Janus nanocarriers for magnetically targeted and hyperthermia-enhanced curcumin therapy of liver cancer

Curcumin is regarded as a promising chemotherapeutic agent due to its anti-cancer activity and excellent biosafety. Nevertheless, the poor bioavailability and insufficient therapeutic efficacy have limited its further application in the clinic. Hence, we designed Janus magnetic mesoporous silica nanoparticles (Janus M-MSNs) for magnetically targeted and hyperthermia-enhanced curcumin treatment of liver cancer. In this study, curcumin was loaded into the silica components of Janus M-MSNs via surface-decorated pH-sensitive groups. Janus M-MSNs-Cur exhibited superior superparamagnetic properties, high curcumin loading ability and a tumor microenvironment-responsive curcumin release fashion. Additionally, an external magnetic field promoted the anti-tumor effectiveness of Janus M-MSNs-Cur through increasing the cellular internalization of Janus M-MSNs-Cur. More importantly, magnetic hyperthermia therapy supplemented the chemotherapeutic effect through a synergistic effect. Our outcomes demonstrated that Janus M-MSNs-Cur possessed a high therapeutic efficiency and excellent biosafety both in vitro and in vivo, indicating that Janus M-MSNs-Cur might be a promising therapeutic agent for liver cancer treatment.

Curcumin is regarded as a promising chemotherapeutic agent due to its anti-cancer activity and excellent biosafety.     

Conjugation with gold nanoparticles improves the stability of the KT2 peptide and maintains its anticancer properties

One of the major weaknesses of therapeutic peptides is their sensitivity to degradation by proteolytic enzymes in vivo. Gold nanoparticles (GNPs) are a good carrier for therapeutic peptides to improve their stability and cellular uptake in vitro and in vivo. We conjugated the anticancer KT2 peptide as an anticancer peptide model to PEGylated GNPs (GNPs-PEG) and investigated the peptide stability, cellular uptake and ability of the GNPs-KT2-PEG conjugates to induce MDA-MB-231 human breast cancer cell death. We found that 11 nm GNPs protected the conjugated KT2 peptide from trypsin proteolysis, keeping it stable up to 0.128% trypsin, which is higher than the serum trypsin concentration (range 0.0000285 ± 0.0000125%) reported by Lake-Bakaar, G. et al., 1979. GNPs significantly enhanced the cellular uptake of KT2 peptides after conjugation. Free KT2 peptides pretreated with trypsin were not able to kill MDA-MB-231 cells due to proteolysis, while GNPs-KT2-PEG was still able to exert effective cancer cell killing after trypsin treatment at levels comparable to GNPs-KT2-PEG without enzyme pretreatment. The outcome of this study highlights the utility of conjugated anticancer peptides on nanoparticles to improve peptide stability and retain anticancer ability.

One of the major weaknesses of therapeutic peptides is their sensitivity to degradation by proteolytic enzymes in vivo.     

A comprehensive study of eriocitrin metabolism in vivo and in vitro based on an efficient UHPLC-Q-TOF-MS/MS strategy

Eriocitrin, a main flavonoid in lemons, possesses strong antioxidant, lipid-lowering and anticancer activities and has long been used in food, beverages and wine. However, its metabolism in vivo and in vitro is still unclear. In this study, an efficient strategy was developed to detect and identify metabolites of eriocitrin by using ultra-high-performance liquid chromatography coupled with hybrid triple quadrupole time-of-flight mass spectrometry (UHPLC-Q-TOF-MS) based on online data acquisition and multiple data processing techniques. A total of 32 metabolites in vivo and 27 metabolites in vitro were obtained based on the above method. Furthermore, the main metabolic pathways of eriocitrin included reduction, hydrogenation, N-acetylation, ketone formation, oxidation, methylation, sulfate conjugation, glutamine conjugation, glycine conjugation, desaturation and demethylation to carboxylic acid. This study will lay a foundation for further studies on the metabolic mechanisms of eriocitrin.

41 metabolites of eriocitrin in vivo and in vitro was identified based on the efficient UHPLC-Q-TOF-MS/MS strategy.     

