Biocompatible Nanocarriers Research Articles

EGF Receptor-Targeting Cancer Therapy Using CD47-Engineered Cell-Derived Nanoplatforms.

IntroductionAvoiding phagocytic cells and reducing off-target toxicity are the primary hurdles in the clinical application of nanoparticles containing therapeutics. For overcoming these errors, in this study, nanoparticles expressing CD47 proteins inhibiting the phagocytic attack of immune cells were prepared and then evaluated as an anti-cancer drug delivery vehicle.MethodsThe CD47+ cell-derived nanoparticles (CDNs) were prepared from the plasma membranes of human embryonic kidney cells transfected with a plasmid encoding CD47. And the doxorubicin (DOX) was loaded into the CDNs, and anti-EGF receptor (EGFR) antibodies were conjugated to the surface of the CDNs to target tumors overexpressing EGFR.ResultsThe CD47+iCDNs-DOX was successfully synthesized having a stable structure. The CD47+CDNs were taken up less by RAW264.7 macrophages compared to control CDNs. Anti-EGFR CD47+CDNs (iCDNs) selectively recognized EGFR-positive MDA-MB-231 cells in vitro and accumulated more effectively in the target tumor xenografts in mice. Moreover, iCDNs encapsulating doxorubicin (iCDNs-DOX) exhibited the highest suppression of tumor growth in mice, presumably due to the enhanced DOX delivery to tumor tissues, compared to non-targeting CDNs or CD47- iCDNs.DiscussionThese results suggest that the clinical application of biocompatible cell membrane-derived nanocarriers could be facilitated by functionalization with macrophage-avoiding CD47 and tumor-targeting antibodies.

Enhanced antibacterial activity of a novel protein-arginine deiminase type-4 (PADI4) inhibitor after conjugation with a biocompatible nanocarrier

The present study reveals a simple and cost-effective method to enhance the antibacterial activity of a model antibiotic drug azithromycin which can also be used as an inhibitor of protein-arginine deiminase type-4 (PADI4). At first, molecular docking has been used for obtaining binding modes and binding affinities of this drug to prove its role as an effective inhibitor for protein-arginine deiminase type-4 (PADI4). In the next step, a biocompatible nanocarrier has been synthesized for successful targeting of the drug azithromycin to enhance its efficiency to a greater extent. For the formation of the nanocarrier, Cu–Ag–Fe2O3 nanocomposite has been synthesized by mechanical alloying the Cu, Ag and Fe2O3 powder for 3 h. After the successful formation of the nanocomposite, 10 wt% of the drug has been conjugated with the nanocomposite by further milling for 1 h under the same experimental condition. The nanocomposite (NC) and drug conjugated nanocomposite (NC-DC) samples are well-characterized by the Rietveld refinement of the XRD pattern of the NC-DC sample, analyzing FTIR, EDS spectra, and FESEM images. It has been observed that both the samples are non-toxic to human normal lung fibroblast WI38 cells. The antibacterial activity of the drug conjugated nanocomposite sample has been enhanced significantly compared to the pure drug azithromycin. These investigations have been made by agar cup assay and minimum inhibitory concentrations (MIC) studies. As a minimal amount of drug is required for the conjugation, side effects and the cost of an expensive drug can be minimized to a great extent following the proposed synthesis route. The enhancement of the antibacterial activity of azithromycin conjugated nanocomposite gives a possibility that drug conjugated nanocomposite may have enhanced activity in the inhibition of PADI4. It may cure the harmful effects of COVID-19 or inhibit the growth of tumour cells more efficiently by improving the cell membrane penetration power of the drug due to its conjugation with the nanocomposite.

Probing the Local Polarity in Biocompatible Nanocarriers with Solvatofluorochromism of a 4-Carbazole-1,8-naphthalimide Dye

The study of local polarity at the nanoscale is of crucial importance for the development of smart drug delivery systems and photonic materials and is frequently accomplished with the use of luminescent tracer dyes. Nile Red is often used for this purpose, owing to its polarity-sensitive internal charge transfer transition, but its performance is affected by specific solute-solvent interactions that prevent its widespread applicability. Herein, we develop a new 1,8-naphthalimide dye with a strong charge-transfer transition that results in a large dipole moment change upon excitation. This leads to luminescence properties with high sensitivity to solvent polarity, that are independent of specific or inductive interactions. These properties are explored to probe the polarity of biocompatible nanocarriers. This dye was effective in probing the properties of polymeric nanoparticles, allowing the accurate calculation of polarity descriptors and dielectric constants.

