Targeted Anticancer Drug Delivery Research Articles

Phenylboronic Acid-Modified pH/Glucose Dual-Responsive Polymeric Micelles for Targeted Anticancer Drug Delivery

Phenylboronic Acid-Modified pH/Glucose Dual-Responsive Polymeric Micelles for Targeted Anticancer Drug Delivery

ROS-Responsive Self-Degradable DNA Nanogels for Targeted Anticancer Drug Delivery.

Here, a reactive oxygen species (ROS)-responsive targeted anticancer drug delivery system was developed by embedding a nitrophenyl tetramethyl-dioxaborolanyl benzyl carbamate (NBC)-modified deoxyribonuclease I (DNase I) in a DNase-degradable aptamer-based DNA nanogel. The DNA nanogel was formed by hybridization of three types of building blocks, namely, Y-shaped monomer 1 with three sticky ends, Y-shaped monomer 2 with two sticky ends and an aptamer end, and a DNA linker with two sticky ends. Single doxorubicin (DOX) or ribonuclease A (RNase A) as well as the combination of DOX and RNase A were effectively loaded into the nanogels, wherein DOX was embedded into DNA skeleton, while RNase A was encapsulated into nanogel matrix. The blocked enzymatic activity of DNase I due to NBC modification could be restored upon intracellular ROS-triggered NBC deprotection, resulting in self-degradation of the nanogels to release both DOX and RNase A. Consequently, the DOX and RNase A coloaded nanogels significantly inhibited the proliferation of MCF-7 cells through a synergistic effect. To sum up, this DNA-based drug delivery system with ROS-responsive self-degradation properties should be promising for application in targeted and synergistic cancer therapy.

Targeted Anticancer Drug Delivery Using Chitosan, Carbon Quantum Dots, and Aptamers to Deliver Ganoderic Acid and 5-Fluorouracil.

Breast cancer is a malignancy that affects mostly females and is among the most lethal types of cancer. The ligand-functionalized nanoparticles used in the nano-drug delivery system offer enormous potential for cancer treatments. This work devised a promising approach to increase drug loading efficacy and produce sustained release of 5-fluorouracil (5-FU) and Ganoderic acid (GA) as model drugs for breast cancer. Chitosan, aptamer, and carbon quantum dot (CS/Apt/COQ) hydrogels were initially synthesized as a pH-sensitive and biocompatible delivery system. Then, CS/Apt/COQ NPs loaded with 5-FU-GA were made using the W/O/W emulsification method. FT-IR, XRD, DLS, zeta potentiometer, and SEM were used to analyze NP's chemical structure, particle size, and shape. Cell viability was measured using MTT assays in vitro using the MCF-7 cell lines. Real-time PCR measured cell apoptotic gene expression. XRD and FT-IR investigations validated nanocarrier production and revealed their crystalline structure and molecular interactions. DLS showed that nanocarriers include NPs with an average size of 250.6 nm and PDI of 0.057. SEM showed their spherical form, and zeta potential studies showed an average surface charge of +37.8 mV. pH 5.4 had a highly effective and prolonged drug release profile, releasing virtually all 5-FU and GA in 48 h. Entrapment efficiency percentages for 5-FU and GA were 84.7±5.2 and 80.2 %±2.3, respectively. The 5-FU-GA-CS-CQD-Apt group induced the highest cell death, with just 57.9 % of the MCF-7 cells surviving following treatment. 5-FU and GA in CS-CQD-Apt enhanced apoptotic induction by flow cytometry. 5-FU-GA-CS-CQD-Apt also elevated Caspase 9 and downregulated Bcl2. Accordingly, the produced NPs may serve as pH-sensitive nano vehicles for the controlled release of 5-FU and GA in treating breast cancer.

Green synthesis of magnetic Fe3O4 nanoparticles (MNPs) using plant extract and Biomedicine Applications: Targeted Anticancer Drug Delivery System

