Anticancer Drug Carrier Research Articles

Synthesis and characterization of binary selenides of transition metals to investigate its photocatalytic, antimicrobial and anticancer efficacy

Development of resilient and efficient composite materials that exhibit substantial antimicrobial activity, ample photocatalytic ability and considerable capacity for drug delivery is highly desirable. The present study demonstrates the incorporation of selenium (Se) in transition metals (vanadium-V, niobium-Nb, and tantalum-Ta) via standard solid-state hydrothermal reaction method. Generated nanostructures (V:Se, Nb:Se, Ta:Se) were characterized using various techniques. XRD analysis confirmed the presence of monoclinic phase compounds while crystallite size (~ 13.5–26.2 nm) was calculated using Debye–Scherrer equation. FESEM was used to examine surface morphologies of V:Se (rod-like and disc-shaped) and of Nb and Ta selenides (irregular agglomerated nanospheres). Compositional and functional group analysis was undertaken through FTIR spectroscopy and EDS coupled with SEM, respectively. Raman spectroscopy was carried out to ascertain the bending and stretching vibrational modes in samples. Optical properties were investigated through UV–Vis spectroscopy and the PL emission spectra were acquired to evaluate the charge separation and recombination behavior of compounds. Thermal stability of designed composites was measured using TGA/DSC. Potential uses of the prepared nanoparticles were explored in multiple fields including photocatalysis, antimicrobial and drug delivery systems. Methylene blue dye was degraded under 400–700 nm wavelength in the presence of synthesized wide band gap composites as photocatalysts. The selenium–metal particles were subjected as antimicrobial agents against gram (−ve) and gram (+ve) bacteria and experimental results suggested this material to be an effective antibiotic. Furthermore, synthesized nanocomposites were examined as carrier of anticancer drug (DOX) and their drug delivery profile was also investigated.

Dialysis Preparation of Smart Redox and Acidity Dual Responsive Tea Polyphenol Functionalized Calcium Phosphate Nanospheres as Anticancer Drug Carriers.

Large-scale preparation of biocompatible drug delivery systems with targeted recognition and controlled release properties has always been attractive. However, this strategy has been constrained by a lot of design challenges, such as complicated steps and premature drug release. Herein, in this paper, we address these problems by a facile in situ mineralization method, which synthesizes biodegradable tea polyphenol coated monodisperse calcium phosphate nanospheres using for targeted and controlled delivery of doxorubicin. Dialysis diffusion method was used to control ion release to form mineralized nanospheres. The polyphenol coatings and calcium phosphate used in this work could be biodegraded by intracellular glutathione and acidic microenvironment, respectively, resulting the release of encapsulated drug. According to confocal fluorescence microscopy, and cytotoxicity experiments, the prepared tea polyphenol functionalized, doxorubicin loaded calcium phosphate nanospheres were confirmed to have highly efficient internalization and obvious cell killing effect on target tumor cells, but not normal cells. Our results suggest that these tea polyphenols functionalized calcium phosphate nanospheres are promising vehicles for controlled release of an anticancer drug in cancer therapy.

All-Trans Retinoic Acid Grafted Poly Beta-Amino Ester Nanoparticles: A Novel Anti-angiogenic Drug Delivery System.

Purpose: Developing chemotherapy with nanoplatforms offers a promising strategy for effective cancer treatment. In the present study, we propose a novel all-trans retinoic acid (ATRA) grafted poly beta-amino ester (PBAE) copolymer for preparing nanoparticles (NPs). Methods: ATRA grafted PBAE (ATRA-g-PBAE) copolymer was synthesized by grafting ATRA to PBAE; it was characterized by proton nuclear magnetic resonance, Fourier transform infrared, and thermogravimetric analysis. ATRA-g-PBAE NPs were prepared by the solvent displacement method. Design-Expert software was employed to optimize size of NPs. The morphology was evaluated by transmission electron microscope, and ultraviolet-visible spectroscopy was applied for drug release. Cytotoxicity was evaluated toward HUVEC cell line, and the 3D collagencytodex model was used to evaluate anti-angiogenic property of PBAE, ATRA, and NPs. Results: The optimum size of the NPs was 139.4 ± 1.41 nm. After 21 days, 66.09% ± 1.39 and 42.14% ± 1.07 of ATRA were released from NPs at pH 5.8 and 7.4, respectively. Cell culture studies demonstrated antiangiogenic effects of ATRA-g-PBAE NPs. Anti-angiogenesis IC50 was 0.007 mg/mL for NPs (equal to 0.002 mg/mL of ATRA) and 0.005 mg/mL for free ATRA. Conclusion: This study proposes the ATRA-g-PBAE NPs with inherent anti-angiogenic effects as promising carrier for anticancer drugs with purpose of dual drug delivery.

