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The present study is an attempt to evaluate the in vitro anti‐inflammatory and in silico anticancer potentials of the plant Cassia auriculata (CA). The aerial parts of CA were subjected to solvent extraction, and the extracts were fractionised by gas chromatography and mass spectrometry analysis for its phytochemical content. The antiinflammatory activity of the extracts were confirmed by the IC50 value of 125.02 µg/ml for red blood cell membrane stabilisation and 195.7 µg/ml for inhibition of protein denaturation activity. The interaction of bioactive compounds of CA ethanol extract with target protein was predicted through molecular docking studies, serine/threonine–protein kinase B (AKT1), responsible for development and progression of lung cancer using AutoDock tools. Extensive studies have been carried out on a range of kinase inhibitors targeting Akt, but obtaining promising results is a challenge yet due to its toxicity and resistance issues. Yohimbine, undecanoic acid 10‐methyl‐ethyl ester and chrysin significantly bind to the target protein with least binding energy. Hence, the present paper establishes the anti‐inflammatory and anticancer capacities of CA ethanol extract as an alternative to the existing therapeutic approach to inflammation and cancer through a systematic in vitro and in silico approaches supplementing the findings. [ABSTRACT FROM AUTHOR]

The main objective of this work was to investigate the uptake channels of skin cells through which coumarin 6, transported by deoxycholate‐mediated liposomes (DOC‐LS), was internalised; this was also compared against the action of conventional LS. Coumarin 6‐loaded DOC‐LS and LS were characterised for size distribution, zeta potential, and shape, and analysed in vitro in human epidermal immortal keratinocyte (HaCaT) (epidermal) and human embryonic skin fibroblast (CCC‐ESF‐1) (dermal) cell lines. Various endocytosis inhibitors were incubated with cells treated with the nanocarriers. Flow cytometry results indicated that HaCaT and CCC‐ESF‐1 cells internalise the tested preparations through pinocytotic vesicles, macropinocytosis, clathrin‐mediated endocytic pathways, and via lysosomes, which consume a considerable amount of energy. The endocytosis pathways of DOC‐LS and LS showed no difference. This study provides a basis for the application of LS being combined with a microneedle system for efficient intracellular drug delivery, targeting cutaneous histocyte disorders. [ABSTRACT FROM AUTHOR]

Silver (Ag) complexes of drugs and their nanosystems have great potential as antibacterials. Recently, an Ag complex of furosemide (Ag–FSE) has shown to be a promising antimicrobial. However, poor solubility of Ag–FSE could hamper its introduction into clinics. Therefore, the authors developed a nanosuspension of Ag–FSE (Ag–FSE_NS) for its solubility and antibacterial activity enhancement. The aim of this study was to introduce a novel nanoantibiotic with enhanced antibacterial efficacy. Ag–FSE_NS was prepared by precipitation–ultrasonication technique. Size, polydispersity index (PI) and zeta potential (ZP) of prepared Ag–FSE_NS were measured by dynamic light scattering, whereas surface morphology was determined using scanning electron microscopy (SEM). In vitro antibacterial activity was evaluated against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa using broth microdilution method. Size, PI and ZP of optimised Ag–FSE_NS1 were 191.2 ± 19.34 nm, 0.465 ± 0.059 and −55.7 ± 8.18 mV, respectively. SEM revealed that Ag–FSE_NS1 particles were rod or needle‐like with smooth surfaces. Saturation solubility of Ag–FSE in NS increased eight‐fold than pure Ag–FSE. Ag–FSE_NS1 exhibited two‐fold and eight‐fold enhancements in activity against E. coli and S. aureus, respectively. The results obtained showed that developed Ag–FSE_NS1 holds a promise as a topical antibacterial. [ABSTRACT FROM AUTHOR]

The treatment of periodontitis focuses on controlling the progression of inflammation, reducing plaque accumulation, and promoting bone tissue reconstruction. Among them, the reconstruction of irregular bone resorption caused by periodontitis is a long‐standing challenge. At present, the local drug treatment of periodontitis is mainly anti‐inflammatory and antibacterial drugs. In this study, psoralen (Pso), a Chinese herbal medicine with anti‐inflammatory, antibacterial, and osteogenic effects, was selected for the local treatment of periodontitis. Meanwhile, an injectable methacrylate gelatin (GelMA) platform loading with Pso was constructed. Pso‐GelMA had the properties of fluidity, light cohesion, self‐healing, and slow release, which could be better used in the deep and narrow structure of the periodontal pocket, and greatly increased the effectiveness of local drug delivery. The pore size of Gelma hydrogel did not change after loading Pso by SEM. In vitro, Pso‐GelMA effectively upregulated the expression of osteogenic genes and proteins, increased alkaline phosphatase activity, promoted the mineralisation of rat bone marrow mesenchymal stem cells (BMSCs) extracellular matrix, and had significant antibacterial effects on Staphylococcus aureus and Fusobacterium nucleatum. Therefore, Pso‐GelMA has immense promise in the adjuvant treatment of periodontitis. [ABSTRACT FROM AUTHOR]

Ellagic acid (EA), which is widely distributed in many foods, has been found to possess inhibitory activity against xanthine oxidase (XO). However, there is ongoing debate about the difference in XO inhibitory activity between EA and allopurinol. Additionally, the inhibitory kinetics and mechanism of EA on XO are still unclear. Herein, the authors systematically studied the inhibitory effects of EA on XO. The authors' findings showed that EA is a reversible inhibitor with mixed‐type inhibition, and its inhibitory activity is weaker than allopurinol. Fluorescence quenching experiments suggested that the generation of EA‐XO complex was exothermic and spontaneous. In silico analysis further confirmed that EA entered the XO catalytic centre. Furthermore, the authors verified the anti‐hyperuricemia effect of EA in vivo. This study elucidates the inhibition kinetics and mechanism of EA on XO, and lays a theoretical foundation for the further development of drugs and functional foods containing EA for the treatment of hyperuricemia. [ABSTRACT FROM AUTHOR]

