Search

Goeun Choi,1 Huiyan Piao,1 Zeid A Alothman,2 Ajayan Vinu,3 Chae-Ok Yun,4 Jin-Ho Choy1 1Center for Intelligent Nano-Bio Materials, Department of Chemistry and Nano Science, Ewha Womans University, Seoul, Korea; 2Advanced Materials Research Chair, Chemistry Department, College of Science, King Saud University, Riyadh, Saudi Arabia; 3Future Industries Institute, University of South Australia, Mawson Lakes, SA, Australia; 4Department of Bioengineering, College of Engineering, Hanyang University, Seoul, Korea Abstract: Methotrexate (MTX), an anticancer agent, was successfully intercalated into the anionic clay, layered double hydroxides to form a new nanohybrid drug. The coprecipitation and subsequent hydrothermal method were used to prepare chemically, structurally, and morphologically well-defined two-dimensional drug-clay nanohybrid. The resulting two-dimensional drug-clay nanohybrid showed excellent colloidal stability not only in deionized water but also in an electrolyte solution of Dulbecco’s Modified Eagle’s Medium with 10% fetal bovine serum, in which the average particle size in colloid and the polydispersity index were determined to be around 100 and 0.250 nm, respectively. The targeting property of the nanohybrid drug was confirmed by evaluating the tumor-to-blood and tumor-to-liver ratios of the MTX with anionic clay carrier, and these ratios were compared to those of free MTX in the C33A orthotopic cervical cancer model. The biodistribution studies indicated that the mice treated with the former showed 3.5-fold higher tumor-to-liver ratio and fivefold higher tumor-to-blood ratio of MTX than those treated with the latter at 30 minutes postinjection. Keywords: anionic clay, biodistribution, cervical cancer, colloidal stability, layered double hydroxide, methotrexate

Soo-Jin Choi,1 Jin-Ho Choy2 1Department of Food Science and Technology, Seoul Women's University, 2Center for Intelligent Nano Bio Materials (CINBM), Department of Bioinspired Science and Department of Chemistry and Nanoscience, Ewha Womans University, Seoul, South Korea Abstract: Biokinetic studies of zinc oxide (ZnO) nanoparticles involve systematic and quantitative analyses of absorption, distribution, metabolism, and excretion in plasma and tissues of whole animals after exposure. A full understanding of the biokinetics provides basic information about nanoparticle entry into systemic circulation, target organs of accumulation and toxicity, and elimination time, which is important for predicting the long-term toxic potential of nanoparticles. Biokinetic behaviors can be dependent on physicochemical properties, dissolution property in biological fluids, and nanoparticle–protein interaction. Moreover, the determination of biological fates of ZnO nanoparticles in the systemic circulation and tissues is critical in interpreting biokinetic behaviors and predicting toxicity potential as well as mechanism. This review focuses on physicochemical factors affecting the biokinetics of ZnO nanoparticles, in concert with understanding bioavailable fates and their interaction with proteins. Keywords: ZnO nanoparticles, biokinetics, distribution, excretion, fate, interaction

Miri Baek,1,* Hae-Eun Chung,1,* Jin Yu,1,* Jung-A Lee,1 Tae-Hyun Kim,2 Jae-Min Oh,2 Won-Jae Lee,3 Seung-Min Paek,3 Jong Kwon Lee,4 Jayoung Jeong, 4 Jin-Ho Choy,5 Soo-Jin Choi1 1Department of Food Science and Technology, Seoul Women's University, Seoul, 2Department of Chemistry and Medical Chemistry, College of Science and Technology, Yonsei University, Wonju, Gangwondo; 3Department of Chemistry and Green-Nano Materials Research Center, Kyungpook National University, Taegu, 4Toxicological Research Division, National Institute of Food and Drug Safety Evaluation, Chungchungbuk-do, 5Center for Intelligent Nano-Bio Materials, Department of Bioinspired Science and Department of Chemistry and Nano Science, Ewha Womans University, Seoul, Republic of Korea*These authors contributed equally to this workBackground: This study explored the pharmacokinetics, tissue distribution, and excretion profile of zinc oxide (ZnO) nanoparticles with respect to their particle size in rats.Methods: Two ZnO nanoparticles of different size (20 nm and 70 nm) were orally administered to male and female rats, respectively. The area under the plasma concentration-time curve, tissue distribution, excretion, and the fate of the nanoparticles in organs were analyzed.Results: The plasma zinc concentration of both sizes of ZnO nanoparticles increased during the 24 hours after administration in a dose-dependent manner. They were mainly distributed to organs such as the liver, lung, and kidney within 72 hours without any significant difference being found according to particle size or rat gender. Elimination kinetics showed that a small amount of ZnO nanoparticles was excreted via the urine, while most of nanoparticles were excreted via the feces. Transmission electron microscopy and x-ray absorption spectroscopy studies in the tissues showed no noticeable ZnO nanoparticles, while new Zn-S bonds were observed in tissues.Conclusion: ZnO nanoparticles of different size were not easily absorbed into the bloodstream via the gastrointestinal tract after a single oral dose. The liver, lung, and kidney could be possible target organs for accumulation and toxicity of ZnO nanoparticles was independent of particle size or gender. ZnO nanoparticles appear to be absorbed in the organs in an ionic form rather than in a particulate form due to newly formed Zn-S bonds. The nanoparticles were mainly excreted via the feces, and smaller particles were cleared more rapidly than the larger ones. ZnO nanoparticles at a concentration below 300 mg/kg were distributed in tissues and excreted within 24 hours. These findings provide crucial information on possible acute and chronic toxicity of ZnO nanoparticles in potential target organs.Keywords: ZnO nanoparticles, pharmacokinetics, tissue distribution, excretion, fate