Sekarang, nanosains memberikan dasar ilmiah dan pemahaman tentang sifat dan perilaku materi pada skala nanometer (ukuran » 1-100 nm), adapun nanoteknologi adalah terapan nanosain untuk merancang dan menciptakan struktur serta perangkat baru dengan ukuran nanometer. Bagian penting dari hal tersebut adalah bagaimana membuat material dengan ukuran skala nano (e.i: nanopartikel), berbagai metode sudah dikembangkan baik secara top-down maupun bottom-up. Metode yang paling sederhana adalah secara bottom-up, melakukan fabrikasi dengan menyusun atom demi atom. Untuk metode ini yang paling ramah lingkungan adalah dengan metode green synthesis, dengan memanfaatkan ekstraksi tanaman. Di Indonesia memiliki keunggulan dengan keragaman aneka tanaman yang sangat banyak. Pada studi ini akan ditunjukan bahwa untuk membuat material magnetic, seperti magnetic nanopartikel Fe3O4 (MNPs) yang dapat disintesis dengan mudah dengan menggunakan aneka ektraski tanaman seperti: biji jinten (Syzygium cumini seed), kulit delima (Punica Granatum rind), bunga api-api putih (Avicennia marina flower), akar Chromolaena Odorata, daun Thunbergia Grandiflora, buah Couroupita Guianensis Aubl., dan daun Moringa Oleifera. Pada bidang biomedis khususnya untuk deteksi penyakit, pengiriman obat yang terkontrol. Nanopartikel pengiriman obat harus terutama dapat terdegradasi dan kompatibel dengan organisme. Hasil studi menunjukan MNPs memiliki potensi untuk mengubah secara total metode diagnostik dan terapi klinis, dan ini sangat menarik perhatian. Dan yang terbaru antara lain transfeksi yang ditingkatkan secara magnetik, terapi gen yang dibantu secara magnetik, hipertermia yang diinduksi secara magnetik, dan rekayasa jaringan berdasarkan gaya magnetic.
 Kata Kunci: Magnetik Nanopartikel (Fe3O4), Green synthesis, DDS, teranostik kanker, terapi genetik
 Abstract
 Today, Nanoscience provides the scientific basis and understanding of the properties and behavior of matter at the nanometer scale (size » 1-100 nm). At the same time, nanotechnology is the application of Nanoscience to design and create new structures and devices with nanometer size. An essential part of this is making materials with nanoscale sizes (e.g., nanoparticles); various methods have been developed both top-down and bottom-up. The simplest method is bottom-up, fabricating by assembling atom by atom. For this method, the most environmentally friendly is the green synthesis method, by utilizing plant extraction. Indonesia has an advantage with a vast diversity of various plants. This study will show that to make magnetic materials, such as magnetic nanoparticles Fe3O4 (MNPs), which can be synthesized easily using various plant extracts such as cumin seeds (Syzygium cumin seed), pomegranate peel (Punica Granatum rind), sparks. white (Avicennia marina flower), Chromolaena odorata root, Thunbergia Grandiflora leaf, Couroupita guianensis Aubl. fruit, and Moringa oleifera leaf. In the biomedical field, especially for disease detection, controlled drug delivery. Drug delivery nanoparticles must be primarily degradable and compatible with organisms. The study results show that MNPs have the potential to change clinical diagnostic and therapeutic methods completely, and this is of great interest. Moreover, recent ones include magnetically enhanced transfection, assisted gene therapy, magnetically induced hyperthermia, and magnetic force-based tissue engineering.
 Keywords: Magnetic Nanoparticles (Fe3O4), Green synthesis, DDS, cancer diagnostics, genetic therapy

Efficient Preparation of a Magnetic Helical Carbon Nanomotor for Targeted Anticancer Drug Delivery.

The applications of nanomotors in the biomedical field have been attracting extensive attention. However, it remains a challenge to fabricate nanomotors in a facile way and effectively load drugs for active targeted therapy. In this work, we combine the microwave heating method and chemical vapor deposition (CVD) to fabricate magnetic helical nanomotors efficiently. The microwave heating method can accelerate intermolecular movement, which converts kinetic energy into heat energy and shortens the preparation time of the catalyst used for carbon nanocoil (CNC) synthesis by 15 times. Fe3O4 nanoparticles are in situ nucleated on the CNC surface by the microwave heating method to fabricate magnetically driven CNC/Fe3O4 nanomotors. In addition, we achieved precise control of the magnetically driven CNC/Fe3O4 nanomotors through remote manipulation of magnetic fields. Anticancer drug doxorubicin (DOX) is then efficiently loaded onto the nanomotors via π-π stacking interactions. Finally, the drug-loaded CNC/Fe3O4@DOX nanomotor can accurately accomplish cell targeting under external magnetic field control. Under short-time irradiation of near-infrared light, DOX can be quickly released onto target cells to effectively kill the cells. More importantly, CNC/Fe3O4@DOX nanomotors allow for single-cell or cell-cluster-targeted anticancer drug delivery, providing a dexterous platform to potentially perform many medically relevant tasks in vivo. The efficient preparation method and application in drug delivery are beneficial for future industrial production and provide inspiration for advanced micro/nanorobotic systems using the CNC as a carrier for a wide range of biomedical applications.