The authors report a novel, effective and enhanced method of conjugating anticancer drug, paclitaxel and gallic acid with magnetosomes. Here, anticancer drugs were functionalised with magnetosomes membrane by direct and indirect (via crosslinkers: glutaraldehyde and 3‐aminopropyltriethoxysilane) adsorption methods. The prepared magnetosome–drug conjugates were characterised by Fourier transform infrared, zeta potential, field‐emission scanning electron microscope and thermogravimetric analysis/differential scanning calorimetry. The drug‐loading efficiency and capacity were found to be 87.874% for paclitaxel (MP) and 71.3% for gallic acid (MG), respectively as calculated by ultraviolet spectroscopy and high‐performance liquid chromatography. The drug release demonstrated by the diffusion method in phosphate buffer (PBS), showing a prolonged drug release for MP and MG, respectively. The cytotoxicity effect of the MP and MG displayed cytotoxicity of 69.71%, 55.194% against HeLa and MCF‐7 cell lines, respectively. The reactive oxygen species, acridine orange and ethidium bromide and 4, 6‐diamidino‐2‐phenylindole staining of the drug conjugates revealed the apoptotic effect of MP and MG. Further, the regulation of tumour suppressor protein, p53 was determined by western blotting which showed an upregulation of p53. Comparatively, the magnetosome–drug conjugates prepared by direct adsorption achieved the best effects on the drug‐loading efficiency and the increased percentage of cancer cell mortality and the upregulation of P53. The proposed research ascertains that magnetosomes could be used as effective nanocarriers in cancer therapy. [ABSTRACT FROM AUTHOR]

The therapeutics for type 2 diabetes mellitus has emerged in the current century towards nanomedicine incorporated with plant active compounds. In this study, Tinospora cordifolia loaded poly (D, L‐lactide) (PLA) nanoparticles (NPs) were evaluated in vivo for their anti‐hyperglycemic potency towards streptozotocin‐induced type 2 diabetic rats. T. cordifolia loaded PLA NPs were synthesised by the double solvent evaporation method using PLA polymer. The NPs were then characterised and administrated orally for 28 successive days to streptozotocin‐induced diabetic rats. The PLA NPs had significant anti‐diabetic effects which were equal to the existing anti‐diabetic drug glibenclamide. The antidiabetic activity is due to the synergism of compounds present in stem extract of the plant which reduced the side effects and anti‐diabetic. [ABSTRACT FROM AUTHOR]

Sulphonylureas are extensively used in the treatment of type II diabetes; however, these drugs have complications of hypoglycaemia and weight gain. The current study aims at developing a potent antidiabetic drug that has lesser side effects and better management of its associated conditions. Zinc oxide nanoparticles (ZnO NPs) were synthesised using Syzygium cumini seed extract with an average size of 18.92 nm. In vitro studies on rat insulinoma (RIN‐5F) cells revealed that cells treated with synthesised ZnO NPs showed a dose‐dependent increase in insulin secretion. Streptozotocin‐fructose‐induced type II diabetic rats treated with ZnO NPS exhibited a significant reduction (p < 0.01) in the blood glucose levels, total cholesterol, triglycerides, and low‐density lipoprotein levels and increase (p < 0.01) in serum insulin and liver antioxidant enzyme levels proclaiming its role as a hypoglycaemic and hypolipidaemic drug. Treatment of ZnO NPs in diabetic rats exhibited an increased number of beta cells which was responsible for its increased insulin levels and reduced glucose levels. From the overall observations, biosynthesised ZnO NPs exhibited an efficacious hypoglycaemic effect in diabetic rats, so it can be suggested as a potent antidiabetic drug. [ABSTRACT FROM AUTHOR]

In this report, the site‐specific co‐delivery of green tea/aluminium magnesium silicate (AMS) was reported and the specific target delivery was achieved orally. The new co‐precipitation process was developed to synthesis the green tea/AMS hybrid complex and using energy‐dispersive X‐ray spectroscopy, Fourier‐transform infrared spectroscopy and Raman confirmed its successful synthesis. The blood biocompatibility of the green tea/AMS was tested using chicken blood, and the compound is safe up to 500 mg/ml. After mixed with hydroxypropyl methylcellulose phthalate, the oral beads were synthesised using a linking agent. The oral beads underwent different pH‐based dissolution studies and the results indicated that the beads specifically dissolved in gastric pH (6.5). The pharmaco kinetic studies were performed to estimate the delivery kinetics. The results revealed that the beads underwent as per the Higuchi model. The anticoccidial effects of the beads were tested using chicken. The animal studies were performed in two different modes such as prophylactic treatment and active treatment after Eimeria species challenge. The results indicated that the prophylactic treatment with beads 100% protected the chicken and the active treatment with beads after the Eimeria challenge significantly protected against the intestinal damage and it also enhanced the anticoccidial effect. [ABSTRACT FROM AUTHOR]

In this study, the extract of two strains of cyanobacteria was used for the synthesis of silver nanoparticles (NPs). UV–vis spectroscopy, X‐ray diffraction, dynamic light scattering and field emission scanning electron microscopy (FESEM) analyses were carried out to characterise the NPs. The antioxidant activity and heavy metal detection properties were investigated; moreover, their minimum inhibitory concentration and minimum bactericidal concentration against the multi‐drug resistant bacteria were determined. The most abundant materials in these extracts were carbohydrates, so the biosynthesis of NPs using exopolysaccharide (EPS) was also investigated. The surface plasmon resonance of NPs had a peak at 435 nm and EPS NPs at 350–450 nm. The NPs produced by Nostoc sp. IBRC‐M5064 extract revealed the face‐centred cubic (fcc) structure of AgCl, while NPs of N. pruniforme showed the fcc crystalline structure of Ag3 PO4 and AgCl. The FESEM showed the spherical shape of these NPs. The AgCl/Ag3 PO4 colloid, in comparison with AgCl, showed better antioxidant activity and antibacterial effect. The heavy metal detection analysis of NPs revealed that the NPs of both stains involved in Hg (NO3)2 detection. [ABSTRACT FROM AUTHOR]

Drug delivery is one of the major challenges in the treatment of central nervous system disorders. The brain needs to be protected from harmful agents, which are done by the capillary network, the so‐called blood–brain barrier (BBB). This protective guard also prevents the delivery of therapeutic agents to the brain and limits the effectiveness of treatment. For this reason, various strategies have been explored by scientists for overcoming the BBB from disruption of the BBB to targeted delivery of nanoparticles (NPs) and cells and immunotherapy. In this review, different promising brain drug delivery strategies including disruption of tight junctions in the BBB, enhanced transcellular transport by peptide‐based delivery, local delivery strategies, NP delivery, and cell‐based delivery have been fully discussed. [ABSTRACT FROM AUTHOR]