Ji-Hee Lee1,*, Goeun Choi1,*, Yeon-Ji Oh1, Je Won Park1, Young Bin Choy3, Mung Chul Park1, Yeo Joon Yoon1, Hwa Jeong Lee2, Hee Chul Chang4, Jin-Ho Choy1 1Center for Intelligent Nano-Bio Materials (CINBM), Department of Bioinspired Science and Department of Chemistry and Nano Science, 2Division of Life and Pharmaceutical Sciences and College of Pharmacy, Ewha Womans University, Seoul, Korea; 3Department of Biomedical Engineering, College of Medicine and Institute of Medical and Biological Engineering, Medical Research Center, Seoul National University, Seoul, Korea; 4Global Strategy Center and Pharmaceutical Research Institute, Daewoong Pharmaceutical Co., Ltd., Seoul, Korea*These authors contributed equally to this workAbstract: A nanohybrid was prepared with an inorganic clay material, montmorillonite (MMT), for taste masking of sildenafil (SDN). To further improve the taste-masking efficiency and enhance the drug-release rate, we coated the nanohybrid of SDN–MMT with a basic polymer, polyvinylacetal diethylaminoacetate (AEA). Powder X-ray diffraction and Fourier transform infrared experiments showed that SDN was successfully intercalated into the interlayer space of MMT. The AEA-coated SDN–MMT nanohybrid showed drug release was much suppressed at neutral pH (release rate, 4.70 ± 0.53%), suggesting a potential for drug taste masking at the buccal cavity. We also performed in vitro drug release experiments in a simulated gastric fluid (pH = 1.2) and compared the drug-release profiles of AEA-coated SDN–MMT and Viagra®, an approved dosage form of SDN. As a result, about 90% of SDN was released from the AEA-coated SDN–MMT during the first 2 hours while almost 100% of drug was released from Viagra®. However, an in vivo experiment showed that the AEA-coated SDN–MMT exhibited higher drug exposure than Viagra®. For the AEA-coated SDN–MMT, the area under the plasma concentration–time curve from 0 hours to infinity (AUC0-∞) and maximum concentration (Cmax) were 78.8 ± 2.32 µg • hour/mL and 12.4 ± 0.673 µg/mL, respectively, both of which were larger than those obtained with Viagra® (AUC0-∞ = 69.2 ± 3.19 µg • hour/mL; Cmax = 10.5 ± 0.641 µg/mL). Therefore, we concluded that the MMT-based nanohybrid is a promising delivery system for taste masking of SDN with possibly improved drug exposure.Keywords: montmorillonite, nanohybrids, polyvinylacetal diethylaminoacetate, sildenafil citrate, taste masking

The coronavirus disease 2019 (COVID-19) pandemic is a serious global threat with surging new variants of concern. Although global vaccinations have slowed the pandemic, their longevity is still unknown. Therefore, new orally administrable antiviral agents are highly demanded. Among various repurposed drugs, niclosamide (NIC) is the most potential one for various viral diseases such as COVID-19, SARS (severe acute respiratory syndrome), MERS (middle east respiratory syndrome), influenza, RSV (respiratory syncytial virus), etc. Since NIC cannot be effectively absorbed, a required plasma concentration for antiviral potency is hard to maintain, thereby restricting its entry into the infected cells. Such a 60-year-old bioavailability challenging issue has been overcome by engineering with MgO and hydroxypropyl methylcellulose (HPMC), forming hydrophilic NIC-MgO-HPMC, with improved intestinal permeability without altering NIC metabolism as confirmed by parallel artificial membrane permeability assay. The inhibitory effect on SARS-CoV-2  replication is confirmed in the Syrian hamster model to reduce lung injury. Clinical studies reveal that the bioavailability of NIC hybrid drug can go 4 times higher than the intact NIC. The phase II clinical trial shows a dose-dependent bioavailability of NIC from hybrid drug  suggesting its potential applicability as a game changer in achieving the much-anticipated endemic phase., (© 2023 Wiley‐VCH GmbH.)

Millions of cases of dengue virus (DENV) infection yearly from Aedes mosquitoes stress the need for effective antivirals. No current drug effectively combats dengue efficiently. Transient immunity and severe risks highlight the need for broad-spectrum antivirals targeting all serotypes of DENV. Niclosamide, an antiparasitic, shows promising antiviral activity against the dengue virus, but enhancing its bioavailability is challenging. To overcome this issue and enable niclosamide to address the global dengue problem, nanoengineered niclosamides can be the solution. Not only does it address cost issues but also with its broad-spectrum antiviral effects nanoengineered niclosamide offers hope in addressing the current health crisis associated with DENV and will play a crucial role in combating other arboviruses as well.

The development of nanoformulations with simple compositions that can exert targeted combination therapy still remains a great challenge in the area of precision cancer nanomedicine. Herein, we report the design of a multifunctional nanoplatform based on methotrexate (MTX)-loaded layered double hydroxide (LDH) coated with chlorin e6 (Ce6)-modified MCF-7 cell membranes (CM M ) for combined chemo/sonodynamic therapy of breast cancer. LDH nanoparticles were in situ loaded with MTX via coprecipitation, and coated with CM M that were finally functionalized with phospholipid-modified Ce6. The created nanoformulation of LDH-MTX@CM M -Ce6 displays good colloidal stability under physiological conditions and can release MTX in a pH-dependent manner. We show that the formulation can homologously target breast cancer cells, and induce their significant apoptosis through arresting the cell cycle via cooperative MTX-based chemotherapy and ultrasound (US)-activated sonodynamic therapy. The assistance of US can not only trigger sonosensitizer Ce6 to produce reactive oxygen species, but also enhance the cellular uptake of LDH-MTX@CM M -Ce6 via an acoustic cavitation effect. Upon intravenous injection and US irradiation, LDH-MTX@CM M -Ce6 displays an admirable antitumor performance towards a xenografted breast tumor mouse model. Furthermore, the modification of Ce6 on the CM M endows the LDH-based nanoplatform with fluorescence imaging capability. The developed LDH-based nanoformulation here provides a general intelligent cancer nanomedicine platform with simple composition and homologous targeting specificity for combined chemo/sonodynamic therapy and fluorescence imaging of tumors.

Rationally designed ∼ 100 nm sized curcumin (CRC) loaded exfoliated layered double hydroxide nanoparticles (X-LDH/CRC-NPs) have been tested for its suitability as nanomedicine in non-small cell lung cancer (NSCLC) cell lines (A549 and NCI-H460) resulting enhanced apoptosis. Preclinical evaluation on A549 tumor bearing nude mouse model confirmed that such a well-designed X-LDH/CRC NPs would be highly advantageous for treating lung cancers., Competing Interests: Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier B.V. All rights reserved.)

Two-dimensional nanomaterials, particularly layered double hydroxides (LDHs), have been widely applied in the biomedical field owing to their biocompatibility, biodegradability, controllable drug release/loading ability, and enhanced cellular permeability. Since the first study analyzing intercalative LDHs in 1999, numerous studies have investigated their biomedical applications, including drug delivery and imaging; recent research has focused on the design and development of multifunctional LDHs. This review summarizes the synthetic strategies and in-vivo and in-vitro therapeutic actions and targeting properties of single-function LDH-based nanohybrids and recently reported (from 2019 to 2023) multifunctional systems developed for drug delivery and/or bio-imaging.

To date, cancer therapies largely consist of five pillars: surgery, radiation, chemotherapy, targeted therapy, and immunotherapy. Still, researchers are trying to innovate the current cancer therapies to pursue an ideal one without side effects. For developing such a therapy, we designed a chemically well-defined route to a PEG- and docetaxel (DTX)-conjugated inorganic polymer, polyphosphazene, named "polytaxel (PTX)" with a prolonged blood circulation time and tumor localization. Here, we conducted the proof-of-concept study of the ideal therapy in orthotopic and xenograft pancreatic cancer models. We found that the average tumor inhibition rates of PTX were similar to those of DTX without any DTX toxicity-related side effects, such as neutropenia and weight loss. In conclusion, PTX met the requirements of an ideal anticancer drug with high anticancer efficacy and 100% survival rate. PTX is expected to replace any existing anticancer therapies in clinical practice.

