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The Internet of Bio-Nano Things concept (IoBNT) emerged from the need to establish connections between biological nanomachines, the intra-body nanonetwork, and the cyber internet to facilitate information exchange. While extensive research has concentrated on optimizing communication efficiency among nanodevices within networks, challenges such as IoBNT security and the interface linking nanonetwork to the internet have remained unaddressed. Consequently, this study introduces a privacy scheme designed to operate atop the Physical Cyber Interface (pHCI) within the IoBNT framework. Our proposed chaotic system derives its foundation from the command signals issued by medical personnel to pHCI devices implanted within the human body. It employs a concealed version of features generated through a Modified Quadratic Map (MQM) to enhance the privacy of patient information and to ensure a precise dosage release. Additionally, our scheme incorporates Binary Phase Shifting Key (BPSK) modulation through the incorporation of a carrier wave, along with feature extraction with zero-crossing rates. This privacy scheme significantly amplifies the key space, thereby guaranteeing an accurate right dose release with the protection of patient privacy. To assess the performance of our proposed scheme, we evaluate its operation on top of the pHCI device using various performance metrics. Subsequently, we study its performance by employing multi-compartmental models in both the forward and reverse pHCI directions of the IoBNT paradigm. The results from our simulation model clearly illustrate that the IoBNT-based privacy scheme has potential to enhance the delivery of therapeutic drugs to target cells while effectively addressing privacy concerns. An evaluation of performance metrics for two binary codes (thermal and light) reveals sensitivity and specificity rates of 95.333% and 95%, 100%, and 100%, respectively. Furthermore, the performance of our proposed privacy scheme, as measured by EER, accuracy, NPV, and PPV, has proven to be highly satisfactory. Hence, our proposed scheme makes significant role in enhancing the security of the physical cyber interface device while remaining cost-effective, and ensuring the safety of patients' life and confidentiality. [ABSTRACT FROM AUTHOR]

Chemotherapeutic drug delivery systems are commonly limited by their short half-lives, poor bioavailability, and unsuccessful targetability. Herein, pH-responsive hybrid NPs consist of benzimidazole-coated mesoporous silica nanoparticles (BZ-MSN) loaded with naturally occurring flavonoid quercetin (QUE-BZ-MSN). The NPs were further capped with beta-cyclodextrin (BCD) to obtain our desired BCD-QUE-BZMSN, with a zeta potential around 7.05 ± 2.37 mV and diameter about 115.2 ± 19.02 nm. The abundance of BZ onto the nanoparticles facilitates targeted quercetin chemotherapy against model lung and liver cancer cell lines. FTIR, EDX, and NMR analyses revealed evidence of possible surface functionalizations. Powder XRD analysis showed that our designed BCD-QUE-BZMSN formulation is amorphous in nature. The UV and SEM showed that our designed BCD-QUE-BZMSN has high drug entrapment efficiency and a nearly spherical morphology. In vitro, drug release assessments show controlled pH-dependent release profiles that could enhance the targeted chemotherapeutic response against mildly acidic regions in cancer cell lines. The obtained BCD-QUE-BZMSN nanovalve achieved significantly higher cytotoxic efficacy as compared to QUE alone, which was evaluated by in vitro cellular uptake against liver and lung cancer cell lines, and the cellular morphological ablation was further confirmed via inverted microscopy. The outcomes of the study imply that our designed BCD-QUE-BZMSN nanovalve is a potential carrier for cancer chemotherapeutics. [ABSTRACT FROM AUTHOR]

Given the inherent complexity of cancer treatment and the limitations of singular therapeutic modalities, the development of an optimal nanocarrier system capable of facilitating synergistic organic therapy remains a profound challenge. Herein, a synergetic chemo/photothermal therapy nanoplatform was exploited to specifically tailor for the augmented treatment of oral cancer. A cancer cell membrane-camouflaged nanocarrier was developed with a polymeric core encapsulating doxorubicin (DOX). The designed nanoparticles (CC@DOXNPs) inherited the functional membrane proteins from the source cancer cells, endowing their remarkable ability to selectively target cancer cells delivery both in vitro and in vivo. Moreover, indocyanine green (ICG), modified with the phospholipid polymer DSPE-PEG 2000 , was introduced into the cancer cell membrane to enable photothermal therapy. Remarkably, as evaluated in a preclinical subcutaneous and orthotopic mice model of oral cancer, biomimetic composite nanotherapeutics (lip-CC@DOXNPs) could significantly accumulate into tumor lesion and effectively suppress tumor growth under the near-infrared (NIR, 808 nm) irradiation, without causing the undesirable systematic toxicity. Moreover, RNA sequence analyses indicated that chemo/photothermal therapy triggers the intrinsic mitochondria-mediated apoptosis through the p53 signaling pathway. Combined with gene expression results, this intrinsic mitochondria-mediated apoptosis pathway was further demonstrated. Collectively, this multifaceted nanoplatforms possess a remarkable capability for tumor-targeting drug delivery, and the proficient photothermal conversion ability, rendering them an ideal therapeutic approach for oral cancer treatment. [Display omitted] • Biomimetic Nanotherapeutics were fabricated for synergetic therapy of oral cancer. • Both subcutaneous and orthotopic models of oral cancer were constructed. • Synergetic therapy induced HSC-3 cells apoptosis through p53 pathway. • Provides a new idea for clinical treatment of oral cancer. [ABSTRACT FROM AUTHOR]

The molecular communication system (MCS) is mainly based on the design structure of the nanodevices which are employed as nano-transmitter (Nano-TX) and nano-receiver (Nano-RX), owing to the limited drug-reservoir capacity. The current work addresses the physical design of such nanodevices and the coordination of molecular communication to accomplish an end-to-end capacity system model, which can be employed in the targeted drug delivery system (TDDS). In MCS, Nano-RX is a spherical structure with a cylindrical shell with adapting receptors that enables an increase in the received number of drug molecules according to the transmission rate. On the other hand, the more realistic structure of Nano-TX is a cylindrical reservoir capable of controlling the emitted nanocarriers in the blood vessel. The analytical framework and the performance of the proposed MCS are presented by using a compartmental model while a closed-form expression of the proposed end-to-end channel capacity is obtained. The performance evaluation is evaluated by applying network performance metrics such as channel capacity, throughput, and efficiency. The simulation results show that the proposed model can enhance the delivery of the therapeutic dose and thus minimize the side effects on healthy cells compared with conventional schemes. [ABSTRACT FROM AUTHOR]