The emergence of the huge number of multi‐drug resistant (MDR) bacteria requires an alternative to the drugs. Silver nanoparticles (AgNPs) are a strong candidate for this due to their bactericidal properties, which can be better concluded by understanding their morphology and chemistry. The study hypothesised that AgNPs synthesised using leaves of Syzygium cumini can be used to treat locally emerging MDRs forming biofilms on indwelling medical devices. Synthesised particles were characterised by methods like UV–visible spectroscopy, X‐ray powder diffraction, scanning electron microscopy, transmission electron microscopy, and Zetasizer. Fourier transform infrared spectroscopy, and high‐performance liquid chromatography were used to predict phytochemicals present in the leaves. The shape of particles is revealed to be relatively spherical, with average size to be around 10–100 nm. Phenolic compounds are attributed to the formation of nanoparticles, stability analysis shows particles to be stable, and zeta potential determined the surface charge to be −20.1 mV. Biosynthesised particles are found to possess efficient antibacterial activity MDR bacteria developing biofilms in medical devices; hence, it is concluded that S. cumini based NPs can be used to develop a layer on implant‐related medical devices. Toxicity evaluation against A594 cancer cells portrays AgNPs to be potential tumour reduction agents in a concentration‐dependent manner. [ABSTRACT FROM AUTHOR]

Bio‐fabrication of gold nanoparticles (AuNPs) has several advantages like biocompatibility, less toxicity, and eco‐friendly in nature over their chemical and physical methods. Currently, the authors fabricated AuNPs using aqueous root extract of Momordica dioica (M. dioica) and explored their anticancer application with mechanistic approaches. Different biophysical techniques such as UV–visible spectroscopy, Fourier transform infrared, X‐ray diffraction, transmission electron microscopy, selected area electron diffraction, and dynamic light scattering were employed for AuNPs characterisation. The synthesised AuNPs were mono‐dispersed, crystalline in nature, anionic surface (−23.9 mV), and spherical particle of an average diameter of 9.4 nm. In addition, the AuNPs were stable in buffers solutions and also biocompatible towards normal human cells (human vascular endothelial cells and human lung cells). The AuNPs were exhibited anticancer activity against different cancer cell lines such as human breast cancer cells, human cervical cancer cells (HeLa) and human lung cancer cells. Further, the pro‐apoptotic genes such as Bcl2 were down‐regulated and BAX, Caspase‐3, −8, and −9 were up‐regulated in HeLa cells as compared to untreated cells. Annexin‐V‐FITC assay results showed that the AuNPs were induced apoptosis by accumulation of intracellular reactive oxygen species. To their knowledge, this is the first report on the synthesis of bioactive metal nanoparticles from M. dioica and it may open up new avenues in therapeutic applications. [ABSTRACT FROM AUTHOR]

To sustained release of an anticancer drug, oxaliplatin (OX), a non‐toxic and biocompatible nanocarrier based on bovine serum albumin (BSA) were synthesised by desolvation method and characterised using Fourier‐transform infrared (FTIR) spectroscopy, field emission scanning electron microscopy (FESEM), atomic force microscopy (AFM) and dynamic light scattering. The results showed that the BSA nanoparticles (BSANPs) with a mean magnitude of 187.9 ± 1.2 nm have spherical morphology with a smooth surface and a uniform distribution. Furthermore, OX was loaded onto the BSANPs and the loading was confirmed by FTIR, AFM and FESEM techniques. The percentage of encapsulation efficiency and drug loading were determined by absorption spectroscopy (UV–vis). The drug release studies showed that release of OX from BSANPs exhibited slower release rate. However, the release kinetics followed the first‐order kinetic for both of them with the non‐Fickian release behaviour. The electrochemical analysis showed stability of OX loaded onto the BSANPs (OX@BSANPs) and confirmed the diffusion mechanism. Furthermore, the results of MTT assay revealed increasing of normal cell viability and cancer cell death in the OX@BSANPs compared to only OX. It was shown that the BSANPs could be safely used as a biocompatible nanocarrier for the sustained release of OX. [ABSTRACT FROM AUTHOR]

Drug encapsulation in nanocarriers such as polymeric nanoparticles (Nps) may help to overcome the limitations associated with cannabinoids. In this study, the authors' work aimed to highlight the use of electrospraying techniques for the development of carrier Nps of anandamide (AEA), an endocannabinoid with attractive pharmacological effects but underestimated due to its unfavourable physicochemical and pharmacokinetic properties added to its undesirable effects at the level of the central nervous system. The authors characterised physicochemically and evaluated in vitro biological activity of anandamide/ɛ‐polycaprolactone nanoparticles (Nps‐AEA/PCL) obtained by electrospraying in epithelial cells of the human proximal tubule (HK2), to prove the utility of this method and to validate the biological effect of Nps‐AEA/PCL. They obtained particles from 100 to 900 nm of diameter with a predominance of 200–400 nm. Their zeta potential was −20 ± 1.86 mV. They demonstrated the stable encapsulation of AEA in Nps‐AEA/PCL, as well as its dose‐dependent capacity to induce the expression of iNOS and NO levels and to decrease the Na+ /K+ ATPase activity in HK2 cells. Obtaining Nps‐AEA/PCL by electrospraying would represent a promising methodology for a novel AEA pharmaceutical formulation development with optimal physicochemical properties, physical stability and biological activity on HK2 cells. [ABSTRACT FROM AUTHOR]

Magnetic manotheranostics can be a fascinating charm to diagnose a tumour with MRI, and treatment through hyperthermia. This study aims to synthesise and characterise magnetically responsive polymer colloids (MRPCs). Healthy tissue damage done by chemotherapy session could be minimised by MRPCs. For the colloidal formulation of MRPCs, the oil in water emulsion technique was employed with the aid of sonication and stirring. The organic phase of emulsion contained methotrexate (MTX) drug, Eudragit E100 and CoFe2 O4 (synthesised by co‐precipitation) in ethanol, and the aqueous phase contained tween 80 in deionised water. The emulsion was optimised by studying/adjusting two different parameters, i.e. the concentration of constituents and sonication cycles. Multiple formulations were produced at sonication amplitude of 60% at 20 kHz, followed by centrifugation and lyophilisation. Characterisation of MRPCs was done for morphology, size measurement (23–25 nm), surface charge (∼15.12), coercivity (∼1549.6 G), magnetisation (2.6 emu) and retentivity (1.34 emu). Drug release in simulating physiological environment (pH = 7.4), was observed for up to 48 h, and, to determine the best release kinetic mechanism results were compared with kinetic models. Magnetic hyperthermia studies showed that MRPCs achieved an acceptable temperature of 42°C, for hyperthermia treatments in cancer patients. [ABSTRACT FROM AUTHOR]

