A redox-sensitive core-crosslinked nanosystem combined with ultrasound for enhanced deep penetration of nanodiamonds into tumors

Nanodiamonds (NDs) as drug delivery vehicles are of great significance in anticancer therapy through enhancing drug retention. However, the major barrier to clinical application of NDs is insufficient tumor penetration owing to their strong aggregation and low passive penetration efficiency. Herein, the core-crosslinked pullulan carrier, assembled using the visible light-induced diselenide (Se–Se) bond crosslinking method for encapsulating nanodiamonds-doxorubicin (NDX), is proposed to improve monodispersity. Furthermore, the core-crosslinked diselenide bond provides the nanosystem with redox-responsive capability and improved structural stability in a physiological environment, which prevents premature drug leakage and achieves tumor site-specific controlled release. What''s more, ultrasound (US) is utilized to promote nanosystem intratumoral penetration via enlarged tumor vascular endothelium cell gaps. As expected, the nanosystem combined with ultrasound can enhance anti-tumor efficacy with deep penetration and excellent retention performance in a HepG2 xenograft mouse model. This study highlights the ability of the integrated therapeutic paradigm to overcome the limitation of nanodiamonds and the potential for further application in cancer therapy.

A redox-sensitive core-crosslinked nanosystem is developed as a drug vehicle combined with ultrasound for efficient enhanced deep penetration of nanodiamonds into tumors.     

CD44-targeted hyaluronic acid–curcumin reverses chemotherapeutics resistance by inhibiting P-gp and anti-apoptotic pathways

Chemotherapeutic drug resistance poses a great challenge in cancer therapy. Drug efflux and anti-apoptotic processes are the two most common mechanisms leading to chemotherapy resistance. In this study, we focused on the applicability of curcumin (CUR) as a sensitizer for chemotherapeutics (doxorubicin [DOX] as the model drug) modified with hyaluronic acid (HA) as an effective therapeutic strategy against multidrug resistance (MDR) in cancer cells. We constructed an HA–CUR/DOX delivery system measuring approximately 180 nm with superior encapsulation efficacy and serum stabilities. In vitro, we found that HA modification could facilitate the efficient delivery of chemotherapeutics through CD44 receptor-mediated targeted delivery. MTT assay results confirmed that the combination of CUR and DOX/paclitaxel (PTX) had a significant synergistic effect and significantly reversed MDR. Further experiments including real-time polymerase chain reaction and western blotting proved that the main mechanisms by which CUR reversed MDR in tumor cells were inhibiting the expression and activity of P-glycoprotein (P-gp) and inducing apoptosis through mitochondrial pathway. Taken together, our new engineered tumor-targeting nanoparticle delivery system may have the potential for overcoming MDR in cancer.

Chemotherapeutic drug resistance poses a great challenge in cancer therapy.     

Enhancing cellular morphological changes and ablation of cancer cells via the interaction of drug co-loaded magnetic nanosystems in weak rotating magnetic fields

Magnetic nanoparticles have been widely used in cancer treatment for their potential magnetic functions and synergistic antitumor effect with therapeutic agents. In this work, we developed a polymeric nanosystem by co-loading the natural anticancer drug tetrandrine and superparamagnetic iron oxide nanoparticles for cancer combinatorial therapy. The nanosystem possessed regular morphology and superior magnetic properties. Under the action of external rotating permanent magnets, the nanosystem could transfer a rotational motion to damage the cellular membrane, which would result in the increased permeabilization of the cell membrane and damage to lysosomes. Hence, the specific characteristics of the magnetic nanosystem induced potent cytotoxicity and enhanced the effect of the tetrandrine-induced cell apoptosis. With further exploration, we found that this nanoplatform caused cell death via a lysosomal-mitochondrial apoptotic pathway with the upregulation of proapoptotic proteins (Cathepsin B, Smac/Diablo, Cytochrome C, and Caspase 3) and the down-regulation of antiapoptotic proteins (Bcl-2 and XIAP). These findings demonstrate that the combination therapy mediated by co-loaded magnetic nanosystems can be used for a multi-therapeutic effect against tumors in biomedical applications.