Purpose: In the present study, we investigated the magnetic solid lipid nanoparticles (mSLNs) for targeted delivery of doxorubicin (DOX) into breast cancer cells. Methods: The synthesis of iron oxide nanoparticles was carried out by co-precipitation of a ferrous and ferric aqueous solution with the addition of a base; moreover, during precipitation process, the magnetite nanoparticles should be coated with stearic acid (SA) and tripalmitin (TPG). An emulsification dispersion-ultrasonic method was employed to prepare DOX loaded mSLNs. Fourier transforms infrared spectroscopy, vibrating sample magnetometer, and photon correlation spectroscopy (PCS) were used to characterize the subsequently prepared nanoparticles. In addition, the antitumor efficacy of particles was evaluated on MCF-7 cancer cell lines. Results: The findings showed that entrapment efficiency values for solid lipid and magnetic SLNs were 87±4.5% and 53.7±3.5%, respectively. PCS investigations showed that particle size increased with magnetic loading in the prepared NPs. In vitro drug release of DOX-loaded SLN and DOX-loaded mSLN in phosphate buffer saline (pH=7.4) showed that the amount of drug released approached 60% and 80%, respectively after 96 h of incubation. The electrostatic interactions between magnetite and drug had little effect on the release characteristics of the drug. The higher toxicity of DOX as nanoparticles compared to free drug was inferred from in vitro cytotoxicity. Conclusion: DOX encapsulated magnetic SLNs can act as a suitable and promising candidate for controlled and targeted therapy for cancer.

The epidermal growth factor receptor (EGFR) is vital for many different types of cancer. Nimotuzumab (NmAb), an anti-EGFR monoclonal antibody (mAb), is used against some of EGFR-overexpressed cancers in various countries. It targets malignant cells and is internalized via receptor-mediated endocytosis. We hypothesized that mAb-nanoparticle conjugation would provide an enhanced therapeutic efficacy, and hence we conjugated NmAb with 27 nm spherical gold nanoparticles (AuNPs) to form AuNP-NmAb nanoconjugates. Using biophysical and spectroscopic methods, including ultraviolet-visible spectroscopy (UV-Vis), transmission electron microscopy (TEM), dynamic light scattering (DLS), nanoparticle tracking analysis (NTA), sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), and Fourier-transform infrared spectroscopy (FTIR), the AuNP-NmAb complex was characterized. Furthermore, in vitro studies were performed using a medium-level EGFR-expressing skin cancer cell (A431, EGFRmedium) and low-level EGFR-expressing lung cancer cell (A549, EGFRlow) to evaluate anti-tumor and cellular uptake efficiency via MTT assay and single-particle inductively coupled plasma mass spectrometry (spICP-MS), respectively. In comparison to NmAb monotherapy, the AuNP-NmAb treatment drastically reduced cancer cell survivability: for A431 cells, the IC50 value of AuNP-NmAb conjugate was 142.7 µg/mL, while the IC50 value of free NmAb was 561.3 µg/mL. For A549 cells, the IC50 value of the AuNP-NmAb conjugate was 163.6 µg/mL, while the IC50 value of free NmAb was 1,082.0 µg/mL. Therefore, this study highlights the unique therapeutic potential of AuNP-NmAb in EGFR+ cancers and shows the potential to develop other mAb nanoparticle complexes for a superior therapeutic efficacy. [ABSTRACT FROM AUTHOR]

The need for non-invasive therapies capable of conserving drug efficiency and stability while having specific targetability against colorectal cancer (CRC), has made nanoparticles preferable vehicles and principal building blocks for the development of complex and multi-action anti-tumoral approaches. For that purpose, we herein report the production of a combinatory anti-tumoral nanotherapy using the production of a new targeting towards CRC lines. To do so, Magneto-fluorescent NANO3 nanoparticles were used as nanocarriers for a combination of the drugs doxorubicin (DOX) and ofloxacin (OFLO). NANO3 nanoparticles' surface was modified with two different targeting agents, a newly synthesized (anti-CA IX acetazolamide derivative (AZM-SH)) and a commercially available (anti-epidermal growth factor receptor (EGFR), Cetuximab). The cytotoxicity revealed that only DOX-containing nanosystems showed significant and even competitive cytotoxicity when compared to that of free DOX. Interestingly, surface modification with AZM-SH promoted an increased cellular uptake in the HCT116 cell line, surpassing even those functionalized with Cetuximab. The results show that the new target has high potential to be used as a nanotherapy agent for CRC cells, surpassing commercial targets. As a proof-of-concept, an oral administration form of NANO3 systems was successfully combined with Eudragit® enteric coating and studied under extreme conditions. [ABSTRACT FROM AUTHOR]

Enzyme-activatable drug delivery systems have been developed for cancer diagnosis and therapy. However, targeted intracellular drug delivery is a challenge for precisely tumor imaging and therapy due to the increased stability of copolymer nanoparticles (NPs) is accompanied by a notable decrease in enzyme degradation. Herein, disulfide bond was designed as an enzyme-activatable molecular switch of SS-P(G 2) 2 /DOX NPs. The copolymer NPs consists of polyvinylpyrrolidone (PVP) with disulfide bonds in the center and enzyme-degradable peptide dendrites (Phe-Lys) to form dendritic-linear-dendritic triblock copolymers (TBCs). The amphiphilic TBCs could be split into two identical amphiphilic diblock copolymers (DBCs) by glutathione (GSH) in cancer cells specifically while maintaining the same hydrophilic-lipophilic equilibrium. This structural transformation significantly reduced the stability of copolymer NPs and enhanced sensitivity of DOX release by cathepsin B-activated. Subsequently, the released DOX acted as an indicator of fluorescence imaging and chemotherapy drug for cancer cells. The polymeric NPs achieved excellent drug-loaded stability and prolonged blood circulation in vivo , and realized fluorescence imaging and specific cancer cell killing capabilities by responding to the overexpression of GSH and cathepsin B in tumor cells. Furthermore, the copolymer NPs demonstrated excellent blood compatibility and biosafety. Therefore, a novel strategy based on one tumor marker acting as the switch for another tumor microenvironment responsive drug delivery system could be designed for tumor intracellular imaging and chemotherapy. A highly stable hydrophobic-hydrophilic-hydrophobic three blocks copolymer nanocarriers with the disulfide bond in the center has been designed to respond by tumor-overexpressed GSH, and transform into half molecular weight and enzyme-accessible diblock copolymer nanocarrier. This design enhanced drug-loaded stability of NPs and prolonged blood circulation in vivo , and realized specific fluorescence imaging and antitumor activity by responding to the overexpression of GSH and cathepsin B in tumor cells. [Display omitted] • SS-P(G 2) 2 amphiphilic triblock copolymers of SS-P(G 2) 2 with disulfide bonds as enzyme activity switch were prepared. • The enzyme-activitable drug release of SS-P(G 2) 2 /DOX NPs was activied by reducing the assembly stability. • SS-P(G 2) 2 /DOX NPs achieved cathepsin B-activatable DOX release with GSH treatment. • Biocompatible, excellent tumor targeting, specific fluorescence imaging capability and antitumor activity in vivo were confirmed. [ABSTRACT FROM AUTHOR]