Red-Emissive Carbon Quantum Dots for Nuclear Drug Delivery in Cancer Stem Cells.

Large doses of anticancer drugs entering cancer cell nuclei are found to be effective at killing cancer cells and increasing chemotherapeutic effectiveness. Here we report red-emissive carbon quantum dots, which can enter into the nuclei of not only cancer cells but also cancer stem cells. After doxorubicin was loaded at the concentration of 30 μg/mL on the surfaces of carbon quantum dots, the average cell viability of HeLa cells was decreased to only 21%, while it was decreased to 50% for free doxorubicin. The doxorubicin-loaded carbon quantum dots also exhibited a good therapeutic effect by eliminating cancer stem cells. This work provides a potential strategy for developing carbon quantum-dot-based anticancer drug carriers for effective eradication of cancers.

Oxidation-Triggerable Liposome Incorporating Poly(Hydroxyethyl Acrylate-co-Allyl methyl sulfide) as an Anticancer Carrier of Doxorubicin.

Since cancer cells are oxidative in nature, anti-cancer agents can be delivered to cancer cells specifically without causing severe normal cell toxicity if the drug carriers are designed to be sensitive to the intrinsic characteristic. Oxidation-sensitive liposomes were developed by stabilizing dioleoylphosphatidyl ethanolamine (DOPE) bilayers with folate-conjugated poly(hydroxyethyl acrylate-co-allyl methyl sulfide) (F-P(HEA-AMS)). The copolymer, synthesized by a free radical polymerization, was surface-active but lost its surface activity after AMS unit was oxidized by H2O2 treatment. The liposomes with F-P(HEA-AMS) were sensitive to H2O2 concentration (0%, 0.5%, 1.0%, and 2.0%) in terms of release, possibly because the copolymer lost its surface activity and its bilayer-stabilizing ability upon oxidation. Fluorescence-activated cell sorting (FACS) and confocal laser scanning microscopy (CLSM) revealed that doxorubicin (DOX)-loaded liposomes stabilized with folate-conjugated copolymers markedly promoted the transport of the anti-cancer drug to cancer cells. This was possible because the liposomes were readily translocated into the cancer cells via receptor-mediated endocytosis. This liposome would be applicable to the delivery carrier of anticancer drugs.

Krebs Cycle Intermediate-Modified Carbonate Apatite Nanoparticles Drastically Reduce Mouse Tumor Burden and Toxicity by Restricting Broad Tissue Distribution of Anticancer Drugs.

The morphology, size, and surface area of nanoparticles (NPs), with the existence of functional groups on their surface, contribute to the drug binding affinity, distribution of the payload in different organs, and targeting of a particular tumor for exerting effective antitumor activity in vivo. However, the inherent chemical structure of NPs causing unpredictable biodistribution with a toxic outcome still poses a serious challenge in clinical chemotherapy. In this study, carbonate apatite (CA), citrate-modified CA (CMCA) NPs, and α-ketoglutaric acid-modified CA (α-KAMCA) NPs were employed as carriers of anticancer drugs for antitumor, pharmacokinetic, and toxicological analysis in a murine breast cancer model. The results demonstrated almost five-fold enhanced tumor regression in the cyclophosphamide (CYP)-loaded α-KAMCA NP-treated group compared to the group treated with CYP only. Also, NPs promoted much higher drug accumulation in blood and tumor in comparison with the drug injected without a carrier. In addition, doxorubicin (DOX)-loaded NPs exhibited less accumulation in the heart, indicating less potential myocardial toxicity in mice compared to free DOX. Our findings, thus, conclude that CA, CMCA, and α-KAMCA NPs extended the circulation half-life and enhanced the anticancer effect with reduced toxicity of conventional chemotherapeutics in healthy organs, signifying that they are promising drug delivery devices in breast cancer treatment.