Tetrandrine and Fe₃O₄ nanoparticle co-loaded PLGA nanosystems produce rotational movement and promote tetrandrine release, causing a dual apoptotic effect to tumors.     

Theranostic system for ratiometric fluorescence monitoring of peptide-guided targeted drug delivery

Conjugation of an anticancer drug with a cancer-specific carrier and a fluorescent dye to form a theranostic system enables real time monitoring of targeted drug delivery (TDD). However, the fluorescence signal from the dye is affected by the light absorption and scattering in the body, photobleaching, and instrumental parameters. Ratiometric measurements utilizing two fluorescence signals of different wavelengths are known to improve sensitivity, reliability and quantitation of fluorescence measurements in biological media. Herein, a novel theranostic system comprising the anticancer drug chlorambucil (CLB), cancer-specific peptide octreotide amide (OctA), and a long-wavelength dual fluorescent cyanine dye IRD enabling ratiometric monitoring of drug delivery was developed and evaluated on the cancer cell line PANC-1.

Novel theranostic system that first combines a cancer-targeting peptide with a long-wavelength dual fluorescent dye IRD in order to provide ratiometric monitoring of anticancer drug delivery is developed and evaluated in pancreatic cancer cell line.     

Targeted drug release system based on pH-responsive PAA-POSS nanoparticles

An amphipathic PAA-POSS@DOX drug delivery system that responds sensitively to pH changes in the cancer microenvironment has been developed using a nanoparticle based on inorganic polyhedral oligomeric silsesquioxane (POSS). POSS was introduced to the carboxylic acid group of polyacrylic acid to which doxorubicin anticancer drug was loaded to prepare 480 ± 192 nm self-assembled nanoparticles. PAA-POSS had a high loading efficiency of over 75% and doxorubicin was quickly released to the target area responding sensitively to weakly acidic conditions. The possibility of employing PAA-POSS as a targeted drug delivery system has been confirmed by observing the death of cells of the MDA-MB-231 breast cancer line.

pH-sensitive PAA-POSS@DOX nanoparticles were synthesized and showed high loading efficiency of over 75% and doxorubicin was quickly released to the target area. The ability of PAA-POSS@DOX to kill MDA-MB-231 breast cancer cells has been demonstrated.     

Advances with metal oxide-based nanoparticles as MDR metastatic breast cancer therapeutics and diagnostics

Metal oxide nanoparticles have attracted increased attention due to their emerging applications in cancer detection and therapy. This study envisioned to highlight the great potential of metal oxide NPs due to their interesting properties including high payload, response to magnetic field, affluence of surface modification to overcome biological barriers, and biocompatibility. Mammogram, ultrasound, X-ray computed tomography (CT), MRI, positron emission tomography (PET), optical or fluorescence imaging are used for breast imaging. Drug-loaded metal oxide nanoparticle delivered to the breast cancer cells leads to higher drug uptake. Thus, enhanced the cytotoxicity to target cells compared to free drug. The drug loaded metal oxide nanoparticle formulations hold great promise to enhance efficacy of breast cancer therapy including multidrug resistant (MDR) and metastatic breast cancers. Various metal oxides including magnetic metal oxides and magnetosomes are of current interests to explore cancer drug delivery and diagnostic efficacy especially for metastatic breast cancer. Metal oxide-based nanocarrier formulations are promising for their usage in drug delivery and release to breast cancer cells, cancer diagnosis and their clinical translations.