Age‐related macular degeneration (AMD) is a disease affecting the macula by the new blood vessels formation. AMD is widely treated with a combination of anti‐angiogenic and anti‐vascular endothelial growth factor (VEGF) agents. The topical administration of nanodispersions showed enhanced ocular residence time with controlled and prolonged drug delivery to the disease site at the back of the eye. In the present study we developed and characterized nanodispersion containing anti‐angiogenic (artemisinin) and anti‐VEGF agent (dexamethasone) for the topical ocular administration in order to obtain a required drug concentration in the posterior part of the eye. The nanodispersions were prepared with varying concentration of polymer, polyvinyl pyrrolidone K90 and polymeric surfactant, Poloxamer 407. The nanodispersions were found to be smooth and spherical in shape with a size range of 12–26 nm. In‐vitro drug release studies showed the 90–101% of artemisinin and 55–103% of dexamethasone release from the nanodispersions. The blank formulation with a high concentration of polymer and polymeric surfactant showed an acceptable level of haemolysis and DNA damage. The chorioallantoic membrane assay suggested that the nanodispersion possess good anti‐angiogenic effect. Hence the formulated artemisinin and dexamethasone nanodispersion may have the great potential for the AMD treatment. [ABSTRACT FROM AUTHOR]

Along with the extensive range of exotic nanoparticle (NPs) applications, investigation of magnetic NPs (MNPs) in vitro has ushered modern antibacterial studies into an increasingly attractive research area. A great number of microorganisms exist in the size scales from nanometre to micrometre regions. The enormous potential of engineered MNPs in therapeutic procedures against various drug‐resistant bacteria has declined the menace of fatal bacterial infections. Many biocompatible MNPs have been introduced that possess remarkable impacts on various bacterial strains. Conventional synthesis methods such as co‐precipitation or hydrothermal techniques have been widely adopted in the production of MNPs. The MNPs for antibacterial applications are mainly required to be superparamagnetic, recyclable and biocompatible. To implement novel strategies in developing new generation antimicrobial magnetic nanomaterials, it is essential to obtain a comprehensive preview of recent achievements in synthesis, proposed antibacterial mechanisms and characterisation techniques of these nanomaterials. This review highlights notable aspects of antibacterial activity in engineered MNPs and nanocomposites including their particle properties (size, shape and saturation magnetisation), antibacterial mechanisms, synthesis methods, testing methods, surface modifications and minimum inhibitory concentrations. [ABSTRACT FROM AUTHOR]

The silver oxide nanoparticles (AgO2 ‐NPs) were synthesised using silver foil as a new precursor in wet chemical method. X‐ray diffraction analysis shows crystallographic structures of AgO2 ‐NPs with crystallite size of 35.54 nm well‐matched with standard cubic structure. Scanning electron microscopy analysis clearly shows the random distribution of spherical‐shaped nanoparticles. Energy dispersive X‐ray analysis confirmed the purity of the samples as it shows no impurity element. Fourier transforms infra‐red analysis confirmed the formation of AgO2 ‐NPs with the presence of Ag‐O‐Ag stretching bond. All the techniques also confirmed the loading of ceftriaxone drug on the surface of AgO2 ‐NPs. This study also described the effect of AgO2 ‐NPs having synergistic activity with β lactam antibiotic i.e. ceftriaxone against ESBL generating Escherichia coli (E. coli). Among isolated strains of E. coli, 60.0% were found to be ESBL producer. The synergistic activities of AgO2 ‐NPs with ceftriaxone suggest that these combinations are effective against MDR‐ESBL E. coli strains as evident by increase in zone sizes. The present study observed rise in MDR‐ESBL E. coli with polymorphism of blaCTXM and blaSHV causing UTI infections in Pakistani population. The antibiotic and AgO2 ‐NPs synergistic effect can be used as an efficient approach to combat uro‐pathogenic infections. [ABSTRACT FROM AUTHOR]

Malaria is a dangerous disease affecting humans and animals in tropical and subtropical areas worldwide. According to recent estimates, 3.2 billion people are at risk of malaria. Many drugs are in practices to control this disease and their vectors. Eco‐friendly control tools are needed to fight vectors of this important disease. Nanotechnology is playing a key role in the fight against many public health emergencies. In the present study, Lagenaria siceraria aqueous peel extract was used to prepare zinc oxide nanoparticles (ZnO NPs), then tested on Anopheles stephensi eggs, larvae and pupae. The L. siceraria ‐synthesised ZnO NPs were characterized additionally by FTIR, AFM, XRD, UV‐Vis spectroscopy, EDX, and SEM spectroscopy The ovicidal, larvicidal, pupicidal and repellent activities of L. siceraria and green‐synthesised ZnO NPs were analysed on A. stephensi. The potential mechanism of action of ZnO NPs was studied investigating the changes in various enzyme activities in A. stephensi IV instar larvae. Furthermore, the smoke toxicity of L. siceraria ‐based cones against A. stephensi evoked higher mortality if compared with the control. Overall, the present study concluded that L. siceraria peel extract and its mediated green synthesised ZnO NPs represent a valuable green option to manage against malaria vectors. [ABSTRACT FROM AUTHOR]

The present study is designed to analyse the antibacterial and anticancer effects of silver nanoparticles (AgNPs) synthesised from the Cymbopogon citratus, (lemongrass) (LG‐AgNPs), which is widely used in ayurvedic drugs for treating various diseases. The LG‐AgNPs were synthesised and characterised using ultraviolet (UV) spectroscopy, Fourier transform infrared spectroscopy (FTIR), X‐ray diffraction (XRD) and transmission electron microscopy (TEM) analysis. The characterised LG‐AgNPs was subjected to antimicrobial analysis by disc diffusion method against pathogenic bacteria and fungi. Furthermore, the cytotoxicity and anticancer activity of the LG‐AgNPs were assessed with lung alveolar carcinoma cell line A549. Results depict that UV–visible spectra of LG‐AgNPs showed strong absorption peak at 435 nm. The XRD study exposed LG‐AgNPs crystals, which confirmed with TEM analysis exhibiting particle size ranging between 17 and 25.8 nm. The FTIR spectra recorded peaks at 3347, 2126, 1639, 659, 598 and 553 cm−1. The zone of inhibition study proves the LG‐AgNPs possessed both antibacterial and antifungal activities. 3‐(4, 5‐dimethyl thiazoyl‐2‐yl)‐(2,5‐diphenyltetrazolium bromide) results show the cytotoxicity effect of LG‐AgNPs in lung cancer cells. It also inhibited the cell migration and invasion at the dose of 25 µg ml−1 by increasing the apoptotic gene expression. The results reveal LG‐AgNPs possess anticancer activities, proposing that it may be an alternative drug for allopathic drugs with lots of side effects used in lung cancer treatment. [ABSTRACT FROM AUTHOR]