Doxorubicin-Gelatin/Fe3O4-Alginate Dual-Layer Magnetic Nanoparticles as Targeted Anticancer Drug Delivery Vehicles.

In this study, magnetic nanoparticles composed of a core (doxorubicin–gelatin) and a shell layer (Fe3O4–alginate) were developed to function as targeted anticancer drug delivery vehicles. The anticancer drug doxorubicin (DOX) was selected as a model drug and embedded in the inner gelatin core to obtain high encapsulation efficiency. The advantage of the outer magnetic layer is that it targets the drug to the tumor tissue and provides controlled drug release. The physicochemical properties of doxorubicin–gelatin/Fe3O4–alginate nanoparticles (DG/FA NPs) were characterized using scanning electron microscopy, Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction. The mean diameter of DG/FA NPs, which was determined using a zeta potential analyzer, was 401.8 ± 3.6 nm. The encapsulation rate was 64.6 ± 11.8%. In vitro drug release and accumulation were also studied. It was found that the release of DOX accelerated in an acidic condition. With the manipulation of an external magnetic field, DG/FA NPs efficiently targeted Michigan Cancer Foundation-7 (MCF-7) breast cancer cells and showed in the nucleus after 6 h of incubation. After 12 h of incubation, the relative fluorescence intensity reached 98.4%, and the cell viability of MCF-7 cells decreased to 52.3 ± 4.64%. Dual-layer DG/FA NPs could efficiently encapsulate and deliver DOX into MCF-7 cells to cause the death of cancer cells. The results show that DG/FA NPs have the potential for use in targeted drug delivery and cancer therapy.

Folate and Pegylated Aliphatic Polyester Nanoparticles for Targeted Anticancer Drug Delivery.

PurposeThe use of chemotherapeutic agents to combat cancer is accompanied by high toxicity due to their inability to discriminate between cancer and normal cells. Therefore, cancer therapy research has focused on the targeted delivery of drugs to cancer cells. Here, we report an in vitro study of folate-poly(ethylene glycol)-poly(propylene succinate) nanoparticles (FA-PPSu-PEG-NPs) as a vehicle for targeted delivery of the anticancer drug paclitaxel in breast and cervical cancer cell lines.MethodsPaclitaxel-loaded-FA-PPSu-PEG-NPs characterization was performed by in vitro drug release studies and cytotoxicity assays. The NPs cellular uptake and internalization mechanism were monitored by live-cell imaging in different cancer cell lines. Expression of folate receptor-α (FOLR1) was examined in these cell lines, and specific FOLR1-mediated entry of the FA-PPSu-PEG-NPs was investigated by free folic acid competition. Using inhibitors for other endocytic pathways, alternative, non-FOLR1 dependent routes for NPs uptake were also examined.ResultsDrug release experiments of Paclitaxel-loaded PPSu-PEG-NPs indicated a prolonged release of Paclitaxel over several days. Cytotoxicity of Paclitaxel-loaded PPSu-PEG-NPs was similar to free drug, as monitored in cancer cell lines. Live imaging of cells treated with either free Paclitaxel or Paclitaxel-loaded PPSu-PEG-NPs demonstrated tubulin-specific cell cycle arrest, with similar kinetics. Folate-conjugated NPs (FA-PPSu-PEG-NPs) targeted the FOLR1 receptor, as shown by free folic acid competition of the FA-PPSu-PEG-NPs cellular uptake in some of the cell lines tested. However, due to the differential expression of FOLR1 in the cancer cell lines, as well as the intrinsic differences between the different endocytic pathways utilized by different cell types, other mechanisms of nanoparticle cellular entry were also used, revealing that dynamin-dependent endocytosis and macropinocytosis pathways mediate, at least partially, cellular entry of the FA-PPSu-PEG NPs.ConclusionOur data provide evidence that Paclitaxel-loaded-FA-PPSu-PEG-NPs can be used for targeted delivery of the drug, FA-PPSu-PEG-NPs can be used as vehicles for other anticancer drugs and their cellular uptake is mediated through a combination of FOLR1 receptor-specific endocytosis, and macropinocytosis. The exploration of the different cellular uptake mechanisms could improve treatment efficacy or allow a decrease in dosage of anticancer drugs.