Biomarker targeted therapy approaches for TNBC using metal oxide-based NPs are highly effective and promising.     

pH and redox dual-sensitive drug delivery system constructed based on fluorescent carbon dots

Herein, a pH and redox dual-responsive drug delivery system (CDs–Pt(iv)–PEG) was developed based on fluorescence carbon dots (CDs). In this system, cisplatin(iv) prodrug (Pt(iv)) was selected as a model drug to reduce toxic side effects. The aldehyde-functionalized monomethoxy polyethylene glycol (mPEG-CHO) was conjugated to CDs–Pt(iv) to form pH sensitive benzoic imine bond. Owing to the slightly acidic tumor extracellular microenvironment (pH 6.8), the benzoic imine bond was then hydrolyzed, leading to charge reversal and decrease in the hydration radius of the drug-carrying, which facilitated in vivo circulation and tumor targeting. Notably, the cytotoxicity of the drug delivery system on cancer cells was comparable to that of cisplatin, while the side effects on normal cells were significantly reduced. In addition, the system realized recognition of cancer cells by the high-contrast fluorescent imaging. In conclusion, the CDs–Pt(iv)–PEG system provided a promising potential for effective delivery of anticancer drugs and cancer cells screening.

The system is pH-responsive and redox-controlled release. And the charge reversal and size transitions of the system can enhance the targeted ability. Moreover, the system can recognize the cancer cells by the fluorescence imaging.     

A DOX-loaded polymer micelle for effectively inhibiting cancer cells

A novel triblock polymer is synthesized and self-assembled with doxorubicin to form DOX-loaded micelles. The synthetic process involves the ring-opening polymerization, carboxylation and amidation reactions, and the structures are characterized. The drug release test indicated that the micelles have the ability to control the release of drugs. The cell uptake results indicated that the DOX-loaded micelles could enter cancer cells easily, and the cytotoxicity and apoptosis test confirmed that DOX-loaded micelles have a strong killing effect on tumor cells, while the blank micelles do not have cytotoxicity. Therefore, the novel polymer micelles are a promising carrier for delivery of anticancer drugs to enhance cancer treatment.

A novel triblock polymer is synthesized and self-assembled with doxorubicin to form DOX-loaded micelles.     

Drug-loaded dual targeting graphene oxide-based molecularly imprinted composite and recognition of carcino-embryonic antigen

Despite extensive research on functional graphene oxide for anticancer drug delivery, the sensitivity of traditional protein targeting ligands to the environment limits the practical applications of targeted drug delivery. A unique molecularly imprinted magnetic graphene oxide was used as a novel drug delivery system for the treatment of tumors. Molecularly imprinted polymers (MIPs) synthesized by molecular imprinting technology have the advantages of good stability against chemical and enzymatic attacks, high specificity for a target template, and resistance to harsh environments. In our work, the MIP was used for specificity to tumor cells with carcino-embryonic (CEA) tumor markers as the template, and dopamine as the functional monomer was grafted on boronic acid-functionalized magnetic graphene oxide. The structure of the nanoparticles was optimized and characterized in detail by vibrating sample magnetometry, X-ray diffraction analysis, UV-vis spectroscopy, and flow cytometry. The prepared polymer has magnetic properties, specific recognition to CEA, biocompatibility and pH sensitivity for drug delivery. Cell culture research was carried out on the tumor cells and normal cells. The composites exhibited dual targeting properties that not only magnetically target but also specifically increase the drug cytotoxicity to the tumor cells by selectively binding to CEA. On the basis of these results, this study developed a novel approach for targeting tumor cells for drug delivery without needing to modify the protein ligand.

In the research we designed a CEA-molecularly imprinted polymers using molecular imprinting technique with CEA tumor marker as template, boronic acid functionalized MGO as substrate for dual targeted delivery of drug to tumor cells.     