This study describes ZnO NPs biosynthesis using leaf extracts of Verbena officinalis and Verbena tenuisecta. The extracts serve as natural reducing, capping and stabilization facilitators. Plant extracts phytochemical analysis, revealed that V. officinalis showed higher total phenolic and flavonoid content (22.12 and 6.38 mg g −1 DW) as compared to V. tennuisecta (12.18 and 2.7 mg g −1 DW). ZnO NPs were characterised by ultraviolet–visible spectroscopy, Fourier transform infrared, X‐ray diffraction, scanning electron microscope, transmission electron microscopy (TEM) and energy dispersive X‐ray. TEM analysis of ZnO NPs reveals rod and flower shapes and were in the range of 65–75 and 14–31 nm, for V. tenuisecta and V. officinalis, respectively. Bio‐potential of ZnO NPs was examined through their leishmanicidal potential against Leishmania tropica. ZnO NPs showed potent leishmanicidal activity with 250 µg ml−1 being the most potent concentration. V. officinalis mediated ZnO NPs showed more potent leishmanicidal activity compared to V. tenuisecta mediated ZnO NPs due to their smaller size and increased phenolics doped onto its surface. These results can be a step forward towards the development of novel compounds that can efficiently replace the current medication schemes for leishmaniasis treatment. [ABSTRACT FROM AUTHOR]

Developing nanostructures for cancer treatment is growing significantly. Liposomal doxorubicin is a drug that is used in the clinic and represents a lot of benefits over doxorubicin. The development of multifunctional liposomes with different cancer treatment capability enables broader applications of doxorubicin chemotherapy. Many efforts were carried to prepare more effective liposomal formulation through loading gold nanoparticles (GNPs) in the formulation. Here, GNPs with an average size of 6 nm were loaded in liposomal formulation alongside doxorubicin. The hydrodynamic diameter of final formulation was 177.3 ± 33.9 nm that in comparison with liposomes without GNPs (112.5 ± 10.3 nm), GNPs‐loaded liposomes showed the bigger hydrodynamic diameter. GNPs‐loaded liposomes are slightly positively charged (4.4 ± 1.1 mV), while liposomes without loading the GNPs were negatively charged (−18.5 ± 1.6 mV). Doxorubicin was loaded in this formulation through active loading technique. Doxorubicin loading efficiency in gold‐loaded liposomes is slightly lesser than liposomes without GNPs, but still considerably high in comparison to passive loading techniques. [ABSTRACT FROM AUTHOR]

Research dealing with early diagnosis and efficient treatment in colon cancer to improve patient's survival is still under investigation. Chemotherapeutic agent result in high systemic toxicity due to their non‐specific actions on DNA repair and/or cell replication. Traditional medicine such as Lycopodium clavatum (LC) has been claimed to have therapeutic potentials against cancer. The present study focuses on targeted drug delivery of cationic liposomal nanoformulated LC (CL‐LC) in colon cancer cells (HCT15) and comparing the efficacy with an anti‐colon cancer drug, 7‐ethyl‐10‐hydroxy‐camptothecin (SN38) along with its nanoformulated form (CL‐SN38). The colloidal suspension of LC was made using thin film hydration method. The drugs were characterised using ultraviolet, dynamic light scattering, scanning electron microscopy, energy, dispersive X‐ray spectroscopy. Invitro drug release showed kinetics of 49 and 89% of SN38 and LC, whereas CL‐SN38 and CL‐LC showed 73 and 74% of sustained drug release, respectively. Studies on morphological changes, cell viability, cytotoxicity, apoptosis, cancer‐associated gene expression analysis of Bcl‐2, Bax, p53 by real‐time polymerase chain reaction and western blot analysis of Bad and p53 protein were performed. Nanoformulated LC significantly inhibited growth and increased the apoptosis of colon cancer cells indicating its potential anti‐cancer activity against colon cancer cells. [ABSTRACT FROM AUTHOR]

Here, the authors report a rapid, simple, and eco‐friendly process for synthesis of Bi2 O3 nano‐needles. Dioscorea alata tuber extract was used as both reducing and capping agent for the first time. These nanoparticles were characterised by X‐ray diffraction, field emission scanning electron microscope, and Fourier transform infrared (FTIR) spectrometry, the nano‐structured Bi2 O3 needles have an average diameter of 158 nm with the lengths in the range of 1–3 μm. CLSI M27‐A2 standard was followed for evaluation of anti‐fungal activity. Bi2 O3 nano‐needles show remarkable activity against Candida albicans. It exhibits four time greater activity than bulk Bi2 O3 powder and two time greater activity than itraconazole, which makes it a potent anti‐fungal drug. [ABSTRACT FROM AUTHOR]

Acute lymphoblastic leukemia (ALL) is the white blood cell cancer in children. L‐asparaginase (L‐ASNase) is one of the first drugs used in ALL treatment. Anti‐tumor activity of L‐ASNase is not specific and indicates limited stability in different biological environments, in addition to its quick clearance from blood. The purpose of the present study was to achieve a new L‐ASNase polymer bioconjugate to improve pharmacokinetic, increase half‐life and stability of the enzyme. The conjugations were achieved by the cross‐linking agent of 1‐ethyl‐3‐(3‐ dimethylaminopropyl) carbodiimide (EDC) which activates the carboxylic acid groups of polymeric nanoparticles to create amide bond. EDC conjugated the L‐ASNase to two biodegradable polymers including; Ecoflex® and poly (styrene‐co‐maleic acid) (PSMA) nanoparticles. To achieve optimal L‐ASNase nanoparticles the amounts of each polymer and the crosslinker were optimized and the nanoparticles were characterized according to their particle size, zeta potential and percent of conjugation of the enzyme. The results showed that conjugated enzyme had more stability against pH changes and proteolysis. It had lower Km value (indicating more affinity to the substrate) and greater half‐life in plasma and phosphate buffered saline, in comparison to native enzyme. Generally, the conjugated enzyme to PSMA nanoparticles showed greater results than Ecoflex® nanoparticles. [ABSTRACT FROM AUTHOR]

