Cancer-targeted Drug Delivery Research Articles

Cancer targeted drug delivery using active low-density lipoprotein nanoparticles encapsulated pyrimidines heterocyclic anticancer agents as microtubule inhibitors

Recently, nanomedicine had the potential to increase the delivery of active compounds to specific cell sites. Nano-LDL particles are recognized as an excellent active nano-platform for cancer-targeted delivery. Loading of therapeutic agents into nano-LDL particles achieved by surface loading, core loading, and apolipoprotein-B100 interaction. Therefore, loading nano-LDL particles’ core with pyrimidine heterocyclic anticancer agents will increase cancer cytotoxic activity targeting tubulin protein. First, by mimicking the native LDL particle's metabolic pathway, and second the agent’s chemical functional groups like the native amino acids cytosine and thymine structures will not be recognized as a foreign entity from the cell’s immune system. Nano-LDL particles will internalize through LDL-receptors endocytosis and transport the anticancer agent into the middle of the cancer cell, reducing its side effects on other healthy cells. Generally, the data revealed that pyrimidine heterocyclic anticancer agents’ size is at the nano level. Agents’ morphological examination showed nanofibers, thin sheets, clusters, and rod-like structures. LDL particles’ size became bigger after loading with pyrimidine heterocyclic anticancer agents and ranged between 121.6 and 1045 nm. Then, particles were tested for their cytotoxicity against breast (MDA468) and prostate (DU145) cancer cell lines as surrogate models with dose-response study 10, 5, 1 µM. The IC50 values of the agents against DU145 and MDA468 possessed cell growth inhibition even at the 1 µM concentration ranges of 3.88 ± 1.05 µM and 3.39 ± 0.97 µM, respectively. In sum, nano-LDL particles proved their efficiency as active drug delivery vehicles to target tubulin in cancer cells.

Folic Acid Enables Targeting Delivery of Lipodiscs by Circumventing IgM-Mediated Opsonization.

Folic acid (FA) is one of the most widely utilized small-molecule ligands for cancer targeted drug delivery. Natural IgM was recently found to avidly absorb on the surface of FA-functionalized liposomes (FA-sLip), negatively regulating the in vivo performance by efficiently activating complement. Herein, FA-functionalized lipodiscs (FA-Disc) were constructed to successfully circumvent IgM-mediated opsonization and retained binding activity with folate receptors in vivo. The FA moiety along with the bound IgM was restricted to the highly curved rim of lipodiscs, leading to IgM incapability of presenting the membrane-bound conformation to trigger complement activation. The C1q docking, C3 binding, and C5a release were blocked and accelerated blood clearance phenomenon was mitigated of FA-Disc. FA-Disc retained folate binding activity and could effectively target folate receptor positive tumors in vivo. The present study provides a useful solution to avoid the negative regulation by IgM and achieve FA-enabled targeting by exploring disc-shaped nanocarriers.

Ultrasound and Nanomedicine for Cancer-Targeted Drug Delivery: Screening, Cellular Mechanisms and Therapeutic Opportunities.

Cancer is a disease characterized by abnormal cell growth. According to a report published by the World Health Organization (WHO), cancer is the second leading cause of death globally, responsible for an estimated 9.6 million deaths in 2018. It should be noted that ultrasound is already widely used as a diagnostic procedure for detecting tumorigenesis. In addition, ultrasound energy can also be utilized effectively for treating cancer. By filling the interior of lipospheres with gas molecules, these particles can serve both as contrast agents for ultrasonic imaging and as delivery systems for drugs such as microbubbles and nanobubbles. Therefore, this review aims to describe the nanoparticle-assisted drug delivery system and how it can enhance image analysis and biomedicine. The formation characteristics of nanoparticles indicate that they will accumulate at the tumor site upon ultrasonic imaging, in accordance with their modification characteristics. As a result of changing the accumulation of materials, it is possible to examine the results by comparing images of other tumor cell lines. It is also possible to investigate ultrasound images for evidence of cellular effects. In combination with a precision ultrasound imaging system, drug-carrying lipospheres can precisely track tumor tissue and deliver drugs to tumor cells to enhance the ability of this nanocomposite to treat cancer.