Safety and Short-term Efficacy of Licartin Combined with Conventional Transcatheter Hepatic Arterial Chemoembolization for Unresectable Hepatocellular Carcinoma

To evaluate the safety and short-term efficacy of Licartin combined with conventional transcatheterheaptic arterial chemoembolization for patients with unresectable hepatocellular carcinoma, 13 patients with unresectable primary liver cancer treated with Licartin combined with conventional transcatheter arterial chemoembolization at the First Affiliated Hospital from January 2012 to December 2014, were retrospectively analyzed. Licartin was infused via hepatic artery at a dose of 27.75 MBq/kg prior to conventional transcatheter arterial chemoembolization (pirarubicin 20 mg and iodized oil), supplemented with poly vinyl alcohol particles. Here, the iodized oil is used as an embolic agent and carrier of anticancer drugs. After entering into the small arteries and peritumoral sinusoid of hepatocellular carcinoma through a catheter, the iodized oil gets retained there to block the terminal blood flow. According to mRECIST evaluation criteria, the remission and control rates after 1, 3, 6, and 9 mo were 69.3 and 100; 69.3 and 84.6; 61.5 and 76.9 and 60 % and 80 %, respectively. The survival rate was 100 % after 6 mo. The 1 y and 2 y survival rates estimated with Life Tables were 68 and 45 %, respectively. Liver and kidney function showed no significant difference pre- and posttreatment. No serious infections, jaundice, gastrointestinal bleeding or bone marrow suppression occurred. Licartin combined with conventional transcatheter arterial chemoembolization showed short-term efficacy and minimal side-effects in patients afflicted with unresectable primary liver cancer. Long-term follow-up involving large cohorts is needed to determine the long-term efficacy of the intervention.

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.

Why nanodiamond carriers manage to overcome drug resistance in cancer.

Nanodiamonds represent an attractive potential carrier for anticancer drugs. The main advantages of nanodiamond particles with respect to medical applications are their high compatibility with non-cancerous cells, feasible surface decoration with therapeutic and cancer-cell targeting molecules, and their relatively low manufacturing cost. Additionally, nanodiamond carriers significantly increase treatment efficacy of the loaded drug, so anticancer drugs execute more effectively at a lower dose. Subsequently, lower drug dose results in less extensive side effects. The carriers decorated with a targeting molecule accumulate primarily in the tumor tissue, and those nanodiamond particles impair efflux of the drug from cancer cells. Therapeutic approaches considering nanodiamond carriers were already tested in vitro, as well as in vivo. Now, researchers focus particularly on the possible side effects of nanodiamond carriers applied systemically in vivo. The behavior of nanodiamond carriers depends heavily on their surface coatings, so each therapeutic complex must be evaluated separately. Generally, it seems that site-specific application of nanodiamond carriers is a rather safe therapeutic approach, but intravenous application needs further study. The benefits of nanodiamond carriers are remarkable and represent a potent approach to overcome the drug resistance of many cancers.

Near-infrared light and magnetic field dual-responsive porous silicon-based nanocarriers to overcome multidrug resistance in breast cancer cells with enhanced efficiency.

The development of drug delivery systems based on external stimuli-responsive nanocarriers is important to overcome multidrug resistance in breast cancer cells. Herein, iron oxide/gold (Fe3O4/Au) nanoparticles were first fabricated via a simple hydrothermal reaction, and subsequently loaded into porous silicon nanoparticles (PSiNPs) via electrostatic interactions to construct PSiNPs@(Fe3O4/Au) nanocomposites. The as-prepared PSiNPs@(Fe3O4/Au) nanocomposites exhibited excellent super-paramagnetism, photothermal effect, and T2-weight magnetic resonance imaging capability. In particular, with the help of a magnetic field, the cellular uptake of PSiNPs@(Fe3O4/Au) nanocomposites was significantly enhanced in drug-resistant breast cancer cells. Moreover, PSiNPs@(Fe3O4/Au) nanocomposites as carriers showed a high loading and NIR light-triggered release of anticancer drugs. Based on the synergistic effect of magnetic field-enhanced cellular uptake and NIR light-triggered intracellular release, the amount of anticancer drug carried by PSiNPs@(Fe3O4/Au) nanocarriers into the nuclei of drug-resistant breast cancer cells sharply increased, accompanied by improved chemo-photothermal therapeutic efficacy. Finally, PSiNPs@(Fe3O4/Au) nanocomposites under the combined conditions of magnetic field attraction and NIR light irradiation also showed improved anticancer drug penetration and accumulation in three-dimensional multicellular spheroids composed of drug-resistant breast cancer cells, leading to a better growth inhibition effect. Overall, the fabricated PSiNPs@(Fe3O4/Au) nanocomposites demonstrated great potential for the therapy of multidrug-resistant breast cancer in future.