Parent and nano-encapsulated ytterbium(iii) complex toward binding with biological macromolecules,in vitro cytotoxicity,cleavage and antimicrobial activity studies

To determine the chemotherapeutic and pharmacokinetic aspects of an ytterbium complex containing 2,9-dimethyl-1,10-phenanthroline (Me₂Phen), in vitro binding studies were carried out with FS-DNA/BSA by employing multiple biophysical methods and a molecular modeling study. There are different techniques including absorption spectroscopy, fluorescence spectroscopy, circular dichroism studies, viscosity experiments (only in the case of DNA), and competitive experiments used to determine the interaction mode between DNA/BSA and the ytterbium-complex. The results showed that the Yb-complex exhibited a high propensity for the interaction of BSA and DNA via hydrophobic interactions and van der Waals forces. Further, a competitive examination and docking study showed that the interaction site of the ytterbium complex on BSA is site III. The results of docking calculations for DNA/BSA were in good agreement with experimental findings. The complex displays efficient DNA cleavage in the presence of hydrogen peroxide. Moreover, antimicrobial studies of different bacteria and fungi indicated its promising antibacterial activity. In vitro cytotoxicity studies of the Yb-complex, starch nano-encapsulated, and lipid nano-encapsulated were carried out in MCF-7 and A-549 cell lines, which revealed significantly good activity. The results of anticancer activity studies showed that the cytotoxic activity of the Yb-complex was increased when encapsulated with nanocarriers. Based on biological applications of the Yb-complex, it can be concluded that this complex and its nanocarriers can act as novel anticancer and antimicrobial candidates.

The biological applications of Yb-complexes including anticancer, antimicrobial and DNA cleavage ability, and their interaction with FS-DNA and BSA were examined.     

Effects of pore size on in vitro and in vivo anticancer efficacies of mesoporous silica nanoparticles

Mesoporous silica nanoparticles (MSN) have been widely applied for drug delivery systems. To investigate the effects of pore size on anticancer efficacies, MSN with different pore sizes but similar particle sizes and surface charges were synthesized via a microemulsion method. The pore structures of MSN were characterized by transmission electron microscopy (TEM), small-angle X-ray scattering (SAXS), and N₂ adsorption–desorption isotherms. Doxorubicin loaded MSN (DOX/MSN) were prepared and the minimum drug loading capacity was detected in DOX/MSN with a pore size of 2.3 nm (DOX/MSN2). DOX/MSN with a pore size of 8.2 nm (DOX/MSN8) showed a comparable drug loading amount in comparison with ones with a pore size of 5.4 nm (DOX/MSN5). In vitro drug release profiles showed that DOX/MSN5 could release DOX quickly and completely. Compared with DOX/MSN2 and DOX/MSN8, DOX/MSN5 showed the higher cellular uptake and nucleic concentration of DOX in QGY-7703 cells, which led to efficient cell-apoptosis induction and anti-proliferation effect, and thus the optimal in vivo anticancer activities. Taken together, these results highlighted the importance of pore size in anticancer efficacies, which would serve as a guideline in the rational design of MSN for cancer therapy.

MSN with suitable pore sizes achieved an outstanding performance for in vitro and in vivo antitumor efficacies.     

Dual stimuli-responsive polyphosphazene-based molecular gates for controlled drug delivery in lung cancer cells

A switchable silane derived stimuli-responsive bottle-brush polyphosphazene (PPz) was prepared and attached to the surface of mesoporous silica nanoparticles (MSNs). The hybrid polymer with PEG-like Jeffamine® M-2005 side-arms undergo conformational changes in response to both pH and temperature due to its amphiphilic substituents and protonatable main-chain, hence were investigated as a gatekeeper. Safranin O as control fluorophore or the anticancer drug camptothecin (CPT) were encapsulated in the PPz-coated MSNs. At temperatures below the lower critical solution temperature (LCST), the swollen conformation of PPz efficiently blocked the cargo within the pores. However, above the LCST, the PPz collapsed, allowing release of the payload. Additionally, protonation of the polymer backbone at lower pH values was observed to enhance opening of the pores from the surface of the MSNs and therefore the release of the dye. In vitro studies demonstrated the ability of these nanoparticles loaded with the drug camptothecin to be endocytosed in both models of tumor (A549) and healthy epithelial (BEAS-2B) lung cells. Their accumulation and the release of the chemotherapeutic drug, co-localized within lysosomes, was faster and higher for tumor than for healthy cells, further, the biocompatibility of PPz-gated nanosystem without drug was demonstrated. Tailored dual responsive polyphosphazenes thus represent novel and promising candidates in the construction of future gated mesoporous silica nanocarriers designs for lung cancer-directed treatment.