Green Synthesis of Nanomaterials and Their Utilization as Potential Vehicles for Targeted Cancer Drug Delivery

A nanoparticle (NP) is a microscopic particle with a length of two or three dimensions greater than 0.001 micrometer (1 nanometer =10⁻⁹ metre). NPs may be classified into different classes based on their specific properties, shapes or sizes, and high surface area-to-volume ratio. Nanoparticles have a remarkable capacity as 'magic bullets' stacked with herbicides, fungicides, supplements, fertilizers or nucleic acids, specializing in expressing plant tissues to deliver their charge to the appropriate piece of the plant to perform desired outcomes. The smart design and synthesis of a library of nanomaterials, exact control over their physicochemical properties and simplicity of their surface functionalization to assemble explicitness is to be certain fundamental for the achievement of disease treatment and harmfulness in the biological systems. Green techniques for nanomaterial synthesis observe natural organic systems to nanomaterial production. Green synthesized nanomaterials are at present powerful and significant tools for protecting the drug from the dangerous surroundings in addition to overcoming the organic obstacles to access of the drug in targeted tissues and dealing with drug resistance. NPs were extensively utilized in numerous biomedical applications, site-specific drug delivery systems and cellular uptake because of their inert nature, stability, high dispersity, non-cytotoxicity, and biocompatibility. Nanoparticles may be programmed for recognizing the cancerous cells and giving selective and correct drug delivery avoiding interaction with the healthy cells. However, usage of those NPs is restrained through factors like lack of stability in adversarial environment, concerns regarding bioaccumulation and toxicity, need of relatively trained employees for device assembly and operation, and problems with reproducibility and affordability.

Functionalized graphene oxide loaded GATPT as rationally designed vehicle for cancer-targeted drug delivery

This study focused to demonstrate the impact of the anticancer activity of nanoparticles of 1-{(2-hydroxyethyl) amino}-2-amino-1,2-dideoxy-d-glucose triphenyltin (IV) (GATPT) by using graphene oxide as a drug carrier. The synthesized GATPT was loaded on GO, which was prepared by the simple ultrasonication method. The successful loading of GATPT on GO was characterized by utilizing various physicochemical techniques, and the results showed that the encapsulation of GATPT on GO occurred via π–π stacking and electrostatic mode of interaction. The interaction of GATPT-GO with ct-DNA has been explored by employing absorption, emission, circular dichroic spectral methods, and cyclic voltammetry (CV). The corroborative results of all these techniques along with molecular docking suggested the electrostatic mode of interaction of GATPT-GO towards DNA. Cleavage activity was performed by gel electrophoretic assays which indicated that GATPT-GO cleaves pBR322 via hydrolytic pathway in the presence of EtOH as an active species. The cytotoxic studies of GATPT-GO were evaluated against human prostate cancer (DU145) cell lines and liver carcinoma (Huh-7) cell lines, including normal cell lines (PNT2). These experiment results revealed significant cytotoxic activity against Du145 cancer cells than the Huh-7 cancer cells and were found nontoxic toward the PNT2 cells at a lower concentration. Also, image analysis was performed by confocal microscopy. The results obtained from confocal microscopy provide clear evidence of endocytosis of GATPT, revelling that the released drug (GATPT) from carrier (GO) has specifically entered into the cell nucleus.

Tumor targeted mesoporous silica nanoparticles functionalized with programmed death receptor ligand-1 antibody (anti-PD-L1) for combined chemo- and immunotherapy

Traditional chemotherapy is associated with severe side-effects due to non-specific targeting of healthy tissue. An additional drawback of traditional chemotherapy is the development of multidrug resistance (MDR) phenotypes. Here, we overcome these issues by developing a targeted cancer drug delivery nanoplatform that combines immuno- and chemotherapy. We utilize mesoporous silica nanoparticles (MSNs) that are characterized by a high drug loading capacity (within the pores of the nanoparticles) and subsequent controlled drug release (in target cancer cells).