Dietary fiber tragacanth gum based hydrogels for use in drug delivery applications

There is no doubt that fibers, in particular viscous dietary fibers, have positive effects on the human health, both in the prevention and in the treatment of chronic diseases. The present work explore the potential of dietary fiber tragacanth gum (TG) for developing hydrogels as drug carrier for anti-cancer drug ‘methotrexate’ to improve its pharmacokinetic deficiency due to nonspecific distribution and enhancing. Polymer matrix was characterized by SEMs, FTIR and XRD techniques. Release profile of drug was determined along with evaluation of some properties like blood compatibility, mucoadhesion and mechanical strength. The release profile occurred with non-Fickian diffusion mechanism and was best fitted in the Higuchi kinetic model. The polymer matrix was non-thrombogenic, haemo-compatible and mucoadhesive in nature. The hydrogels adhered to intestinal mucosa with 14.3 ± 4.5 mN force during mucoadhesion test.

Curcumin-loaded zeolite as anticancer drug carrier: effect of curcumin adsorption on zeolite structure

Abstract In this work we used a combination of different techniques to investigate the adsorption properties of curcumin by zeolite type A for potential use as an anticancer drug carrier. Curcumin is a natural water-insoluble drug that has attracted great attention in recent years due to its potential anticancer effect in suppressing many types of cancers, while showing a synergistic antitumor effect with other anticancer agents. However, curcumin is poorly soluble in aqueous solutions leading to the application of high drug dosage in oral formulations. Zeolites, inorganic crystalline aluminosilicates with porous structure on the nano- and micro-scale and high internal surface area, can be useful as pharmaceutical carrier systems to encapsulate drugs with intrinsic low aqueous solubility and improve their dissolution. Here, we explore the use of zeolite type A for encapsulation of curcumin, and we investigate its surface properties and morphology, before and after loading of the anticancer agent, using scanning electron microscopy (SEM), powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and UV-vis spectroscopy. Results are used to assess the loading efficiency of zeolite type A towards curcumin and its structural stability after loading.

PH-Sensitive, Polymer Functionalized, Nonporous Silica Nanoparticles for Quercetin Controlled Release.

Some pH-sensitive, poly(2-(diethylamino)ethyl methacrylate) (PDEAEMA) grafted silica nanoparticles (SNPs) (SNPs-g-PDEAEMA) were designed and synthesized via surface initiated, metal-free, photoinduced atom transfer radical polymerization (ATRP). The structures of the polymers formed in solution were determined by 1H NMR. The modified nanoparticles were characterized by FT-IR spectroscopy, XPS, GPC, TEM and TGA. The analytical results show that α-bromoisobutyryl bromide (BIBB) (ATRP initiator) had been successfully anchored onto SNPs’ surfaces, and was followed by surface-initiated, metal-free ATRP of 2-(diethylamino)ethyl methacrylate (DEAEMA). The resultant SNPs-g-PDEAEMA were uniform spherical nanoparticles with the particles size of about 22–25 nm, and the graft density of PDEAEMA on SNPs’ surfaces obtained by TGA was 19.98 μmol/m2. Owing to the covalent grafting of pH-sensitive PDEAEMA, SNPs-g-PDEAEMA can dispersed well in acidic aqueous solution, but poorly in neutral and alkaline aqueous solutions, which is conducive to being employed as drug carriers to construct a pH-sensitive controlled drug delivery system. In vitro cytotoxicity evaluation results showed that the cytotoxicity of SNPs-g-PDEAEMA to the L929 cells had completely disappeared on the 3rd day. The loading of quercetin on SNPs-g-PDEAEMA was performed using adsorption process from ethanol solutions, and the dialysis release rate increased sharply when the pH value of phosphate-buffered saline (PBS) decreased from 7.4 to 5.5. All these results indicated that the pH-responsive microcapsules could serve as potential anti-cancer drug carriers.

