Cancer-targeted Drug Delivery Research Articles

Efficacy of chondroitin sulfate as an emerging biomaterial for cancer-targeted drug delivery: A short review.

The global increase in cancer incidence over the past decade highlights the urgent need for more effective therapeutic strategies. Conventional cancer treatments face challenges such as drug resistance and off-target toxicity, which affect healthy tissues. Chondroitin sulfate (CHDS), a naturally occurring bioactive macromolecule, has gained attention because of its biocompatibility, biodegradability, and low toxicity, positioning it as an ideal candidate for cancer-targeted drug delivery systems. This review highlights the potential of CHDS as an emerging biomaterial in cancer therapy, focusing on its unique biological properties and applications in drug delivery platforms. Furthermore, we discuss the advantages of CHDS-based biomaterials in enhancing cancer treatment efficacy and minimizing side effects, in order to provide a comprehensive reference for future research on CHDS-based cancer therapeutics.

Exploring the Impact of Chitosan-Based Nanoparticles in Cancer Targeted Drug Delivery: A Bibliometric Review.

Over the last two decades, there has been a considerable increase in the usage of chitosan nanoparticles (CSNPs) for drug delivery applications in cancer treatment. However, a comprehensive bibliometric analysis of this emerging field is lacking. The current analysis pre-sents a detailed bibliometric assessment of the research evolution and trends in CSNPs for can-cer targeted-drug delivery from 2000 to 2022. A total of 626 publications from the Web of Science Core Collection (WoSCC) database were evaluated using VOSviewer, Bibliometrix, and MS Excel. An in-depth exploration was carried out to find publication trends, the most productive authors, affiliations, countries, and journals as well as the highly cited publications within this particular research domain. Ick Chan Kwon was the most prominent author who made significant contributions to this field. China was the leading country in terms of research on CSNPs for cancer-targeted drug delivery, followed by India and Iran. Concerning the total number of publications, The International Journal of Biological Macromolecules excelled as the leading journal in this research area. Furthermore, the research trends and hotspots were also identified through the analysis of the most commonly used keywords by the authors. Our analysis highlights the growing research interest in CSNPs for cancer drug delivery, emphasiz-ing the need for further exploration to unlock their full potential.

Synthesis and characterization of nickel-based MOFs: Enhancing photocatalysis and targeted cancer drug delivery

Metal–organic frameworks (MOFs) are intricate molecular solids formed by connecting organic ligands with metal or metal–cluster binding sites. They have exceptional characteristics such as expansive surface area, adaptability, and meticulously structured porosity, rendering them valuable in various applications including photocatalytic degradation and drug delivery systems. In this investigation, a benign Ni-based MOF was synthesized using benzene 1,4dicarboxylic acid as a linker and dimethyl sulfoxide as a solvent through the hydrothermal approach within a Teflon autoclave. The synthesized MOFs were precisely characterized using techniques such as X-ray diffraction, scanning electron microscope with energy-dispersive X-ray analysis, Fourier-transform infrared (FTIR) spectroscopy, thermogravimetric analysis, and N2-sorption measurements. The photocatalytic efficiency of the Ni-based MOF was explored against Congo red under visible light exposure, with the proposed mechanism involving electron transfer from photoexcited organic ligands to metallic clusters, resulting in a degradation efficiency of 98.68 % after 145 min. Furthermore, the Ni-based MOFs, when loaded with the anticancer drug cisplatin, displayed notable capabilities in drug delivery against the human breast cancer cell line MDA-MB-231, leading to a 35.26 % reduction in cell viability. Cytotoxicity assessments using the MTT assay revealed that the nano-carriers hindered cell proliferation with an IC50 value of 46.84 μg/mL.

Synergistic Effects of Chemotherapy and Phototherapy on Ovarian Cancer Using Follicle-Stimulating Hormone Receptor-Mediated Liposomes Co-Loaded with SN38 and IR820.