Stimuli-Responsive Amphiphilic Pillar[n]arene Nanovesicles for Targeted Delivery of Cancer Drugs.

Cancer chemotherapeutics face several challenges, including uncontrollable drug release, off-target toxic effects, and poor bioavailability. Recently, supramolecular nanovesicles, such as calix[n]arenes (CXs), cyclodextrins (CDs), cucurbiturils (CBs), and pillar[n]arenes (PRs), have attracted attention as potential smart nanocarriers for chemotherapeutics because of their exceptional cavities that can achieve high encapsulation capacity and accommodate both hydrophilic and hydrophobic drugs. In addition, they can be functionalized with different stimuli-responsive groups, which facilitate controlled drug release. Supramolecular nanovesicles, loaded with drugs and decorated with stimuli-responsive targeting moieties, are designed by either host–guest complexation or self-assembly of amphiphilic cavitands. Pillar[n]arenes, in particular, are novel supramolecular host molecules that have recently been employed in cancer targeted drug delivery because of their symmetric pillar-shaped structure, simplicity of functionalization, and biocompatibility. This review summarizes state-of-the-art strategies for developing single or multiple stimuli-responsive pillar[n]arene nanovesicles for effective cancer treatment.

Chimeric virus-like particles (VLPs) designed from shrimp nodavirus (MrNV) capsid protein specifically target EGFR-positive human colorectal cancer cells

Recombinant MrNV capsid protein has been shown to effectively deliver plasmid DNA and dsRNA into Sf9 insect cells and shrimp tissues. To extend its application to cancer cell-targeting drug delivery, we created three different types of chimeric MrNV virus-like particles (VLPs) (R-MrNV, I-MrNV, and E-MrNV) that have specificity toward the epidermal growth factor receptor (EGFR), a cancer cell biomarker, by incorporating the EGFR-specific GE11 peptide at 3 different locations within the host cell recognition site of the capsid. All three chimeric MrNV-VLPs preserved the ability to form a mulberry-like VLP structure and to encapsulate EGFP DNA plasmid with an efficiency comparable to that previously reported for normal MrNV (N-MrNV). Compared to N-MrNV, the chimeric R-MrNV and E-MrNV carrying the exposed GE-11 peptide showed a significantly enhanced binding and internalization abilities that were specific towards EGFR expression in colorectal cancer cells (SW480). Specific targeting of chimeric MrNV to EGFR was proven by both EGFR silencing with siRNA vector and a competition with excess GE-11 peptide as well as the use of EGFR-negative colorectal cells (SW620) and breast cancer cells (MCF7). We demonstrated here that both chimeric R-MrNV and E-MrNV could be used to encapsulate cargo such as exogenous DNA and deliver it specifically to EGFR-positive cells. Our study presents the potential use of surface-modified VLPs of shrimp virus origin as nanocontainers for targeted cancer drug delivery.

Solid Lipid Nanoparticles for Efficient Oral Delivery of Tyrosine Kinase Inhibitors: A Nano Targeted Cancer Drug Delivery.

Tyrosine kinase inhibitors (TKIs) are used as targeted therapy for cancer by inhibiting the signaling pathway and tumor growth. Many TKIs got approved by FDA in recent times for the treatment of cancer by oral route. However, the TKIs have formulation challenges leading to compromised bioavailability which can cause a weak therapeutic response. The cancer nanotherapeutics using nanocarriers based drug delivery has emerged as an advanced tool to provide a solution to formulation challenges and a better cancer therapy by overcoming the limitations in conventional cancer therapy. This review describes the various formulation issues of anticancer drugs with a special reference to TKIs, as well as the capability of solid lipid nanoparticles (SLNs) for an efficient nano targeted cancer drug delivery.