<p>Hexagonal Boron Nitrides (White Graphene): A Promising Method for Cancer Drug Delivery</p>

Advances in low-dimensions nanomaterials drug-carrier have rapidly translated into clinical practice. Interestingly, the two-dimensional (2D) nanomaterials of hexagonal boron nitride (h-BN), so-called “white graphite” are relatively less explored compared to the post popular 2D graphene oxide (GO). However, the unique properties of h-BN nanomaterials make them well suited for the delivery of chemotherapeutic in cancer treatment. Recent studies have shown that the h-BN is a potential candidate in biomedical sciences, both as nanocarriers and nano-transducers. In this review, we discuss the various physicochemical properties and important concepts involved in h-BN nanosheets as anticancer drug carriers.

3D printed biodegradable implants as an individualized drug delivery system for local chemotherapy of osteosarcoma

A 3D printing technique has been developed which enables the treatment of osteosarcoma via personalized local chemotherapy. A series of in vivo trials were conducted which closely mimicked real clinical chemotherapeutic conditions. We have shown that 3D printed poly L-lactic acid (PLLA) implants are exceptional carriers for anticancer drugs and can be designed with finely tuned physical morphologies and controllable micropore structures. Their favorable biodegradability, in vitro cytotoxicity, in vitro blood compatibility, in vivo subacute toxicity, and in vivo sensitization tests have confirmed their biocompatibility and pharmaceutical properties. Furthermore, we have demonstrated that local chemotherapy with the assistance of the as-prepared PLLA implant exhibits an anti-osteosarcoma efficacy superior to traditional chemotherapy through a series of in vivo anti-osteosarcoma tests according to clinical protocols. The proposed 3D printed drug delivery system can simultaneously realize individual local chemotherapy, multi-drug delivery, long-term sustainable drug release, and non-reoperation in osteosarcoma treatment. Our studies enable the utilization of the 3D printing technique in the treatment of osteosarcomas and guide future clinical trials. The established techniques and principles can also be adapted to the local chemotherapy of other tumors.

Chemically Modified Carbon Nanohorns as Nanovectors of the Cisplatin Drug: A Molecular Dynamics Study.

Carbon nanohorns (CNH) have been considered potential anticancer drug carriers, such as the cisplatin drug (cddp), due to their low toxicity, high purity, drug-loading capacity, and biodegradation routes. However, when it comes to nanomedicine applications, chemical functionalization is an essential step in order to overcome undesirable properties of these nanomaterials, such as the high hydrophobicity, low reactivity, and low dispersibility in polar solvents. In this context, the present study involved the modeling of new CNH topologies based on chemical oxidation and reduction mechanisms and the investigation of the influence of these modified structures on the dynamics and stability of inclusion complexes with cddp. The results indicated that these functionalization strategies lead to the opening of nanowindows on the CNH surfaces, which would constitute the main route for drug release, as reported by experimentalists. Also, our results showed that the insertion of polar functional groups on the oxidized CNH (CNHox-N) contributed to an improvement of the cddp@CNHox-N biocompatibility due to the greater number of hydrogen bonds formed with the solvent. Despite the favorable formation of all complexes, the binding free energies pointed out that the oxidation process made the cddp@CNHox-N complexes slightly less stable than the ones with pristine and reduced CNH. Besides, the results suggest the possibility to tune the complex stability by controlling the oxidation degree, which could be explored by the experimentalists in order to design controlled drug delivery systems based on CNH nanocarriers.

Targeted Delivery Prodigiosin to Choriocarcinoma by Peptide-Guided Dendrigraft Poly-l-lysines Nanoparticles.