REDOX Responsive Fluorescence Active Glycopolymer Based Nanogel: A Potential Material for Targeted Anticancer Drug Delivery.

A well-defined glycopolymer based fluorescence active nanogel has been prepared via the combination of reversible addition-fragmentation chain transfer (RAFT) polymerization and Diels-Alder (DA) "click" chemistry. To prepare the nanogel, initially, a functional AB block copolymer (BCP) poly(pentafluorophenyl acrylate)-b-poly(furfuryl methacrylate) (PPFPA-b-PFMA), having activated pentafluorophenyl ester group, was synthesized via RAFT polymerization. The activated pentafluorophenyl functionality was replaced by the amine functionality of glucosamine to introduce the amphiphilic BCP poly[2-(acrylamido) glucopyranose]-b-poly(furfuryl methacrylate) (PAG-b-PFMA). Furthermore, the terminal acid (-COOH) functionality of the RAFT agent was modified by gelatin QDs (GQDs) to generate fluorescence active glycopolymer. An anticancer drug, Doxorubicin, was loaded in the micelle via the successive addition of the drug molecule and cross-linking using dithio-bismaleimidoethane (DTME), a REDOX responsive cross-linker. The anticancer activity of the drug loaded nanogel was observed over MBA-MD-231, human breast cancer cell line, and monitored via fluorescence spectroscopy and flow cytometric analyses (FACS). The cytotoxicity of the prepared glycopolymer based nanogel over the MBA-MD-231 cell line was assessed via MTT assay test, and it was observed that the synthesized nanogel was noncytotoxic in nature.

Hyaluronic Acid-Decorated Laponite® Nanocomposites for Targeted Anticancer Drug Delivery.

In this study, hyaluronic acid (HA), a natural polysaccharide that can specifically bind to CD44 receptors, was conjugated onto laponite® (LAP) nanodisks for the encapsulation and specific delivery of the anti-cancer drug doxorubicin (DOX) to CD44-overexpressed cancer cells. The prepared LM-HA could encapsulate DOX efficiently and release drug in a continuous manner with pH-responsiveness. In vitro cell viability assay proved that LM-HA had good biocompatibility, and drug-loaded LM-HA/DOX exhibited targeted anti-tumor effects against HeLa cells with CD44 receptors overexpressed. In addition, the flow cytometric detection and confocal laser scanning microscope results confirmed that LM-HA/DOX could be specifically internalized by HeLa cells via CD44-mediated endocytosis. Therefore, the HA-modified LAP nanodisks with high drug loading efficiency, pH-sensitive drug release properties and CD44 targetability might be an efficient nanoplatform for cancer chemotherapy.

PH-Responsive Polycarbonate Copolymer-based Nanoparticles for Targeted Anticancer Drug Delivery

A smart polycarbonate(PCA) copolymer-based nanoparticle(NanoPCA) with pH-responsive, long-term stability, and tumor targeting ability was successfully developed by synthesizing and assembling a series of functional PCA-based copolymers including poly(2-amino-1,3-propanediol carbonate-co-L-lactide)[P(CA-co-LA)], poly(2-amino-1,3-propanediol carbonate-co-L-lactide)-g-methoxy-poly(ethylene glycol)[P(CA-co-LA)-g-MPEG], and poly(2-amino-1,3-propanediol carbonate-co-L-lactide)-g-poly(ethylene glycol)-cyclic(Arg-Gly-Asp-D-Phe-Lys) [P(CA-co-LA)-g-PEG-cRGD] for targeted anticancer drug delivery. pH-Responsive studies demonstrated that the loading doxorubicin(DOX) released faster from NanoPCA at acidic conditions due to protonation effects of P(CA-co-LA) copolymers. Furthermore, the in vitro and in vivo investigations demonstrate that the DOX-loaded NanoPCA exhibited significant tumor targeting ability, outstanding antitumor effect and excellent biological safety in the treatment of oral squamous cell carcinoma(OSCC). Therefore, this work provides a promising drug delivery platform for cancer therapy and other applications.

Nanoparticle Optimization for Enhanced Targeted Anticancer Drug Delivery.