Drug Release Studies of SC-514 PLGA Nanoparticles

A major problem associated with prostate cancer treatment is the development of drug resistance. The development of drug resistance often leads to prostate cancer metastasis and prostate cancer-targeted drug delivery systems can be utilized to address this problem. Traditional drug delivery systems have many challenges, including the inability to control the drug release rate, target site inaccuracy, susceptibility to the microenvironment, poor drug solubility, and cytotoxicity of chemotherapeutics to non-malignant cells. As a result, there is an urgent need to formulate and functionalize a drug delivery system that better controls drug release. This study was designed to quantify the release of SC-514 from SC-514 Polylactic-Co-Glycolic Acid (PLGA) nanoparticles and conjugate SC-514-PLGA coated nanoparticles with the NF- κβ antibody, as well as fats. This study further explored new methods to quantify the release of SC-514 drug from the SC-514-PLGA coated nanoparticles after utilizing Liquid Chromatography–Mass Spectrometry (LC-MS) as the standard method to quantify SC-514 drug released. After quantification was completed, cell viability studies indicated that the ligand conjugated nanoparticles demonstrated a considerable ability to reduce tumor growth and SC-514 drug toxicity in the PC-3 cell line. The prepared drug delivery systems also possessed a significantly lower toxicity (P<0.05), bettered controlled-release behaviors in prostate cancer, and increased the solubility of SC-514 in comparison to free SC-514. SC-514 released from SC-514-PLGA, SC-514-PLGA-NF- κβAb, and SC-514-PLGA-Fat nanoparticles, significantly inhibited tumor growth when compared to that of free SC-514. The anti-cancer therapeutic effects of SC-514 were improved through the encapsulation of SC-514 with a PLGA polymer. The functionalized SC-514-PLGA nanoparticles can further control burst release. The new methods utilized in this study for quantifying drug release, may prove to be as effective as the current standard methods, such as LC/MS.

Drug Release Studies of SC‐514 PLGA Nanoparticles

Background A major problem associated with prostate cancer treatment is drug resistance leading to prostate cancer metastasis. Prostate cancer-targeted drug delivery system is one way to address this problem. Traditional drug delivery systems face many challenges, such as inability to control the release rate, inaccurate targeting, susceptibility to the microenvironment, and poor stability of the drug. Hence, there is a need to formulate a drug delivery system and functionalize the surface of delivery system for a better control of drug release. Targeted drug delivery of nanoparticles decorated with site-specific recognition ligands is of considerable interest to minimize cytotoxicity of chemotherapeutics in the normal cells. This study was designed to measure drug release of SC-514-PLGA nanoparticles and conjugate SC-514 polylactic-co-glycolic acid (PLGA) nanoparticles loaded with NF-KB antibody and fats. This study explored new methods to quantify the SC-514 drug released from SC-514-PLGA nanoparticles. The anti-proliferative effects of the SC-514 drug released by the nanoparticle treatments were investigated in PC-3 cells and cord blood cells. MDR expression in PC-3 cells was investigated after treatment with free SC-514 and SC-514 from SC-514-PLGA nanoparticles. Methods SC-514drug release was studied under in vitro conditions in phosphate buffer solution (PBS) at a pH of 7.4, using dialysis method. Liquid chromatography–mass spectrometry (LC-MS) was utilized as the standard method to quantify SC-514 drug released. Furthermore, other experimental methods utilized to quantify SC-514 drug released included: colony assay, wound healing assay, and transwell migration and invasion assays. MTT calorimetric assay was utilized to investigate the impact of the nanoparticle formulations (SC-514-PLGA, SC-514-PLGA-NF-KB, SC-514-PLGA-Fat) on PC-3 cells and cord blood cells. In addition, in vitro cellular uptake of fluorescent nanoparticle formulations in PC-3 and cord blood cells were examined with confocal fluorescence microscope. Results The ligand conjugated nanoparticles showed considerable reduction of tumor growth and toxicity (side-effect of the drug treatment in prostate cancer) of SC-514 drug in prostate cancer treatment. Our results demonstrated that prepared drug delivery system possesses a much lower toxicity, better prostate cancer controlled-release behaviors and confers higher solubility to SC-514 than free SC-514. SC-514 released from SC-514-PLGA, PLGA-SC-514-NF-KB, and PLGA-SC-514-Fat significantly inhibited tumor growth when compared to free SC-514. A more significant reduction of cell viability was recorded in PC-3 cells by all treatments (Free SC-514, SC-514-PLGA, and SC-514-PLGA-NF-KB) compared to cord blood cells, except for SC-514-PLGA-Fat nanoparticle formulation.SC-514 drug from SC-514-PLGA nanoparticles reduced the expression of MDR proteins than free SC-514. Conclusion Encapsulation of SC-514 with PLGA polymer increased the anti-cancer therapeutic effects of SC-514 drug. Burst release from SC-514-PLGA nanoparticles can be controlled by functionalization. New methods of quantifying drug release maybe as effective as the standard methods of drug quantification, such as LC/MS method.