We have developed an ovarian cancer-targeted drug delivery system based on a follicle-stimulating hormone receptor (FSHR) peptide. The lipophilic chemotherapeutic drug SN38 and the photosensitizer IR820 were loaded into the phospholipid bilayer of liposomes. The combination of chemotherapy and phototherapy has become a promising strategy to improve the therapeutic effect of chemotherapy drugs on solid tumors. IR820 can be used for photodynamic therapy (PDT), effectively converting near-infrared light (NIR) into heat and producing reactive oxygen species (ROS), causing damage to intracellular components and leading to cell death. In addition, PDT generates heat in near-infrared, thereby enhancing the sensitivity of tumors to chemotherapy drugs. FSH liposomes loaded with SN38 and IR820 (SN38/IR820-Lipo@FSH) were prepared using thin-film hydration-sonication. FSH peptide binding was analyzed using 1H NMR spectrum and Maldi-Tof. The average size and zeta potential of SN38/IR820-Lipo@FSH were 105.1 ± 1.15 nm (PDI: 0.204 ± 0.03) and -27.8 ± 0.42 mV, respectively. The encapsulation efficiency of SN38 and IR820 in SN38/IR820-Lipo@FSH liposomes were 90.2% and 91.5%, respectively, and their release was slow in vitro. FSH significantly increased the uptake of liposomes, inhibited cell proliferation, and induced apoptosis in A2780 cells. Moreover, SN38/IR820-Lipo@FSH exhibited better tumor-targeting ability and anti-ovarian cancer activity in vivo when compared with non-targeted SN38/IR820-Lipo. The combination of chemotherapy and photodynamic treatment based on an FSH peptide-targeted delivery system may be an effective approach to treating ovarian cancer.

Internet of Bio-NanoThings privacy: securing a multi compartmental targeted cancer drug delivery scheme

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.

Tumor Homing Chimeric Peptide Rhomboids to Improve Photodynamic Performance by Inhibiting Therapy-Upregulated Cyclooxygenase-2.

Negative therapeutic feedback of inflammation would extensively attenuate the antitumor effect of photodynamic therapy (PDT). In this work, tumor homing chimeric peptide rhomboids (designated as NP-Mel) are fabricated to improve photodynamic performance by inhibiting PDT-upregulated cyclooxygenase-2 (COX-2). The hydrophobic photosensitizer of protoporphyrin IX (PpIX) and palmitic acid are conjugated onto the neuropilin receptors (NRPs) targeting peptide motif (CGNKRTR) to obtain tumor homing chimeric peptide (Palmitic-K(PpIX)CGNKRTR), which can encapsulate the COX-2 inhibitor of meloxicam. The well dispersed NP-Mel not only improves the drug stability and reactive oxygen species (ROS) production ability, but also increase the breast cancer targeted drug delivery to intensify the PDT effect. In vitro and in vivo studies verify that NP-Mel will decrease the secretion of prostaglandin E2 (PGE2) after PDT treatment, inducing the downregulation of IL-6 and TNF-α expressions to suppress PDT induced inflammation. Ultimately, an improved PDT performance of NP-Mel is achieved without inducing obvious systemic toxicity, which might inspire the development of sophisticated nanomedicine in consideration of the feedback induced therapeutic resistance.

Ligand-conjugated multiwalled carbon nanotubes for cancer targeted drug delivery.

Multiwalled carbon nanotubes (MWCNTs) are at the forefront of nanotechnology-based advancements in cancer therapy, particularly in the field of targeted drug delivery. The nanotubes are characterized by their concentric graphene layers, which give them outstanding structural strength. They can deliver substantial doses of therapeutic agents, potentially reducing treatment frequency and improving patient compliance. MWCNTs' diminutive size and modifiable surface enable them to have a high drug loading capacity and penetrate biological barriers. As a result of the extensive research on these nanomaterials, they have been studied extensively as synthetic and chemically functionalized molecules, which can be combined with various ligands (such as folic acid, antibodies, peptides, mannose, galactose, polymers) and linkers, and to deliver anticancer drugs, including but not limited to paclitaxel, docetaxel, cisplatin, doxorubicin, tamoxifen, methotrexate, quercetin and others, to cancer cells. This functionalization facilitates selective targeting of cancer cells, as these ligands bind to specific receptors overexpressed in tumor cells. By sparing non-cancerous cells and delivering the therapeutic payload precisely to cancer cells, this therapeutic payload delivery ability reduces chemotherapy systemic toxicity. There is great potential for MWCNTs to be used as targeted delivery systems for drugs. In this review, we discuss techniques for functionalizing and conjugating MWCNTs to drugs using natural and biomacromolecular linkers, which can bind to the cancer cells' receptors/biomolecules. Using MWCNTs to administer cancer drugs is a transformative approach to cancer treatment that combines nanotechnology and pharmacotherapy. It is an exciting and rich field of research to explore and optimize MWCNTs for drug delivery purposes, which could result in significant benefits for cancer patients.