Recently, synthetic polymers have attracted great interest in the field of biomedical science. Among these, polyphosphazenes (PPZs) are regarded as one of the most promising materials, due to their structural flexibility and biodegradability compared to other materials. PPZs have been developed through numerous studies. In particular, multi-functionalized PPZs have been proven to be potential biomaterials in various forms, such as nanoparticles (NPs) and hydrogels, through the introduction of various functional groups. Thus, PPZs have been applied for the delivery of therapeutic molecules (low molecular weight drugs, genes and proteins), bioimaging, phototherapy, bone regeneration, dental liners, modifiers and medical devices. The main goal of the present review is to highlight the recent and the most notable existing PPZ-based biomaterials for aforementioned applications, with future perspectives in mind.

A quintinite nanoplate ( 64 Cu-QT-NP) isomorphically substituted with 64 Cu, as the positron emission tomography (PET) imaging material, was prepared via two-step processes. A 64 Cu labeling efficiency of 99% was realized, for the first time, by immobilizing the 64 Cu radioisotope directly in the octahedral site of the 2-dimensional (2D) quintinite lattice. Furthermore, the 64 Cu labeling stability of 64 Cu-QT-NPs was also achieved to be more than ∼99% in various solutions such as saline, phosphate-buffered saline (PBS), and other biological media (mouse and human serums). In an in vivo xenograft mouse model, the passive targeting behavior of 64 Cu-QT-NPs into tumor tissue based on the enhanced permeability and retention (EPR) effect was also demonstrated by parenteral administration, and successfully visualized using a PET scanner. For enhancing the tumor tissue selectivity, bovine serum albumin (BSA) was coated on 64 Cu-QT-NPs to form 64 Cu-QT-NPs/BSA, resulting in better colloidal stability and longer blood circulation time, which was eventually evidenced by the 2-fold higher tumor uptake rate when intravenousely injected in an animal model. It is, therefore, concluded that the present 64 Cu-QT-NPs/BSA with tumor tissue selectivity could be an advanced nano-device for radio-imaging and diagnosis as well.

Polymeric micelles, nanosized assemblies of amphiphilic polymers with a core-shell architecture, have been used as carriers for various therapeutic compounds. They have gained attention due to specific properties such as their capacity to solubilize poorly water-soluble drugs, biocompatibility, and the ability to accumulate in tumor via enhanced permeability and retention (EPR). Moreover, additional functionality can be provided to the micelles by a further modification. For example, micelle surface modification with targeting ligands allows a specific targeting and enhanced tumor accumulation. The introduction of stimuli-sensitive groups leads to the drug's release in response to environment change. This review highlights the progress in the development of multifunctional polymeric micelles in the field of cancer therapy. This review will also cover some examples of multifunctional polymeric micelles that are applied for tumor imaging and theragnosis.

Artesunic acid (AS 0 ), a derivative of artemisinin, is recommended for the treatment of severe and complicated malaria, but its use is limited because of limitations such as a short half-life, non-specific targeting capability, low bioavailability, etc . To overcome these issues, a novel 2D inorganic delivery shuttle system for an AS 0 drug to target the malarial host, red blood cells (RBCs), is explored by immobilizing AS 0 into 2D metal hydroxides to form AS - (artesunate, the deprotonated form of artesunic acid) nanohybrid drugs. Haemolysis assay showed that the AS - nanohybrids not only are haemo-compatible but also target RBCs due to the electrostatic interaction and hydrogen bonding between RBCs and AS - nanohybrids. As clearly demonstrated by the subsequent parasite lactate dehydrogenase assay, the antimalarial effect of the AS - nanohybrids is determined to be 6 times more effective than that of intact AS 0 against malaria. Therefore, the AS - nanohybrids with haemo-compatible 2D inorganic carriers could be the promising drug delivery systems for targeting the malarial host, RBCs.

Clay-based bio-inorganic nanohybrids, such as layered double hydroxides (LDH), have been extensively researched in the various fields of biomedicine, particularly for drug delivery and bio-imaging applications. Recent trends indicate that such two-dimensional LDH can be hybridized with a variety of photo-active biomolecules to selectively achieve anti-cancer benefits through numerous photo/chemotherapies (PCT), including photothermal therapy, photodynamic therapy, and magnetic hyperthermia, a combination of therapies to achieve the best treatment regimen for patients that cannot be treated either by surgery or radiation alone. Among the novel two-dimensional clay-based bio-inorganic nanohybrids, LDH could enhance the photo-stability and drug release controllability of the PCT agents, which would, in turn, improve the overall phototherapeutic performance. This review article highlights the most recent advances in LDH-based two-dimensional clay-bio-inorganic nanohybrids for the aforementioned applications.

Nanocomposites of hydrophobic organo-clay/polypropylene (organo-clay/PP) were efficiently developed through a solution-blending technique. For this, we utilized various smectite clays as host agents; namely, Na-montmorillonite (Mt, ~1000 nm), Na-fluorine mica (Mica, ~1500 nm), and Na-hectorite (Ht, ~60 nm) with varied sizes, layer charges, and aspect ratios. Such clays were functionalized with cetyltrimethylammonium (CTA) bromide via an intercalation technique to obtain hydrophobic organic clays. The as-made clay particles were further mixed with a PP/xylene solution; the latter was removed to obtain the final product of the CTA-clay/PP nanocomposite. An X-ray diffraction (XRD) analysis confirmed that there were no characteristic (001) diffraction peaks for CTA-Mica in the PP nanocomposites containing CTA-Mica, assuring the fact that the Mica layers could be completely exfoliated and thereby homogenously composited within the PP. On the other hand, the CTA-Mt and CTA-Ht incorporated composites had broader (001) peaks, which might have been due to the partial exfoliation of CTA-Mt and CTA-Ht in the composites. Among the three CTA-clay/PP nanocomposites, the CTA-Mica nanohybrid showed an enhanced thermal stability by ~42 °C compared to the intact host polymer matrix. We also noted that when the CTA-Mica content was ~9 mass % in the nanocomposites, the Young's modulus was drastically maximized to 69%. Our preliminary results therefore validated that out of the three tested clay-PP nanocomposites, the CTA-Mica nanofiller served as the best one to improve both the thermal and mechanical properties of the PP nanocomposites.

Although nicotinic acid (NA) has several clinical benefits, its potency cannot be fully utilized due to several undesirable side effects, including cutaneous flushing, GIT-associated symptoms, etc. To overcome such issues and improve the NA efficacy, a new inorganic-organic nanohybrids system was rationally designed. For making such a hybrid system, NA was intercalated into LDH through a coprecipitation technique and then coated with Eudragit ® S100 to make the final drug delivery system called Eudragit ® S100-coated NA-LDH. The as-made drug delivery system not only improved the NA release profile but also exhibited good bio-compatibility as tested on L929 cells. Such an inorganic-organic nanohybrid drug delivery agent is expected to reduce the undesirable side effects associated with NA and hopefully improve the pharmacological effects without inducing any undesirable toxicity.