Non-idealistic pharmaceutical, pharmacokinetic and therapeutic-characteristic predominately combines to decrease the effectiveness of certain composites. For the vectoring of such compounds to target areas, and liposomes and nanoparticles carrier technology provides an interesting and intelligent approach to drug delivery. It provides drug delivery by conjugating the drug to a transporter particle-like, microscopes, liposomes, nanoparticles, et cetera. Due to their small size and other effective properties, microspheres are an important portion of a drug-particle delivery system. The release systems are very important and can compare with the fabrication methods, this when the drug delivery become inside the body. This review highlights different types of drug delivery and drug delivery methods this article also focuses on different types of microspheres such as radioactive float microspheres biological adhesive microspheres, polymeric microbes, microspheres, and magnetic microspheres.

Abstract Immune cells are attractive targets for therapy as they are direct participants in a variety of diseases. Delivering a therapeutic agent only to cells that act on a disease by distinguishing them from other cells has the advantage of concentrating the therapeutic effect and lowering systemic side effects. Distinguishing each immune cell from other immune cells to deliver substances, including drugs and genes, can be achieved using nanotechnology. And also nanoparticles can ensure in vivo stability and sustained drug release. In addition, there is an ease of surface modification, which is an important characteristic that can be utilized in targeted drug delivery systems. This characteristic allows us to utilize various properties that are specifically expressed in each immune cell. A number of studies have delivered various substances specifically to immune cells through surface engineering with active target ligands that can target each immune cell and enzyme-responsive coating, and demonstrated high therapeutic effects compared to conventional treatments. Progress in research on target delivery has been suggested to be a breakthrough for the treatments of various diseases, including cancer treatment.

Liposomes are applied to various anticancer treatments as representative drug delivery carriers. However, liposomes do not have their own targeting properties; therefore, there are limitations in drug delivery to specific tissues or cells. High targetability in drug delivery is an important factor in improving bioavailability and drug efficacy and reducing side effects; recent research has been actively investigated to modify the surface of liposomes to give them specific functions. In this study, we studied a drug delivery system for anticancer treatment that enhances targeting ability through fusion with exosomes on the surface of liposomes. We designed exosome-liposome hybrid nanoparticles loaded with a gemcitabine prodrug as a treatment for pancreatic ductal adenocarcinoma (PDAC). Membrane fusion with exosomes shows excellent targeting ability to pancreatic cancer cells due to intrinsic targeting ability and expansion of the macropinocytosis pathway.

Atherosclerosis (AS) is characterized by the accumulation of lipids within the walls of coronary arteries, leading to arterial narrowing and hardening. It serves as the primary etiology and pathological basis for cardiovascular diseases affecting the heart and brain. However, conventional pharmacotherapy is constrained by inadequate drug delivery and pronounced toxic side effects. Moreover, the inefficacy of nanomedicine delivery systems in controlling disease progression may be attributed to nonspecific clearance by the mononuclear phagocyte system. Thus, a biomimetic platform spontaneously enveloped by red blood cell membrane is exploited for anti-atherosclerosis applications, offering favorable biocompatibility. The CLIKKPF polypeptide is introduced to develop red blood cell membrane spontaneously encapsulated nanotherapeutics only through simple coincubation. Given the functional modifications, RBC@P-LVTNPs is beneficial to facilitate the target drug delivery to the atherosclerotic lesion, responding precisely to the pathological ROS accumulation, thereby accelerating the on-demand drug release. Both in vivo and in vitro results also confirm the significant therapeutic efficacy and favorable biocompatibility of the biomimetic nanomedicine delivery system, thus providing a promising candidate for nanotherapeutics against AS.

Drug delivery can be defined as the group of approaches a drug or pharmacologically active agent can be transported to the target cell to treat disease or health issue. Conventional routes for drug delivery are oral, buccal, rectal, subcutaneous, intranasal, intramuscular, intravenous, pulmonary and transdermal. These are the commonly used methods for treatment of various medical problems but have certain limitations such as instability, risk of displacement, uncontrolled release, side effect such as irritation and pain, slow absorption, enzymatic deterioration and many others. Incorporation of drug into nanocarrier is one of the efficient methods for targeted and sustained delivery of drug. Applications of nanocarriers such as solid nanoparticles, liposomes, dendrimers, polymeric nanoparticles, polymeric micelles, virus like nanoparticles, carbon nanotube and mesoporous silica nanoparticles are discussed in this review. To overcome drawbacks of drug delivery, innovative delivery systems are designed usually termed as smart drug delivery systems which include nucleic acid-based drug delivery system, cell-based drug delivery system, self-nano emulsifying drug delivery system, self-micro emulsifying drug delivery system, chemical and physical stimuli-based drug delivery system, nanoneedles, patches, ultrasound drug delivery and microchip technology. This article focuses of the basic mechanism of drug delivery, pharmacokinetic study, recent innovations and future trends of the drug delivery system.

The epidermal growth factor receptor (EGFR) is vital for many different types of cancer. Nimotuzumab (NmAb), an anti-EGFR monoclonal antibody (mAb), is used against some of EGFR-overexpressed cancers in various countries. It targets malignant cells and is internalized via receptor-mediated endocytosis. We hypothesized that mAb-nanoparticle conjugation would provide an enhanced therapeutic efficacy, and hence we conjugated NmAb with 27 nm spherical gold nanoparticles (AuNPs) to form AuNP-NmAb nanoconjugates. Using biophysical and spectroscopic methods, including ultraviolet-visible spectroscopy (UV-Vis), transmission electron microscopy (TEM), dynamic light scattering (DLS), nanoparticle tracking analysis (NTA), sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE), and Fourier-transform infrared spectroscopy (FTIR), the AuNP-NmAb complex was characterized. Furthermore, in vitro studies were performed using a medium-level EGFR-expressing skin cancer cell (A431, EGFRmedium) and low-level EGFR-expressing lung cancer cell (A549, EGFRlow) to evaluate anti-tumor and cellular uptake efficiency via MTT assay and single-particle inductively coupled plasma mass spectrometry (spICP-MS), respectively. In comparison to NmAb monotherapy, the AuNP-NmAb treatment drastically reduced cancer cell survivability: for A431 cells, the IC50 value of AuNP-NmAb conjugate was 142.7 µg/mL, while the IC50 value of free NmAb was 561.3 µg/mL. For A549 cells, the IC50 value of the AuNP-NmAb conjugate was 163.6 µg/mL, while the IC50 value of free NmAb was 1,082.0 µg/mL. Therefore, this study highlights the unique therapeutic potential of AuNP-NmAb in EGFR+ cancers and shows the potential to develop other mAb nanoparticle complexes for a superior therapeutic efficacy.