Development of Polymeric Nanoparticles of Sunitinib malate in Eudragit S 100 for anti-colon cancer targeted drug delivery

Sunitinib malate (SM) is a multi-targeted tyrosine kinase (TK) inhibitor. It is proposed as a potent anticancer drug intended for colon cancer. The current work aimed at developing Sunitinib malate -loaded nanoparticles for colon- targeting. SM loaded ES100-nanoparticles were developed by nano-precipitation method using poly vinyl alcohol (PVA) as stabilizer. Different formulation of ESNP (F1-F3) were prepared and evaluated for particle size, poly-dispersity index, and drug entrapment, using Fourier transform infrared spectroscopy (FTIR), x-ray diffraction (XRD), and scanning electron microscopy (SEM). The optimized formulation was further studied by in-vitro drug release and anticancer cell line study. The mean particle size, PDI, %EE of optimized SM loaded ESNPF2 was found to be 384.8±5.53 nm, 0.58, and 60.31% respectively. In vitro release of the optimized ESNPF2 showed 10.2 % drug release till 2 h, at 4h 29.6% and 12 h and 24 h 66.45%, 82.2% respectively at pH 7.4. SEM images and surface morphology confirmed that nanoparticles were spherical and had smooth surfaces. An MTT assay was conducted in the colon cancer cell lines (CACO2) to evaluate anti-cancerous activity of SM. SM loaded ESNPF2 showed a high potential against colon cancer cells. The overall results suggest that SM loaded ES100-nanoparticels could be a potential option for colon targeting.

Epidermal Growth Factor Receptor and Double-Imprinted Nanoparticles for Targeted Cancer Drug Delivery - A Review

The Epidermal Growth Factor Receptor (EGFR) plays a crucial role in maintaining tissue balance, but in conditions like tumors or lung and skin cancer, it acts as a driver for cancer development. Nanoparticles are effective tools for delivering medications to tumor cells while minimizing drug impact on healthy cells. A potent therapeutic approach involves using nanoparticles with tumor-specific ligands for cancer treatment. This review study focuses on double-imprinted nanoparticles, synthesized to target the estrogen alpha cancer cell receptor's linear epitope and loaded with an anti-cancer drug. The challenge in cancer therapy is delivering drugs specifically to cancer cells without causing adverse effects on healthy cells. Advanced high-throughput technologies generate genomic and epigenomic data, and Support Vector Machine (SVM) classification in cancer genomics identifies new indicators, drug targets, and cancer transport genetics. The EGFR-SVM approach is designed to enhance the selectivity and reduce the toxicity of cytotoxic drugs by targeting cancer cells more specifically. Targeted treatment involves interfering with specific proteins that promote tumor growth and spread, and the study demonstrates a molecularly targeted drug delivery method for efficiently and selectively targeting anticancer drugs to tumor cells overexpressing EGFR. This approach has the potential to improve the therapeutic effectiveness of existing anticancer drugs.

Curcumin-loaded porous particles functionalized with pH-responsive cell-penetrating peptide for colorectal cancer targeted drug delivery.

The anticancer properties of curcumin have been broadly examined in several shapes, such as nanoparticles and nanocomposite structures. Despite its benefits, curcumin also has some disadvantages, including rapid metabolism, poor absorption, and rapid systemic excretion. Therefore, numerous strategies have been used to increase curcumin's bioavailability. One of these approaches is the use of porous particles like aerogels as drug carriers. Aerogels are special due to their peculiar physical structure. They have a high specific surface area, a significant amount of porosity, and a solid composition, which make them a good choice for drug delivery systems. In the present study, a pH-sensitive aerogel was constructed and evaluated for targeted drug delivery of curcumin to colon cancer. To control the release of curcumin, trehalose was used as a coating agent, and PLP (poly(l-lysine isophthalamide)) was used as a targeted drug delivery agent. PLP is a pseudo-peptidic polymer that increases the cell permeability. In order to investigate and compare the synthesized aerogel before and after loading curcumin and coating with trehalose, physicochemical characterization analyses were performed. Finally, the efficacy of the final formulation was evaluated on HT29 colon cells using the cell bioavailability test. The results indicated the successful synthesis of the aerogel with porous structure with solitary cavities. The trehalose coating performed well, preventing drug release at lower pH but allowing the drug to be released at its intended site. The designed curcumin-loaded porous particles functionalized with PLP showed significant efficacy due to increasing penetration of curcumin into cells, and has potential for use as a new drug carrier with dual effectivity in cancer therapy.

