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1.
Artigo em Inglês | MEDLINE | ID: mdl-38644717

RESUMO

Quantum dots (QDs) have attracted considerable interest due to their potential applications and economic viability in various industrial sectors, such as communications, displays, and solar cells. This fascination originates from the quantum size effect-induced remarkable optical properties exhibited by QDs. In recent years, significant progress has been made in producing QDs devoid of cadmium, known to be toxic to cells and living organisms. These QDs have generated considerable interest in bioimaging due to their potential for targeting molecules and cells. There is a developing need for diagnostics and therapy at the individual molecule and single-cell level in the medical field. As a result, the application of QDs in the medical industry is gaining momentum. This study provides an overview of the most recent developments in applying QDs for diagnostic and therapeutic purposes, also known as theranostics. It emphasizes specifically the use of QDs in cancer therapy.

2.
Artigo em Inglês | MEDLINE | ID: mdl-38644713

RESUMO

Researchers in various fields continue to discover improved ways of local delivery of drugs to specific locations and try to increase the efficiency of these methods. Extensive research has been done on smart nano-biomaterials for drug delivery systems (DDS) in different dimensions. With the advancement of biomedical nanotechnology, conventional smart DDS with stimuli- responsive capability has been developed. Smart nano-biomaterials can respond to environmental changes caused by endogenous or exogenous elements: endogenous factors such as environmental pH, temperature gradient, enzymes, oxidation, and reduction potential. As well as exogenous factors, including light radiation, ultrasound, electric and magnetic fields. Currently, smart DDSs count as a major category in DDS and disease treatment. Currently, smart DDS are of great interest in drug delivery and treatment of diseases. With the improvements in gene and protein therapy, new methods have been presented to treat diseases without effective conventional treatment, especially cancer. Finally, the use of nanoparticles expanded due to the need for appropriate gene and protein delivery systems. This review discusses the advantages of protein and gene therapy, their challenges, and gene and protein delivery systems with nanoparticle-based delivery.

3.
Int J Biol Macromol ; : 131694, 2024 Apr 18.
Artigo em Inglês | MEDLINE | ID: mdl-38642693

RESUMO

In the last ten years, the field of nanomedicine has experienced significant progress in creating novel drug delivery systems (DDSs). An effective strategy involves employing DNA nanoparticles (NPs) as carriers to encapsulate drugs, genes, or proteins, facilitating regulated drug release. This abstract examines the utilization of DNA NPs and their potential applications in strategies for controlled drug release. Researchers have utilized the distinctive characteristics of DNA molecules, including their ability to self-assemble and their compatibility with living organisms, to create NPs specifically for the purpose of delivering drugs. The DNA NPs possess numerous benefits compared to conventional drug carriers, such as exceptional stability, adjustable dimensions and structure, and convenient customization. Researchers have successfully achieved a highly efficient encapsulation of different therapeutic agents by carefully designing their structure and composition. This advancement enables precise and targeted delivery of drugs. The incorporation of drugs, genes, or proteins into DNA NPs provides notable advantages in terms of augmenting therapeutic effectiveness while reducing adverse effects. DNA NPs serve as a protective barrier for the enclosed payloads, preventing their degradation and extending their duration in the body. The protective effect is especially vital for delicate biologics, such as proteins or gene-based therapies that could otherwise be vulnerable to enzymatic degradation or quick elimination. Moreover, the surface of DNA NPs can be altered to facilitate specific targeting towards particular tissues or cells, thereby augmenting the accuracy of delivery. A significant benefit of DNA NPs is their capacity to regulate the kinetics of drug release. Through the manipulation of the DNA NPs structure, scientists can regulate the rate at which the enclosed cargo is released, enabling a prolonged and regulated dispensation of medication. This control is crucial for medications with limited therapeutic ranges or those necessitating uninterrupted administration to attain optimal therapeutic results. In addition, DNA NPs have the ability to react to external factors, including alterations in temperature, pH, or light, which can initiate the release of the payload at precise locations or moments. This feature enhances the precision of drug release control. The potential uses of DNA NPs in the controlled release of medicines are extensive. The NPs have the ability to transport various therapeutic substances, for example, drugs, peptides, NAs (NAs), and proteins. They exhibit potential for the therapeutic management of diverse ailments, including cancer, genetic disorders, and infectious diseases. In addition, DNA NPs can be employed for targeted drug delivery, traversing biological barriers, and surpassing the constraints of conventional drug administration methods.