Drug delivery is one of the most important challenges in the domain of health. Non‐toxic and biocompatible carriers are provided by human serum albumin nano‐capsule (HSA/NC) for drug delivery applications. In this study, HSA, with high loadings of drug‐modified cobalt ferrite (CoFe2 O4) magnetic nanoparticle (CoFe2 O4 /MNPs) was fabricated for epirubicin anticancer drug delivery. In the initial step, CoFe2 O4 /MNPs was synthesised via co‐precipitation technique and characterised by X‐ray powder diffraction, vibrating sample magnetometry, energy dispersive X‐ray analysis, scanning electron microscopy and map analysis. Furthermore, CoFe2 O4 /MNPs and epirubicin were loaded into HSA/NC and utilised as a novel system against breast cancer cell line (MCF‐7). IC50 for free epirubicin, unloaded CoFe2 O4 /MNPs/HSA/NC, CoFe2 O4 /MNPs and epirubicin‐loaded CoFe2 O4 /MNPs/HSA/NC were 7.7, 2400, 840 and 430 μg/ml, respectively. The results obtained revealed high cytotoxicity effect of epirubicin‐loaded CoFe2 O4 /MNPs on breast cancer cell line. [ABSTRACT FROM AUTHOR]

To grapple with multidrug resistant bacterial infections, implementations of antibacterial nanomedicines have gained prime attention of the researchers across the globe. Nowadays, zinc oxide (ZnO) at nano‐scale has emerged as a promising antibacterial therapeutic agent. Keeping this in view, ZnO nanostructures (ZnO‐NS) have been synthesised through reduction by P. aphylla aqueous extract without the utilisation of any acid or base. Structural examinations via scanning electron microscopy (SEM) and X‐ray diffraction have revealed pure phase morphology with highly homogenised average particle size of 18 nm. SEM findings were further supplemented by transmission electron microscopy examinations. The characteristic Zn–O peak has been observed around 363 nm using ultra‐violet–visible spectroscopy. Fourier‐transform infrared spectroscopy examination has also confirmed the formation of ZnO‐NS through detection of Zn–O bond vibration frequencies. To check the superior antibacterial activity of ZnO‐NS, the authors' team has performed disc diffusion assay and colony forming unit testing against multidrug resistant E. coli, S. marcescens and E. cloacae. Furthermore, protein kinase inhibition assay and cytotoxicity examinations have revealed that green fabricated ZnO‐NS are non‐hazardous, economical, environmental friendly and possess tremendous potential to treat lethal infections caused by multidrug resistant pathogens. [ABSTRACT FROM AUTHOR]

Biotinylated chitosan/poly(methyl vinyl ether‐alt ‐maleic acid) (PMVEMA) copolymer was synthesised by an amide reaction in two steps. Structural characterisation was performed using 1 HNMR and Fourier transform infra‐red (FTIR) spectra. Critical micelle concentration (CMC) of the copolymer was determined by pyrene as a fluorescent probe. Doxorubicin (DOX) was loaded in the micelles by the direct dissolution method. The effects of different variables including type of copolymer, copolymer concentration, stirring rate and stirring time were studied on the physicochemical properties of the micelles including: particle size, zeta potential, release efficiency and loading efficiency of nanoparticles using an irregular factorial design. The in vitro cytotoxicity of DOX‐loaded biotin‐targeted micelles was studied in HepG2 cells which over express biotin receptors by 3, 5‐[dimethylthiazol‐2‐yl]‐2, 5‐diphenyl tetrazolium bromide assay. The successful synthesis of the biotinylated copolymer of chitosan/PMVEMA was confirmed by FTIR and 1 HNMR. The optimised micelles showed the CMC of 33 μg/ml, particle size of 247 ± 2 nm, zeta potential of +9.46 mV, polydispersity index of 0.22, drug‐loading efficiency of 71% and release efficiency of 84.5 ± 1.6%. The synthesised copolymer was not cytotoxic. The cytotoxicity of DOX‐loaded in targeted micelles on HepG2 cell line was about 2.2‐fold compared with free drug. [ABSTRACT FROM AUTHOR]

Drug treatment adherence is one of the biggest issues in tuberculosis (TB) treatment. Including DOTS (Directly Observed Treatment, Short‐course) program, many programs for TB cases have yielded marginal success and the new drug resistance varieties of TB persist. During the 1960s, researchers have projected naphthoquinone–mercuric chloride (N‐M) test as the single most way to objectively track the presence of isoniazid (INH) in urine and hence treatment adherence. INH is metabolised by cytochrome P450s and usually cleared from body within 8 h. Hence, the typical INH levels in biological fluids are within 1–5 μg/ml. The N‐M test practically works at 10–50 μg/ml and the authors developed the sodium polyacrylate (SPA) as a solid surface to improve detection limit of INH by 6–10 fold. The modification involves absorbing the reagents of N‐M test on the SPA surface and lyophilised material is directly used for diagnosis. The dry beads can detect 1–2 μg/ml of INH in saliva. The test performed with spiked as well as clinical samples and the results have good correlation. This new test has a realistic chance of tracking the TB treatment adherence remotely and in that direction a system was projected for implementation. [ABSTRACT FROM AUTHOR]

The authors report a controlled synthesis of biocompatible ZnO and acarbose‐capped nanohybrids, and examined the inhibition activities of these nanosystems with human salivary α ‐amylase (HSA) activity. XRD measurements reveal ZnO present in wurtzite phase with hexagonal structure. The average size of ZnO particles for the two studied nanosystems was estimated to lie between 10 to 12 nm using Scherrer equation. These particles depict the onset of absorption at about 320 nm and the band‐gap emission at about 370 nm, which are fairly blue shifted as compared with the bulk ZnO and have been understood due to the size quantisation effect. The inhibitory action of thioglycerol capped ZnO nanoparticles (SP1) and acarbose drug (used for diabetes type II) capped ZnO (SP2) for HSA was observed to 61 and72%, respectively. The inhibition activity of the SP1 alone was found to be very similar to that of acarbose and the coating of these particles with drug (SP2) demonstrated an enhancement in inhibition activity of the enzyme by about 30%. From the inhibition studies, it is confirmed that these nanosystems showed better inhibition activity at physiological temperature and pH. These nanosystems are projected to have potential applications in diabetes type II control. [ABSTRACT FROM AUTHOR]