Bottle-brush polyphosphazenes as dual, thermosensitive and pH responsive gatekeepers for mesoporous silica nanoparticles, and their use in controlled drug release.     

Comparative study of young shoots and the mature red headed cabbage as antioxidant food resources with antiproliferative effect on prostate cancer cells

The increasing knowledge on health benefit properties of plant origin food ingredients supports recommendations for the use of edible plants in the prevention of diet related diseases, including cancer. The beneficial effects of young shoots of red cabbage can be attributed to their mixture of phytochemicals possessing antioxidant and potential anticancer activity. The objective of this study was to compare the content of bioactive compounds, including HPLC analysis of polyphenols and antioxidant activity of young shoots of red cabbage and the vegetable at full maturity. The content of vitamin C and polyphenols in juices obtained from young shoots and the mature vegetable were also determined. The other aim of this study was to confirm the hypothesis that juice of young shoots more effectively, compared to juice of the mature vegetable, reduces the proliferation of prostate cancer cell lines DU145 and LNCaP in vitro. A significantly higher content of vitamin C and carotenoids, as well as a higher antioxidant activity were found in edible young shoots in comparison to the mature vegetable. In addition, studies have shown higher amount of vitamin C in the juice of young shoots than in the juice of the mature vegetable and similar content of polyphenolic compounds. The level of total polyphenol content in the studied plant samples did not differ significantly. Flavonoids were the main polyphenols in young shoots and juice obtained from them, while phenolic acids were dominant in the mature vegetable and in juice obtained from it. The juice of young shoots has shown stronger in vitro anti-proliferation effect against prostate cancer cells than juice of the mature vegetable.

Young shoots of red cabbage could be a good source of phytochemicals with potential anticancer activity.     

Fungal melanin as a biocompatible broad-spectrum sunscreen with high antioxidant activity

Melanin is considered a bio-inspired dermo-cosmetic component due to its high UV absorption and antioxidant activity. Among various melanin sources, fungal melanin is a promising candidate for sunscreen because of its sustainability and scalability; however, quantitative assessment of its function has not yet been sufficiently explored. In this study, melanin samples derived from Amorphotheca resinae were prepared, followed by the evaluation of their sunscreen performance, antioxidant activity, and cytotoxicity. Melanin-blended cream was prepared by blending a melanin suspension and a pure cream. The cream showed an in vitro sun protection factor value of 2.5 when the pigment content was 5%. The cream showed a critical wavelength of approximately 388 nm and a UVA/UVB ratio of more than 0.81, satisfying the broad-spectrum sunscreen requirement. Oxygen radical absorbance capacity assays indicated that fungal melanin had antioxidant activity similar to ascorbic acid but higher than reduced glutathione. Fungal melanin had no statistically significant cytotoxicity to human keratinocyte cell lines until 72 h of exposure, even at a concentration of 4 mg mL⁻¹. Consequently, melanin pigment can be used as a biocompatible broad-spectrum sunscreen with high antioxidant activity and as a practical alternative in dermo-cosmetic formulations.

Fungal melanin was utilized as a broad-spectrum sunscreen with antioxidant activity.     

Controlled delivery of a protein tyrosine phosphatase inhibitor,SHP099, using cyclodextrin-mediated host–guest interactions in polyelectrolyte multilayer films for cancer therapy

The Src homology 2 domain containing protein tyrosine phosphatase-2 (SHP2) is a key enzyme in pathways regulating tumor growth signaling, and recently gained interest as a promising anticancer drug target. Many SHP2 inhibitors are currently under development, including SHP099, which has shown potent anticancer activity at low concentrations in vivo. In this work, we developed multilayer coatings for localized delivery of SHP099 to improve upon current cancer therapies. Layer-by-layer self-assembly was used to develop films composed of chitosan and poly-carboxymethyl-β-cyclodextrin (PβCD) for the delivery of SHP099. SHP099 was successfully loaded into multilayer films via host–guest interactions with PβCD. Nuclear magnetic resonance spectroscopy confirmed the occurrence of this supramolecular assembly by identifying the interaction of specific terminal SHP099 protons with the protons of the CD. SHP099 release from assembled films was detected over 96 hours, and was found to inhibit colony formation of human breast adenocarcinoma cells in vitro. These multilayer films have the potential to be used in a range of anticancer applications and overcome common complications of systemic chemotherapeutic administration, while maximizing SHP099 efficacy.