Lung cancer is one of the most common cancers, affecting more than 2.1 million people across the globe every year. A very high occurrence and mortality rate of lung cancer have prompted active research in this area with both conventional and novel forms of therapies including the use of nanomaterials based drug delivery agents. Specifically, the unique physico-chemical and biological properties of porous nanomaterials have gained significant momentum as drug delivery agents for delivering a combination of drugs or merging diagnosis with targeted therapy for cancer treatment. This review focuses on the emergence of nano-porous materials for drug delivery in lung cancer. The review analyses the currently used nanoporous materials, including inorganic, organic and hybrid porous materials for delivering drugs for various types of therapies, including chemo, radio and phototherapy. It also analyses the selected research on stimuli-responsive nanoporous materials for drug delivery in lung cancer before summarizing the various findings and projecting the future of emerging trends. This review provides a strong foundation for the current status of the research on nanoporous materials, their limitations and the potential for improving their design to overcome the unique challenges of delivering drugs for the treatment of lung cancer., Competing Interests: No potential conflict of interest was reported by the author(s)., (© 2022 The Author(s). Published by National Institute for Materials Science in partnership with Taylor & Francis Group.)

Highlights: The g-C 3 N 4 monolayer in the perfect 2D limit was successfully realized, for the first time, by the well-defined chemical strategy based on the bottom-up process. The most striking evidence was made from Cs-high resolution transmission electron microscopy measurements by observing directly the atomic structure of g-C 3 N 4 unit cell, which was again supported by the corresponding high resolution transmission electron microscopy image simulation results. We demonstrated that the newly prepared g-C 3 N 4 monolayer showed outstanding photocatalytic activity for H 2 O 2 generation as well as excellent electrocatalytic activity for oxygen reduction reaction. The exfoliation of bulk graphitic carbon nitride (g-C 3 N 4 ) into monolayer has been intensively studied to induce maximum surface area for fundamental studies, but ended in failure to realize chemically and physically well-defined monolayer of g-C 3 N 4 mostly due to the difficulty in reducing the layer thickness down to an atomic level. It has, therefore, remained as a challenging issue in two-dimensional (2D) chemistry and physics communities. In this study, an "atomic monolayer of g-C 3 N 4 with perfect two-dimensional limit" was successfully prepared by the chemically well-defined two-step routes. The atomically resolved monolayer of g-C 3 N 4 was also confirmed by spectroscopic and microscopic analyses. In addition, the experimental Cs-HRTEM image was collected, for the first time, which was in excellent agreement with the theoretically simulated; the evidence of monolayer of g-C 3 N 4 in the perfect 2D limit becomes now clear from the HRTEM image of orderly hexagonal symmetry with a cavity formed by encirclement of three adjacent heptazine units. Compared to bulk g-C 3 N 4 , the present g-C 3 N 4 monolayer showed significantly higher photocatalytic generation of H 2 O 2 and H 2 , and electrocatalytic oxygen reduction reaction. In addition, its photocatalytic efficiency for H 2 O 2 production was found to be the best for any known g-C 3 N 4 nanomaterials, underscoring the remarkable advantage of monolayer formation in optimizing the catalyst performance of g-C 3 N 4 ., (© 2022. The Author(s).)

COVID-19 is a rapidly evolving emergency, which necessitates scientific community to come up with novel formulations that could find quick relief to the millions affected around the globe. Remdesivir being the only injectable drug by FDA for COVID-19, it initially showed promising results, however, later on failed to retain its claims, hence rejected by the WHO. Therefore, it is important to develop injectable formulation that are effective and affordable. Here in this work, we formulated poly ethylene glycol (PEG) coated bovine serum albumin (BSA) stabilized Niclosamide (NIC) nanoparticles (NPs) (∼BSA-NIC-PEG NPs) as an effective injectable formulation. Here, serum albumin mediated strategy was proposed as an effective strategy to specifically target SARS-CoV-2, the virus that causes COVID-19. The in-vitro results showed that the developed readily water dispersible formulation with a particle size <120 nm size were well stable even after 3 weeks. Even though the in-vitro studies showed promising results, the in-vivo pharmaco-kinetic (PK) study in rats demands the need of conducting further experiments to specifically target the SARS-CoV-2 in the virus infected model. We expect that this present formulation would be highly preferred for targeting hypoalbuminemia conditions, which was often reported in elderly COVID-19 patients. Such studies are on the way to summarize its potential applications in the near future., (Copyright © 2021. Published by Elsevier B.V.)

COVID-19 is a rapidly evolving emergency, for which there have been no specific medication found yet. Therefore, it is necessary to find a solution for this ongoing pandemic with the aid of advanced pharmaceutics. What is proposed as a solution is the repurposing of FDA approved drug such as niclosamide (NIC) having multiple pathways to inactivate the SARS-CoV-2, the specific virion that induces COVID-19. However, NIC is hardly soluble in an aqueous solution, thereby poor bioavailability, resulting in low drug efficacy. To overcome such a disadvantage, we propose here an oral formulation based on Tween 60 coated drug delivery system comprised of three different mesoporous silica biomaterials like MCM-41, SBA-15, and geopolymer encapsulated with NIC molecules. According to the release studies under a gastro/intestinal solution, the cumulative NIC release out of NIC-silica nanohybrids was found to be greatly enhanced to ~97% compared to the solubility of intact NIC (~40%) under the same condition. We also confirmed the therapeutically relevant bioavailability for NIC by performing pharmacokinetic (PK) study in rats with NIC-silica oral formulations. In addition, we discussed in detail how the PK parameters could be altered not only by the engineered porous structure and property, but also by interfacial interactions between ion-NIC dipole, NIC-NIC dipoles and/or pore wall-NIC van der Waals in the intra-pores of silica nanoparticles., Competing Interests: The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (© 2021 Published by Elsevier Inc.)

(1) Background: COVID-19 has affected millions of people worldwide, but countries with high experimental anti-SARS-CoV-2 vaccination rates among the general population respectively show progress in achieving general herd immunity in the population (a combination of natural and vaccine-induced acquired immunity), resulting in a significant reduction in both newly detected infections and mortality rates. However, the longevity of the vaccines' ability to provide protection against the ongoing pandemic is still unclear. Therefore, it is of utmost importance to have new medications to fight against the pandemic at the earliest point possible. Recently, it has been found that repurposing already existing drugs could, in fact, be an ideal strategy to formulate effective medication for COVID-19. Though there are many FDA-approved drugs, it has been found that niclosamide (NIC), an anthelmintic drug, has significantly high potential against the SARS-CoV-2 virus. (2) Methods: Here we deployed a simple self-assembling technique through which Zein nanoparticles were successfully used to encapsulate NIC, which was then coated with bovine serum albumin (BSA) in order to improve the drugs' stability, injectablity, and selectivity towards the virus-infected cells. (3) Results: The particle size for the BSA-stabilized Zein-NIC nanohybrid was found to be less than 200 nm, with excellent colloidal stability and sustained drug release properties. In addition, the nanohybrid showed enhanced drug release behavior under serum conditions, indicating that such a hybrid drug delivery system could be highly beneficial for treating COVID-19 patients suffering from high endothelial glycocalyx damage followed by a cytokine storm related to the severe inflammations.

