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A visible light-induced oxidative esterification reaction of mandelic acid with alcohols has been developed for the synthesis of α-ketoesters. The reaction is characterised by transition metal-free nature, good yields, broad functional group tolerance, and ease of operation. A practical, neutral and mild synthetic approach is provided for α-ketoesters, which are important units of many bioactive compounds and useful precursors in a wide range of drugs. Preliminary mechanistic studies suggest that this reaction takes place via the free radical pathway. [ABSTRACT FROM AUTHOR]

The emerging field of liquid biopsy has garnered significant interest in precision diagnostics, offering a non-invasive and repetitive method for analyzing bodily fluids to procure real-time diagnostic data. The precision and accuracy offered by the clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR-associated protein (CRISPR/Cas) technology have advanced and broadened the applications of liquid biopsy. Significantly, when combined with swiftly advancing nanotechnology, CRISPR/Cas-mediated nanodevices show vast potential in precise liquid biopsy applications. However, persistent challenges are still associated with off-target effects, and the current platforms also constrain the performance of the assays. In this review, we highlight the merits of CRISPR/Cas systems in liquid biopsy, tracing the development of CRISPR/Cas systems and their current applications in disease diagnosis particularly in liquid biopsies. We also outline ongoing efforts to design nanoscale devices with improved sensing and readout capabilities, aiming to enhance the performance of CRISPR/Cas detectors in liquid biopsy. Finally, we identify the critical obstacles hindering the widespread adoption of CRISPR/Cas liquid biopsy and explore potential solutions. This feature article presents a comprehensive overview of CRISPR/Cas-mediated liquid biopsies, emphasizing the progress in integrating nanodevices to improve specificity and sensitivity. It also sheds light on future research directions in employing nanodevices for CRISPR/Cas-based liquid biopsies in the realm of precision medicine. [ABSTRACT FROM AUTHOR]

Cutaneous squamous cell carcinoma (cSCC) is one of the most common skin cancers with increasing incidence worldwide. However, it is still challenging to prevent the relapse of cSCC due to poor drug penetration across the stratum corneum. Herein, we report the design of a microneedle patch loaded with MnO2/Cu2O nanosheets and combretastatin A4 (MN-MnO2/Cu2O-CA4) for the enhanced therapy of cSCC. The prepared MN-MnO2/Cu2O-CA4 patch could effectively deliver adequate drugs locally into the tumor sites. Moreover, the glucose oxidase (GOx)-mimicking activity of MnO2/Cu2O could catalyze glucose to produce H2O2, which combined with the released Cu to induce a Fenton-like reaction to efficiently generate hydroxyl radicals for chemodynamic therapy. Meanwhile, the released CA4 could inhibit cancer cell migration and tumor growth by disrupting the tumor vasculature. Moreover, MnO2/Cu2O was endowed with the ability of photothermal conversion under the irradiation of near-infrared (NIR) laser, which could not only kill the cancer cells but also promote the efficiency of the Fenton-like reaction. Significantly, the photothermal effect did not compromise the GOx-like activity of MnO2/Cu2O, which guaranteed enough production of H2O2 for the sufficient generation of hydroxyl radicals. This work may open avenues for constructing MN-based multimodal treatment for the efficient therapy of skin cancers. [ABSTRACT FROM AUTHOR]

Enzyme clustering is widely used in many organisms to increase the catalytic efficiency of cascade reactions. Inspired by nature, organizing enzymes within a cascade reaction also draws much attention in both basic research and industrial processes. An important step for organizing enzymes precisely in vitro is enzyme modification. However, modifying enzymes without sacrificing their activity remains challenging until now. For example, labeling enzymes with DNA, one of the well-established enzyme modification methods, has been shown to significantly reduce the enzymatic activity. Herein we report an enzyme conjugation method that can rescue the reduction of enzymatic activity caused by DNA labeling. We demonstrate that immobilizing DNA-modified enzymes on the vertex of TDNs (tetrahedral DNA nanostructures) enhances the enzymatic activity compared with their unmodified counterparts. Using this strategy, we have further developed an ultra-sensitive and high-throughput electrochemical biosensor for sarcosine detection, which holds great promise for prostate cancer screening. [ABSTRACT FROM AUTHOR]