Controlled delivery of a potent anticancer drug, SHP099, after supramolecular complexation into a versatile multilayer film.     

Gold nanoparticles conjugated with anti-CD133 monoclonal antibody and 5-fluorouracil chemotherapeutic agent as nanocarriers for cancer cell targeting

The enhanced permeability and retention effect allows for passive targeting of solid tumours by nanoparticles carrying anticancer drugs. However, active targeting by incorporation of various ligands onto nanoparticles can provide for a more selective and enhanced chemotherapeutic effect and complement the deficiencies of the passive targeting approach. Here we report on the design of the carboxyl-terminated PEGylated gold nanoparticles (AuNPs), their functionalization with anti-CD133 monoclonal antibody (mAb) via a crosslinking reaction, and subsequent 5-fluorouracil (5-FU) drug loading. The synthesized products in the form of stable colloids were characterised using a range of physicochemical techniques, including X-ray diffraction (XRD), UV-Vis spectroscopy, transmission electron microscopy (TEM), and dynamic light scattering (DLS). Conjugation of anti-CD133 mAb onto PEGylated AuNPs was confirmed with the use of UV-Vis, BCA protein assay and fluorescence microscopy. HCT116 colorectal cancer cells abundantly expressed CD133: 92.4 ± 1.3%, as measured by flow cytometry. Whereas PEGylated AuNPs not conjugated with anti-CD133 mAb accumulated mainly at the cellular membrane, nanoparticles conjugated with anti-CD133 mAb were contained within the nuclear region of the cells. Anti-CD133 mAb conjugation facilitated the specific intracellular uptake due to specific antigen–antibody binding interaction. In vitro cytotoxicity studies on HCT116 cells showed that PEGylated AuNPs and PEGylated AuNPs-CD133 did not elicit any toxicity at any of the tested concentrations. Meanwhile, 5-FU-PEGylated AuNPs-CD133 significantly reduced the cell viability relative to the treatment with 5-FU-PEGylated AuNPs without anti-CD133 mAb conjugates (p < 0.0001). This study shows that the conjugation of nanocarriers with the anti-CD133 antibody improves the specific targeting of 5-FU against colorectal cancer cells. These results demonstrate that simultaneous functionalisation of PEGylated AuNPs with antibodies and chemotherapeutic drugs is a viable strategy to combat cancer through targeted drug delivery.

5-FU-PEGylated AuNPs-CD133 is designed to improve specific targeting of 5-FU against colorectal cancer cells which abundantly express CD133.     

Bioactive silver phosphate/polyindole nanocomposites

Materials capable of releasing reactive oxygen species (ROS) can display antibacterial and anticancer activity, and may also have anti-oxidant capacity if they suppress intracellular ROS (e.g. nitric oxide, NO) resulting in anti-inflammatory activity. Herein we report silver phosphate (Ag₃PO₄)/polyindole (Pln) nanocomposites which display antibacterial, anticancer and anti-inflammatory activity, and have therefore potential for a variety of biomedical applications.

Materials capable of releasing reactive oxygen species (ROS) can display antibacterial and anticancer activity, and may also have antioxidant capacity if they suppress intracellular ROS (e.g. nitric oxide, NO) resulting in anti-inflammatory activity.     

Mitochondria targeting IR780-based nanoGUMBOS for enhanced selective toxicity towards cancer cells