Augmented anti-cancer effect of hypoxia-inducible factor 2α (HIF2α)- targeting PT2385 delivered in α-synuclein-AuNP microcapsules for clear cell renal carcinoma mouse model

Development of anti-cancer drug carrier system capable of delivering chemotherapeutic and immunotherapeutic agents to cancerous lesions is essential to overcome severe side effects and reduced therapeutic efficacy of the drugs. The microcapsules of gold nanoparticles (AuNPs) fabricated with a self-assembly protein of alpha-synuclein (αS) have been employed to carry the hypoxia-inducible factor 2α (HIF2α)-targeting PT2385 in a mouse model xenografted with clear cell renal cell carcinoma (ccRCC). Hydrophobic cargo like rhodamine 6G entrapped within the microcapsules was demonstrated to be selectively released under cancer-related stimuli including acidic pH, local hyperthermia, and proteases such as matrix metalloproteinases. The αS-AuNP microcapsules containing the hydrophobic drug of PT2385 suppressed the expression of HIF2α and its downstream genes in ccRCC A498 cells in vitro to the level comparable to that obtained with direct PT2385 treatment, indicating that the PT2385 remained active inside the capsules. In the A498 xenograft mouse model, intraperitoneal administration of the αS-AuNP-PT2385 microcapsules significantly reduced the tumor volume and Ki-67 scores from those monitored in the PT2385-treated group. Therefore, the αS-AuNP microcapsule is suggested to be a promising cancer-targeting drug delivery system which exhibits several merits such as improved loading efficiency for hydrophobic drugs, their protection from metabolism, and selective cargo release in tumor microenvironments in addition to its physicotherapeutic potential due to the photothermal effect of AuNPs.

A Novel pH-Responsive Iron Oxide Core-Shell Magnetic Mesoporous Silica Nanoparticle (M-MSN) System Encapsulating Doxorubicin (DOX) and Glucose Oxidase (Gox) for Pancreatic Cancer Treatment.

This study developed a pancreatic cancer targeted drug delivery system that responds to changes in acidity. The system was based on iron oxide core-shell magnetic mesoporous silica nanoparticles (M-MSNs) to treat pancreatic cancer through combined chemotherapy and starvation therapy. Glucose oxidase (Gox) was coupled to the cancer cell surface to reduce glucose availability for cancer cells, exacerbating the heterogeneity of the tumor microenvironment. Reduced pH accelerated the depolymerization of pH-sensitive polydopamine (PDA), thereby controlling the spatial distribution of Gox and release of doxorubicin (DOX) within tumor cells. Characterization results showed the successful synthesis of DG@M-MSN-PDA-PEG-FA (DG@NPs) with a diameter of 66.02 ± 3.6 nm. In vitro data indicated DG@NPs were highly effective and stable with good cellular uptake shown by confocal laser scanning microscopy (CLSM). DG@NPs exhibited high cytotoxicity and induced apoptosis. Additionally, in vivo experiments confirmed DG@NPs effectively inhibited tumor growth in nude mice with good biosafety. The combination of starvation therapy and chemotherapy facilitated drug release, suggesting DG@NPs as a novel drug delivery system for pancreatic cancer treatment. This study successfully constructed a doxorubicin release system responsive to acidity changes for targeted delivery in pancreatic cancer, providing a new strategy for combination therapy.