Membrane fusion, a fundamental biological process of the fusion of the membrane composition between cells, is vital for cell–cell communication and cargo transport between living cells. This fusion interaction achieves the transportation of the inner content to the cellular cytosol as well as the simultaneous blending of foreign substances with the cell membrane. Inspired by this biological process, emerging membrane-fusogenic particles have been developed, opening a new area for bioengineering and biomedical applications. Especially, membrane-fusion-mediated transfer of inner cargoes can bypass endosomal entrapment to maximize the transportation efficiency, emerging as a unique cytoplasmic delivery platform distinct from those depending on conventional endocytosis-based pathways. In addition, the membrane fusion enables cell surface modification through lipid diffusion and mixing, providing a tool for direct cell membrane engineering. In this review, we focus on the development of membrane-fusogenic particles and their up-to-date progress. We briefly introduce the concept of membrane fusion, elaborate inspiring strategies of membrane-fusogenic particles, and highlight the recent advances and the promising applications of membrane-fusogenic particles as a next-generation bioengineering tool. In the end, we conclude with the present challenges and opportunities, providing insights in the future research of membrane-fusogenic particles. [ABSTRACT FROM AUTHOR]

Herein we examined the utilization of the orthogonal noncovalent interaction to program the self-assembly of amphiphilic DNA frameworks (am-FNAs). By finely controlling reaction parameters such as ionic strength, the length of amphiphilic DNA, and mechanical agitation, we constructed a series of amphiphilic DNA-based primary logic gates (NOT, AND, OR and INH) and a secondary logic gate (NOT-OR). [ABSTRACT FROM AUTHOR]

Herein we utilized the thermal hysteresis method to directly probe the self-assembly process of amphiphilic DNA nanostructures, with the use of an amphiphilic tetrahedral DNA framework (am-TDF) as a model system. The analysis of the reaction rate surfaces under different ionic strengths revealed that strands of amphiphilic DNA first formed metastable micelles via an entropy-driven process, which were then enthalpically transformed into am-TDF. [ABSTRACT FROM AUTHOR]

Despite the significant progress in the discovery of biomarkers and the exploitation of technologies for prostate cancer (PCa) detection and diagnosis, the initial screening of these PCa-related biomarkers using current technologies is always demanded with a bioassay or probe with high sensitivity, specificity, and noninvasiveness. Nanomaterials have emerged as novel alternative probes for PCa detection and diagnosis because of their nanoscale size, large ratio of surface area to volume, special surface chemistry, and particularly distinct physical properties. By selecting appropriate nanomaterials, a series of nanosensors or nanoprobes could be constructed for PCa bioassay with high sensitivity, selectivity, and accuracy. Meanwhile, nanosized particles also show significant potential to transport directors or contrast agents to desired sites in vivo for accurate and safe visualization of PCa tissues. Based on these advancements, this review will first outline the recent exploration of PCa biomarkers and the development of technologies for clinical PCa diagnosis. Then, the commonly used nanomaterials for PCa detection and diagnosis will be summarized. Finally, the current challenges and prospects of nanoparticle-based PCa detection and diagnosis methods are also discussed. [ABSTRACT FROM AUTHOR]

Bacteria-induced acute lung injury (ALI) is associated with a high mortality rate due to the lack of an effective treatment. Patients often rely on supportive care such as low tidal volume ventilation to alleviate the symptoms. Nanomedicine has recently received much attention owing to its premium benefits of delivering drugs in a sustainable and controllable manner while minimizing the potential side effects. It can effectively improve the prognosis of bacteria-induced ALI through targeted delivery of drugs, regulation of multiple inflammatory pathways, and combating antibiotic resistance. Hence, in this review, we first discuss the pathogenesis of ALI and its potential therapeutics. In particular, the state-of-the-art nanomedicines for the treatment of bacteria-induced ALI are highlighted, including their administration routes, in vivo distribution, and clearance. Furthermore, the available bacteria-induced ALI animal models are also summarized. In the end, future perspectives of nanomedicine for ALI treatment are proposed. [ABSTRACT FROM AUTHOR]

