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Beyond Formulation: Contributions of Nanotechnology for Translation of Anticancer Natural Products into New Drugs.

Nature is the largest pharmacy in the world. Doxorubicin (DOX) and paclitaxel (PTX) are two examples of natural-product-derived drugs employed as first-line treatment of various cancer types due to their broad mechanisms of action. These drugs are marketed as conventional and nanotechnology-based formulations, which is quite curious since the research and development (R&D) course of nanoformulations are even more expensive and prone to failure than the conventional ones. Nonetheless, nanosystems are cost-effective and represent both novel and safer dosage forms with fewer side effects due to m

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… Polymeric Micelles Another formulation approved for PTX is Nanoxel ® ( Figure 3 , Table 1 ), a nanoformulation comprised of polymeric micelles developed by Dabur Pharma Ltd. … In the case of polymeric micelles, other mechanisms play important roles in PTX release: the surface erosion of the hydrophilic core of the micelle and the pH sensibility of the nanocarrier (more specifically for Nanoxel ® ). …

Progress on the Application of Bortezomib and Bortezomib-Based Nanoformulations.

Bortezomib (BTZ) is the first proteasome inhibitor approved by the Food and Drug Administration. It can bind to the amino acid residues of the 26S proteasome, thereby causing the death of tumor cells. BTZ plays an irreplaceable role in the treatment of mantle cell lymphoma and multiple myeloma. Moreover, its use in the treatment of other hematological cancers and solid tumors has been investigated in numerous clinical trials and preclinical studies. Nevertheless, the applications of BTZ are limited due to its insufficient specificity, poor permeability, and low bioavailability. Therefore, in r

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… Polymeric Micelles Polymer micelles are a type of nanoparticle with a core-shell structure formed by the self-assembly of amphiphilic block copolymers in aqueous solution. The hydrophobic core can accommodate the insoluble substances to improve solubility. … BTZ-loaded micelles (HA-core-disulfide-crosslinked biodegradable micelles-BTZ-pinanediol [HA-CCMS-BP]) were prepared by encapsulating alcohol-esterified BTZ in the carriers. …

Glucocorticoids-based prodrug design: Current strategies and research progress.

Attributing to their broad pharmacological effects encompassing anti-inflammation, antitoxin, and immunosuppression, glucocorticoids (GCs) are extensively utilized in the clinic for the treatment of diverse diseases such as lupus erythematosus, nephritis, arthritis, ulcerative colitis, asthma, keratitis, macular edema, and leukemia. However, long-term use often causes undesirable side effects, including metabolic disorders-induced Cushing's syndrome (buffalo back, full moon face, hyperglycemia, etc.), osteoporosis, aggravated infection, psychosis, glaucoma, and cataract. These notorious side e

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… micelle-based products are even less available. … Biodistribution experiments verified that SA-PEG-Dex micelles accumulated more in inflammatory cells and inflammatory kidneys than PEG-Dex. As a result, SA-PEG-Dex micelles had better therapeutic efficacy in treating AKI than free Dex and PEG-Dex ( P < 0.05). …

Нанотехнология в области гематологии: усиление терапевтической эффективности с помощью нанопчастей.

Фон и цели Гематологические заболевания, такие, как лейкемия, лимфома и множественная миелома, вносят значительный вклад в глобальный диагноз рака. Несмотря на прогресс в традиционных методах лечения, таких, как химиотерапия и иммунотерапия, эти методы лечения сталкиваются с ограничениями, включая неконкретную адресность, побочные эффекты и резистентность к лекарствам. Цель этого обзора заключается в изучении потенциала нанотехнологии, в частности наночастиц (НФ), для улучшения терапевтических последствий для этих раковых заболеваний путем расширения поставок наркотиков и снижения токсичности.