Radiotherapy Potentiates the P-Selectin Targeted Cancer Drug Delivery Based on a Cisplatin and Mitoxantrone Coassembled Fucoidan Nanogel

Radiotherapy Potentiates the P-Selectin Targeted Cancer Drug Delivery Based on a Cisplatin and Mitoxantrone Coassembled Fucoidan Nanogel

Hyaluronan nanogel co-loaded with chloroquine to enhance intracellular cisplatin delivery through lysosomal permeabilization and lysophagy inhibition

Hyaluronan (HA) has been widely used to construct nanocarriers for cancer-targeted drug delivery, due to its excellent biocompatibility and intrinsic affinity towards CD44 that is overexpressed in most cancer types. However, the HA-based nanocarriers are prone to trapping in lysosomes following the HA-mediated endocytosis, which limited the delivered drug to access its pharmacological action sites and subsequently compromised the therapeutic efficacy. To overcome this intracellular obstacle, here we demonstrated the co-loading of chloroquine (CQ) in HA nanogel could efficiently promote the intracellular delivery of cisplatin. The cisplatin coordination with HA generated the nanogel that could also co-encapsulate CQ (HA/Cis/CQ nanogel). Compared with cisplatin-loaded HA nanogel (HA/Cis), HA/Cis/CQ significantly promoted the lysosomal escape of cisplatin as well as enhanced tumor inhibition in the triple-negative breast cancer model. Mechanism studies suggested that co-delivery of CQ not only induced the lysosomal membrane permeabilization but also inhibited the lysophagy, which collectively contributed to the lysosomal instability and cisplatin escape. This HA/Cis/CQ nanogel elicited less toxicity compared with the combination of free Cis and CQ, thus suggesting a promising HA nanocarrier to boost the cisplatin delivery towards cancer-targeted therapy.

Liposomal Encapsulation of Chemotherapeutics Agents Combined with the Use of Ultrasound in Cancer Treatment

Ultrasound (US) has numerous uses in the medical field, including imaging, tumor ablation, and lithotripsy; another interesting application of US in cancer therapy is as an external trigger in targeted drug delivery. Cancer-targeted drug delivery involves delivering chemotherapeutic drugs to tumor sites with a high degree of precision, which would minimize the adverse side effects experienced by patients. Several nanocarriers have been studied as possible nanocarriers; however, liposomes stood out from the rest because of their non-immunogenicity, amphiphilic nature, ease of functionalization, and stimuli-responsiveness. This review addresses the role of US in the synthesis of liposomes, its ability to induce localized and controlled drug release from liposomes, as well as the integration of US-induced release and US-imaging using liposomes as contrast agents utilizing thermal and/or mechanical effects.

RGD-engineered nanoparticles as an innovative drug delivery system in cancer therapy

The poor efficiency and drastic adverse effects of current cancer therapies entail a radical shift in treatment paradigms, which require developing cutting-edge therapeutics in laboratories and bringing them to rigorous preclinical and clinical testing. The principal drawbacks of present cancer therapies are the incapability of tumor targeting, uneven drug accumulation at the site of action, and poor tumor monitoring. Accordingly, incorporating nanoparticles (NPs) has made clinical progress in conveying conventional or candidate therapeutic molecules to the site of action, encouraging anticancer impacts. Interestingly, modern cancer therapy has lately been redefined by the functionalizing NPs with active targeting ligands like the Arginine-Glycine-Aspartic acid (RGD) peptide, remarkably strengthening the therapeutic outcomes and diminishing off-target effects. The overexpression of integrin receptors on the surface of cancerous cells brought a unique opportunity for cancer-targeted drug delivery since RGD-decorated nanocarriers precisely recognize these receptors and selectively transport their chemotherapeutic or diagnostic payloads to the cancerous cells. Subsequently, RGD-conjugated NPs have frequently been enlisted for cancer diagnosis and imaging-guided surgery, improving therapeutics strength and overwhelming drug resistance. Here, we discussed the relevance of integrin receptors in carcinogenesis and thoroughly deliberated the potential of RGD-functionalized NPs as innovative drug delivery platforms in modern cancer therapy.

Role of nanoparticles in pancreatic drug delivery: Including a bibliography on Targeted drug delivery

The number of times a publication or an individual author has been discussed in the scientific community is a common metric for measuring their impact. The goal of the bibliometric study was to look at the maximum cited articles in the area of "pancreatic cancer, nanoparticles, targeted ligand, binding, drug delivery and treatment.".The database SCOPUS was used to conduct a computerised literature search. The top 100 articles with the most citations were chosen and studied furtherThere were 298 citations in the most cited article, with an average of 62 citations per publication. These highly cited publications appeared in 33 journals, with the Journal of Controlled Release leading the pack (27 articles). The United States contributed 53 articles, which originated from 19 different countries. These 100 citations were provided by 85 institutions, with the “Department of Chemical and Biomolecular Engineering” leading the way (4). The investigation of the top highly cited articles concedes for recognizing significant advances in pancreatic cancer targeted drug delivery study and gives a historical perspective on the advancement of this speciality of cancer research.