Herein, a simple counter-ion variation strategy is proposed and demonstrated for design of an array of near infrared IR780-based nanoGUMBOS (nanomaterials from a Group of Uniform Materials Based on Organic Salts) to produce enhanced anticancer activity. These nanomaterials were synthesized by direct nanoengineering of IR780-based GUMBOS using a reprecipitation method, without addition of any other materials. Thus, these novel nanomaterials can serve as carrier-free nanodrugs, providing several distinct advantages over conventional chemotherapeutics. Examination of the size and stability of these nanoGUMBOS indicates formation of approximately 100 nm nanoparticles that are stable under biological conditions. Interestingly, in vitro chemotherapeutic applications of these nanoGUMBOS indicate two to four-fold enhanced toxicity towards breast cancer cells as compared to the parent dye, while still maintaining minimal toxicity towards normal cells. The mechanism of cancer toxicity for these nanoGUMBOS was also examined by a study of their sub-cellular localization as well as using a mitochondrial toxicity assay. Analyses of data from these studies revealed that all nanoGUMBOS primarily accumulate in the mitochondria of cancer cells and produce dysfunction in the mitochondria to induce cell death. Using these studies, we demonstrate tunable properties of IR780-based nanoGUMBOS through simple variation of counter-ions, thus providing a promising strategy for future design of better nanomedicines to be used for cancer therapy.

Mitochondria targeting nanoGUMBOS were successfully fabricated based on self-assembly of IR780 GUMBOS with different counter-anions that show promising anticancer effects.     

Characterization and targeting ability evaluation of cell-penetrating peptide LyP-1 modified alginate-based nanoparticles

Doxorubicin hydrochloride (DOX) shows a powerful treatment effect on breast cancer. However, for its indiscriminate distribution after systemic administration, the therapeutic response of DOX will reduce and even result in serious adverse reactions during the long-term administration. To achieve better treatment, in this study we established a non-condensing sodium alginate-based nanoparticle-encapsulated DOX (DOX/NP), the surface of which was modified with cell-penetrating peptide LyP-1 (namely LyP-1-DOX/NP) to attain active targeting towards breast cancer cells. The size of LyP-1-DOX/NP was 138.50 ± 4.65 nm, with a polydispersity index (PDI) of 0.22 ± 0.02, and the zeta potential was 18.60 ± 0.49 mV. The drug loading efficiency (DLE) for the preparation was 91.21 ± 2.01%, with an encapsulation efficiency (EE) of 12.37 ± 0.35%. The nanoparticles exhibited good stability in vitro and slower release trend compared with free DOX in PBS at pH7.4. In vitro cytopharmacodynamics showed that LyP-1-DOX/NP had an excellent anti-breast cancer effect against MDA-MB-231 cells by the MTT test. The uptake amount of LyP-1-DOX/NP by MDA-MB-231 cells was much higher than that of free DOX or unmodified DOX/NP at all time points. Further in vivo pharmacokinetics studies showed that the concentration of LyP-1-DOX/NP was higher than that of free DOX or DOX/NP both in plasma and in tumor, suggesting its favorable long circulation and enhancing targeting property. The present study provides a promising strategy for using the LyP-1 cell-penetrating peptide to modify nanoparticles for enhancing their targeting ability towards breast cancer.

Doxorubicin hydrochloride (DOX) shows a powerful treatment effect on breast cancer.     

Nanoparticles based on retinoic acid caped with ferrocenium: a novel synthesized targetable nanoparticle both with anti-cancer effect and drug loading capacity

To date, there is an urgent need for cancer treatment to improve in many ways in order to successfully cure all cancers. Retinoic acid (RA) is a promising anti-cancer drug through influencing cancer stem cells (CSCs). Taxol is a chemotherapy drug for many cancers. To increase the anti-cancer effects of RA and taxol, we created a novel RA nanoparticle, FCRAN, which has the ability of carrying a second anti-cancer drug, taxol, using nanotechnological methods. The results of this study demonstrated that this RA nanoparticle was water-soluble and retained the same effects as RA on cancer cells, such as inhibiting the proliferation of CSCs, inducing the differentiation of CSCs, and enhancing the sensitivity of CSCs to chemotherapeutic drugs. In addition, this RA nanoparticle can be used to carry a second anticancer drug, taxol, to become FCRAN/T and synergistically enhance the anti-cancer effects of both drugs in vivo. Interestingly, the FCRAN/T is a targetable anti-cancer nanoparticle in the presence of higher levels of glutathione (GSH) in cancer cells. Our results demonstrate that our novel synthesized nanoparticles not only retain the RA functions, but can also carry a second anticancer drug to play a synergistic anticancer role with good water solubility, in particular FCRAN/T can target cancer cells. Therefore, our novel synthesized targetable anti-cancer nanoparticles have a better application prospect than that of RA or taxol alone.

A retinoic acid nanoparticle with the ability of carrying a second anti-cancer drug, taxol, was developed. The anti-cancer nanoparticles were shown to have a better application prospect than that of RA or taxol alone.     