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… Micelles Micelles represent a distinct category of biocompatible nanosystems, characterized by their size ranging from 5 to 100 nm. … Lu Y., Zhang E., Yang J., and Cao Z., “Strategies to Improve Micelle Stability for Drug Delivery,” Nano Research 11, no. 10 (October 2018): 4985–4998. 89. …

Enhancing the Bioavailability of Resveratrol: Combine It, Derivatize It, or Encapsulate It?

Overcoming the limited bioavailability and extensive metabolism of effective in vitro drugs remains a challenge that limits the translation of promising drugs into clinical trials. Resveratrol, despite its well-reported therapeutic benefits, is not metabolically stable and thus has not been utilized as an effective clinical drug. This is because it needs to be consumed in large amounts to overcome the burdens of bioavailability and conversion into less effective metabolites. Herein, we summarize the more relevant approaches to modify resveratrol, aiming to increase its biological and therapeut

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… Polymeric micelles tend to be more stable than surfactant micelles because they have lower critical micelle concentrations (CMC), slower dissociation rates, and reach a high drug concentration at the target site [ 203 ]. … In fact, pluronics alone have insufficient drug encapsulation capacity and high critical micelle concentration (CMC), leading to the dissociation of micelles after intravenous injections. To overcome this, pluronics are often used with other micelle copolymers to increase drug loading capacity. …

Stage-specific treatment of colorectal cancer: A microRNA-nanocomposite approach.

Colorectal cancer (CRC) is among the leading causes of cancer mortality. The lifetime risk of developing CRC is about 5% in adult males and females. CRC is usually diagnosed at an advanced stage, and at this point therapy has a limited impact on cure rates and long-term survival. Novel and/or improved CRC therapeutic options are needed. The involvement of microRNAs (miRNAs) in cancer development has been reported, and their regulation in many oncogenic pathways suggests their potent tumor suppressor action. Although miRNAs provide a promising therapeutic approach for cancer, challenges such as

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… Many micelle nanocarriers have been developed for siRNA delivery over the years [ 113 ]. … Design and development of polymeric micelles as nanocarriers for anti-cancer Ribociclib drug. J. Mol. Liq. 2021;329 113. Marzbali M.Y., Khosroushahi A.Y. Polymeric micelles as mighty nanocarriers for cancer gene therapy: A review, Cancer Chemother. …

An Overview of Polymeric Nanoparticles-Based Drug Delivery System in Cancer Treatment.

Cancer is recognized as one of the world's deadliest diseases, with more than 10 million new cases each year. Over the past 2 decades, several studies have been performed on cancer to pursue solutions for effective treatment. One of the vital benefits of utilizing nanoparticles (NPs) in cancer treatment is their high adaptability for modification and amalgamation of different physicochemical properties to boost their anti-cancer activity. Various nanomaterials have been designed as nanocarriers attributing nontoxic and biocompatible drug delivery systems with improved bioactivity. The present

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… The ultrasonic drug delivery from micelles basically employs polyether block polymers. With the collapse of cavitation bubbles via shock waves and shear stress, ultrasound liberates drugs from micelles. The small packaging allows the nanoparticles to discharge into tumor tissue. … Therefore, cross-linked polymer micelles are developed to overcome this issue. 60 , 61 Additionally, in cancer theranostics, the surface of micelles can be coupled with site-specific ligands to promote active tumor targeting. …

Metastatic Breast Cancer: Review of Emerging Nanotherapeutics.

Metastases of breast cancer (BC) are often referred to as stage IV breast cancer due to their severity and high rate of mortality. The median survival time of patients with metastatic BC is reduced to 3 years. Currently, the treatment regimens for metastatic BC are similar to the primary cancer therapeutics and are limited to conventional chemotherapy, immunotherapy, radiotherapy, and surgery. However, metastatic BC shows organ-specific complex tumor cell heterogeneity, plasticity, and a distinct tumor microenvironment, leading to therapeutic failure. This issue can be successfully addressed b

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… The detailed synthetic procedure of micelle development is depicted in Figure 2 . … The 3-MPs-coated micelles showed about 6.5-fold higher affinity for the bone tissue compared to nontargeted micelles in vivo. …

A Recent Review on Cancer Nanomedicine.