Nowadays, the use of nanoparticle‐based drug delivery systems has received much more attention. In this regard, here, graphene quantum dots (GQD) were used as drug carriers as well as imaging agents for cancer cells. In order to optimize the dose of the drug and reduce its side effects for healthy cells, hyaluronic acid was decorated on the surface of GQD to target cancer cells. The morphology and size of the synthesized nanoparticles alone and conjugated with hyaluronic acid were investigated using scanning electron microscopy (SEM) and transmission electron microscopy (TEM); TEM images revealed a particles size of ∼5.67 and ∼8.69 nm, respectively. In the presence of 1‐ethyl‐3‐[3(dimethylamino)propyl]carbodiimide hydrochloride/N‐hydroxysuccinimide (EDC/NHS), hyaluronic acid was bounded to dopamine hydrochloride and was prepared to react with GQD. After synthesis of graphene quantum dot‐hyaluronic acid nanocomposite, curcumin (CUR) as a drug model was loaded on the synthesized nanocarriers, and its loading percentage was measured. The results showed that 98.02% of the drug was loaded on the nanocarriers. Also, the conjugation of each agent on the nanocarrier was approved by photoluminescence spectroscopy, Fourier transform infrared spectroscopy (FTIR), and UV–visible absorption techniques, and the results showed that the reactions were performed correctly. The effect of GQD, graphene quantum dot–hyaluronic acid, CUR, graphene quantum dot‐hyaluronic acid–CUR on the viability of HeLa and L929 cells was evaluated by the MTT test. The results showed that the synthesized nanocarrier is completely biocompatible, and the drug nanocarriers reduce HeLa cell viability significantly due to the mediation of hyaluronic acid–CD44 for drug cell uptake. Simultaneously with drug delivery, the other goal of these nanocarriers is to image cancer cells by emitting fluorescent light. Fluorescent microscopy showed that these nanocarriers were adsorbed on HeLa cells, unlike L929 cells. [ABSTRACT FROM AUTHOR]

Abstract Antibodies have been widely used to provide targeting ability and to enhance bioactivity owing to their high specificity, availability, and diversity. Recent advances in biotechnology and nanotechnology permit site-specific engineering of antibodies and their conjugation to the surfaces of nanoparticles (NPs) in various orientations through chemical conjugations and physical adhesions. This study proposes the conjugation of poly(lactic-co-glycolic acid) (PLGA) NPs with antibodies by using two distinct methods, followed by a comparison between the cell-targeting efficiencies of both techniques. Full-length antibodies were conjugated to the PLGA-poly(ethylene glycol)-carboxylic acid (PLGA-PEG-COOH) NPs through the conventional carbodiimide coupling reaction, and f(ab′)2 antibody fragments were conjugated to the PLGA-poly(ethylene glycol)-maleimide(PLGA-PEG-Mal) NPs through interactions between the f(ab′)2 fragment thiol groups and the maleimide located on the nanoparticle surface. The results demonstrate that the PLGA nanoparticles conjugated with the f(ab′)2 antibody fragments had a higher targeting efficiency in vitro and in vivo than that of the PLGA nanoparticles conjugated with the full-length antibodies. The results of this study can be built upon to design a delivery technique for drugs through biocompatible nanoparticles.

Abstract Nanobubbles are nanometer size bubbles having different constituents of varying physicochemical characteristic for the inner core and outer shell. Nanobubbles are mainly fabricated to improve the stability, bioavailability and improve the biodistribution of the delivered drug to the specific targeted site. Their small sizes bubbles allow the possibility of extravasation from blood vessels into the surrounding tissues and ultrasound-targeted site-specific release with minimal invasiveness. Nanobubbles are developing as important contrast agents for imaging and carriers for drug delivery at targeted region. Sonication is the primary method for preparation of nanobubbles followed by thin-layer evaporation, high shear emulsification, mechanical agitation and coacervation or coalescence. With exposure to ultrasound/extracorporeal shock waves, the drug is liberated from the nanobubbles into the target cells. This review paper is an effort to reveal the different formulation development techniques briefly and varying shell and core content for developing nanobubbles.

The need for non-invasive therapies capable of conserving drug efficiency and stability while having specific targetability against colorectal cancer (CRC), has made nanoparticles preferable vehicles and principal building blocks for the development of complex and multi-action anti-tumoral approaches. For that purpose, we herein report the production of a combinatory anti-tumoral nanotherapy using the production of a new targeting towards CRC lines. To do so, Magneto-fluorescent NANO3 nanoparticles were used as nanocarriers for a combination of the drugs doxorubicin (DOX) and ofloxacin (OFLO). NANO3 nanoparticles’ surface was modified with two different targeting agents, a newly synthesized (anti-CA IX acetazolamide derivative (AZM-SH)) and a commercially available (anti-epidermal growth factor receptor (EGFR), Cetuximab). The cytotoxicity revealed that only DOX-containing nanosystems showed significant and even competitive cytotoxicity when compared to that of free DOX. Interestingly, surface modification with AZM-SH promoted an increased cellular uptake in the HCT116 cell line, surpassing even those functionalized with Cetuximab. The results show that the new target has high potential to be used as a nanotherapy agent for CRC cells, surpassing commercial targets. As a proof-of-concept, an oral administration form of NANO3 systems was successfully combined with Eudragit® enteric coating and studied under extreme conditions.