Microwave-assisted delivery of an anticancer drug to cancer cells

Exposure of MCF-7 breast and PC-3 prostate cancer cells to 10 W microwaves at 2.45 GHz increased their uptake of the cancer drug doxorubicin from media by almost 100%, concomitantly increasing cell death, while microwave exposure alone had no cellular toxicity. Addition of inhibitors of endocytosis during the treatment of MCF-7 cells with doxorubicin and microwaves showed no impact on the uptake of the anticancer drug. Furthermore, the uptake of oligonucleotides by MCF-7 cells is not affected by the treatment with microwaves. These observations suggest that endocytosis is not involved in the uptake of doxorubicin while cells are exposed to microwave irradiation. Thus, targeted low power microwave irradiation could be a safe and effective means of promoting chemotoxin delivery to cancer cells, potentially reducing the dosages and side effects of anti-cancer drugs.

Exposure of MCF-7 breast and PC-3 prostate cancer cells to 10 W microwaves at 2.45 GHz increased their uptake of doxorubicin from media by almost 100%, concomitantly increasing cell death, while microwave exposure alone had no cellular toxicity.     

2D-BN nanoparticles as a spectroscopic marker and drug delivery system with protection properties

An application of 2D-BN nanoparticles as a spectroscopic marker, weak luminescent marker and anticancer drug (doxorubicin, DOX) delivery system with protection properties was studied for the LNCaP strains of cancer cells using FTIR and Raman spectroscopy for analysing the cancer cells, cells with BN, the cancer cells with DOX, and the cancer cells with BN nanoparticles loaded by DOX. Study of IR absorption and Raman spectra of the LNCaP strains of cancer cells incubated with 2D-BN nanoparticles for 1 hour showed that the 2D-BN nanoparticles could pass through the cell membrane and localize inside the membrane or close to the membrane in the cytoplasm of the cells. We registered the spectra of the disturbed lipids during the DOX-2D-BN passing through the membrane. After incubation for 2 hours and more, spectral changes in other structural components of the cell (nuclei, cytoplasm, mitochondria) can be registered. Confocal microscopy showed that a gold nanostructured support enhances the fluorescence of the cancer cells with 2D-BN as well as that with DOX, however the double action of 2D-BN and DOX on the cancer cells aggravates the emission property of the studied system. An MTT test showed that the toxicity of DOX on the 2D-BN nanoparticles is less than that on the reference cells, and at the same time the efficiency of the DOX action on the cancer cells does not change.

An application of 2D-BN nanoparticles as spectroscopic marker, weak luminescent marker and anticancer drug (doxorubicin, DOX) delivery system with protection property was studied for the LNCaP strains of cancer cells.     

Polymer grafted magnetic graphene oxide as a potential nanocarrier for pH-responsive delivery of sparingly soluble quercetin against breast cancer cells

In this work, polymer grafted magnetic graphene oxide (GO–PVP–Fe₃O₄) was successfully synthesized for efficient delivery of anticancer drug. Firstly, GO was functionalized with the hydrophilic and biocompatible polymer polyvinylpyrrolidone (PVP) and then grafted with magnetic nanoparticles (Fe₃O₄) through an easy and effective chemical co-precipitation method. Quercetin (QSR) as an anticancer drug was loaded onto the surface of GO–PVP–Fe₃O₄via non-covalent interactions. The drug loading capacity was as high as 1.69 mg mg⁻¹ and the synthesized magnetic nanocarrier shows pH-responsive controlled release of QSR. The cellular cytotoxicity of the synthesized nanocarrier with and without drugs was investigated in human breast cancer MDA MB 231 cells and their effects compared on non-tumorigenic epithelial HEK 293T cells. These results reveal that the drug loaded GO–PVP–Fe₃O₄ nanohybrid was found to be more toxic than the free drug towards MDA MB 231 cells and exhibits biocompatibility towards HEK 293T cells. Overall, a smart drug delivery system including polymer grafted magnetic graphene oxide as a pH-responsive potential nanocarrier could be beneficial for targeted drug delivery, controlled by an external magnetic field as an advancement in chemotherapy against cancer.

Polymer grafted magnetic graphene oxide (GO–PVP–Fe₃O₄) as an efficient nanocarrier for the delivery of anticancer drug quercetin.     