The early diagnosis of cancer can significantly improve patient survival rates. Colorimetric methods for real-time naked-eye detection have aroused growing interest owing to their low cost, simplicity, and practicability. With the rapid development of nanotechnology, compared with conventional diagnostic methods, nanomaterials with unique physical and chemical properties were applied to improve selectivity and sensitivity in colorimetric detection of cancer biomarkers, such as MUC1 aptamer conjugated PtAuNPs to specifically recognize MUC1 proteins on the cancer cell surfaces, etching of silver nanoprisms to detect prostate-specific antigen, and aggregation or dispersion of AuNPs to sense prostate cancer antigen gene 3 or glutathione, by which the limit of detection (LOD) could approach values down to a few cancer cells per mL, several fg per mL proteins, several ng of nucleic acids, or even tens of nM of organic molecules. Herein, we review the recent progress achieved in developing colorimetric nanosensors for cancer diagnosis, particularly providing an overview of the sensing principles, target biomarkers, advanced nanomaterials employed in the fabrication of sensing platforms, and strategies for improving signal sensitivity and specificity. Finally, we sum up the nanomaterial-based colorimetric cancer detection as well as existing challenges that should be resolved to extend their clinical application. [ABSTRACT FROM AUTHOR]

Interstitial cystitis/bladder pain syndrome (IC/BPS) is a chronic and painful bladder condition afflicting patients with increased urinary urgency and frequency as well as incontinence. Owing to the elusive pathogenesis of IC/BPS, obtaining effective therapeutic outcomes remains challenging. Current administrational routes such as intravesical-bladder injection improve the treatment efficacy and reduce systemic side effects. However, the bladder permeability barrier hinders drug penetration into the bladder wall to meet the desired therapeutic expectation. These issues can be addressed by encapsulating drugs into biomaterials. When appropriately exploited, they would increase the drug dwelling time in the bladder, enhance the penetration of mucosa and improve the therapeutic response of IC/BPS. In this review, we first elucidate the pathogenesis and animal models of IC/BPS. Then, we highlight recent representative biomaterial-assisted drug delivery systems for IC/BPS treatment. Finally, we discuss the challenges and outlook for further developing biomaterial-based delivery systems for IC/BPS management. [ABSTRACT FROM AUTHOR]

The clustered regularly interspaced short palindromic repeats (CRISPR)/associated protein 9 (CRISPR/Cas9) technology enables genome editing with high precision and versatility and has been widely utilized to combat viruses, bacteria, cancers, and genetic diseases. Nonviral nanocarriers can overcome several limitations of viral vehicles, including immunogenicity, inflammation, carcinogenicity, and low versatility, and thus represent promising platforms for CRISPR/Cas9 delivery. Herein, we for the first time develop the application of protamine-capped gold nanoclusters (protamine–AuNCs) as an effective nanocarrier for Cas9–sgRNA plasmid transport and release to achieve efficient genome editing. The protamine–AuNCs integrate the merits of AuNCs and protamine: AuNCs are able to promptly assemble with Cas9–sgRNA plasmids to allow efficient cellular delivery, while the cationic protamine facilitates the effective release of Cas9–sgRNA plasmids into the cellular nucleus. The AuNCs/Cas9–gRNA plasmid nanocomplexes can not only achieve successful gene editing in cells but also knock out the oncogenic gene for cancer therapy. Moreover, the AuNCs with excellent photoluminescence characteristics endow our nanoplatform with the functionality of bioimaging. Overall, our study provides strong evidence that demonstrates protamine–AuNCs as an effective CRISPR/Cas9 delivery tool for gene therapy. [ABSTRACT FROM AUTHOR]

The oxygen evolution reaction (OER) is of prime importance in the development of highly efficient electrochemical energy conversion and storage technologies such as water splitting and zinc air batteries. Ru-based nanocatalysts are still the best catalytic system for the OER; however, one of the greatest challenges is their relatively poor stability for the OER. Here, we report a novel architecture of ultrathin RuRh@(RuRh)O2 core/shell nanosheets with a core of ultrathin metallic RuRh nanosheets and a shell of RuO2/RhO2 oxides as superb electrocatalysts toward the OER. The RuRh@(RuRh)O2 core/shell nanosheets can achieve a high electrocatalytic activity toward the OER, with a low 245 mV overpotential at 10 mA cm−2 and a Tafel slope of 51.2 mV dec−1, better than most state-of-the-art Ru-based or Ir-based electrocatalysts for the OER. Moreover, the RuO2/RhO2 oxides shell protect the normally labile RuRh NSs core against dissolution during the OER process, revealed by detailed rotating ring disk electrode (RRDE) measurements for simultaneously recording the dissolution of Ru on the ring electrode and the ex situ measurement of Ru dissolution using the galvanostatic method. Therefore, the RuRh@(RuRh)O2 core/shell nanosheets exhibit much better OER stability in acid media compared with RuRh nanosheets and commercial RuO2. Theoretical calculations reveal that once the formation of the surface oxidation layers is achieved, the O-sites evidentially crossover the Fermi level which could guarantee the high electroactivity towards adsorbates while the RuRh core serves as an electron reservoir with high electrical conductivity. The synergistic effect between the core and shell structure leads to the superior OER performance. [ABSTRACT FROM AUTHOR]