Fibrous palygorskite clays as versatile nanocarriers for skin delivery of tea tree oils in efficient acne therapy

This paper presents a facile approach to develop palygorskite (Pal), a fibrous clay mineral, as a delivery system of tea tree oil (TTO) for topical acne therapy. The obtained TTO-Pal composite showed an efficient loading of TTO (27.4%) with a selective accumulation of terpine-4-ol and 1,8-cineole (two major antimicrobial TTO constituents), sustained release of TTO at skin physiological conditions (pH5.4, 32 °C) and superior skin sebum (2.2 g/g) absorbability. In vitro toxicological assessments showed that the Pal incorporation strategy significantly reduced the acute contact toxicity of TTO. The antimicrobial results revealed a preferable bacteriostatic effect for the TTO-Pal system towards opportunistic dermal pathogens (Escherichia coli, Staphylococcus aureus and Propionibacterium acnes) over the beneficial bacterium (Staphylococcus epidermis). Moreover, TTO-Pal based formulations exhibited pronounced clinical therapeutic efficacy in treating facial acne by rapidly reducing inflamed lesions, modulating skin sebum overproduction and restoring barrier function. This is the first report of using fibrous clay as a biocompatible nanocarrier system for topical delivery of essential oils in efficient management of facial acne with both in vitro and in vivo evidences, which may open perspectives for fibrous clay-drug delivery system in topical application and expand the high added value development of this mineral resource in the advanced healthcare fields.

Mesoporous mixed oxides prepared by hard template methodology as novel drug delivery carriers for methotrexate

Non-silica-based metal oxide nanomaterials, especially those possessing significant porosity, are emerging as good candidates for the delivery of a range of chemotherapeutic drugs providing an enhanced biocompatibility in compares with silica-based nanocarriers. Herein, mesoporous materials were synthesized from hard-templated lanthanum-manganese (NC–LaMn) and barium-titanium (NC–BaTi) mixed oxides are evaluated as new drug nanocarriers, using methotrexate (MTX) as a model therapeutic compound. The SBA-15 material was used as a hard template to assist the sol-gel synthesis to provide the corresponding nanocarriers. The templated nanomaterials were characterized by X-ray diffraction (XRD), attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR), dynamic light scattering (DLS), zeta potential analysis, transmission electron microscopy (TEM), N2 adsorption-desorption isotherms, and thermogravimetric analysis (TGA), which revealed remarkably high surface area (SBET ∼ 180 m2/g) and displayed mean nanoparticle sizes ∼ 700–1100 nm. The NC-LaMn and NC-BaTi carriers showed a loading efficiency of 47.2 mg/g and 70.1 mg/g for the encapsulation of MTX, respectively. Both mixed-metal oxides showed higher drug uptake than SBA-15 (22.6 mg/g) due to the higher alkalinity of the carriers, which promoted host-guest affinity by acid/base interactions. The carriers showed pH-dependent release of MTX and adjust their release profile at Korsmeyer-Peppas kinetics model. The release at pH = 5.5 for both mixed-oxides (kNC-LaMn 0.077 and kNC-BaTi 0.068) was faster than that at pH = 7.4 for (kNC-LaMn 0.022 and kNC-BaTi 0.019). Additionally, hemolysis and cell viability assays indicated that NC-BaTi was a biocompatible nanocarrier with no toxicity, whereas NC-LaMn was toxic even at low dosages for both red blood and HeLa cells. The results suggested that the synthesized NC-BaTi metal oxide had great potential as a nanocarrier in cancer therapy with optimal loading content and sustained release of MTX.