Cancer is one of the most prevalent diseases globally and is the second major cause of death in the United States. Despite the continuous efforts to understand tumor mechanisms and various approaches taken for treatment over decades, no significant improvements have been observed in cancer therapy. Lack of tumor specificity, dose-related toxicity, low bioavailability, and lack of stability of chemotherapeutics are major hindrances to cancer treatment. Nanomedicine has drawn the attention of many researchers due to its potential for tumor-specific delivery while minimizing unwanted side effects

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… Tumor-specific ligands can be added to polymeric micelles to increase tumor accumulation. As a result, polymeric micelles can play a significant role in delivering hydrophobic medicinal compounds for cancer treatment [ 152 ]. … Thus, to enhance the uptake, cRGD peptide ligand-decorated polymeric micelles composed of PEG–poly( l -lysine) (PEG–PLL) block copolymers were synthesized. Antiangiogenic plasmid DNA was incorporated into the central core of polymeric micelles via electrostatic complexation. …

Direct immunoactivation by chemotherapeutic drugs in cancer treatment.

The immune system plays a crucial role in recognizing and eliminating pathogenic substances and malignant cells in the body. For cancer treatment, immunotherapy is becoming the standard treatment for many types of cancer and is often combined with chemotherapy. Although chemotherapeutic agents are often reported to have adverse effects, including immunosuppression, they can also play a positive role in immunotherapy by directly stimulating the immune system. This has been demonstrated in preclinical and clinical studies in the past decades. Chemotherapeutics can activate immune cells through d

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… The efficacy of the polymeric micelles loaded with docetaxel was evaluated using a subcutaneous CDX model of SGC7901 cells. Free docetaxel slightly inhibited tumor growth while the polymeric micelles loaded with docetaxel showed significantly higher efficacy at two dose levels (5 and 10 mg/kg). … Importantly, the micelle formulation of docetaxel showed more effective macrophage polarization than free docetaxel ( Figure 2D ). …

Current advance of nanotechnology in diagnosis and treatment for malignant tumors.

Cancer remains a significant risk to human health. Nanomedicine is a new multidisciplinary field that is garnering a lot of interest and investigation. Nanomedicine shows great potential for cancer diagnosis and treatment. Specifically engineered nanoparticles can be employed as contrast agents in cancer diagnostics to enable high sensitivity and high-resolution tumor detection by imaging examinations. Novel approaches for tumor labeling and detection are also made possible by the use of nanoprobes and nanobiosensors. The achievement of targeted medication delivery in cancer therapy can be acc

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… Micelles Micelles are spheres composed of self-aggregated amphiphilic molecules with a size between 10 and 100 nm in diameter. … The average diameter of the micelles was 20 ± 0.6 nm, and their distribution was relatively narrow. The entrapment efficiency of the micelles was more than 90%. QA-M micelles could remarkably inhibit the tumor of colon cancer in situ in mice. …

Exploration of Site-Specific Drug Targeting-A Review on EPR-, Stimuli-, Chemical-, and Receptor-Based Approaches as Potential Drug Targeting Methods in Cancer Treatment.

Cancer has been one of the most dominant causes of mortality globally over the last few decades. In cancer treatment, the selective targeting of tumor cells is indispensable, making it a better replacement for conventional chemotherapies by diminishing their adverse side effects. While designing a drug to be delivered selectively in the target organ, the drug development scientists should focus on various factors such as the type of cancer they are dealing with according to which drug, targeting moieties, and pharmaceutical carriers should be targeted. All published articles have been collecte

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… Leakage of camptothecin due to the sudden disassembly of PEG-poly ( β -amino ester) micelles [ 168 ] and delivery of protein in ischemic areas with piperidine- and imidazole-modifiedPEG-poly ( β -amino ester) micelles [ 169 ] are some of the examples of pH-sensitive drug release. … Light-responsive block copolymer micelles Macromolecules 2012 45 3647 3657 10.1021/ma300094t 2-s2.0-84860744179 144 Yen H.-C. Cabral H. Mi P. …

Polymerization Reactions and Modifications of Polymers by Ionizing Radiation.