The blood brain barrier (BBB) maintains the homeostasis of the central nervous system (CNS) and protects the brain from toxic substances present in the circulating blood. However, the impermeability of the BBB to drugs is a hurdle for CNS drug development, which hinders the distribution of the most therapeutic molecules into the brain. Therefore, scientists have been striving to develop safe and effective technologies to advance drug penetration into the CNS with higher targeting properties and lower off-targeting side effects. This review will discuss the limitation of artificial nanomedicine in CNS drug delivery and the use of natural extracellular vesicles (EVs), as therapeutic vehicles to achieve targeted delivery to the CNS. Information on clinical trials regarding CNS targeted drug delivery using EVs is very limited. Thus, this review will also briefly highlight the recent clinical studies on targeted drug delivery in the peripheral nervous system to shed light on potential strategies for CNS drug delivery. Different technologies engaged in pre- and post-isolation have been implemented to further utilize and optimize the natural property of EVs. EVs from various sources have also been applied in the engineering of EVs for CNS targeted drug delivery in vitro and in vivo. Here, the future feasibility of those studies in clinic will be discussed. [ABSTRACT FROM AUTHOR]

A number of preclinical and clinical studies have demonstrated the efficiency of mesenchymal stromal cells to serve as an excellent base for a cell-mediated drug delivery system. Cell-based targeted drug delivery has received much attention as a system to facilitate the uptake a nd transfer of active substances to specific organs and tissues with high efficiency. Human mesenchymal stem cells (MSCs) are attracting increased interest as a promising tool for cell-based therapy due to their high proliferative capacity, multi-potency, and anti-inflammatory and immunomodulatory properties. In particular, these cells are potentially suitable for use as encapsulated drug transporters to sites of inflammation. Here, we studied the in vitro effects of incorporating synthetic polymer microcapsules at various microcapsule-to-cell ratios on the morphology, ultrastructure, cytokine profile, and migration ability of human adipose-derived MSCs at various time points post-phagocytosis. The data show that under appropriate conditions, human MSCs can be efficiently loaded with synthesized microcapsules without damaging the cell’s structural integrity with unexpressed cytokine secretion, retained motility, and ability to migrate through 8 μm pores. Thus, the strategy of using human MSCs as a delivery vehicle for transferring microcapsules, containing bioactive material, across the tissue–blood or tumor–blood barriers to facilitate the treatment of stroke, cancer, or inflammatory diseases may open a new therapeutic perspective.

Artemisinin is used as an antimalarial and anticancer agent with minimal toxic effects on the host body. Biotin-PEG-PCL polymers have been used for targeted drug delivery to cancer, as well as to improve the pharmacokinetics of the drug and reduce its effects. In this study, biotin-conjugated copolymers were fabricated with polymerization of the ring opening method and the properties of copolymer and nanoparticles were investigated using various techniques. The toxicity of artemisinin and its nanoparticles have been investigated on MCF-7 and normal HFF2 cells. The results showed that the encapsulation efficacy of artemisinin in nanoparticles was 45.5 ± 0.41%. The release profile of the drug indicates that the release is slow and controlled and is approximately pH dependent. The results of artemisinin cell culture on human breast cancer cells showed that biotin-PEG-PCL nanoparticles had an inhibitory effect on MCF-7 cells and had no toxic effects on HFF2 cells. Anticancer activity in vivo in the 4T1 breast cancer model showed that tumour volumes were decreased up 40 mm3 by ART-loaded micelles and 76 mm3 by free ART, compared to the control group (2150 mm). In vivo results showed that this formulation significantly increases the accumulation of substances in the tumours. Therefore, the molecular formulation of ART-based copolymers can be a desirable process for cancer treatment purposes.

Phytochemicals are compounds found in plants that have various biological activities and health benefits. Although phytochemicals have diverse therapeutic applications, they confront several challenges, such as poor solubility, instability, and low bioavailability. Phytosomes are used to overcome those challenges. The phytosome is a complex of phytochemicals and phospholipids that transports the drug to the target site, thereby increasing phytochemical absorption and bioavailability. The present study focuses on phytosome preparation methods and evaluation parameters, as well as the role of phytosomes in various ailments such as COVID-19, pulmonary fibrosis, asthma, migraine, arthritis, obesity, neuroprotective, antioxidant, anti-inflammatory, cancer, diabetes, metabolic syndrome, hyperlipidemic, and antimicrobial, which demonstrates phytosome complexes are more potent when compared to free extracts. Due to poor absorption and metabolism, phytoconstituents may not be effective in their free form. Phytosomes make phytoconstituents more bioavailable, stable, and effective. It also discusses recent formulations of phytosomes that can act as an effective or alternative regimen for various health conditions., Competing Interests: Conflicts of interest: In compliance with the ICMJE uniform disclosure form, all authors declare the following: Payment/services info: All authors have declared that no financial support was received from any organization for the submitted work. Financial relationships: All authors have declared that they have no financial relationships at present or within the previous three years with any organizations that might have an interest in the submitted work. Other relationships: All authors have declared that there are no other relationships or activities that could appear to have influenced the submitted work., (Copyright © 2024, P et al.)

Non-idealistic pharmaceutical, pharmacokinetic and therapeutic-characteristic predominately combines to decrease the effectiveness of certain composites. For the vectoring of such compounds to target areas, and liposomes and nanoparticles carrier technology provides an interesting and intelligent approach to drug delivery. It provides drug delivery by conjugating the drug to a transporter particlelike, microscopes, liposomes, nanoparticles, et cetera. Due to their small size and other effective properties, microspheres are an important portion of a drug-particle delivery system. The release systems are very important and can compare with the fabrication methods, this when the drug delivery become inside the body. This review highlights different types of drug delivery and drug delivery methods this article also focuses on different types of microspheres such as radioactive float microspheres biological adhesive microspheres, polymeric microbes, microspheres, and magnetic microspheres. [ABSTRACT FROM AUTHOR]

The Internet of Bio-NanoThings (IoBNTs) is a novel paradigm that derives from synthetic biology and advances in nanotechnology for controlling the embedded nanodevices in various medical applications. However, numerous studies have focused on communication efficiency among the nanodevices in a given network, the challenges such as the design and the development of the nanodevices, and the coordination of molecular communication within the wireless body area network (BAN), and the interface connection between the BAN and the Internet are yet to be addressed. Therefore, in this study, we present a framework analysis comprising of the compartmental model, for studying the effects and variances in drug concentration that occur inside intra-body nanonetworks through IoBNT, while taking into account the properties of target cells as well as the ligand-receptor binding mechanism. A performance analysis of the proposed framework for the forward link (i.e., from the Internet to the intra-body nanonetwork) and reverse link (i.e., from the intra-body nanonetwork to the Internet) is presented. The simulation results of the developed framework reveal its ability to enhance the delivery of therapeutic drugs to the target cell while minimizing the side effects in healthy cells. [ABSTRACT FROM AUTHOR]