In vitro anticancer activity of Nε-acyl lysine methyl ester through folate receptor targeted liposomes

Delivering anticancer drugs to tumor tissues with high specificity to realize minimal adverse effects is currently the main research focus of cancer treatment. Nε-acyl lysine methyl esters (Nε-lys) have the potential to serve as novel and safe anticancer agents owing to their pH-responsive membrane-disruptive activity and non-toxic metabolic products. In this study, we synthesized three Nε-lys with different hydrophobic chain lengths and evaluated their cytotoxicity to cancer and normal cells. One of the compounds with an acyl chain of 14 carbon atoms (MKM) showed moderate cytotoxicity and was delivered to cancer cells encapsulated in liposomes (MKM-LP). We additionally modified the liposomes with folate and PEG as a cancer-targeting drug delivery system (FA-PEG-MKM-LP) to enhance the cell selectivity. We tested the difference in the cellular uptake of liposomes between a folate receptor-positive human ovarian cancer cell line (SKOV3) and a healthy human ovary epithelial cell line (IOSE). The experimental results showed that FA-PEG-MKM-LP had low cytotoxicity to IOSE and higher cancer-targeting ability than other tested liposomes. Fluorescence imaging of dead cells and a LDH release assay further demonstrated that the cytotoxicity of FA-PEG-MKM-LP possessed time- and dose-dependent activity and specificity to cancer cells. These results lay a foundation for the development of Nε-lys as a promising anticancer drug.

Selenium nanoparticles coated with pH responsive silk fibroin complex for fingolimod release and enhanced targeting in thyroid cancer

Cancer-targeted drug delivery systems based on nanoparticles (NPs) have been considered promising therapies. In this study, we developed a pH-responsive smart NPs drug delivery system using silk fibroin (SF), selenium nanoparticles (Se NPs), fingolimod (FTY720), and heptapeptide (T7). The prepared FTY720@T7-SF-Se NPs were spheres with an average diameter of 120 nm, which would contribute to the enhanced permeability and retention effects in tumour regions. The encapsulation efficiency (EE) of the FTY720@T7-SF-Se NPs was 71.95 ± 3.81%. The release of FTY720 from the nanocarriers was pH-dependent, and the release of FTY720 was accelerated in an acidic environment. Both in vitro and in vivo studies showed that FTY720@T7-SF-Se NPs had an enhanced cellular uptake selectivity and antitumor activity for thyroid cancer. The bio-distribution study in vivo further demonstrated that FTY720@T7-SF-Se NPs could effectively accumulate in the tumour region, thereby enhancing the ability to kill cancer cells in vivo. In addition, studies of histology and immunohistochemistry showed that FTY720@T7-SF-Se NPs had low toxicity to the major organs of tumour-bearing mice, indicating the prepared NPs has good biocompatibility in vivo. These results suggest that the tumour-targeted NPs delivery system (FTY720@T7-SF-Se NPs) has great potential as a new tool for thyroid cancer therapy.

Glycosylated Nanoparticles for Cancer-Targeted Drug Delivery.

