the peel constant. After 8 weeks of refrigerated storage, the cellulose-encapsulated probiotics retained viability above 7 log CFU/g. This study demonstrates the potential of the structurally intact, sustainably-sourced cellulosic pomelo pith for probiotic encapsulation and controlled delivery.

Sky-Worker: a heterogeneous dual-arm robot with dynamic authority assignment for live-line working

Purpose The current difficulties of distribution network working robots are mainly in the performance and operation mode. On the one hand, high-altitude power operation tasks require high load-carrying capacity and dexterity of the robot; on the other hand, the fully autonomous mode is uncontrollable and the teleoperation mode has a high failure rate. Therefore, this study aims to design a distribution network operation robot named Sky-Worker to solve the above two problems. Design/methodology/approach The heterogeneous arms of Sky-Worker are driven by hydraulics and electric motors to solve the contradiction between high load-carrying capacity and high flexibility. A human–robot collaborative shared control architecture is built to realize real-time human intervention during autonomous operation, and control weights are dynamically assigned based on energy optimization. Findings Simulations and tests show that Sky-Worker has good dexterity while having a high load capacity. Based on Sky-Worker, multiuser tests and practical application experiments show that the designed shared-control mode effectively improves the success rate and efficiency of operations compared with other current operation modes. Practical implications The designed heterogeneous dual-arm distribution robot aims to better serve distribution line operation tasks. Originality/value For the first time, the integration of hydraulic and motor drives into a distribution network operation robot has achieved better overall performance. A human–robot cooperative shared control framework is proposed for remote live-line working robots, which provides better operation results than other current operation modes.

Coordinative Double Hydrophilic All-Polyether Micelles for pH-Responsive Delivery of Cisplatin.

Despite its widespread use in the treatment of numerous cancers, the use of cisplatin still raises concerns about its high toxicity and limited selectivity. Consequently, the necessity arises for the development of an effective drug delivery system. Here, we present an effective approach that introduces a double hydrophilic block copolyether for the controlled delivery of cisplatin. Specifically, poly(ethylene glycol)-block-poly(glycidoxy acetic acid) (mPEG-b-PGA) was synthesized via anionic ring-opening polymerization using the oxazoline-based epoxide monomer 4,4-dimethyl-2-oxazoline glycidyl ether, followed by subsequent acidic deprotection. The coordinative metal-ligand interaction between cisplatin and the carboxylate group within the PGA block facilitated the formation of micelles from the double hydrophilic mPEG-b-PGA copolyether. Cisplatin-loaded polymeric micelles had a high loading capacity, controlled pH-responsive release kinetics, and high cell viability. Furthermore, in vitro biological assays revealed cellular apoptosis induced by the cisplatin-loaded micelles. This study thus successfully demonstrates the potential use of double hydrophilic block copolyethers as a versatile platform for biomedical applications.

Metal-Phenolic-Mediated Assembly of Functional Small Molecules into Nanoparticles: Assembly and Bioapplications.

Small molecules, including therapeutic drugs and tracer molecules, play a vital role in biological processing, disease treatment and diagnosis, and have inspired various nanobiotechnology approaches to realize their biological function, particularly in drug delivery. Desirable features of a delivery system for functional small molecules (FSMs) include high biocompatibility, high loading capacity, and simple manufacturing processes, without the need for chemical modification of the FSM itself. Herein, we report a simple and versatile approach, based on metal-phenolic-mediated assembly, for assembling FSMs into nanoparticles (i.e., FSM-MPN NPs) under aqueous and ambient conditions. We demonstrate loading of anticancer drugs, latency reversal agents, and fluorophores at up to ~80 % that is mostly facilitated by π and hydrophobic interactions between the FSM and nanoparticle components. Secondary nanoparticle engineering involving coating with a polyphenol-antibody thin film or sequential co-loading of multiple FSMs enables cancer cell targeting and combination delivery, respectively. Incorporating fluorophores into FSM-MPN NPs enables the visualization of biodistribution at different time points, revealing that most of these NPs are retained in the kidney and heart 24 h post intravenous administration. This work provides a viable pathway for the rational design of small molecule nanoparticle delivery platforms for diverse biological applications.

Metal–Phenolic‐Mediated Assembly of Functional Small Molecules into Nanoparticles: Assembly and Bioapplications

AbstractSmall molecules, including therapeutic drugs and tracer molecules, play a vital role in biological processing, disease treatment and diagnosis, and have inspired various nanobiotechnology approaches to realize their biological function, particularly in drug delivery. Desirable features of a delivery system for functional small molecules (FSMs) include high biocompatibility, high loading capacity, and simple manufacturing processes, without the need for chemical modification of the FSM itself. Herein, we report a simple and versatile approach, based on metal–phenolic‐mediated assembly, for assembling FSMs into nanoparticles (i.e., FSM‐MPN NPs) under aqueous and ambient conditions. We demonstrate loading of anticancer drugs, latency reversal agents, and fluorophores at up to ~80 % that is mostly facilitated by π and hydrophobic interactions between the FSM and nanoparticle components. Secondary nanoparticle engineering involving coating with a polyphenol–antibody thin film or sequential co‐loading of multiple FSMs enables cancer cell targeting and combination delivery, respectively. Incorporating fluorophores into FSM‐MPN NPs enables the visualization of biodistribution at different time points, revealing that most of these NPs are retained in the kidney and heart 24 h post intravenous administration. This work provides a viable pathway for the rational design of small molecule nanoparticle delivery platforms for diverse biological applications.