This study reports screening of 102 Iranian medicinal plant species belonging to 49 families for the biosynthesis of colloidal silver nanoparticles (AgNPs). Among tested plants, 37 species in 19 plant families are new bio‐resources in this regard. Water extracts of macerated plant parts are used in this survey. Six of the bioactive plants are selected for further analysis. They produced amorphous spherical 40–70 nm AgNPs. Biosynthesised colloidal AgNPs are characterised by UV–visible spectroscopy, transmission electron microscopy and scanning electron microscopy. Families of Lamiaceae (8 out of 12), Leguminosae (7 out of 9), Liliaceae (4 out of 7) contained most bio active species. No correlation noticed between bioactivity and pH of plant water‐extracts. The simple procedure used in this study may form a platform for mass production of environmentally safe and eco‐friendly green production of these multipurpose AgNPs in future; however, optimisation protocols need to be well documented. [ABSTRACT FROM AUTHOR]

Biological synthesis of nanomaterials is a growing innovative approach and it was broadly utilised in the field of nanotechnology and nanomedicine. This study illustrates that biosynthesis of silver nanoparticles (AgNPs) using fucoidan extracted from seaweed Padina tetrastromatica. The functional groups of extracted fucoidan were characterised by Fourier transform infrared spectroscopy (FTIR) and used to NPs synthesis. Synthesised AgNPs were characterised by ultraviolet–visible spectra, scanning electron microscope, energy dispersive X‐ray, transmission electron microscope, selected area electron diffraction and FTIR. In this study, their main focus is enhancement antibacterial activity of AgNPs coated antibiotics against antibiotic resistant bacteria. Among the microorganisms, Serratia nematodiphila was resistant to novobiocin and penicillin, but it was sensitive to AgNPs impregnated antibiotic discs. The zone of inhibition was 12 and 15 mm. The synergistic effect of combined antibiotics and AgNPs resulted in increased fold area which was greater than the sum of their separate effects. It reveals that AgNPs are highly sought in the medicinal field due to their broad spectrum of antibacterial activity and relatively cheaper. This enhanced synergistic effect potentially superior to control the growth of bacteria and it is the budding process for the development of new remedial agents for severe diseases. [ABSTRACT FROM AUTHOR]

Silver nanoparticles (AgNPs) were synthesised from aqueous Ag nitrate through a simple, competent and eco‐friendly method using the leaf extract of Ipomoea eriocarpa as reducing as well as capping agent. Ultraviolet–visible absorption spectroscopy was used to confirm the formation of AgNPs which displayed the substantiation of surface plasmon bands at 425 nm. The NPs were also characterised using Fourier transformer infrared spectroscopy, X‐ray diffraction method, transmission electron microscope and zeta potential. The characterisation study confirmed the formation of AgNPs, their spherical shape and average diameter of 12.85 ± 8.65 nm. Zeta potential value of −20.5 mV suggested that the AgNPs are stable in the suspension. The aqueous extract and the AgNPs were further screened for in vivo anti‐inflammatory activity using carrageenan‐induced paw edema in male Wistar rats. The study demonstrated that the AgNPs (1 ml kg−1) had a significant (p < 0.05) anti‐edemic effect and inhibition was observed from the first hour (21.31 ± 1.34) until the sixth hour (52.67 ± 1.41), when the inhibitory effect was greatest and superior to the aqueous extract and the standard, diclofenac. [ABSTRACT FROM AUTHOR]

Breast cancer accounts for the first highest mortality rate in India and second in world. Though current treatment strategies are effectively killing cancer cells, they also end in causing severe side effects and drug resistance. Curcumin is a nutraceutical with multipotent activity but its insolubility in water limits its therapeutic potential as an anti‐cancer drug. The hydrophilicity of curcumin could be increased by nanoformulation or changing its functional groups. In this study, curcumin is loaded on mesoporous silica nanoparticle and its anti‐cancer activity is elucidated with MCF‐7 cell death. Structural characteristics of Mobil Composition of Matter ‐ 41(MCM‐41) as determined by high‐resolution transmission electron microscopy (HR‐TEM) shows that MCM‐41 size ranges from 100 to 200 nm diameters with pore size 2–10 nm for drug adsorption. The authors found 80–90% of curcumin is loaded on MCM‐41 and curcumin is released efficiently at pH 3.0. The 50 µM curcumin‐loaded MCM‐41 induced 50% mortality of MCF‐7 cells. Altogether, their results suggested that increased curcumin loading and sustained release from MCM‐41 effectively decreased cell survival of MCF‐7 cells in vitro. [ABSTRACT FROM AUTHOR]

Excessive use of antibiotics has posed two major challenges in public healthcare. One of them is associated with the development of multi‐drug resistance while the other one is linked to side effects. In the present investigation, the authors report an innovative approach to tackle the challenges of multi‐drug resistance and acute toxicity of antibiotics by using antibiotics adsorbed metal nanoparticles. Monodisperse silver nanoparticles (SNPs) have been synthesised by two‐step process. In the first step, SNPs were prepared by chemical reduction of AgNO3 with oleylamine and in the second step, oleylamine capped SNPs were phase‐transferred into an aqueous medium by ligand exchange. Antibiotics – tetracycline and kanamycin were further adsorbed on the surface of SNPs. Antibacterial activities of SNPs and antibiotic adsorbed SNPs have been investigated on gram‐positive (Staphylococcus aureus, Bacillus megaterium, Bacillus subtilis), and gram‐negative (Proteus vulgaris, Shigella sonnei, Pseudomonas fluorescens) bacterial strains. Synergistic effect of SNPs on antibacterial activities of tetracycline and kanamycin has been observed. Biocidal activity of tetracycline is improved by 0–346% when adsorbed on SNPs; while for kanamycin, the improvement is 110–289%. This synergistic effect of SNPs on biocidal activities of antibiotics may be helpful in reducing their effective dosages. [ABSTRACT FROM AUTHOR]