Nanoparticle (NP)-based drug delivery is a promising method to increase the therapeutic index of anticancer agents with low median toxic dose. The delivery efficiency, corresponding to the fraction of the injected NPs that adhere to the tumor site, depends on NP size a and aspect ratio AR. Values for these variables are currently chosen empirically, which may not result in optimal targeted drug delivery. This study applies rigorous optimization to the design of NPs. A preliminary investigation revealed that delivery efficiency increases monotonically with a and AR. However, maximizing a and AR results in nonuniform drug distribution, which impairs tumor regression. Therefore, a multiobjective optimization (MO) problem is formulated to quantify the trade-off between NPs accumulation and distribution. The MO is solved using the derivative-free mesh adaptive direct search algorithm. Theoretically, the Pareto-optimal set consists of an infinite number of mathematically equivalent solutions to the MO problem. However, interesting design solutions can be identified subjectively, e.g., the ellipsoid with a major axis of 720 nm and an aspect ratio of 7.45, as the solution closest to the utopia point. The MO problem formulation is then extended to optimize NP biochemical properties: ligand-receptor binding affinity and ligand density. Optimizing physical and chemical properties simultaneously results in optimal designs with reduced NP sizes and thus enhanced cellular uptake. The presented study provides an insight into NP structures that have potential for producing desirable drug delivery.

Multiresponsive Nanogels for Targeted Anticancer Drug Delivery.

Nanogels with a biomolecular coating (biocoating) were shown to be capable of triggered delivery of anticancer drug Doxorubicin. The biocoating was formed utilizing binding between glycogen and the tetra-functional lectin Concanavalin A, which can be triggered to disassemble (and release) upon exposure to glucose and changes in solution pH. We also show the nanogel's thermoresponsivity can be used to accelerate Doxorubicin release. Moreover, we showed that transferrin immobilized on the nanogel surface could accelerate nanogel uptake by cancer cells. In these experiments, we showed that Doxorubicin was able to be released to the nucleus of human liver cancer cell line (HepG2) within 3 h. Doxorubicin-loaded nanogels exhibit a strong growth inhibition ability toward HepG2. This investigation showcases how nanogel design and chemistry can be tuned to achieve useful biomedical applications.

Carbon Dots Embedded Magnetic Nanoparticles @Chitosan @Metal Organic Framework as a Nanoprobe for pH Sensitive Targeted Anticancer Drug Delivery.

Recently, nanoscale metal organic frameworks (NMOFs) have been demonstrated as a promising carrier for drug delivery, as they possess many advantages like large surface area, high porosity, and tunable functionality. However, there are no reports about the functionalization of NMOFs, which combines cancer-targeted drug delivery/imaging, magnetic property, high drug loading content, and pH-sensitive drug release into one system. Existing formulations for integrating target molecules into NMOF are based on multistep synthetic processes. However, in this study, we report an approach that combines NMOF (IRMOF-3) synthesis and target molecule (Folic acid) encapsulation on the surface of chitosan modified magnetic nanoparticles in a single step. A noticeable feature of chitosan is control and pH responsive drug release for several days. More importantly, doxorubicin (DOX) was incorporated into magnetic NMOF formulation and showed high drug loading (1.63 g DOX g(-1) magnetic NMOFs). To demonstrate the optical imaging, carbon dots (CDs) are encapsulated into the synthesized magnetic NMOF, thereby endowing fluorescence features to the nanoparticles. These folate targeted magnetic NMOF possess more specific cellular internalization toward folate-overexpressed cancer (HeLa) cells in comparison to normal (L929) cells.

Drug Delivery: Silica Nanopills for Targeted Anticancer Drug Delivery (Small 36/2015)

Drug Delivery: Silica Nanopills for Targeted Anticancer Drug Delivery (Small 36/2015)

Cisplatin-Induced Formation of Biocompatible and Biodegradable Polypeptide-Based Vesicles for Targeted Anticancer Drug Delivery.