Magnetic thermoresponsive nanogels present a promising new approach for targeted drug delivery. In the present study, bovine serum albumin (BSA) loaded thermo-responsive magnetic semi-IPN nanogels (MTRSI-NGs) were developed. At first poly(N-vinyl caprolactam) (PNVCL) was synthesized by free radical polymerization and then MTRSI-NGs were prepared by crosslinking chitosan in presence of chitosan and Fe3O4. The formation of MTRSI-NGs has been confirmed by FTIR, and the average molecular weight of PNVCL was determined by GPC analysis. Rheological and turbidimetry analysis were used to determine lower critical solution temperature (LCST) of PNVCL and magnetic thermo-responsive nanogels (MTRSI-NGs) around 32 and 37 °C, respectively. FE-SEM analysis showed particle size at less than 20 nm in the dried state. Dynamic light scattering determined particle size at about 30 nm in a swelling state. The analysis of release behavior showed that the BSA release ratio at 40 °C was faster than 25 °C. The pH release behavior was evaluated at pH 5.5 and 7.4 and showed that the drug release rate at pH 5.5 was more rapid than pH 7.4. The results show MTRSI-NGs are applicable to protein targeted delivery by thermosensitive targeted drug delivery systems. [ABSTRACT FROM AUTHOR]

Antibodies have been widely used to provide targeting ability and to enhance bioactivity owing to their high specificity, availability, and diversity. Recent advances in biotechnology and nanotechnology permit site-specific engineering of antibodies and their conjugation to the surfaces of nanoparticles (NPs) in various orientations through chemical conjugations and physical adhesions. This study proposes the conjugation of poly(lactic-co-glycolic acid) (PLGA) NPs with antibodies by using two distinct methods, followed by a comparison between the cell-targeting efficiencies of both techniques. Full-length antibodies were conjugated to the PLGA-poly(ethylene glycol)-carboxylic acid (PLGA-PEG-COOH) NPs through the conventional carbodiimide coupling reaction, and f(ab′)2 antibody fragments were conjugated to the PLGA-poly(ethylene glycol)-maleimide(PLGA-PEG-Mal) NPs through interactions between the f(ab′)2 fragment thiol groups and the maleimide located on the nanoparticle surface. The results demonstrate that the PLGA nanoparticles conjugated with the f(ab′)2 antibody fragments had a higher targeting efficiency in vitro and in vivo than that of the PLGA nanoparticles conjugated with the full-length antibodies. The results of this study can be built upon to design a delivery technique for drugs through biocompatible nanoparticles. [ABSTRACT FROM AUTHOR]

[Display omitted] Intranasal delivery provides a direct and non-invasive method for drugs to reach the central nervous system. Nanoparticles play a crucial role as carriers in augmenting the efficacy of brain delivery. However, the interaction between nanoparticles and the nose-to-brain pathway and how the various biopharmaceutical factors affect brain delivery efficacy remains unclear. In this review, we comprehensively summarized the anatomical and physiological characteristics of the nose-to-brain pathway and the obstacles that hinder brain delivery. We then outlined the interaction between nanoparticles and this pathway and reviewed the biomedical applications of various nanoparticulate drug delivery systems for nose-to-brain drug delivery. This review aims at inspiring innovative approaches for enhancing the effectiveness of nose-to-brain drug delivery in the treatment of different brain disorders. [ABSTRACT FROM AUTHOR]

The blood brain barrier (BBB) maintains the homeostasis of the central nervous system (CNS) and protects the brain from toxic substances present in the circulating blood. However, the impermeability of the BBB to drugs is a hurdle for CNS drug development, which hinders the distribution of the most therapeutic molecules into the brain. Therefore, scientists have been striving to develop safe and effective technologies to advance drug penetration into the CNS with higher targeting properties and lower off-targeting side effects. This review will discuss the limitation of artificial nanomedicine in CNS drug delivery and the use of natural extracellular vesicles (EVs), as therapeutic vehicles to achieve targeted delivery to the CNS. Information on clinical trials regarding CNS targeted drug delivery using EVs is very limited. Thus, this review will also briefly highlight the recent clinical studies on targeted drug delivery in the peripheral nervous system to shed light on potential strategies for CNS drug delivery. Different technologies engaged in pre- and post-isolation have been implemented to further utilize and optimize the natural property of EVs. EVs from various sources have also been applied in the engineering of EVs for CNS targeted drug delivery in vitro and in vivo. Here, the future feasibility of those studies in clinic will be discussed.

Dipole field navigation (DFN) is a method that has been developed to deliver therapeutics toward tumoral regions by navigating microcarriers in the vascular network. To do so, DFN distorts the high uniform magnetic field of a clinical magnetic resonance imaging (MRI) scanner using precisely located ferromagnetic balls to create magnetic gradients to implement the directional forces required to navigate magnetically saturated therapeutic microcarriers along a planned trajectory in the vasculature. Such local distortions of the magnetic field prevent MRI-based targeting assessments. As such, a system must be put in place to precisely move the ferromagnetic balls back-and-forth to alternate between MRI targeting assessment and DFN. Here, a piezoelectric actuation system is proposed. In vitro experiments conducted inside the bore of a 3T clinical MRI scanner show the feasibility for reliable targeting assessments with magnetic distortions sufficient to achieve a 100% success rate of magnetic microparticles being navigated through a predefined target branch at a bifurcation. Results show a 21.6% decrease in SNR with a maximum value of 2.2% MR-image distortion and a faintly visible image artifact after the piezoelectric system moved the soft ferromagnetic balls in the MRI targeting assessment position. [ABSTRACT FROM AUTHOR]

Selective ligands of an urea-based prostate specific membrane antigen with a phenylalanine/tyrosine-based dipeptide linker and with a mingled chiral centers configuration and/or substituted aromatic fragments were prepared in seven steps by liquid- and in six steps by solid-phase synthesis. In vitro test for inhibiting the cleavage of N -acetylaspartylglutamate revealed the optimum linker containing l -phenylalanine in the structure on the N-terminus of a dipeptide chain. [ABSTRACT FROM AUTHOR]