Colloidal silver nanoparticles (AgNPs) have attracted much attention in recent years as diagnostics and new drug delivery system in cancer medicine. To study the effects of plumbagin (PLB), a relatively non‐toxic napthaquinone isolated from the roots of Plumbago indica in human cervical cancer cell line and developed a formulation to enhance its cytotoxic activities. Silver nanoparticles were synthesised by chemical reduction method and complexed with PLB. Both the AgNPs and the complex PLB‐AgNPs were characterised by dynamic light scattering, high‐resolution scanning electron microscopy and transmission electron microscopy. The amount of PLB and PLB‐AgNPs internalised was determined by ultra‐violet–visible spectrophotometer. Cell inhibition was determined by sulphorhodamine B assay. Mitotic index was determined by Wright–Giemsa staining. Apoptosis induction was assessed by western blot using cleaved poly adenosine diphosphate‐ribose polymerase antibody. The scanning electron microscope analysis indicated an average particle size of 32 ± 8 nm in diameter. Enhanced internalisation of PLB into the HeLa cells was observed in PLB‐AgNPs. PLB inhibited proliferation of cells with IC50 value of about 18 ± 0.6 µM and blocked the cells at mitosis in a concentration‐dependent manner. PLB also inhibited the post‐drug exposure clonogenic survival of cells and induced apoptosis. The antiproliferative, antimitotic and apoptotic activities were also found to be increased when cells were treated with PLB‐AgNPs. The authors results support the idea that AgNP could be a promising and effective drug delivery system for enhanced activity of PLB in cancer treatment. [ABSTRACT FROM AUTHOR]

In this work, N, O‐carboxymethyl chitosan (CMCS) samples from virgin chitosan (CS) were synthesised and CMCS/polyethylene oxide (PEO) (50/50) blend nanofibrous samples were successfully electrospun from their aqueous solution. The electrospinning conditions to achieve smooth and fine diameter nanofibrous mats were optimised via D‐optimal design approach. Afterwards, vitamin C and phenytoin sodium (PHT‐Na) were added to these samples for producing wound dressing materials. H‐nuclear magnetic resonance, scanning electron microscopy and Fourier transform infrared tests for the evaluation of functionalised CS, morphology and biodegradability studies of CMCS/PEO blend nanofibrous samples were applied. The kinetic and drug release mechanism for vitamin C and PHT‐Na drug‐loaded electrospun samples were also investigated by UV‐vis spectrophotometer and high performance liquid chromatography, respectively. The results showed an approximately similar drug release rate of the two drugs and followed Higuchi's kinetic model. The stem cells viability and their adhesion on the surface of the samples containing PHT‐Na and vitamin C were carried out using MTT assay and the best cells' biocompatibility was obtained using both drugs into the CMCS/PEO nanofibrous samples. Moreover, the in vivo animal wound model results revealed that the electrospun samples containing vitamin C and PHT‐Na (1%) had a remarkable efficiency in the wounds' closure and their healing process compared with vitamin C/PHT‐Na (50/50) ointment. Finally, the histology observations showed that the wound treated with optimised electrospun samples containing two drugs enabled regeneration of epidermis layers due to collagen fibres accumulation followed by granulating tissues formation without necrosis. [ABSTRACT FROM AUTHOR]

A novel hierarchical porous bioactive glasses were synthesised with cattail stem and triblock polyethylene oxide–propylene oxide block copolymer (P123) as macroporous template and mesoporous template, respectively. The structural and textural properties of materials were characterised by X‐ray diffraction, scanning electron microscope, Fourier transform infrared spectroscopy, nitrogen adsorption–desorption, energy dispersive spectrometer and vibrating sample magnetometer technique. The results reveal the bioglasses possess multilevel porous structure with the macroporous size about 50 μm and the mesopore with the diameter of 3.86 nm. Furthermore, metformin HCl was used as the model drug. The drug release kinetics and hydroxyapatite (HAP, (Ca10 (PO4)6 (OH)2)) inducing‐growth ability of the composites were studied, respectively. The system exhibits the fast HAP inducing‐growth ability and long‐term drug delivery, making them a good candidate for bone tissue regeneration. [ABSTRACT FROM AUTHOR]

A novel pH‐sensitive drug release system has been synthesised by functional mesoporous silica materials. SBA‐15, calcium modified SBA‐15 (Ca‐SBA‐15) and phosphate modified SBA‐15 (PO4 ‐SBA‐15) were synthesised using solvent evaporation method. It is a simple and feasible way to prepare the doping mesoporous silica materials. They show the large surface are, high pore volume and uniform pore size. Metformin hydrochloride was used as the model drug, and the control release behaviour was investigated. The functional mesoporous silica materials show the pH sensitive drug release behaviour because of the adjustable interaction between the drug molecule and the host. [ABSTRACT FROM AUTHOR]

Lawsonia inermis mediated synthesis of silver nanoparticles (Ag‐NPs) and its efficacy against Candida albicans, Microsporum canis, Propioniabacterium acne and Trichophyton mentagrophytes is reported. A two‐step mechanism has been proposed for bioreduction and formation of an intermediate complex leading to the synthesis of capped nanoparticles was developed. In addition, antimicrobial gel for M. canis and T. mentagrophytes was also formulated. Ag‐NPs were synthesized by challenging the leaft extract of L. inermis with 1 mM AgNO3. The Ag‐NPs were characterized by Ultraviolet‐Visible (UV–Vis) spectrophotometer and Fourier transform infrared spectroscopy (FTIR). Transmission electron microscopy (TEM), nanoparticle tracking and analysis sytem (NTA) and zeta potential was measured to detect the size of Ag‐NPs. The antimicrobial activity of Ag‐NPs was evaluated by disc diffusion method against the test organisms. Thus these Ag‐NPs may prove as a better candidate drug due to their biogenic nature. Moreover, Ag‐NPs may be an answer to the drug‐resistant microorganisms. [ABSTRACT FROM AUTHOR]

Ligand–receptor binding site model is used to elucidate the binding affinity between ligands and receptors, with transistor‐based sensors. AlGaN/GaN high electron mobility transistors (HEMTs) were immobilised with antibodies and human immunodeficiency virus type 1 reverse transcriptase enzymes to detect peptides and human immunodeficiency virus drugs, respectively. The signals generated by the sensors because of the binding of the ligands to the receptors were fitted into the binding‐site models and analysed. The dissociation constants of the ligand–receptor pairs and the number of the binding sites on the receptors were revealed. The results are very consistent with the data reported by the other methods from the literatures. The incorporation of the HEMTs and the binding‐site models is demonstrated to be useful for studying the mechanism of the biomolecular interaction and the application for quick and cost‐effective drug developments. [ABSTRACT FROM AUTHOR]