Amphiphilic irinotecan–melampomagnolide B conjugate nanoparticles for cancer chemotherapy

Melampomagnolide B (MMB) is a natural sesquiterpene lactone product structurally related to parthenolide (PTL). Although MMB has been widely used to treat various types of cancers, such as glioma, leukemia and colon cancer, the effective delivery of MMB to cancer cells remains a challenge. An amphiphilic drug–drug conjugate (ADDC) strategy has been proposed and developed as a promising drug self-delivery system for cancer therapy because of its simple preparation, carrier-free nature, and high therapeutic activity. Herein, we present a new ADDC, which is synthesized by linking the hydrophilic anticancer drug irinotecan (Ir) and the hydrophobic anticancer drug MMB through a carbonate bond. The obtained amphiphilic irinotecan–melampomagnolide B conjugate (Ir–C–MMB) can self-assemble in water into stable nanoparticles with an average diameter of around 122.1 nm. After cellular uptake, the carbonate bond between the hydrophilic drug and hydrophobic drug can be cleaved to release free Ir and MMB under acidic conditions, which exhibit a synergistic effect in tumor cells. MTT results reveal that the Ir–C–MMB nanoparticles can effectively inhibit proliferation of cancer cells. The apoptosis data indicate that the apoptosis rate of cells treated with Ir–C–MMB nanoparticles is about 50% within 24 h, which is much higher than that of free Ir or MMB. Our results suggest that this ADDC strategy could be used as a drug delivery platform for MMB and its derivatives, and that it offers effective synergistic therapeutic efficacy.

Ir–C–MMB nanoparticles can be easily fabricated using an ADDC strategy, and used as a MMB drug self-delivery platform for synergistic cancer therapy.     

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

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

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

Computational methods directed towards drug repurposing for COVID-19: advantages and limitations

Novel coronavirus disease 2019 (COVID-19) has significantly altered the socio-economic status of countries. Although vaccines are now available against the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a causative agent for COVID-19, it continues to transmit and newer variants of concern have been consistently emerging world-wide. Computational strategies involving drug repurposing offer a viable opportunity to choose a medication from a rundown of affirmed drugs against distinct diseases including COVID-19. While pandemics impede the healthcare systems, drug repurposing or repositioning represents a hopeful approach in which existing drugs can be remodeled and employed to treat newer diseases. In this review, we summarize the diverse computational approaches attempted for developing drugs through drug repurposing or repositioning against COVID-19 and discuss their advantages and limitations. To this end, we have outlined studies that utilized computational techniques such as molecular docking, molecular dynamic simulation, disease–disease association, drug–drug interaction, integrated biological network, artificial intelligence, machine learning and network medicine to accelerate creation of smart and safe drugs against COVID-19.

Different kind of methods utilized in expediting drug repurposing.     

Target-specific mononuclear and binuclear rhenium(i) tricarbonyl complexes as upcoming anticancer drugs

Metal complexes have gradually been attracting interest from researchers worldwide as potential cancer therapeutics. Driven by the many side effects of the popular platinum-based anticancer drug cisplatin, the tireless endeavours of researchers have afforded strategies for the design of appropriate metal complexes with minimal side effects compared to cisplatin and its congeners to limit the unrestricted propagation of cancer. In this regard, transition metal complexes, especially rhenium-based complexes are being identified and highlighted as promising cancer theranostics, which are endowed with the ability to detect and annihilate cancer cells in the body. This is attributed the amazing photophysical properties of rhenium complexes together with their ability to selectively attack different organelles in cancer cells. Therefore, this review presents the properties of different rhenium-based complexes to highlight their recent advances as anticancer agents based on their cytotoxicity results.

In this review, rhenium-based complexes are highlighted as promising cancer theranostics, which are endowed with the ability to detect and annihilate cancer cells in the body.     