Ionizing radiation has become the most effective way to modify natural and synthetic polymers through crosslinking, degradation, and graft p … osslinking of hydrophilic monomers in "nanocompartments", i.e., within the aqueous phase of inverse micelles, or by intramolecular crosslinking of suitable water-soluble polymers. The radiolytically produced oxidizing species from water, •OH radicals, can easily abstract H-atoms from the backbone of the dissolved polymers (or can add to the unsaturated bon …

A technical note on emerging combination approach involved in the onconanotherapeutics.

Cancer is the second cause of mortality worldwide, and the currently available conventional treatment approach is associated with serious side effects and poor clinical outcomes. Based on the outcome of the exploratory preclinical and clinical studies, it was found that therapeutic response increases multiple folds when anticancer drugs are used in combination. However, the conventional combination of anticancer drugs was associated with various limitations such as increased cost of treatment, systemic toxicity, drug resistance, and reduced pharmacokinetic attributes. Hence, attempts were made

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… The optimized formulation of TOS or curcumin-loaded micelles was in the size range of 172.93 ± 1.1 nm and 194.17 ± 1.7 nm, respectively, and the encapsulation efficiency of the PAH-SS-PLGA micelle was reported to be 85% for TOS and 95.5% for curcumin. … The micelles were reported to have a critical micellization concentration (CMC) value of about 29.6 µg/mL. Telodendrimer micelles (TM) exhibited different zeta potential, i.e., about −11.3 mV in pure water, whereas about 3.1 mV after cisplatin complexation. …

Advances and Prospects of Prolamine Corn Protein Zein as Promising Multifunctional Drug Delivery System for Cancer Treatment.

Zein is a type of prolamine protein that is derived from corn, and it has been recognized by the US FDA as one of the safest biological materials available. Zein possesses valuable characteristics that have made it a popular choice for the preparation of drug carriers, which can be administered through various routes to improve the therapeutic effect of antitumor drugs. Additionally, zein contains free hydroxyl and amino groups that offer numerous modification sites, enabling it to be hybridized with other materials to create functionalized drug delivery systems. However, despite its potential

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… Additionally, magnetic micelles exhibited more drug release rate in acidic condition compared to neutral condition. [ 191 ] Etoposide, all-trans retinoic acid Chondroitin sulfate, CaCl 2 , zein The CR micelles demonstrated the most powerful sustained release pattern of both, ETP and ATRA, in comparison … Additionally, magnetic micelles exhibited more drug release rate in acidic condition compared to neutral condition. | [ 191 ] Etoposide, all-trans retinoic acid | Chondroitin sulfate, CaCl 2 , zein | The CR micelles demonstrated the most powerful sustained release pattern of both, ETP and ATRA, in comparison …

Emerging Nanotherapeutic Approaches to Overcome Drug Resistance in Cancers with Update on Clinical Trials.

A key issue with modern cancer treatments is the emergence of resistance to conventional chemotherapy and molecularly targeted medicines. Cancer nanotherapeutics were created in order to overcome the inherent limitations of traditional chemotherapeutics. Over the last few decades, cancer nanotherapeutics provided unparalleled opportunities to understand and overcome drug resistance through clinical assessment of rationally designed nanoparticulate delivery systems. In this context, various design strategies such as passive targeting, active targeting, nano-drug, and multimodal nano-drug combin

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… Some of the commonly utilized nano vehicles include lipid- and micelle-based nanoparticles, polymeric/non-polymeric nanoparticles, nanoconjugates, carbon nanotubes, nanogels, nano capsules, dendrimers, polymer micelles, and quantum dots for the enhancement of the efficacy of therapeutic interventions … Several therapeutic nanoparticle (NP) platforms, such as liposomes, polymeric micelles, and albumin nanoparticles are FDA-approved for cancer treatment. …

Drug Delivery Approaches for the Treatment of Cervical Cancer.