Synthesis of NMOF-5 Using Microwave and Coating with Chitosan: A Smart Biocompatible pH-Responsive Nanocarrier for 6-Mercaptopurine Release on MCF-7 Cell Lines

Cancer is one of the most difficult diseases to treat, threatening the lives of millions of people today. So far, various methods have been used to treat cancer, each having its drawbacks. One of these methods is treatment with anticancer drugs, which unfortunately have severe side effects. One of the causes of these complications is the nonspecific effects of anticancer drugs, which attack normal cells in addition to cancer cells and damage healthy tissues. In this study, we are trying to reduce the side effects and increase the efficacy of the drug by providing smart drug delivery. The metal-organic framework (MOF) was rapidly synthesized using a microwave method and at the nanoscale. The particle size of NMOF-5 was 18-20 nm, and its surface area was 2690 m2·g-1. A chitosan polymer coating was formed on the nanocarrier after 6-mercaptopurine was introduced. The biocompatible nanocarrier exhibited a high capacity to adsorb the drug. The biocompatible nanocarrier slowly and uniformly released 96.78% of the drug in a simulated solution at pH 5 and 20.52% at pH 7.4. This showed that CS-6-MP-NMOF-5 released the drug smartly and pH-sensitively. The stability of the biocompatible nanocarrier was studied at different pH values and remained stable at pH 5 for up to 48 h. The toxicity study of the MCF-7 cell line at different concentrations for 24 h showed the excellent performance of the biocompatible nanocarrier compared to the free drug in terms of toxicity to breast cancer cells.

Biosynthesis and optimization of highly stable gold nanoparticles, nanoconjugates, nanodrug conjugates and chitosan nanoconjugates using medicinal plants

BackgroundIn the present study, the medicinal plants were exclusively selected based on their significant anti-HIV and anticancer activities. The green synthesis of gold nanoparticles was carried out using the 15 medicinal plant extracts on reduction with chloroauric acid. The present study also focused on a novel pharmacognostic approach over the usage of plants source. The nanoparticle synthesized through medicinal plants possessed the potential therapeutic properties of the plants. The resultant nanoparticle carried the attributes of a nanomaterial alongside the phytoactivity.ResultsInitially, individual nanoparticle (NP) was synthesized through a single plant extract and studied for its effective anti-HIV and anticancer activity. Finally, a nanoconjugate (NC) comprising of the 3 extracts (trio extract) in one nanoparticle was synthesized. The nanoparticles which exhibited comparatively high anti-HIV and anticancer activity were chosen for the synthesis of nanoconjugate, thereby achieving a synergistic anticancer and anti-HIV activity. Further, a nanodrug conjugate (NDC) was prepared in combination of AuNPs and the chemotherapeutic drug, doxorubicin (Dox) for cancer and AuNPs with antiretroviral drug azidothymidine (AZT) for HIV.ConclusionsA nanodrug conjugate helps to enhance the efficiency of the drug. The nanodrug conjugate brings about a combinatorial effect of the nanomaterials and the drug. Further, a biocompatible nanocarrier was developed as a conjugate with chitosan and gold nanoparticles using STPP as gelating agent for the drug doxorubicin. The synthesis reaction was optimized under various underlying parameters. The gold nanoparticles proved to be stable at high temperature and different buffers and ensured to be a safe option for bioassays and in vivo applications. Upon storing the synthesized AuNPs at different storage conditions, the nanoparticles were observed to be highly stable for a period of more than 48 months. The present study resulted in biosynthesis of highly stable gold nanoparticles using medicinal plant extracts as reducing and stabilizing agents.

Self-assembled dehydropeptide nanocarrier as a delivery system for antitumor drug temozolomide

Stable molecular conformation and intermolecular forces are essential for peptide self-assembly. In this study, one novel dehydropeptide (DDP) monomer (Boc-(Z)Cα,β-ΔPhe-Gly-NHMe, DDP 1) was prepared; its conformation was confirmed to be more stable than the normal peptide 2 by nuclear magnetic resonance (NMR) and X-ray crystal diffraction experiments. DDP 1 was self-assembled to one novel dehydropeptide nanomaterial (DDPN 1). Fourier transform infrared (FTIR) spectroscopy results showed that hydrogen bonding was the main driving force of self-assembly. Electron microscope images displayed that the DDPN 1 fibers were longer and more stable than peptide 2 nanomaterials. Results of cell activity and enzyme hydrolysis proved that DDPN 1 had excellent biocompatibility and resistance to the enzymatic hydrolysis of protease K. Therefore, the DDPN 1 was used to load the antitumor drug temozolomide (TMZ). Due to intermolecular hydrogen bonds formed between TMZ and DDPN 1, TMZ-loaded DDPN 1 had a high percent entrapment efficiency (EE) of 83.72 ± 4.30% (n = 8) and a percent drug loading efficiency (LE) of 6.70 ± 0.34% (n = 8), and the half-life of TMZ-loaded DDPN 1 was 2.5–3 times longer than that of TMZ at pH 7. The in vitro cell viability results revealed that TMZ-loaded DDPN 1 exhibited higher antitumor activity (IC50 = 552.1 μM) against U118-MG than that of TMZ (IC50 = 1980.1 μM), possibly because that U118-MG cells uptook more TMZ from TMZ-loaded DDPN 1 than from free TMZ directly. This study is expected to inspire the design of biocompatible nanocarriers applied for anti-enzymatic hydrolysis in drug delivery systems.