The concept of Internet of bio-nano thing (IoBNT) arose from the need for Biological nanomachines to interconnect intra-body nanonetwork with the cyber Internet aiming to exchange information. However, while numerous studies have focused on communication efficiency among the nanodevices in a given network, challenges such as the IoBNT security, and the interface connection between the nanonetwork and the Internet are yet to be addressed. Thus, in this study, we propose a privacy scheme working on the top of the biocyber interface in the IoBNT paradigm. The proposed chaotic-system is based on the command signal coming from medical personnel to biocyber device embedded on the human body wherein a masked version of feature generated by applying modified Logistic map for increasing the privacy of the human life and released the exact dose. Additionally, the proposed scheme includes BPSK modulation and feature extraction with zero crossing rate. Finally, the privacy scheme increases the key space, thereby ensuring that the right dose is released and the privacy of human life is achieved. The performance analysis of the proposed scheme is presented firstly, by evaluating the proposed privacy scheme working on the top of biocyber interface device by using receiver operating characteristics curve and bit error rate. Then, we study the performance proposed scheme by employing the compartmental models in the forward and reverse biocyber interface of the IoBNT paradigm. The simulation results of the developed model reveal that the proposed IoBNT-based the privacy scheme can enhance the delivery of therapeutic drugs to the target cells while maximizing the privacy issues. [ABSTRACT FROM AUTHOR]

Nowadays, the Internet of Bio-NanoThings (IoBNT) is playing an important role to become the leading technique used in healthcare delivery systems. The IoBNT is considered a promising paradigm for efficient communication between nanodevices to deliver therapeutic drug molecules and thus achieve the target concentration to the diseased cell/tissue inside intra-body nanonetworks. However, ignoring the physical architecture of these nanodevices may effect on the delivered concentration when employing the IoBNT paradigm. Therefore, in this paper, we propose a spherical transmitter nanodevice, namely reservoir for controlling the drug molecules to be released and showing the effects of the geometry design of such nanodevice on the concentration arrived inside intra-body nanonetwork. Moreover, we present a pharmacokinetic system comprising of a mathematical model for studying the effects and variance in drug concentration, while taking into consideration the distance from the center of the nanotransmitter to the center of the nanoreceiver. The performance analysis of the proposed IoBNT system is numerically investigated. The performance is evaluated by employing the pharmacokinetic model in terms of bio-cyber interface forward and reverse links. The simulation results reveal that the proposed model is able to achieve a high concentration around the targeted cells and thus decrease side effects around healthy cells compared with the state-of-the-art. Additionally, the results illustrate that proposed reservoir is capable of controlling the emission of the therapeutic drug molecules and thus improving the delivery of the dose at target time. [ABSTRACT FROM AUTHOR]

Here, a novel pH-responsive block copolymer, poly (ethylene glycol)-poly(ε-caprolactone)-poly(L-histidine) (PEG-PCL-PHis), was synthesized and designed for anti-cancer drug delivery with excellent biocompatible, biodegradable, and strong drug loading efficiency. 1H-NMR, IF-IR, and GPC were used to characterize the structure of the PEG-PCL-PHis copolymer. In addition, the morphology, particle size, Zeta potential, and critical micelle concentration (CMC) of different degree of polymerization were determined by transmission electron microscopy (TEM), dynamic light scattering granulometer (DLS), and fluorescence spectrometer, respectively. The strong affinity between the core of micelles and hydrophobic drug was manifested with 15.09% drug loading content and 84.65% entrapment efficiency. In vitro release of DOX from the block copolymer micelle demonstrated, the PEG-PCL-PHis copolymer micelle has stable and durable drug releasing ability accompanied with pH-sensitivity. From the mechanism of cellular uptake the micelles, the pathway of drug release was captured by confocal laser scanning microscope. These experiments demonstrated the safe delivery for anticancer medicine through this novel copolymer. In conclusion, the PEG-PCL-PHis copolymer micelle has great potential to become a safe drug carrier for cancer chemotherapy. [ABSTRACT FROM AUTHOR]

Picotechnology development in vast disciplines is mainly attributed to the research and development (R and D) on nanotechnology. Being a parent technology, nanotechnology is the cornerstone of picotechnology. Like nanotechnology, the reference standard for picotechnology is nature, the cellular and subcellular functioning. Some studies have highlighted that the functional margin of similar type of molecules at picoscale (10−12) goes higher than at nanoscale (10−9). In this review, the potential applications of picotechnology have been evaluated especially in the disciplines of biomedical and environmental sciences. Extended surface area and improved electrical, chemical, optical, and mechanical properties make picotechnological products even better than nanomaterials. The fundamental objective of this study is to bring the attention of the scientific world towards the picoscale interventions and to highlight the wide scope of picotechnology as a newly emerging technology with applications in numerous sectors. Picotechnology has made it possible to measure very small structure in advance biomedical and environmental sciences studies. Adequate developments in picotechnology will certainly change human lives in near future because it will make possible for the research world to dive into systems and structures on picoscale. It will render a platform through which explorers can travel into ultra-small areas, which will lead to the creation of new dimensions as well as new opportunities. Eventually, in future, the picotechnology will become smaller enough to give birth to femtotechnology (10−15) in real-world applications. [ABSTRACT FROM AUTHOR]

Liposomes are spherical shaped vesicles having 0.05- 5.0 micrometer in diameter consist of phospholipids and cholesterol. This novel drug delivery system aims to target the drug directly to the site of action. Liposomes are biocompatible and stable and have unique property to entrap both hydrophilic drug and lipophilic drug. The aim of the present study is to formulate and evaluate the liposomes of Indomethacin using HPMC, PVP, Sodium lauryl sulphate which leads to increase the solubility. Various formulations from LS1 to LS7 of Indomethacin Liposomes were developed using different concentrations of polymers like PVP, HPMC etc. The Liposomes were prepared by thin film hydration method. Liposomes were characterized by polymer compatibility by using spectral analysis of drug. The prepared Liposomes were evaluated for solubility, viscosity determination, entrapment efficiency in vitro drug release and stability studies. Finally, batch LS1 is concluded as optimum formulation. [ABSTRACT FROM AUTHOR]

Artemisinin is used as an antimalarial and anticancer agent with minimal toxic effects on the host body. Biotin-PEG-PCL polymers have been used for targeted drug delivery to cancer, as well as to improve the pharmacokinetics of the drug and reduce its effects. In this study, biotin-conjugated copolymers were fabricated with polymerization of the ring opening method and the properties of copolymer and nanoparticles were investigated using various techniques. The toxicity of artemisinin and its nanoparticles have been investigated on MCF-7 and normal HFF2 cells. The results showed that the encapsulation efficacy of artemisinin in nanoparticles was 45.5 ± 0.41%. The release profile of the drug indicates that the release is slow and controlled and is approximately pH dependent. The results of artemisinin cell culture on human breast cancer cells showed that biotin-PEG-PCL nanoparticles had an inhibitory effect on MCF-7 cells and had no toxic effects on HFF2 cells. Anticancer activity in vivo in the 4T1 breast cancer model showed that tumour volumes were decreased up 40 mm3 by ART-loaded micelles and 76 mm3 by free ART, compared to the control group (2150 mm). In vivo results showed that this formulation significantly increases the accumulation of substances in the tumours. Therefore, the molecular formulation of ART-based copolymers can be a desirable process for cancer treatment purposes. [ABSTRACT FROM AUTHOR]