Nanoparticles (NPs) are novel platforms that can carry both cancer-targeting molecules and drugs to avoid severe side effects due to nonspecific drug delivery in standard chemotherapy treatments. Cancer cells are characterized by abnormal membranes, metabolic changes, the presence of lectin receptors, glucose transporters (GLUT) overexpression, and glycosylation of immune receptors of programmed death on cell surfaces. These characteristics have led to the development of several strategies for cancer therapy, including a large number of carbohydrate-modified NPs, which have become desirable for use in cell-selective drug delivery systems because they increase nanoparticle-cell interactions and uptake of carried drugs. Currently, the potential of NP glycosylation to enhance the safety and efficacy of carried therapeutic antitumor agents has been widely acknowledged, and much information is accumulating in this field. This review seeks to highlight recent advances in NP stabilization, toxicity reduction, and pharmacokinetic improvement and the promising potential of NP glycosylation from the perspective of molecular mechanisms described for drug delivery systems for cancer therapy. From preclinical proof-of-concept to demonstration of therapeutic value in the clinic, the challenges and opportunities presented by glycosylated NPs, with a focus on their applicability in the development of nanodrugs, are discussed in this review.

Structural requirement of G-quadruplex/aptamer-combined DNA macromolecule serving as efficient drug carrier for cancer-targeted drug delivery

Photodynamic therapy (PDT) as a clinical cancer treatment method has been used to treat carcinomas in different organs, and G-quadruplex-based DNA nanocompartments serving as the carriers of cationic porphyrin photosensitizers, especially combined with cell-targeting aptamers, is considered to offer new opportunities for future cancer treatment. However, the structural features of G-quadruplex/aptamer complexes suitable for the capsulation of photosensitizers and target cell recognition is unexplored so far. In this study, unimolecular (UM), bimolecular (BM) and tetramolecular (TM) G-quadruplex structures were used as the drug loading compartments and grafted onto tumor cell-targeting aptamer Sgc8, constructing several targeting drug delivery vehicles (T-GMVs). Besides the binding affinity of resulting DNA architectures for target cells and cell recognition specificity were explored in a comparative fashion, the drug loading capability and cancer therapy efficacy were evaluated using TMPyP4 as the model porphyrin-based drug. The experimental results show that only TM G-quadruplex structure is suitable to combine with Sgc8 for the development of drug delivery vehicle and the as-prepared T-GMV- TMPyP4 complexes display the desirable cancer therapy efficacy, holding the potential application in the future cancer therapy. More importantly, T-GMV- TMPyP4 is expected to lay the scientific groundwork for the successful development of G-quadruplex-based photosensitizer drug delivery carriers for the targeted cancer therapy.

Enhanced Cancer-targeted Drug Delivery Using Precoated Nanoparticles.

While protein coronas (PCs) are an important barrier in the clinical application of nanomedicines, the specific effects of PCs on nanoparticles (NPs) in vivo are unclear. Herein, we demonstrated that PCs from clinical sources greatly influenced the active targeting capacities of transferrin-modified NPs (Tf-NPs). Compared to PCs from healthy volunteers, PCs from the plasma of patients with nonsmall cell lung cancer (NSCLC) decreased the A549 uptake of Tf-NPs to a greater degree. The PC proteome revealed that this difference may be mediated by certain proteins in plasma. To attenuate the negative influence of PCs from patients, precoating Tf-NPs with PCs derived from healthy mice significantly enhanced active targeting capacities. Paclitaxel-loaded Tf-NPs with PCs derived from healthy mice showed the strongest antitumor effects in mice with NSCLC. This work illustrates the influence of PCs of ligand-modified NPs in clinical practice and proposes the use of corona-enabled active targeting for precision nanomedicine.

A Review on Nanocarriers for Cancer Targeted Drug Delivery

Nanoparticles in the drugs are useful for the treatment of cancer due to their unique properties and can act as drug carriers in different ways. Unlike the traditional chemotherapy, the entrance of nanotechnology enabled wide applications in treatment of cancer. Although nanoparticles provides safe and effective drug delivery systems but the factor of toxicity still limits the utilisation of several nanoparticles. The properties of nanodrug carriers are controllable by various factors. The use of nanoparticles in cancer therapy by drug delivery and their advantages as been reviewed.
 