Unveiling the Bio-corona Fingerprinting of Potential Anticancer Carbon Nanotubes Coupled with d-Amino Acid Oxidase

The oxidation therapy, based on the controlled production of Reactive Oxygen Species directly into the tumor site, was introduced as alternative antitumor approach. For this purpose, d-amino acid oxidase (DAAO) from the yeast Rhodotorula gracilis, an enzyme able to efficiently catalyze the production of hydrogen peroxide from d-amino acids, was adsorbed onto multi-walled carbon nanotubes (MWCNTs), previously functionalized with polylactic-co-glycolic acid (PLGA) or polyethylene glycol (PEG) at different degrees to reduce their toxicity, to be targeted directly into the tumor. In vitro activity and cytotoxicity assays demonstrated that DAAO-functionalized nanotubes (f-MWCNTs) produced H2O2 and induced toxic effects to selected tumor cell lines. After incubation in human plasma, the protein corona was investigated by SDS-PAGE and mass spectrometry analysis. The enzyme nanocarriers generally seemed to favor their biocompatibility, promoting the interaction with dysopsonins. Despite this, PLGA or high degree of PEGylation promoted the adsorption of immunoglobulins with a possible activation of immune response and this effect was probably due to PLGA hydrophobicity and dimensions and to the production of specific antibodies against PEG. In conclusion, the PEGylated MWCNTs at low degree seemed the most biocompatible nanocarrier for adsorbed DAAO, preserving its anticancer activity and forming a bio-corona able to reduce both defensive responses and blood clearance.

Bioactive Keratin and Fibroin Nanoparticles: An Overview of Their Preparation Strategies.

In recent years, several studies have focused their attention on the preparation of biocompatible and biodegradable nanocarriers of potential interest in the biomedical field, ranging from drug delivery systems to imaging and diagnosis. In this regard, natural biomolecules—such as proteins—represent an attractive alternative to synthetic polymers or inorganic materials, thanks to their numerous advantages, such as biocompatibility, biodegradability, and low immunogenicity. Among the most interesting proteins, keratin extracted from wool and feathers, as well as fibroin extracted from Bombyx mori cocoons, possess all of the abovementioned features required for biomedical applications. In the present review, we therefore aim to give an overview of the most important and efficient methodologies for obtaining drug-loaded keratin and fibroin nanoparticles, and of their potential for biomedical applications.

Self‐Assembled Nanovehicle for Intracellular Enzyme‐Triggered Antitumor Drug Release

AbstractEnzyme‐responsive and biocompatible supramolecular nanocarriers (NCs) have attracted intensive attention in the field of biomaterials, and have found many feasible applications, particularly for controlling drug‐release at specific anchor sites where the enzyme is overexpressed. However, the introduction of specific enzyme‐responsive sites in drug nanocarriers that can be enzymatically triggered to release drugs within tumor cells remains a challenge. In this manuscript, an enzyme‐responsive supramolecular nanoparticle, (SBE)7m‐β‐CD ⊃ PS NPs is successfully prepared, based on inducing aggregation of negatively charged cyclodextrin toward positively charged protein. The obtained nanoparticles showed trypsin‐trigger disassemble behavior that is considered as drug vehicles to load antitumor drug celastrol (CSL). Furthermore, CSL‐loaded NPs exhibit controlled release behavior of CSL in response to trypsin (TPS) stimulation. Notably, cell biology experiments reveal that loading CSL by (SBE)7m‐β‐CD ⊃ PS NPs not only reduces cytotoxicity for normal cells but also presents a similar therapeutic effect of free CSL for five tumor cells. The obtained nanoparticle appears to hold practical potential for the controllable release of CSL in tumor cells.