Synthesis and biological study of acridine-based imidazolium salts

A new series of acridine based imidazolium salts was synthesized and evaluated for in vitro cytotoxicity against human cancer cell lines by an MTT assay. The synthesis applied a coupling of imidazoles with 9-chloroacridines, which originated from an Ullmann condensation of a 2-chloro-benzoic acid with an aniline. The target compounds were obtained in high yields. The DPPH assay indicated considerable antioxidant activity for target compounds with simple and short alkyl chains on the imidazole, while increasing chain length and the introduction of an additional π-electron system in most cases reduced the activity. All compounds exhibited low biotoxicity against non-cancerous cell lines, whereas a few compounds showed promising anticancer activity. Unlike for the reference drugs Tamoxifen and Paclitaxel, the anticancer activity of acridine imidazolium ions is specific for only selected cancer types. Reasonable fluorescent behaviour of the products provide potential for visualization of the distribution of active drugs in tissue.

A series of acridine-based imidazolium salts was synthesized and studied on cytotoxicity against human cancer cell lines.     

Antioxidant activities of anastatin A & B derivatives and compound 38c's protective effect in a mouse model of CCl4-induced acute liver injury

Anastatins A and B, two flavonoid compounds isolated from desert plant Anastatica hierochuntica, have protective activities for primary rat hepatocytes. Anastatins A and B, and their derivatives, were synthesized by our group previously. In this study, the antioxidant activity and cytotoxicity of these compounds were studied using chemical assessment methods, cell proliferation inhibition experiments, and cell oxidative damage models. The best compound, 38c, was used to study the hepatoprotection activity and mechanism by using a CCl₄-induced liver injury model in mice. The results show that most of these flavonoid compounds have good antioxidant activity and low cytotoxicity in vitro. Among them, the most potent compound was 38c, which exhibited a protective effect on CCl₄-induced hepatic injury by suppressing the amount of CYP2E1. These findings indicate that anastatin flavonoid derivatives have potential therapeutic utility against oxidative hepatic injury.

Anastatins B derivative 38c both had good antioxidant activity in vitro and in vivo.     

Magnetically targeted co-delivery of hydrophilic and hydrophobic drugs with hollow mesoporous ferrite nanoparticles

A magnetically targeted drug delivery system (DDS) is developed to solve the delivery problem of hydrophobic drugs by using hollow mesoporous ferrite nanoparticles (HMFNs). The HMFNs are synthesized by a one-pot hydrothermal method based on the Ostwald ripening process. The biocompatibility of the synthesized HMFNs was determined by MTT assay, lactate dehydrogenase (LDH) leakage assay and hemolyticity against rabbit red blood cells. Moreover, Prussian blue staining and bio-TEM observations showed that the cell uptake of nanocarriers was in a dose and time-dependent manner, and the nanoparticles accumulate mostly in the cytoplasm. A typical highly hydrophobic anti-tuberculosis drug, rifampin (RFP) was loaded into HMFNs using supercritical carbon dioxide (SC-CO₂) impregnation, and the drug loading amount reached as high as 18.25 wt%. In addition, HMFNs could co-encapsulate and co-deliver hydrophobic (RFP) and hydrophilic (isoniazide, INH) drugs simultaneously. The in vitro release tests demonstrated extra sustained co-release profiles of rifampicin and isoniazide from HMFNs. Based on this novel design strategy, the co-delivery of drugs in the same carrier enables a drug delivery system with efficient enhanced chemotherapeutic effect.

A magnetically targeted drug delivery system (DDS) is developed to solve the delivery problem of hydrophobic drugs by using hollow mesoporous ferrite nanoparticles (HMFNs).     