Viologens, functional organic materials composed of conjugated bi-/multi-pyridyl groups, have attracted much attention for decades owing to their properties such as unique electrochromic and radical-rich features under redox manipulation, biosensitive properties, and ionic and localized conjugation. Considerable efforts have been devoted to synthesizing novel viologen-based functional materials to study their properties and develop applications. So far, viologens and viologen-based materials have been widely applied in many fields, including electrochromism, molecular machines, memory devices, gas storage and separation, energy storage, and biochemistry. The rapid development of functional materials in the 21st century has inspired extensive integration of viologens into many types of novel and famous materials (e.g., host–guest supramolecules, porous polymers, and metal–organic frameworks), and therefore, viologens seem to no longer be a key player. However, the features of viologens (or bi-/multi-pyridyl-based materials) have always dominated the properties of target functional materials and long been neglected by researchers. In order to provide an overview of this field, this perspective paper focuses on reasonable design and synthesis of viologen-based functional materials and their representative applications. The remaining challenges and future potential applications are also discussed. [ABSTRACT FROM AUTHOR]

To advance emulsion droplet technology, we synthesize functional derivatives of Pluronic F127 that can simultaneously act as surfactants and as reactive sites for droplet surface decoration. The amine-, carboxyl-, N-hydroxysuccinimide ester-, maleimide- and biotin-terminated Pluronic F127 allows ligand immobilization on single-emulsion or double-emulsion droplets via electrostatic adsorption, covalent conjugation or site-specific avidin–biotin interaction. [ABSTRACT FROM AUTHOR]

Regeneration of diseased tissue is one of the foremost concerns for millions of patients who suffer from tissue damage each year. Local delivery of cell-laden hydrogels offers an attractive approach for tissue repair. However, due to the typical macroscopic size of these cell constructs, the encapsulated cells often suffer from poor nutrient exchange. These issues can be mitigated by incorporating cells into microscopic hydrogels, or microgels, whose large surface-to-volume ratio promotes efficient mass transport and enhanced cell–matrix interactions. Using microfluidic technology, monodisperse cell-laden microgels with tunable sizes can be generated in a high-throughput manner, making them useful building blocks that can be assembled into tissue constructs with spatially controlled physicochemical properties. In this review, we examine microfluidics-generated cell-laden microgels for tissue regeneration applications. We provide a brief overview of the common biomaterials, gelation mechanisms, and microfluidic device designs that are used to generate these microgels, and summarize the most recent works on how they are applied to tissue regeneration. Finally, we discuss future applications of microfluidic cell-laden microgels as well as existing challenges that should be resolved to stimulate their clinical application. [ABSTRACT FROM AUTHOR]

Metal nanoclusters, composed of several to a few hundred metal atoms, have received worldwide attention due to their extraordinary physical and chemical characteristics. Recently, great efforts have been devoted to the exploration of the potential diagnostic and therapeutic applications of metal nanoclusters. Here we focus on the recent advances and new horizons in this area, and introduce the rising progress on the use of metal nanoclusters for biological analysis, biological imaging, therapeutic applications, DNA assembly and logic gate construction, enzyme mimic catalysis, as well as thermometers and pH meters. Furthermore, the future challenges in the construction of biofunctional metal nanoclusters for diagnostic and therapeutic applications are also discussed. We expect that the rapidly growing interest in metal nanocluster-based theranostic applications will certainly not only fuel the excitement and stimulate research in this highly active field, but also inspire broader concerns across various disciplines. [ABSTRACT FROM AUTHOR]

Fabrication of a hybridized single-walled carbon nanotube (SWCNT) device based on novel sensing material mono-6-deoxy-6-(p-aminophenylamino)-β-cyclodextrin (PCD) viaa facile approach has been reported for the first time; moreover, the hybridized material PCD-decorated SWCNTs (SWCNT–PCD) can be characterized by ultraviolet–visible–near infrared spectroscopy, Raman spectroscopy, thermogravimetric analysis, field-emission scanning electron microscopy and high resolution transmission electron microscopy. The PCD-decorated SWCNT devices have been employed to detect Persistent Organic Pollutants (POPs) on the basis of formation of an inclusion complex with guest molecules between SWCNT–PCD and POPs, such as 2,4,5-trichlorobiphenyl (TCB), etc.The significant variation of the electrical conductance of the SWCNT–PCD hybrid corresponding to the presence of several POPs with different adsorption efficiencies on the surface indicates that the hybrid is highly sensitive to some specific POP molecules, implying that hybridized SWCNT–PCD has great potential in application as an environmental monitor. In order to make a quantitative assessment of the inclusion complexation behavior of PCD with these POP molecules, microcalorimetric titration experiments and discussions have been carried out. [ABSTRACT FROM AUTHOR]