Starch Janus Particles: Bulk Synthesis, Self-Assembly, Rheology, and Potential Food Applications.

Although incredible progress in the field of Janus particles over the last three decades has delivered many promising smart-material prototypes, from cancer-targeting drug delivery vehicles to self-motile nanobots, their real-world applications have been somewhat tempered by concerns over scalability and sustainability. In this study, we adapt a simple, scalable 3D mask method to synthesize Janus particles in bulk using starch as the base material: a natural biopolymer that is safe, biocompatible, biodegradable, cheap, widely available, and versatile. Using this method, starch granules are first embedded on a wax droplet such that half of the starch is covered; then, the uncovered half is treated with octenyl succinic anhydride, after which the wax coating is removed. Janus particles with 49% Janus balance can be produced in this way and were observed to self-assemble into wormlike strings in water due to their hydrophobic/hydrophilic nature. Our Janus starch granules outperform the non-Janus controls as thickening and gelling agents: they exhibit a fourfold increase in water-holding capacity, a 30% lower critical caking concentration, and a viscosity greater by orders of magnitude. They also form gels that are much firmer and more stable. Starch Janus particles with these functional properties can be used as novel, lower-calorie, highly efficient, plant-based super-thickeners in the food industry, potentially reducing starch use in food by 55%.

Multifunctional Oxygenated Particles for Targeted Cancer Drug Delivery and Evaluation with Darkfield Hyperspectral Imaging.

We propose a novel multifunctional nanocarrier system for targeted drug delivery for lung cancer theranostics. Oxygenated particles (OPs) synthesized with an oxygen-encapsulating carboxymethyl cellulose shell were used as a platform to deliver oxygen to the hypoxic tumor microenvironment. The OPs synthesized could also be conjugated with ligands (e.g., antibodies) to target cancer cells expressing the corresponding antigens to deliver a drug, doxorubicin. In vitro testing of functionalized OPs showed increased efficacy of doxorubicin against the proliferation of lung cancer cells. Both confocal fluorescence imaging and darkfield microscopy hyperspectral imaging validated the OP complex and its efficient targeting of specific cells to deliver the therapeutic. The nanocarrier platform developed can also serve as a diagnostic imaging reagent as demonstrated by darkfield microscopy. Results show that the theranostic OPs developed with multifunctional modalities enabled targeted drug delivery with improved efficacy and tracking of drug delivery vehicles by imaging.

Orange-Peel-Derived Nanobiochar for Targeted Cancer Therapy.

Cancer-targeted drug delivery systems (DDS) based on carbon nanostructures have shown great promise in cancer therapy due to their ability to selectively recognize specific receptors overexpressed in cancer cells. In this paper, we have explored a green route to synthesize nanobiochar (NBC) endowed with graphene structure from the hydrothermal carbonization (HTC) of orange peels and evaluated the suitability of this nanomaterial as a nanoplatform for cancer therapy. In order to compare the cancer-targeting ability of different widely used targeting ligands (TL), we have conjugated NBC with biotin, riboflavin, folic acid and hyaluronic acid and have tested, in vitro, their biocompatibility and uptake ability towards a human alveolar cancer cell line (A549 cells). The nanosystems which showed the best biological performances—namely, the biotin- and riboflavin- conjugated systems—have been loaded with the poorly water-soluble drug DHF (5,5-dimethyl-6a-phenyl-3-(trimethylsilyl)-6,6a-dihydrofuro[3,2-b]furan-2(5H)-one) and tested for their anticancer activity. The in vitro biological tests demonstrated the ability of both systems to internalize the drug in A549 cells. In particular, the biotin-functionalized NBC caused cell death percentages to more than double with respect to the drug alone. The reported results also highlight the positive effect of the presence of oxygen-containing functional groups, present on the NBC surface, to improve the water dispersion stability of the DDS and thus make the approach of using this nanomaterial as nanocarrier for poorly water-soluble drugs effective.