Maillard induced glycation of β-casein for enhanced stability of the self-assembly micelles against acidic and calcium environment

Bovine β-casein (β-CN) has attracted increasingly interest as biocompatible nanocarrier for hydrophobic flavonoid due to its self-assembly ability to form micelles. This paper reported Maillard induced glycation reaction of β-CN using dextran in order to improve stability of naringenin-loaded β-CN micelles under acidic and high calcium environments. Our results showed that solubility of β-CN-graft-dextran was remarkable increased at acidic pH and the conjugation with 20 kDa dextran had the highest level of graft degree. Glycation restrained β-CN from aggregating around pH 5.0 where was close to the isoelectric point, forming spherical micelles with irregular and rough surfaces, which were significantly larger than the micelles at pH 7.0. β-CN-graft-dextran also overcame destabilization of the micelles induced by excess calcium and had no impact on the chelating ability of calcium. These findings appeared to be promising for future applications of modified β-CN-graft-dextran based on Maillard reaction as fairly stable nanocarrier under extreme condition.

Indocyanine-type Infrared-820 Encapsulated Polymeric Nanoparticle-Assisted Photothermal Therapy of Cancer.

Organic small-molecule photosensitizers are well-characterized and known for the light-responsive treatment modality including photodynamic therapy. Compared with ultraviolet–visible (UV–vis) light used in conventional photodynamic therapy with organic photosensitizers, near-infrared (NIR) light from 700 to 900 nm is less absorbed and scattered by biological tissue such as hemoglobin, lipids, and water, and thus, the use of NIR excitation can greatly increase the penetration depth and emission. Additionally, NIR light has lower energy than UV–vis that can be beneficial due to less activation of fluorophores present in tissues upon NIR irradiation. However, the low water stability, nonspecific distribution, and short circulation half-life of the organic photosensitizers limit its broad biological application. NIR responsive small-molecule fluorescent agents are the focus of extensive research for combined molecular imaging and hyperthermia. Recently a new class of NIR dye, IR-820 with excitation and emission wavelengths of 710 and 820 nm, has been developed and explored as an alternative platform to overcome some of the limitations of the most commonly used gold nanoparticles for photothermal therapy of cancer. Herein, we synthesized a core–shell biocompatible nanocarrier envelope made up of a phospholipid conjugated with poly(ethylene glycol) as a shell, while poly(lactic glycolic acid) (PLGA) was used as a core to encapsulate IR-820 dye. The IR-820-loaded nanoparticles were prepared by nanoprecipitation and characterized for their physicochemical properties and photothermal efficiency. These nanoparticles were monodispersed and highly stable in physiological pH with the hydrodynamic size of 103 ± 8 nm and polydispersity index of 0.163 ± 0.031. The IR-820-loaded nanocarrier showed excellent biocompatibility in the dark, whereas remarkable phototoxicity was observed with breast cancer cells (MCF-7) upon NIR laser excitation. Therefore, the IR-820-loaded phospholipid mimicking biodegradable lipid-polymer composite nanoparticles could have great potential for cancer theranostics.

Intranasal lipid nanocarriers: Uptake studies with fluorescently labeled formulations

Drug delivery by the intranasal route allows both systemic absorption and non-invasive brain targeting, due to the unique connection provided by the olfactory and trigeminal nerves between the brain and the external environment. Lipid nanocarriers can improve intranasal drug delivery by enhancing bioadhesion to nasal mucosa, and by protecting the encapsulated drug from biological degradation and transport efflux proteins. In this study two different biocompatible lipid nanocarriers were compared: nanoemulsions and solid lipid nanoparticles. The nasal uptake was investigated by labeling the nanocarriers lipid matrix with two fluorescent probes, 6-coumarin and rhodamine B, both lipophilic, yet characterized by different water solubility, in order to mimic the behavior of hypothetic drug compounds. Ex vivo permeation, in vivo pharmacokinetics and biodistribution studies were performed. 6-coumarin, water insoluble and therefore integral with the lipid matrix, was taken up to a limited extent, within a long timeframe, but with a proportionally more pronounced brain accumulation. In nanoemulsions soluble rhodamine B showed a relevant systemic uptake, with good bioavailability, likely due to the prompt release of the probe at the nasal mucosa.

Mesoporous Biodegradable Magnesium Phosphate-Citrate Nanocarriers Amplify Methotrexate Anticancer Activity in HeLa Cells.