Novel cisplatin (CDDP)-loaded, polypeptide-based vesicles for the targeted delivery of cisplatin to cancer cells have been prepared. These vesicles were formed from biocompatible and biodegradable maleimide-poly(ethylene oxide)114-b-poly(L-glutamic acid)12 (Mal-PEG114-b-PLG12) block copolymers upon conjugation with the drug itself. CDDP conjugation forms a short, rigid, cross-linked, drug-loaded, hydrophobic block in the copolymer, and subsequently induces self-assembly into hollow vesicle structures with average hydrodynamic diameters (Dh) of ∼ 270 nm. CDDP conjugation is critical to the formation of the vesicles. The reactive maleimide-PEG moieties that form the corona and inner layer of the vesicles were protected via formation of a reversible Diels-Alder (DA) adduct throughout the block copolymer synthesis so as to maintain their integrity. Drug release studies demonstrated a low and sustained drug release profile in systemic conditions (pH = 7.4, [Cl(-)] = 140 mM) with a higher "burst-like" release rate being observed under late endosomal/lysosomal conditions (pH = 5.2, [Cl(-)] = 35 mM). Further, the peripheral maleimide functionalities on the vesicle corona were conjugated to thiol-functionalized folic acid (FA) (via in situ reduction of a novel bis-FA disulfide, FA-SS-FA) to form an active targeting drug delivery system. These targeting vesicles exhibited significantly higher cellular binding/uptake into and dose-dependent cytotoxicity toward cancer cells (HeLa) compared to noncancerous cells (NIH-3T3), which show high and low folic acid receptor (FR) expression, respectively. This work thus demonstrates a novel approach to polypeptide-based vesicle assembly and a promising strategy for targeted, effective CDDP anticancer drug delivery.

Silica Nanopills for Targeted Anticancer Drug Delivery.

Multifunctional SiO2 microtubes for targeted drug delivery are produced with precise control over shape and size by combining lithography and electrochemical etching. The hollow core is loaded with a lipophilic anticancer drug generating nanopills and an antibody is conjugated to the external surface for cancer cell targeting. Results demonstrate selective killing of neuroblastoma cells that express the cognate receptor.

Cover Picture: Intracellular Reduction‐Responsive Sheddable Copolymer Micelles for Targeted Anticancer Drug Delivery (Asian J. Org. Chem. 3/2015)

Cover Picture: Intracellular Reduction‐Responsive Sheddable Copolymer Micelles for Targeted Anticancer Drug Delivery (Asian J. Org. Chem. 3/2015)

Intracellular Reduction‐Responsive Sheddable Copolymer Micelles for Targeted Anticancer Drug Delivery

AbstractIntracellular, reduction‐responsive, amphiphilic, copolymer micelles with cancer cell specificity were developed. The copolymer was prepared with controlled molecular weight and functionalities using a double‐headed initiator consisting of a disulfide linkage and folic acid targeting unit. The polymer could self‐assemble into spherical micelles, which were stable under physiological conditions. Anticancer drug doxorubicin (DOX) was encapsulated into the micelles during the micellization and then released rapidly into the environment under the stimulus of intracellular reducing agent glutathione. Flow cytometry and confocal laser scanning microscopy observations further indicated that DOX was successfully released from the internalized micelles into the cytoplasm, inducing apoptosis and cell death. The potential of the present copolymer micelles for application as anticancer drug carriers for targeted cancer therapy is promising.

EPR-effect: Utilizing size-dependent Nanoparticle Delivery to Solid Tumors

EPR-effect: Utilizing size-dependent Nanoparticle Delivery to Solid Tumors

Polymer Micelle with pH-Triggered Hydrophobic–Hydrophilic Transition and De-Cross-Linking Process in the Core and Its Application for Targeted Anticancer Drug Delivery

In this study, an novel amphiphilic block copolymer P[PEGMA-b-(DEMA-co-APMA)]-FA and its cross-linker uracil-(CH2)6-uracil (U-(CH2)6-U) were synthesized and used as the targeted and pH-responsive nanocarriers for anticancer drug delivery. The hydrophobic block of the copolymer contains adenine (A) and tertiary amine moieties and the hydrophilic block is terminated with a targeting ligand folic acid (FA). Under neutral pH, the hydrophobic chain segments of the copolymer are cross-linked by U-(CH2)6-U through the A-U nucleobase pairing based on complementary multiple hydrogen bonding, and the copolymer forms stable micelles with their mean diameter of around 170 nm in water. While under acidic pH, the micelles dissociate as a result of protonation of tertiary amines and disruption of the A-U nucleobase pairing. Flow cytometry and fluorescent microscope observation show that, when loaded with an anticancer drug DOX, the micelles can preferably enter folate receptor (FR)-positive cancer cells and kill the cells via intracellular release of the anticancer drug. Cytotoxicity tests (MTT tests) indicate that the micelles with FA on their surfaces exhibit higher cytotoxicity toward FR-positive cells than those without FA. This study provides useful insights on designing and improving the applicability of copolymer micelles for other targeted drug delivery systems.