COVID-19 has been affecting millions of individuals worldwide and, thus far, there is no accurate therapeutic strategy. This critical situation necessitates novel formulations for already existing, FDA approved, but poorly absorbable drug candidates, such as niclosamide (NIC), which is of great relevance. In this context, we have rationally designed NIC-loaded hydrotalcite composite nanohybrids, which were further coated with Tween 60 or hydroxypropyl methyl cellulose (HPMC), and characterized them in vitro. The optimized nanohybrids showed particle sizes <300 nm and were orally administrated to rats to determine whether they could retain an optimum plasma therapeutic concentration of NIC that would be effective for treating COVID-19. The pharmacokinetic (PK) results clearly indicated that hydrotalcite-based NIC formulations could be highly potential options for treating the ongoing pandemic and we are on our way to understanding the in vivo anti-viral efficacy sooner. It is worth mentioning that hydrotalcite-NIC nanohybrids maintained a therapeutic NIC level, even above the required IC 50 value, after just a single administration in 8-12 h. In conclusion, we were very successfully able to develop a NIC oral formulation by immobilizing with hydrotalcite nanoparticles, which were further coated with Tween 60 or HPMC, in order to enhance their emulsification in the gastrointestinal tract.

Niclosamide (NIC), a conventional anthelmintic agent, is emerging as a repurposed drug for COVID-19 treatment. However, the clinical efficacy is very limited due to its low oral bioavailability resulting from its poor aqueous solubility. In the present study, a new hybrid drug delivery system made of NIC, montmorillonite (MMT), and Tween 60 is proposed to overcome this obstacle. At first, NIC molecules were immobilized into the interlayer space of cationic clay, MMT, to form NIC-MMT hybrids, which could enhance the solubility of NIC, and then the polymer surfactant, Tween 60, was further coated on the external surface of NIC-MMT to improve the release rate and the solubility of NIC and eventually the bioavailability under gastrointestinal condition when orally administered. Finally, we have performed an in vivo pharmacokinetic study to compare the oral bioavailability of NIC for the Tween 60-coated NIC-MMT hybrid with Yomesan ® , which is a commercially available NIC. Exceptionally, the Tween 60-coated NIC-MMT hybrid showed higher systemic exposure of NIC than Yomesan ® . Therefore, the present NIC-MMT-Tween 60 hybrid can be a potent NIC drug formulation with enhanced solubility and bioavailability in vivo for treating Covid-19.

Semiconducting polymer nanoparticles (SPN) have been emerging as novel functional nano materials for phototherapy which includes PTT (photo-thermal therapy), PDT (photodynamic therapy), and their combination. Therefore, it is important to look into their recent developments and further explorations specifically in cancer treatment. Therefore, the present review describes novel semiconducting polymers at the nanoscale, along with their applications and limitations with a specific emphasis on future perspectives. Special focus is given on emerging and trending semiconducting polymeric nanoparticles in this review based on the research findings that have been published mostly within the last five years.

Advanced nanotechnology has been emerging rapidly in terms of novel hybrid nanomaterials that have found various applications in day-to-day life for the betterment of the public. Specifically, gold, iron, silica, hydroxy apatite, and layered double hydroxide based nanohybrids have shown tremendous progress in biomedical applications, including bio-imaging, therapeutic delivery and photothermal/dynamic therapy. Moreover, recent progress in up-conversion nanohybrid materials is also notable because they have excellent NIR imaging capability along with therapeutic benefits which would be useful for treating deep-rooted tumor tissues. Our present review highlights recent developments in inorganic-inorganic nanohybrids, and their applications in bio-imaging, drug delivery, and photo-therapy. In addition, their future scope is also discussed in detail., Competing Interests: There are no conflicts to declare., (This journal is © The Royal Society of Chemistry.)

Layered double hydroxide (LDH) has been a big challenge in exploring new hybrid materials by intercalating inorganic, organic, or bio molecules into their lamellar lattice, those which often showed dual functions from each other or new mutative properties. Recently, nano-bio convergence technology becomes one of the most extensively studied research fields in the view point of developing advanced drugs and diagnostic agents to fight against disease and eventually to improve the lives of human beings. Therefore, LDH as one of the nanomaterials have been intensively investigated not only as biocompatible drug delivery vehicle for cancer chemotherapy but also as diagnostic and imaging agents. In the present review, we have attempted to summarize theranostic functions of drug-LDH hybrid nanoparticles including their synthetic methods, physico-chemical and biological properties, and their unique mechanism overcoming drug resistance, and targeting properties based on in vitro and finally in vivo results. This article is categorized under: Diagnostic Tools > Diagnostic Nanodevices Diagnostic Tools > in vivo Nanodiagnostics and Imaging., (© 2020 Wiley Periodicals LLC.)

The ongoing pandemic, COVID-19 (SARS-CoV-2), has afflicted millions of people around the world, necessitating that the scientific community work, diligently and promptly, on suitable medicaments. Although vaccination programs have been run globally, the new variants of COVID-19 make it difficult to restrict the spread of the virus by vaccination alone. The combination of vaccination with anti-viral drug formulation is an ideal strategy for tackling the current pandemic situation. Drugs approved by the United States Food and Drug Administration (FDA), such as Remdesivir, have been found to be of little or no benefit. On the other hand, re-purposing of FDA-approved drugs, such as niclosamide (NIC), has offered promise but its applicability is limited due to its poor aqueous solubility and, therefore, low bioavailability. With advanced nano-pharmaceutical approaches, re-purposing this drug in a suitable drug-carrier for a better outcome may be possible. In the current study, an attempt was made to explore the loading of NIC into exfoliated layered double hydroxide nanoparticles (X-LDH NPs); prepared NIC-X-LDH NPs were further modified with eudragit S100 (ES100), an enteric coating polymer, to make the final product, ES100-NIC-X-LDH NPs, to improve absorption by the gastro/intestinal tract (GIT). Furthermore, Tween 60 was added as a coating on ES100-NIC-X-LDH NPs, not just to enhance its in vitro and in vivo stability, but also to enhance its mucoadhesive property, and to obtain, ultimately, better in vivo pharmacokinetic (PK) parameters upon oral administration. Release of NIC from Tween 60-ES100-NIC-X-LDH NPs was found to be greater under gastro/intestinal solution within a shorter period of time than the uncoated samples. The in vivo analysis revealed that Tween 60-ES100-NIC-X-LDH NPs were able to maintain a therapeutically relevant NIC plasma concentration in terms of PK parameters compared to the commercially available Yomesan®, proving that the new formulation might prove to be an effective oral drug-delivery system to deal with the SARS-CoV-2 viral infections. Further studies are required to ensure their safety and anti-viral efficacy., Supplementary Information: The online version contains supplementary material available at 10.1007/s42860-021-00153-6., Competing Interests: Conflict of InterestThe authors declare that they have no conflict of interest., (© The Clay Minerals Society 2021.)