Controlled drug release and targeted drug delivery can reduce systemic toxicity of chemotherapeutics by restricting drugs to the target organ and increasing the local concentration. As tumors and inflamed tissue are often surrounded by an acidic microenvironment, pH-responsive calcium carbonates (CaCO3) are promising vehicles for controlled drug delivery applications. The aim of this study was to evaluate the loading efficacy and release of a chemotherapeutic drug, Hydroxyurea (HU), into the crystal structure of calcite. Incorporation of HU did not alter the crystallinity, crystal size, or morphology of precipitated calcite crystals, as assessed by XRD and SEM. The amount of HU was quantified by High-Pressure Liquid Chromatography (HPLC) and showed that 6.7 ± 0.7 µg of HU could be for each milligram of calcite (0.016 mol% ± 0.002). In cell media, the optimal pH for controlled release was 5 (0.1 mg/mL released after 1 h). However, in vitro, pH below 6.5 was cytotoxic to human breast cancer cells (MCF-7). Direct contact studies, where particles were incubated with MCF-7 cells, showed that the amount of HU release from calcite was not high enough to kill the cell or arrest growth at pH 6.5. Pre-dissolved release studies, where the particles were pre-dissolved in acidic media to simulate complete drug release in vivo, pH neutralized, and exposed to the cells, showed that the amount of loaded HU reduced the survival/proliferation of MCF7. In conclusion, it is possible to integrate HU into the crystal structure of a calcite crystal and release the drug in vitro at concentrations that can slow the growth of cancer cells, without affecting calcite morphology and crystallinity. Further research is needed to investigate the in vivo behavior of the particles and whether the actual tumor pH is low enough to achieve complete drug release in vivo.

In the present investigation, we have strategically synthesized Glutathione (GSH) stimuli-sensitive analogues using carbamate linkers (CL) of DOX (DOX-CL) and RB (RB-CL) which were then anchored to gold nanoparticles (Au-DOX-CL, Au-RB-CL) using mPEG as a spacer. It was observed that carbamate linkage (CL) with four carbon spacer is critical, to position the terminal thiol group, to access the carbamate group efficiently to achieve GSH-assisted release of DOX and RB in tumor-specific environment. When assessed for GSH reductase activity in MDA-MB 231 cell lines, Au-DOX-CL and Au-RB-CL showed nearly 4.18 and 3.13 fold higher GSH reductive activity as compared to the control group respectively. To achieve spatial tumor targeting with a high payload of DOX and RB, Au-DOX-CL and Au-RB-CL were encapsulated in the cell-penetrating peptide (CPP) modified liquid crystalline cubosomes i.e. CPP-Cu(Au@CL-DR). After internalization, the prototype nanocarriers release respective drugs at a precise GSH concentration inside the tumor tissues, amplifying drug concentration to a tune of five-fold. The drug concentrations remain within the therapeutic window for 72 h with a significant reduction of RB (7.8-fold) and DOX (6-fold) concentrations in vital organs, rendering reduced toxicity and improved survival. Overall, this constitutes a promising chemotherapeutic strategy against cancer and its potential application in the offing., Competing Interests: Declaration of competing interest The authors declare no competing financial interest., (Copyright © 2023. Published by Elsevier B.V.)

Introduction: Diabetes is the common disorder found in case of metabolic dysfunction leads to high blood glucose level in our body. Type two polygenic diseases are the most typical type of polygenic disease. If we have type II diabetes, our body does not use insulin properly. This is called insulin resistance. Materials and Methods: At first, our pancreas makes extra insulin to make up for it. However, overtime it is not able to carry on and cannot create enough internal secretion to stay your blood sugar at traditional levels. To cure Type II diabetes, we have identified the gene responsible for the insulin resistance gene from the genomic information resource database. The gene is further analyzed and docked with the four herbal components and checked its minimum energy value for further studies. This will be the combination drug and using nanomedicine which will be the target drug delivery toward the target gene which stimulates the activity of the insulin-resistant gene. Since its targets toward the gene, it will be considered as the gene therapy and new combinatorial medicine, here, bioinformatics, combinatorial chemistry, pharmacology, and nanomedicine play a key role in the treatment of diabetes. Type II diabetes is the high risk of day-to-day life, so considering these facts, the gene responsible for diabetes is identified and diagnosis of DNA is done used molecular techniques and mutated gene is identified for further treatment. In this project, suitable drug targets are identified and targeted toward the type II diabetes. [ABSTRACT FROM AUTHOR]

Abstract A magnetic-pH dual responsive drug delivery system was prepared for antibacterial therapy to reduce the side effects on nonpathological cells or tissues. Iron oxide (Fe 3 O 4) core was surface-functionalized with silane coupling agents to link β‑cyclodextrin (β-CD) (CDMNP), and a polypseudorotaxanes shell where polyethyleneglycol chains threaded much CD molecules was further prepared on the magnetic Fe 3 O 4 core (CDMNP-PEG-CD) to enhance loading capacity of roxithromycin (ROX). CDMNP-PEG-CD with a hydrodynamic diameter of ~168 nm was cytocompatible, superparamagnetic, magnetic-responsive and stable for 180 min of storage. No significant interaction with serum albumin was shown for the nanocomposites. The in vitro release from ROX-loaded CDMNP-PEG-CD nanocomposites was about 76% of total drug within 30 min at pH 1.0, 1.6-fold of that at pH 7.4 and 2-fold of that at pH 8.0, presenting pH-responsive drug release behaviors. The nanocomposites showed positive antibacterial activity against both E. coli and S. aureus based on an agar diffusion method. The antibacterial activity of the nanocomposites was more sensitive against E. coli than S. aureus , and the inhibition halo against E. coli was 85% more than that of Fe 3 O 4. CDMNP-PEG-CD nanocomposites allowed for the localization and fast concentration of hydrophobic drugs, providing a broad potential range of therapeutic applications. Highlights • A polypseudorotaxanes coating where PEG threaded much CD molecules was successfully synthesized. • The polypseudorotaxanes coated magnetic nanoparticles repelled BSA absorption and did not induce conformational change of BSA. • The magnetic-pH responsive nanoparticles can target and rapidly release antibacterial drugs in acidic environment. [ABSTRACT FROM AUTHOR]