We present the synthesis of amorphous, mesoporous, colloidal magnesium phosphate-citrate nanoparticles (MPCs) from biogenic precursors, resulting in a biocompatible and biodegradable nanocarrier that amplifies the action of the anticancer drug methotrexate (MTX). Synthesis conditions were gradually tuned to investigate the influence of the chelating agent citric acid on the colloidal stability and the mesoporosity of the obtained nanoparticles. With optimized synthesis conditions, a large BET surface area of 560 m2/g was achieved. We demonstrate the potential of these biocompatible and biodegradable mesoporous MPCs as a drug delivery system. Lipid-coated MPCs were used to load the fluorescent dye calcein and the chemotherapeutic agent MTX into the mesopores. In vitro experiments show very low premature release of the cargo but efficient stimuli-responsive release in an environment of pH 5.5, in which MPCs degrade. Lipid-coated MPCs are taken up by cancer cells and are nontoxic up to concentrations of 100 μg/mL. When loaded with MTX serving as a representative model drug for in vitro studies, MPCs induced efficient cell death with an IC50 value of 1.1 μg/mL. Compared to free MTX, its delivery with MPCs enhances its efficiency by an order of magnitude. In summary, we have developed a biodegradable nanomaterial synthesized from biocompatible precursors that are neither toxic by themselves nor in the form of nanoparticles. With these features, MPCs may be applied as drug delivery systems and have the potential to reduce the side effects of current chemotherapies.

High-Density Horizontal Stacking of Chondrocytes via the Synergy of Biocompatible Magnetic Gelatin Nanocarriers and Internal Magnetic Navigation for Enhancing Cartilage Repair.

Osteoarthritis (OA) is a globally occurring articular cartilage degeneration disease that adversely affects both the physical and mental well-being of the patient, including limited mobility. One major pathological characteristic of OA is primarily related to articular cartilage defects resulting from abrasion and catabolic and proinflammatory mediators in OA joints. Although cell therapy has hitherto been regarded as a promising treatment for OA, the therapeutic effects did not meet expectations due to the outflow of implanted cells. Here, we aimed to explore the repair effect of magnetized chondrocytes using magnetic amphiphilic-gelatin nanocarrier (MAGNC) to enhance cellular anchored efficiency and cellular magnetic guidance (MG) toward the superficial zone of damaged cartilage. The results of in vitro experiments showed that magnetized chondrocytes could be rapidly guided along the magnetic force line to form cellular amassment. Furthermore, the Arg-Gly-Asp (RGD) motif of gelatin in MAGNC could integrate the interaction among cells to form cellular stacking. In addition, MAGNCs upregulated the gene expression of collagen II (Col II), aggrecan, and downregulated that of collagen I (Col I) to reduce cell dedifferentiation. In animal models, the magnetized chondrocytes can be guided into the superficial zone with the interaction between the internal magnetic field and MAGNC to form cellular stacking. In vivo results showed that the intensity of N-sulfated-glycosaminoglycans (sGAG) and Col II in the group of magnetized cells with magnetic guiding was higher than that in the other groups. Furthermore, smooth closure of OA cartilage defects was observed in the superficial zone after 8 weeks of implantation. The study revealed the significant potential of MAGNC in promoting the high-density stacking of chondrocytes into the cartilage surface and retaining the biological functions of implanted chondrocytes for OA cartilage repair.

Biodegradable polydopamine and tetrasulfide bond co-doped hollowed mesoporous silica nanospheres as GSH-triggered nanosystem for synergistic chemo-photothermal therapy of breast cancer

Breast cancer, as the common malignant carcinoma in women, seriously reduces the life quality and increases mortality of female worldwide. Fortunately, insufficient chemotherapy with external photothermal therapy could remarkably improve the therapeutic efficiency of breast cancer. In this work, we proposed a polydopamine (PDA) and tetrasulfide bond co-doped hollowed mesoporous silica nanospheres with Dox loading and surface hyaluronic acid coating for drug leakage avoidance (PhMSON@Dox-HA). After intravenously injected into tumor bearing-mice, this therapeutic agent could effectively target to the tumor site owing to the HA modification. The biocompatible property and GSH-induced decomposition capability endows the precise release of drugs in the cytoplasm of tumor cells. Meanwhile, PDA facilitated the efficient photothermal therapy under 808 nm laser irradiation. Therefore, the synergistic effect of chemo-photothermal therapy possessed most effective tumor eradication ability. Our work exploits the design approach of biocompatible and degradable drug delivery nanocarriers and sheds bright light on the chemotherapy and photothermal therapy combination for the malignant tumor elimination.