Brimonidine (BMD) is often prescribed as an eye drop to reduce the intraocular pressure (IOP) for glaucoma treatment. However, eye drops are limited by rapid clearance from the preocular surface, and hence a low ocular drug bioavailability. Therefore, in this study, we propose montmorillonite (MMT), as a delivery carrier, hybridized with BMD (BMD-MMT) for topical drug delivery to the eye. The BMD-MMT hybrid was prepared by intercalating the BMD molecules in the interlayer space of the MMT lattice via ion-exchange reaction; it was then formulated with polyvinyl alcohol (PVA) to produce a dry tablet (i.e., BMD-MMT@PVA). The BMD-MMT@PVA hybrid drug released BMD in a sustained manner for more than 5 h under in vitro conditions. When the hybrid drug was administered to rabbit eyes in vivo, 43% and 18.5% BMD-MMT still remained on the preocular surface for 10 and 60 min after administration, respectively. Thus, the BMD-MMT@PVA hybrid drug exhibited a prolonged decrease in IOP, that is, for 12 h, which was approximately two times longer than that observed with the commercially available BMD eye drop, Alphagan® P.

Multidrug resistance (MDR) is regarded as a main obstacle for effective chemotherapy, and P-glycoprotein (P-gp)-mediated drug efflux has been demonstrated to be the key factor responsible for MDR. In this study, a novel pH-responsive hybrid drug delivery system was developed by conjugating d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), a kind of P-gp inhibitor, on the surface of laponite nanodisks to overcome MDR. The prepared LM-TPGS display excellent colloidal stability, a high encapsulation efficiency of doxorubicin (DOX), and a pH-responsive drug release profile. In vitro experiments verified that LM-TPGS/DOX could exhibit significantly enhanced therapeutic efficacy in treating DOX-resistant breast cancer cells (MCF-7/ADR) through inhibiting the activity of P-gp-mediated drug efflux and effectively accumulating DOX within cancer cells. In vivo results revealed that LM-TPGS/DOX outstandingly suppressed MCF-7/ADR tumors with low side effects. Therefore, the high drug payload, enhanced inhibition efficacy to drug-resistant cells, and low side effects make the LM-TPGS/DOX a promising nanoplatform to reverse MDR for effective chemotherapy., (© 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Hexagonal and wormhole-type mesoporous geopolymers were developed by controlling the concentration of a structure directing agent (cetrimonium bromide, CTAB) with fixed ratios of Si/Al, KOH/(Si + Al), and H 2 O/(Si + Al), and their detailed porous structures were confirmed by TEM, N 2 adsorption-desorption and X-ray diffraction measurements. The as-prepared geopolymers were then used as templates to replicate porous carbons with various structures and porosities for CO 2 adsorption. To understand the correlation between the CO 2 adsorptivity and porous structures, we tuned the porosity of the geopolymer-templated carbons by modifying the structures of the geopolymers. The porous carbons obtained from the hexagonal-type porous geopolymers were found to be composed of the aggregates of carbon nanowires exhibiting large particles, while those obtained from the wormhole-like porous geopolymers were determined to be wormhole type as well, as evidenced by TEM and X-ray diffraction studies. According to the CO 2 adsorption isotherms of the porous carbons, the aggregates of carbon nanowires exhibited the highest CO 2 adsorptivity due to their highest microporosity and largest specific surface area., Competing Interests: There are no conflicts to declare., (This journal is © The Royal Society of Chemistry.)

Implantable devices for on-demand and pulsatile drug delivery have attracted considerable attention; however, many devices in clinical use are embedded with the electronic units and battery inside, hence making them large and heavy for implantation. Therefore, we propose an implantable device with multiple drug reservoirs capped with a stimulus-responsive membrane (SRM) for on-demand and pulsatile drug delivery. The SRM is made of thermosensitive POSS(MEO 2 MA-co-OEGMA) and photothermal nanoparticles of reduced graphene oxide (rGO), and each of the drug reservoirs is filled with the same amount of human growth hormone (hGH). Therefore, with noninvasive near-infrared (NIR) irradiation from the outside skin, the rGO nanoparticles generate heat to rupture the SRM in the implanted device, which can open a single selected drug reservoir to release hGH. Therefore, the device herein is shown to release hGH reproducibly only at the times of NIR irradiation without drug leakage during no irradiation. When implanted in rats with growth hormone deficiency and irradiated with an NIR light from the outside skin, the device exhibits profiles of hGH and IGF1 plasma concentrations, as well as body weight change, similar to those in animals treated with conventional s.c. hGH injections., Competing Interests: The authors declare no conflict of interest.

The nanostructure and morphology of mesoporous carbon obtained from a newly designed porous geopolymer template were characterized by low-voltage high-resolution scanning electron microscopy. The present porous carbon exhibited a large specific surface area and pore volume, resulting in a high CO2 uptake capacity.

Background: Alendronate (AL), a drug for inhibiting osteoclast-mediated bone-resorption, was intercalated into an inorganic drug delivery nanovehicle, layered double hydroxide (LDH), to form a new nanohybrid, AL-LDH, with 1:1 heterostructure along the crystallographic C-axis. Based on the intercalation reaction strategy, the present AL-LDH drug delivery system (DDS) was realized with an enhanced drug efficacy of AL, which was confirmed by the improved proliferation and osteogenic differentiation of osteoblast-like cells (MG63)., Methods: The AL-LDH nanohybrid was synthesized by conventional ion-exchange reaction and characterized by powder X-ray diffraction (PXRD), high-resolution transmission electron microscopy (HR-TEM), and Fourier transform infrared (FT-IR) spectroscopy. Additionally, in vitro efficacy tests, such as cell proliferation and alkaline phosphatase (ALP) activity, were analyzed., Results: The AL was successfully intercalated into LDH via ion-exchange reaction, and thus prepared AL-LDH DDS was X-ray single phasic and chemically well defined. The accumulated AL content in MG63 cells treated with the AL-LDH DDS nanoparticles was determined to be 10.6-fold higher than that within those treated with the intact AL after incubation for 1 hour, suggesting that intercellular permeation of AL was facilitated thanks to the hybridization with drug delivery vehicle, LDH. Furthermore, both in vitro proliferation level and ALP activity of MG63 treated with the present hybrid drug, AL-LDH, were found to be much more enhanced than those treated with the intact AL. This is surely due to the fact that LDH could deliver AL drug very efficiently, although LDH itself does not show any effect on proliferation and osteogenic differentiation of MG63 cells., Conclusion: The present AL-LDH could be considered as a promising DDS for improving efficacy of AL., Competing Interests: Disclosure: The authors have no potential conflicts of interest to disclose.