Cervical cancer is a highly prevalent cancer that affects women around the world. With the availability of new technologies, researchers have increased their efforts to develop new drug delivery systems in cervical cancer chemotherapy. In this review, we summarized some of the recent research in systematic and localized drug delivery systems and compared the advantages and disadvantages of these methods.

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… Micelles Made up of amphiphilic block copolymers, polymeric micelles are colloidal particles that can assemble themselves [ 73 ]. … Anti-tumor activity of biodegradable polymer-paclitaxel conjugated micelle against mice U14 cervical cancers Chem. Res. Chin. Univ. 2012 28 656 661 77. Guo Q. Guan D. Dong B. Nan F. Zhang Y. …

Nano-formulations in disease therapy: designs, advances, challenges, and future directions.

Nano-formulations, as an innovative drug delivery system, offer distinct advantages in enhancing drug administration methods, improving bioavailability, promoting biodegradability, and enabling targeted delivery. By exploiting the unique size advantages of nano-formulations, therapeutic agents, including drugs, genes, and proteins, can be precisely reorganized at the microscale level. This modification not only facilitates the precise release of these agents but also significantly enhances their efficacy while minimizing adverse effects, thereby creating novel opportunities for treatment of a

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… The drug-loaded micelles exhibited high stability and demonstrated significantly enhanced inhibition of tumor cell growth, exhibiting superior anti-breast cancer efficacy. Xiao et al . have developed a novel borate cross-linked micelle (BCM) for loading paclitaxel (PTX) [ 104 ]. … Facile Fabrication of an Amentoflavone-Loaded Micelle System for Oral Delivery To Improve Bioavailability and Hypoglycemic Effects in KKAy Mice. …

Ferroptosis in Haematological Malignancies and Associated Therapeutic Nanotechnologies.

Haematological malignancies are heterogeneous groups of cancers of the bone marrow, blood or lymph nodes, and while therapeutic advances have greatly improved the lifespan and quality of life of those afflicted, many of these cancers remain incurable. The iron-dependent, lipid oxidation-mediated form of cell death, ferroptosis, has emerged as a promising pathway to induce cancer cell death, particularly in those malignancies that are resistant to traditional apoptosis-inducing therapies. Although promising findings have been published in several solid and haematological malignancies, the major

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… Micelles, in their most basic form, are amphiphilic molecules (surfactants) arranged spherically in aqueous solutions [ 148 ]. … The micelles were shown to be more effective at reducing tumour volume in doxorubicin-resistant human ovarian adenocarcinoma-bearing mice compared to drugs administered by more conventional means, and no adverse side effects were observed in mice treated with the micelles [ 150 ]. …

Nanoparticles for Effective Combination Therapy of Cancer.

Cancer continues to remains a major healthcare problem across the world despite strong translational research efforts towards tackling the disease. Surgery, when possible, along with radiation and chemotherapy continue to remain the mainstay of cancer treatment. Novel targeted therapies or biologics and immunotherapies have recently been approved to improve treatment efficacies while reducing collateral damage to normal, non-cancerous tissues. Combination therapies have shown better results than individual monotherapies in the clinic but often the improvements in therapeutic indices remain mar

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… The PEGPE/ vitamin E micelles have shown greater bioavailability and higher drug loading capacity. … Intracellular accumulation was significantly enhanced by the micelle formulation, as compared with free drug, in the MCF-7/ ADR cells overexpressing Pgp. The micelle vehicle also showed increased effectiveness during in vivo studies against tumors established with MCF-7/ADR cells in mice [ 40 ]. …