Fabrication of hybridized single-walled carbon nanotube (SWNT) device based on novel sensing material N-4-Hexafluoroisopropanolphenyl-1-pyrenebutyramide (HFIPP) viafacile approach has been reported for the first time. Considered that strong hydrogen-bonding can be formed between HFIPP and dimethyl methylphosphonate (DMMP) (simulant of nerve agent sarin), the HFIPP-decorated SWNT device has been employed to detect DMMP. The detection limit achieved with our sensor is as low as 50 ppb; moreover, the response and reproducibility can be presented clearly even at very low concentration of DMMP. Excellent sensitivity and selectivity of the hybridized SWNT-HFIPP device suggest that it has great potential application for detecting explosives and nerve agents. In order to investigate sensing mechanism of SWNT-HFIPP for DMMP, control electrical and fluorescent experiments have been carried out and discussed in the present paper. [ABSTRACT FROM AUTHOR]

Unmethylated cytosine-phosphate-guanine (CpG) oligodeoxynucleotides (ODNs), which were therapeutic DNA with high immunostimulatory activity, have been applied in widespread applications from basic research to clinics as therapeutic agents for cancer immunotherapy, viral infection, allergic diseases and asthma since their discovery in 1995. The major factors to consider for clinical translation using CpG motifs are the protection of CpG ODNs from DNase degradation and the delivery of CpG ODNs to the Toll-like receptor-9 expressed human B-cells and plasmacytoid dendritic cells. Therefore, great efforts have been devoted to the advances of efficient delivery systems for CpG ODNs. In this review, we outline new horizons and recent developments in this field, providing a comprehensive summary of the nanoparticle-based CpG delivery systems developed to improve the efficacy of CpG-mediated immune responses, including DNA nanostructures, inorganic nanoparticles, polymer nanoparticles, metal-organic-frameworks, lipid-based nanosystems, proteins and peptides, as well as exosomes and cell membrane nanoparticles. Moreover, future challenges in the establishment of CpG delivery systems for immunotherapeutic applications are discussed. We expect that the continuously growing interest in the development of CpG-based immunotherapy will certainly fuel the excitement and stimulation in medicine research.

Cutaneous squamous cell carcinoma (cSCC) is one of the most common skin cancers with increasing incidence worldwide. However, it is still challenging to prevent the relapse of cSCC due to poor drug penetration across the stratum corneum. Herein, we report the design of a microneedle patch loaded with MnO 2 /Cu 2 O nanosheets and combretastatin A4 (MN-MnO 2 /Cu 2 O-CA4) for the enhanced therapy of cSCC. The prepared MN-MnO 2 /Cu 2 O-CA4 patch could effectively deliver adequate drugs locally into the tumor sites. Moreover, the glucose oxidase (GOx)-mimicking activity of MnO 2 /Cu 2 O could catalyze glucose to produce H 2 O 2 , which combined with the released Cu to induce a Fenton-like reaction to efficiently generate hydroxyl radicals for chemodynamic therapy. Meanwhile, the released CA4 could inhibit cancer cell migration and tumor growth by disrupting the tumor vasculature. Moreover, MnO 2 /Cu 2 O was endowed with the ability of photothermal conversion under the irradiation of near-infrared (NIR) laser, which could not only kill the cancer cells but also promote the efficiency of the Fenton-like reaction. Significantly, the photothermal effect did not compromise the GOx-like activity of MnO 2 /Cu 2 O, which guaranteed enough production of H 2 O 2 for the sufficient generation of hydroxyl radicals. This work may open avenues for constructing MN-based multimodal treatment for the efficient therapy of skin cancers.