The available and effective therapeutic means to treat choriocarcinoma is seriously lacking, mainly due to the toxic effects caused by chemotherapy and radiotherapy. Accordingly, we developed a method for targeting delivery of chemotherapeutical drugs only to cancer cells, not normal cells, in vivo, by using a synthetic placental chondroitin sulfate (CSA)-binding peptide (plCSA-BP) derived from malarial protein VAR2CSA. A 28 amino acids placental CSA-binding peptide (plCSA-BP) from the VAR2CSA was synthesized as a guiding peptide for tumor-targeting delivery, dendrigraft poly-L-lysines (DGL) was modified with plCSA-BP and served as a novel targeted delivery carrier. Choriocarcinoma was selected to test the effect of targeted delivery carrier, and prodigiosin isolated from Serratia marcescens subsp. lawsoniana was selected as a chemotherapeutical drug and encapsulated in the DGL modified by the plCSA-BP nanoparticles (DGL/CSA-PNPs). DGL/CSA-PNPs had a sustained slow-release feature at pH 7.4, which could specifically bind to the JEG3 cells and exhibited better anticancer activity than that of the controls. The DGL/CSA-PNPs induced the apoptosis of JEG3 cells through caspase-3 and the P53 signaling pathway. DGL/CSA-PNPs can be used as an excellent targeted delivery carrier for anticancer drugs, and the prodigiosin could be an alternative chemotherapeutical drug for choriocarcinoma.

One-step fabrication of low cytotoxic anisotropic poly(2-hydroxyethyl methacrylate-co-methacrylic acid) particles for efficient release of DOX

Herein, we report a one-step process of distillation precipitation polymerization (DPP) to fabricate anisotropic particles in which no stabilizing agent is used. This method is based on in situ crosslinking of poly(2-hydroxyethyl methacrylate-co-methacrylic acid) random copolymers with variety of feed composition that determine morphology of resultant particles. As a result, variation of feed composition led to formation of spherical, spherical with a lobe and a lobed spherical (multiple lobes) particles. These morphologies are discussed according to thermodynamics of colloids and polymerization-induced phase separation. As one of the most important applications, selected morphologies are used as carriers of anti-cancer DOX drug. Results showed high drug loading amount for all carriers those released DOX significantly at pH = 1 whereas no mentionable release was observed at pH = 7.4. Also, release profiles were fitted by well-known mathematical models to understand kinetics of release. Finally, cytotoxicity of carriers are measured by an MTT assay that showed all carriers are biocompatible whereas DOX-loaded particles were significantly cytotoxic.

Covalent triazine-based polyimine framework as a biocompatible pH-dependent sustained-release nanocarrier for sorafenib: An in vitro approach

In the present study, a novel polyimine-based covalent triazine framework (PI-CTF) was introduced as a promising biocompatible carrier for sorafenib (SFN) delivery. High specific surface area and porosity allowed us to achieve drug loading and encapsulation efficiency as high as 83% and 98%, respectively. The in vitro drug release study of SFN-loaded PI-CTF showed a sustained and pH-dependent release behavior in which acidic pH accelerated drug release compared with the neutral pH. Notably, cytotoxicity assay against L929 cells revealed the safety and biocompatibility of PI-CTF. Moreover, MTT assay against LNCaP prostate cancer cells expressed that the anticancer activity of SFN had no diminution after incorporating into PI-CTF. Thus, PI-CTF has envisaged as a great promise toward anti-cancer drug carrier.

Stereocomplexed micelles based on polylactides with β-cyclodextrin core as anti-cancer drug carriers

Biocompatible and biodegradable stereocomplexed micelles (SCMs) based on polylactides (PLAs) with β-cyclodextrin (β-CD) core were designed and used as efficient intracellular drug carriers. The micelles formation, stability and drug release behavior of enantiomeric and stereocomplexed micelles with β-CD core were systematically investigated in comparison to the micelles composed of PLAs with dipentaerythritol (DPE) core. The presence of β-CD core allows for the formation of inclusion complex with a model anticancer drug: doxorubicin (DOX), whereas stereocomplexation between PLLA and PDLA enhanced the stability of obtained micelles. By the utility of different supramolecular interactions, we were able to control the release of DOX from obtained micelles. The release tests of DOX from supramolecular nanocarriers showed that DOX release changes in the order of DPE core micelles >β-CD core micelles >SCMs. The antitumor activities of the enantiomeric and stereocomplexed micelles toward HeLa (cervical cancer) and K562 (chronic myelogenous leukemia) cells were tested in vitro. Our data demonstrated that the SCMs/DOX more effectively inhibited the cell proliferation than similar enantiomeric micelles and for the highest concentration of DOX inside the SCMs. Most importantly, micelles were more efficient than free DOX. In summary, the supramolecular interactions can provide a favourable tool to construct a drug delivery system with controlled drug release and efficient tumor cell suppression which is beneficial for cancer therapy.