Cubosomes and Hexosomes as Novel Nanocarriers for Bioactive Compounds.

Cubosomes and hexosomes are nanostructured liquid crystalline particles, known as biocompatible nanocarriers for drug delivery. In recent years, there has been good interest in using cubosomes and hexosomes for the delivery of bioactive compounds in functional foods. These systems feature thermodynamic stability, encapsulate both hydrophobic and hydrophilic substances, and have a high tolerance to environmental stresses and potential for controlled release. This review outlines the recent advances in cubosomes and hexosomes in the food industry, focusing on their structure, composition, formation mechanisms, and factors influencing phase transformation between cubosomes and hexosomes. The potential applications especially for the bioactive delivery are presented. The integration of cubosomes and hexosomes with other emerging encapsulation technologies such as surface coating, gelation, and incorporation of polymers are also discussed.

Design of an efficient fluorescent nanoplatform carrier for hydrophobic drugs along with green carbon dot: Possible application in cancer image-guided drug therapy

Nanotechnology has taken novel approaches to advance cancer therapeutic efficacy employing multifunctional nanocarriers with drug delivery and imaging function. In this work, we designed a biocompatible and affordable fluorescence nanocarrier called chitosan (CS)-carbon dot (CD) hybrid nanogel for cell imaging. The green CDs were synthesized using tomato juice through a simple single-step hydrothermal method. Chitosan polymer was used as a carrier for co-delivery CDs and the anti-cancer drug with low solubility, silibinin (Sil), to design the Sil-chitosan carbon dots hybrid nanogels (CCHNs) system. After optimizing the physicochemical properties of nanostructure by DLS, FTIR, FESEM, TEM, and UV-visible techniques, the successful uptake of the fluorescent nanoparticle conjugates into MCF-7 breast cancer cells occurred. Then we embedded CDs in chitosan nanogel. The resultant CCHNs demonstrated optical properties similar to free-CDs, a desirable size distribution (55.22 nm) with a positive surface charge, a suitable loading capacity for Sil (35%), and drug release vulnerable to pH changes. The fluorescent nanocarrier could transfer Sil to MCF-7 cancer cells without remarkable toxicity. The results of the fluorescent microscope indicated that after 4 h, the solid fluorescent signal was received from cells containing CCHNs compared to free CDs and confirmed the ability of hybrid nanogels to high cellular uptake. This study demonstrates a multifunctional nanocarrier containing therapeutic compounds and fluorescent agents that provide cellular imaging to enhance therapeutic efficacy.

Design and Characterisation of pH-Responsive Photosensitiser-Loaded Nano-Transfersomes for Enhanced Photodynamic Therapy.

Photodynamic therapy (PDT) is a non-invasive and tumour-specific therapy. Photosensitizers (PSs) (essential ingredients in PDT) aggregate easily owing to their lipophilic properties. The aim of this study was to synthesise a PS (methyl pheophorbide a, MPa) and design a biocompatible lipid-based nanocarrier to improve its bioavailability and pharmacological effects. MPa-loaded nano-transfersomes were fabricated by sonication. The characteristics of synthesised PS and nano-transfersomes were assessed. The effects of PDT were evaluated by 1,3-diphenylisobenzofuran assay and by measuring photo-cytotoxicity against HeLa and A549 cell lines. The mean particle size and zeta potential for nano-transfersomes ranged from 95.84 to 267.53 nm and −19.53 to −45.08 mV, respectively. Nano-transfersomes exhibited sustained drug release for 48 h in a physiological environment (as against burst release in an acidic environment), which enables its use as a pH-responsive drug release system in PDT with enhanced photodynamic activity and reduced side effects. The formulations showed light cytotoxicity, but no dark toxicity, which meant that light irradiation resulted in anti-cancer effects. Additionally, formulations with the smallest size exhibited photodynamic activity to a larger extent than those with the highest loading capacity or free MPa. These results suggest that our MPa-loaded nano-transfersome system is a promising anti-cancer strategy for PDT.