Reasonable design of bimetallic nanomaterials with support is beneficial to improve catalytic performance. This work reports a new kind of sodium sesquicarbonate-supporting Fe 2 O 3 @Pt via etching Fe 3 O 4 @Pt@SiO 2 , which exhibits highly efficient and stable catalytic reduction performance towards 4-NP. Sodium sesquicarbonate-supporting Fe 2 O 3 @Pt has an interconnected one-dimensional network structure that provides sufficient channels for mass transfer. At the same time, a large amount of Fe 2 O 3 @Pt is exposed on its surface, which hinders the aggregation of pt clusters and Fe 2 O 3 nanoparticles, and facilitates the direct contact of Fe 2 O 3 @Pt reaction sites with reactant molecules, thus improving the catalytic rate of 4-NP reduction reaction. Moreover, the introduction of non-metallic Fe can not only reduce the consumption of precious metal Pt, but also improve the catalytic efficiency due to the synergistic effect. This study opens up a new avenue to develop robust catalysts for heterogeneous catalytic reactions., Competing Interests: There are no conflicts to declare, (This journal is © The Royal Society of Chemistry.)

Helicobacter pylori ( H. pylori ) infection is considered to be the main cause of most digestive diseases,such as chronic active gastritis, gastroduodenal ulcers, or even gastric cancer. Oral medication is a transformative approach to treat H. pylori -induced infections. However, unlike intravenous administration, orally administrated drugs have to overcome various barriers before reaching the infected sites, which significantly limits the therapeutic efficacy. These challenges may be addressed by emerging nanomedicine that is equipped with nanotechnology approaches to enable efficient and effective targeted delivery of drugs. Herein, in this review, we first discuss the conventional therapy for the eradication of H. pylori . Through the introduction of the critical barriers of oral administration, the benefits of nanomedicine are highlighted. Recently-published examples of nanocarriers for combating H. pylori in terms of design, preparation, and antimicrobial mechanisms are then presented, followed by our perspective on potential future research directions of oral nanomedicines.

Precious metal nanometric catalysts are widely used in the removal of harmful substances. In the process of synthesis and catalytic reaction, it is particularly important to study green and simple synthesis methods and high catalytic efficiency. In this paper, a green one-step method was used to synthesize the Fe(OH) 3 /Fe 2 O 3 @Au composite catalyst, in which Au was single atom-dispersed. The removal of 4-nitrophenol (4-NP), a typical dangerous chemical widely existing in factory waste gas, waste water and automobile exhaust gas, was catalysed by Fe(OH) 3 /Fe 2 O 3 @Au. The catalytic performance of Fe(OH) 3 /Fe 2 O 3 @Au with different synthesis conditions (different amounts of MES, NaBH 4 , FeSO 4 , Au and Pt) on the 4-NP reduction reaction were systematically studied. Finally, the stability and recyclability of Fe(OH) 3 /Fe 2 O 3 @Au composite nanocatalyst were investigated thoroughly., Competing Interests: The authors declare no competing financial interest., (This journal is © The Royal Society of Chemistry.)

Cisplatin is one of the most common anticancer agents for treating different kinds of solid tumors today. However, its broader therapeutic applications are limited by the severe side effects and nonspecific biodistribution. In this study, luteinizing hormone-releasing hormone (LHRH)-targeted polysaccharide nanoparticles for tumor-targeted delivery and controlled release of cisplatin were developed. This nanoparticle delivery system possessed the following unique properties: (1) as the degradation products of the carrier, both dextran and succinic acid have been proved by the United States Food and Drug Administration for parenteral use, indicating good safety and great application potential; (2) both the drug loading and LHRH conjugation procedures were carried out with efficiency in aqueous medium without the use of organic solvents, thus representing a green chemistry approach; and (3) the design followed the principle of drug encapsulation first and subsequent targeting ligand modification, guaranteeing that the targeting molecules were conjugated on the surface of nanoparticles. As compared to free cisplatin, both the non-targeted and targeted nanoparticles displayed sustained drug release, prolonged blood circulation and reduced systemic toxicity. Foremost, the LHRH-targeted nanoparticles led to significant higher cellular internalization in MCF-7 tumor cells in vitro and enhanced accumulation in MCF-7 xenograft tumors in vivo, compared with the non-targeted counterparts. Systemic delivery of the targeted nanoparticles carrying cisplatin via intravenous injection showed enhanced tumor suppression in MCF-7 tumor bearing mice compared to the non-targeted nanoparticles and free CDDP. Collectively, the LHRH-mediated polysaccharide nanoparticles appeared to be a promising nanomedicine drug delivery system for tumor-targeted delivery of cisplatin.