Layered double hydroxides (LDHs) with two dimensional structure have been attracted considerable interest in exploring new intercalative nanohybrids, such as inorganic-LDHs, organic-LDHs and bio-LDHs ones, which often exhibit extraordinarily synergetic effects and complementary performances. More recently, bio-related nanotechnology becomes one of the most essential research field in the viewpoint of the health and safety of human being. In this regard, LDHs have been focused as an important inorganic material for gene and drug delivery carriers with imaging and targeting functions. In the present review, an attempt has been made to describe gene delivery systems based on LDH nanoparticles in terms of synthetic routes of gene-LDH nanohybrids, their physico-chemical properties, intercellular uptake mechanisms, intracellular trafficking pathways and drug resistance, and passive and active targeting functions in in-vitro and in-vivo, and finally imaging functions. And recent studies of gene-therapies with LDHs are also discussed from the viewpoint of state-of-the-art nanohybrids technology., (© 2018 The Chemical Society of Japan & Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

This paper presents the results of zeta potential, water contact angle, atomic force microscopy image, in vitro solubility, and content of heavy metals in polylactic acid (PLA)/chitosan (CS) nanoparticles loading nifedipine. In addition, the In Vivo test of the PLA/CS nanoparticles loading nifedipine in the mice is also one of highlights of this work. The Zeta potential result shows that the charged surface of the PLA/CS nanoparticles loading nifedipine is neutral, negative or complex depending on nifedipine content. Nifedipine plays a role in increase of hydrophobic property, swelling degree and regular surface as well as decrease of surface rough of the nanoparticles. The PLA/CS/nifedipine nanoparticles are dissolved in the solutions with pH 6.8, pH 4.5 and pH 1.2. The In Vivo test of PLA/CS nanoparticles loading nifedipine on mice was evaluated by the change in diastolic pressure, systolic pressure, arterial pressure and heart rate. The obtained results confirm that the PLA/CS nanoparticles loading nifedipine is suitable to apply in the treatment of hypertension patients lately.

Efficient visible light active hybrid photocatalysts for H 2 production can be synthesized by the intercalative hybridization of Zn-Cr-layered double hydroxide (Zn-Cr-LDH) with a mesoporous g-C 3 N 4 lattice. Small Zn-Cr-LDH nanocrystals with a size of ∼6 nm are immobilized in the mesopores of g-C 3 N 4 . Beyond an optimal LDH/g-C 3 N 4 molar ratio of 0.3, a further increase in the LDH content leads to the surface deposition of LDH crystals on the g-C 3 N 4 material as well as the intercalative immobilization of LDH into its mesopores, indicating the controllability of the LDH deposition site. The Zn-Cr-LDH-g-C 3 N 4 nanohybrids exhibit smaller surface areas than the pristine g-C 3 N 4 , confirming the intercalative stabilization of Zn-Cr-LDH nanocrystals in the mesopore of g-C 3 N 4 . The hybridization between Zn-Cr-LDH and g-C 3 N 4 is effective in enhancing visible light absorptivity and also in depressing electron-hole recombination, which is attributable to an efficient electronic coupling between both the hybridized components. The present Zn-Cr-LDH-g-C 3 N 4 nanohybrid exhibits promising photocatalytic activities for visible light-induced H 2 production at a rate of 155.7 μmol g -1 h -1 , which is much superior to that of the pristine g-C 3 N 4 (21.7 μmol g -1 h -1 ). The present study underscores that the intercalative immobilization of Zn-Cr-LDH crystals in the limited space of a mesopore is quite useful in improving the visible light active photocatalyst functionality of mesoporous carbon nitride.

Stem cell therapy for damaged cartilage suffers from low rates of retention, survival, and differentiation into chondrocytes at the target site. To solve these problems, here we propose a two-dimensional/three-dimensional (2D/3D) nanocomposite system. As a new two-dimensional (2D) material, hexagonal layered double hydroxides (LDHs) with a uniform lateral length of 2-3 μm were prepared by a hydrothermal process. Then, tonsil-derived mesenchymal stem cells (TMSCs), arginylglycylaspartic acid-coated LDHs, and kartogenin (KGN) were incorporated into the gel through the thermal-energy-driven gelation of the system. The cells exhibited a tendency to aggregate in the nanocomposite system. In particular, chondrogenic biomarkers of type II collagen and transcription factor SOX 9 significantly increased at both the mRNA and protein levels in the nanocomposite system, compared to the pure thermogel systems. The inorganic 2D materials increased the rigidity of the matrix, slowed down the release of a soluble factor (KGN), and improved cell-material interactions in the gel. The current 2D/3D nanocomposite system of bioactive LDH/thermogel can be a new platform material overcoming drawbacks of hydrogel-based 3D cell culture systems and is eventually expected to be applied as an injectable stem cell therapy.

Single particle Mie calculations of near micron-sized TiO 2 particles predict strong light scattering dominating the visible range that would give rise to a white appearance. We demonstrate that a polydisperse collection of these "white" particles can result in the generation of visible colors through ensemble scattering. The weighted averaging of the scattering over the particle size distribution modifies the sharp, multiple, high order scattering modes from individual particles into broad variations in the collective extinction. These extinction variations are apparent as visible colors for particles suspended in organic solvent at low concentration, or for a monolayer of particles supported on a transparent substrate viewed in front of a white light source. We further exploit the color variations on optical sensitivity to the surrounding environment to promote micron-sized TiO 2 particles as stable and robust agents for detecting the optical index of homogeneous media with high contrast sensitivities. Such distribution-modulated scattering properties provide TiO 2 particles an intriguing opportunity to impart color and optical sensitivity to their widespread electronic and chemical platforms such as antibacterial windows, catalysis, photocatalysis, optical sensors, and photovoltaics.

Correction for 'Mesoporous carbon nitrides: synthesis, functionalization, and applications' by Kripal S. Lakhi et al., Chem. Soc. Rev., 2017, DOI: .

Mesoporous carbon nitrides (MCNs) with large surface areas and uniform pore diameters are unique semiconducting materials and exhibit highly versatile structural and excellent physicochemical properties, which promote their application in diverse fields such as metal free catalysis, photocatalytic water splitting, energy storage and conversion, gas adsorption, separation, and even sensing. These fascinating MCN materials can be obtained through the polymerization of different aromatic and/or aliphatic carbons and high nitrogen containing molecular precursors via hard and/or soft templating approaches. One of the unique characteristics of these materials is that they exhibit both semiconducting and basic properties, which make them excellent platforms for the photoelectrochemical conversion and sensing of molecules such as CO 2 , and the selective sensing of toxic organic acids. The semiconducting features of these materials are finely controlled by varying the nitrogen content or local electronic structure of the MCNs. The incorporation of different functionalities including metal nanoparticles or organic molecules is further achieved in various ways to develop new electronic, semiconducting, catalytic, and energy harvesting materials. Dual functionalities including acidic and basic groups are also introduced in the wall structure of MCNs through simple UV-light irradiation, which offers enzyme-like properties in a single MCN system. In this review article, we summarize and highlight the existing literature covering every aspect of MCNs including their templating synthesis, modification and functionalization, and potential applications of these MCN materials with an overview of the key and relevant results. A special emphasis is given on the catalytic applications of MCNs including hydrogenation, oxidation, photocatalysis, and CO 2 activation.