 

Chitosan nano-vehicles as biocompatible delivering tools for a new Ag(I)curcuminoid-Gboxin analog complex in cancer and inflammation therapy

A novel anticancer and anti-inflammatory agent based on hybrid curcuminoid-Gboxin analog (FLLL49-GbA) and its macromolecular silver(I) complex (Ag(I)FLLL49-GbA) have successfully synthesized. In addition, chitosan nanoparticles (CNPs) were used to encapsulate this macromolecular complex, targeting enhancing its therapeutic effect and minimizing its side impacts. The encapsulated Ag(I) complex was significantly triggered apoptosis (P < 0.05) with much more rapidly release of Ag(I)FLLL49-GbA from the CNPs at pH 5.3 than at pH 7.4, which is beneficial for cancer-targeted drug delivery. Free complex showed promising ability in preventing glucose uptake and lactate production coupled with cellular ATP depletion in cancer cells. Additionally, there was significant decrease in the inflammatory cytokines in breast cancer (MCF-7) and lung cancer (A549) cells with values of P < 0.01 and P < 0.001 after 24 h incubation. Furthermore, the death-inducing proteins have been significantly up-regulated (P < 0.01 to P < 0.001) after 36 h incubation of cancer cells. Consequently, the novel curcuminoid macromolecule showed significant feasibility in triggering the high expression of apoptotic caspases caspase 3, caspase 8, P53, and Bax (P < 0.01 to P < 0.001) after 48 h of chemotherapy. Noteworthy, the cytotoxicity of Ag(I)FLLL49-GbA was significantly increased toward cancer cells (MCF-7 > A549), while, reduced toward normal cells (HeLa) after loading on chitosan Nano-vehicles.

Alginate-Based Platforms for Cancer-Targeted Drug Delivery.

As an acidic, ocean colloid polysaccharide, alginate is both a biopolymer and a polyelectrolyte that is considered to be biocompatible, nontoxic, nonimmunogenic, and biodegradable. A significant number of studies have confirmed the potential use of alginate-based platforms as effective vehicles for drug delivery for cancer-targeted treatment. In this review, the focus is on the formation of alginate-based cancer-targeted delivery systems. Specifically, some general chemical and physical properties of alginate and different types of alginate-based delivery systems are discussed, and various kinds of alginate-based carriers are introduced. Finally, recent innovative strategies to functionalize alginate-based vehicles for cancer targeting are described to highlight research towards the optimization of alginate.

Development of ErbB2-Targeting Liposomes for Enhancing Drug Delivery to ErbB2-Positive Breast Cancer.

ErbB2 is a type of receptor tyrosine kinase, which is known to be involved in tumorigenesis, tumor aggressiveness, and clinical outcome. ErbB2-targeting therapy using therapeutic antibodies has been successful in breast cancer treatment. However, the need for repeated treatments and the high cost are major disadvantages with monoclonal antibody therapies. Compared with antibodies, peptides are cheap, relatively stable, and have low immunogenicity. We have developed a highly specific cancer-targeting drug delivery system using a targeting peptide to maximize the therapeutic efficiency of rapamycin and to help prevent drug resistance in ErbB2-positive breast cancer. Physicochemical characterization confirmed the successful construction of ErbB2-targeting liposomes (ErbB2Lipo). A comparison of a scrambled peptide (ScrErbB2) with the ErbB2-targeting peptide confirmed that these peptides had similar properties except for the targeting ability. The ErbB2Lipo exhibited higher delivery efficiency in ErbB2 positive BT-474 cells than non-targeting liposomes conjugated with ScrErbB2 (ScrErbB2Lipo). This peptide-targeting strategy has the potential to improve the efficacy of chemotherapy in ErbB2-positive cancers.