Nobiletin,a citrus polymethoxyflavone,enhances the effects of bicalutamide on prostate cancer cells via down regulation of NF-κB,STAT3, and ERK activation

Natural products have shown potential to be combined with current cancer therapies to improve patient outcomes. Nobiletin (NBT) is a citrus polymethoxyflavone and has been shown to exert an anticancer effect in various cancer cells. We investigated the effects and mechanisms of NBT in combination with bicalutamide (BCT), a commonly used anti-androgen drug in prostate cancer therapy, on prostate cancer cells. Our results demonstrate that the combined treatment with NBT and BCT produces an enhanced inhibitory effect on the growth of prostate cancer cells compared to either compound alone. The synergistic action of NBT and BCT was confirmed using isobologram analysis. Moreover, this study has shown that NBT and BCT synergistically inhibited colony formation and migration as well as induced apoptosis. Mechanistic studies demonstrate that NBT and BCT combination reduced key cellular signaling regulators including: p-Erk/Erk, p-STAT3/STAT3 and NF-κB. Overall, these results suggest that NBT combination with BCT may be an effective treatment for prostate cancer.

Nobiletin enhance the anticancer effect of bicalutamide on prostate cancer cells via down regulation of NF-κB, STAT3, Erk activation.     

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

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

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

Preparation and evaluation of a Rubropunctatin-loaded liposome anticancer drug carrier

Rubropunctatin is a naturally occurring constituent of polyketide compounds that has great potential in the development of cancer-assisted chemotherapy. However, it has certain shortcomings such as water insolubility and photo instability that limit its clinical application. In this study, we constructed a Rubropunctatin-loaded liposome (R-Liposome) anticancer drug carrier for the first time. The results indicate that R-Liposome is water soluble, has spherical morphology, great homogeneity and dispersibility with high encapsulation efficiency (EE%, 90 ± 3.5%) and loading rate (LR%, 5.60 ± 2.5%) values. Moreover, the carrier improves the photostability, storage and pH stabilities of Rubropunctatin. The R-Liposome also prolongs the release of Rubropunctatin, enhances the anticancer activity of Rubropunctatin and encourages the mechanism of Rubropunctatin to promote apoptosis. Therefore, liposomal nanoparticles have great potential as drug delivery vehicles of Rubropunctatin for cancer treatment.

Rubropunctatin-loaded liposomes were constructed using a thin film evaporation method, followed by sonication, forming a stable nanoparticle preparation, and improving the water solubility, stability and anticancer activity of Rubropunctatin.     

RAFT polymerization mediated core–shell supramolecular assembly of PEGMA-co-stearic acid block co-polymer for efficient anticancer drug delivery

In this work, core–shell supramolecular assembly polymeric nano-architectures containing hydrophilic and hydrophobic segments were synthesized via reversible addition fragmentation chain transfer (RAFT) polymerization. Herein, polyethylene glycol methyl ether methacrylate (PEGMA), and stearic acid were used to synthesize the poly(PEGMA) homopolymer and stearyl ethyl methacrylate (SEMA), respectively. Then, PEGMA and SEMA were polymerized through controlled RAFT polymerization to obtain the final diblock copolymer, poly(PEGMA-co-SEMA) (BCP). Model anticancer drug, doxorubicin (DOX) was loaded on BCPs. Interestingly, efficient DOX release was observed at acidic pH, similar to the cancerous environment pH level. Significant cellular uptake of DOX loaded BCP50 (BCP50-DOX) was observed in MDA-MB-231 triple negative breast cancer cells and resulted in a 35 fold increase in anticancer activity against MDA MB-231 cells compared to free DOX. Scanning electron microscopy (SEM) imaging confirmed the apoptosis mediated cellular death. These core–shell supramolecular assembly polymeric nano-architectures may be an efficient anti-cancer drug delivery system in the future.

In this work, core–shell supramolecular assembly polymeric nano-architectures containing hydrophilic and hydrophobic segments were synthesized via reversible addition fragmentation chain transfer (RAFT) polymerization.