A bioabsorbable polymeric bone plate enabled with both diagnostic and therapeutic functionalities (radiopacity and sustained drug release, respectively) is proposed. To this end, a drug-inorganic nanohybrid (RS-LDH) is examined as a theranostic agent by intercalating an anti-resorptive bone remodeling drug, risedronate (RS) into a layered double hydroxide (LDH) via an ion-exchange reaction. The RS-LDH is prepared as a sheet with a biodegradable polymer, poly(lactic-co-glycolic acid), and is then attached onto the clinically approved bioabsorbable bone plate to produce the theranostic plate. Because of the presence of the metals in the LDH, the theranostic plate results in discernible in vivo X-ray images for up to four weeks after implantation. Concurrently, bone regeneration is also significantly improved compared with the other control groups, likely because of this material's sustained drug-release property. The theranostic plate is also largely biocompatible, similar to the plate already approved for clinical use. It is concluded that the combination of a biodegradable bone plate with RS-LDH nanohybrids can constitute a promising system with theranostic ability in both X-ray diagnosis and expedited bone repair., (© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

The biodegradable inorganic nanovector based on a layered double hydroxide (LDH) holds great promise for gene and drug delivery systems. However, in vivo targeted delivery of genes through LDH still remains a key challenge in the development of RNA interference therapeutics. Here, we describe in vivo and in vitro delivery system for Survivin siRNA (siSurvivin) assembled with passive LDH with a particle size of 100 nm or active LDH conjugated with a cancer overexpressing receptor targeting ligand, folic acid (LDHFA), conferring them an ability to target the tumor by either EPR-based clathrin-mediated or folate receptor-mediated endocytosis. When not only transfected into KB cells but also injected into xenograft mice, LDHFA/siSurvivin induced potent gene silencing at mRNA and protein levels in vitro, and consequently achieved a 3.0-fold higher suppression of tumor volume than LDH/siSurvivin in vivo. This anti-tumor effect was attributed to a selectively 1.2-fold higher accumulation of siSurvivin in tumor tissue compared with other organs. Targeting to the tumor with inorganic nanovector can guide and accelerate an evolution of next-generation theranosis system., (© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

A universal technology for the encapsulative protection of unstable anionic species by highly stable layered metal oxide has been developed via the surface modification of a metal oxide nanosheet. The surface anchoring of (3-aminopropyl)triethoxysilane (APTES) on exfoliated titanate nanosheet yields a novel cationic metal oxide nanosheet, which can be universally used for the hybridization with various biological and inorganic anions. The encapsulation of deoxyribonucleic acid (DNA) in the cationic APTES-anchored titanate lattice makes possible the reliable long-term protection of DNA against enzymatic, chemical, and UV-vis light corrosions. The encapsulated DNA can be easily released from the titanate lattice via sonication, underscoring the functionality of the cationic APTES-anchored titanate nanosheet as a stable nanocontainer for DNA. The APTES-anchored titanate nanosheet can be also used as an efficient CO2 adsorbent and a versatile host material for various inorganic anions like polyoxometalates, leading to the synthesis of novel intercalative nanohybrids with unexplored properties and useful functionalities.

Focus here is placed on the pharmaceutical and biomedical applications of novel clay-drug hybrid materials categorized by methods of administration. Clay minerals have been used for many years as pharmaceutical and medicinal ingredients for therapeutic purposes. A number of studies have attempted to explore clay-drug hybrid materials for biomedical applications with desired functions, such as sustained release, increased solubility, enhanced adsorption, mucoadhesion, biocompatibility, targeting, etc. The present review attempts not only to summarize the state-of-the-art of clay-drug hybrid materials and their advantages, depending on the methods of administration, but also to deal with challenges and future perspectives of clay mineral-based hybrids for biomedical applications., (© The Clay Minerals Society 2016.)

Artesunic acid (ASH), an antimalarial drug, has low oral bioavailability due to its low aqueous solubility. To overcome this problem, artesunate (AS) was intercalated into zinc basic salt (ZBS) via co-precipitation. AS was immobilized with a tilted double layer arrangement, which was also confirmed by XRD and 1-D electron density mapping. In order to decrease the release rate of AS under gastrointestinal conditions and to simultaneously increase the release rate of AS under intestinal conditions, ZBS-AS was coated with EUDRAGIT L100 (ZBS-AS-L100). Finally, we performed an in-vivo pharmacokinetic study to compare the oral bioavailability of AS of ZBS-AS-L100 with that of ASH. Surprisingly, it was found that the former is 5.5 times greater than the latter due to an enhanced solubility of AS thanks to the ternary hybridization with ZBS and EUDRAGIT L100. Therefore, the present ZBS-AS-L100 system has a great potential as a novel antimalarial drug formulation with pH selectivity and enhanced bioavailability., (© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Ordered porous carbon films with tunable pore diameters, immobilized with glucose oxidase (GOD) have been fabricated and employed for the construction of a biosensor for glucose molecules. The as-prepared porous films have large specific surface areas and highly ordered porous structure with uniform pore sizes, which are critical for the immobilization of large amounts of GOD and support the promotion of heterogeneous electron transfer. The developed biosensors give enough room for the encapsulation of a high amount of GOD molecules and show excellent biosensing performance with a linear response to glucose concentration ranging from 0.5 to 9 mM and a detection limit of 1.5 μM. It is also demonstrated that the sensitivity of the biosensor can be easily tuned by modulating the pore size of carbon film as it dictates the amount of immobilization of GOD in the porous channels. The fabricated carbon-film-based biosensor has a good stability and a high reproducibility, which opens the gateway for the commercialization of this excellent technology., (© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Novel mesoporous BN and BCN materials with cage type porous structure and spherical morphology have been synthesized using carbon nanocages with 3D porous structure as a template via an elemental substitution method at a low synthesis temperature. The obtained materials exhibit a large specific pore volume with uniform pore size distribution and the specific surface area ranging from 945 to 1023 m(2) g(-1).

The preparation of size-controllable Fe2O3 nanoparticles grown in nanoporous carbon with tuneable pore diameters is reported. These hybrid materials exhibit strong non-linear magnetic properties and a magnetic moment of approximately 229 emu g(-1), which is the highest value ever reported for nanoporous hybrids, and can be attributed to the nanosieve effect and the strong interaction between the nanoparticles and the carbon walls., (© 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)