Ameliorative effect of biofabricated ZnO nanoparticles of Trianthema portulacastrum Linn. on dermal wounds via removal of oxidative stress and inflammation

An impediment in the process of wound healing can be attributed to reactive oxygen species and inflammation. The curative efficacy of green synthesized Trianthema portulacastrum Linn. zinc oxide nanoparticles (ZnOTP) was investigated in the present study for evaluation of their wound healing potential in rodents. Total phenolic and flavonoid content of ZnOTP was determined, and antioxidant potential was evaluated by the DPPH method. In vitro anti-inflammatory activity of ZnOTP was evaluated by membrane stabilization and albumin denaturation, along with proteinase inhibitory assays. The synthesized ZnOTP were characterized by UV-Visible spectroscopy, Fourier transform infrared (FT-IR) studies, Field Emission Scanning Electron Microscopy (FESEM) and Energy Dispersive X-ray (EDX) studies. The wound healing potential of ZnOTP was monitored by excision and incision wound models. Analyses confirmed the formation of spherical nanoparticles of 10–20 nm size along with strong signals of zinc and oxygen atoms. Significant results (p < 0.05) of wound contraction rate, epithelialization and histopathology of the healed tissues of rats confirmed the promising wound healing property of ZnOTP. In addition, inflammatory markers, biochemical estimation such as the hydroxyproline content of granulation tissue, and the profile of antioxidant enzymes also supported the wound healing potential of ZnOTP. The present study advocated the attenuation of wounds via antioxidant and anti-inflammatory activities of a green synthesized nano-ointment.

The curative efficacy of a green synthesized zinc oxide nano-ointment on wound healing was investigated.     

Preparation and in vitro characterization of valsartan-loaded ethyl cellulose and poly(methyl methacrylate) nanoparticles

Valsartan is an antihypertensive drug used primarily orally, however, due to its hydrophobic nature it has got low bio-availability thus requiring higher dosage/frequency and causing more side effects. The aim of our work was to prepare valsartan-loaded nanoparticles by using ethyl cellulose and poly(methyl methacrylate) polymers which can be administered orally and to investigate the preparation conditions and their significance as potential drug carriers for valsartan delivery by in vitro release studies. Ethyl cellulose and poly(methyl methacrylate) polymers were used for the preparation of nanoparticles by single emulsion-solvent evaporation technique. The formation of drug-loaded nanoparticles was designed by experimental design for size and encapsulation efficiency, in addition the prepared nanosuspensions were nano spray dried in order to gain a powder form that is easy to handle and store. Both of the nano spray dried formulations had an amorphous structure in contrast to the pure drug according to differential scanning calorimetry and X-ray diffraction analysis, which can be advantageous in drug absorption. The originally processed ethyl cellulose-valsartan nanoparticles increased the solubility of the drug in the model intestinal medium, while poly(methyl methacrylate)-valsartan nanoparticles enabled substantially prolonged drug release. The release kinetics of both types of nanoparticles could be described by the Weibull model.

Valsartan-loaded ethyl cellulose and poly(methyl methacrylate) nanoparticles were prepared and nano spray-dried. The active agent was structurally changed in the nanoparticles, which could be advantageous in the intestinal absorption.     

Curcumin loaded zinc oxide nanoparticles for activity-enhanced antibacterial and anticancer applications

Zinc oxide nanoparticles and curcumin have been shown to be excellent antimicrobial agents and promising anticancer agents, both on their own as well as in combination. Together, they have potential as alternatives/supplements to antibiotics and traditional anticancer drugs. In this study, different morphologies of zinc oxide-grafted curcumin nanocomposites (ZNP–Cs) were synthesized and characterized using SEM, TGA, FTIR, XRD and UV-vis spectrophotometry. Antimicrobial assays were conducted against both Gram negative and Gram-positive bacterial stains. Spherical ZnO–curcumin nanoparticles (SZNP–Cs) and rod-shaped ZnO–curcumin nanoparticles showed the most promising activity against tested bacterial strains. The inhibition zones for these curcumin-loaded ZnO nanocomposites were consistently larger than their bare counterparts or pure curcumin, revealing an additve effect between the ZnO and curcumin components. The potential anticancer activity of the synthesized nanocomposites was studied on the rhabdomyosarcoma RD cell line via MTT assay, while their cytotoxic effects were tested against human embryonic kidney cells using the resazurin assay. SZNP–Cs exhibited the best balance between the two, showing the lowest toxicity against healthy cells and good anticancer activity. The results of this investigation demonstrate that the nanomatrix synthesized can act as an effective, additively-enhanced combination delivery/therapeutic agent, holding promise for anticancer therapy and other biomedical applications.

Curcumin-loaded ZnO nanocomposites act as an effective, synergistically-enhanced combination delivery/therapeutic agent, holding promise for anticancer and antimicrobial therapy with reduced toxicities.