4.
Artigo em Inglês | MEDLINE | ID: mdl-38529608

RESUMO

Breast cancer is a highly prevalent disease on a global scale, with a 30% incidence rate among women and a 14% mortality rate. Developing countries bear a disproportionate share of the disease burden, while countries with greater technological advancements exhibit a higher incidence. A mere 7% of women under the age of 40 are diagnosed with breast cancer, and the prevalence of this ailment is significantly diminished among those aged 35 and younger. Chemotherapy, radiation therapy, and surgical intervention comprise the treatment protocol. However, the ongoing quest for a definitive cure for breast cancer continues. The propensity for cancer stem cells to metastasize and resistance to treatment constitute their Achilles' heel. The advancement of drug delivery techniques that target cancer cells specifically holds significant promise in terms of facilitating timely detection and effective intervention. Novel approaches to pharmaceutical delivery, including nanostructures and liposomes, may bring about substantial changes in the way breast cancer is managed. These systems offer a multitude of advantages, such as heightened bioavailability, enhanced solubility, targeted tumor destruction, and diminished adverse effects. The application of nano-drug delivery systems to administer anti-breast cancer medications is a significant subject of research. This article delves into the domain of breast cancer, conventional treatment methods, the incorporation of nanotechnology into managerial tactics, and strategic approaches aimed at tackling the disease at its core.

5.
Pharmaceutics ; 15(7)2023 Jul 11.
Artigo em Inglês | MEDLINE | ID: mdl-37514106

RESUMO

Doxorubicin is one of the most effective chemotherapeutic agents; however, it has various side effects, such as cardiotoxicity. Therefore, novel methods are needed to reduce its adverse effects. Quercetin is a natural flavonoid with many biological activities. Liposomes are lipid-based carriers widely used in medicine for drug delivery. In this study, liposomal doxorubicin with favorable characteristics was designed and synthesized by the thin-film method, and its physicochemical properties were investigated by different laboratory techniques. Then, the impact of the carrier, empty liposomes, free doxorubicin, liposomal doxorubicin, and quercetin were analyzed in animal models. To evaluate the interventions, measurements of cardiac enzymes, oxidative stress and antioxidant markers, and protein expression were performed, as well as histopathological studies. Additionally, cytotoxicity assay and cellular uptake were carried out on H9c2 cells. The mean size of the designed liposomes was 98.8 nm, and the encapsulation efficiency (EE%) was about 85%. The designed liposomes were anionic and pH-sensitive and had a controlled release pattern with excellent stability. Co-administration of liposomal doxorubicin with free quercetin to rats led to decreased weight loss, creatine kinase (CK-MB), lactate dehydrogenase (LDH), and malondialdehyde (MDA), while it increased the activity of glutathione peroxidase, catalase, and superoxide dismutase enzymes in their left ventricles. Additionally, it changed the expression of NOX1, Rac1, Rac1-GTP, SIRT3, and Bcl-2 proteins, and caused tissue injury and cell cytotoxicity. Our data showed that interventions can increase antioxidant capacity, reduce oxidative stress and apoptosis in heart tissue, and lead to fewer complications. Overall, the use of liposomal doxorubicin alone or the co-administration of free doxorubicin with free quercetin showed promising results.

6.
Life Sci ; 328: 121865, 2023 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-37336360

RESUMO

Immunosuppressive factors within the tumor microenvironment (TME), such as Transforming growth factor beta (TGF-ß), constitute a crucial hindrance to immunotherapeutic approaches in colorectal cancer (CRC). Furthermore, immune checkpoint factors (e.g., programmed death-ligand 1 [PD-L1]) inhibit T-cell proliferation and activation. To cope with the inhibitory effect of immune checkpoints, the therapeutic value of dual targeting PD-L1 and TGF-ß pathways via M7824 plus 5-FU in CRC has been evaluated. Integrative-systems biology approaches and RNAseq were used to assess the differential level of genes associated with 88 metastatic-CRC patients. The level of PD-L1 and TGF-ß was evaluated in a validation cohort. The anti-proliferative, migratory, and apoptotic effects of PD-L1/TGF-ß inhibitor, M7824, were assessed by MTT, wound-healing assay, and flow cytometry. Anti-tumor activity was assessed in a xenograft model, followed by biochemical studies and histological staining, and gene/protein expression analyses by RT-PCR and ELISA/IHC. The result of differentially expressed genes (DEGs) analysis showed 1268 upregulated and 1074 downregulated genes in CRC patients. Among the highest scoring genes and dysregulated pathways associated with CRC, PD-L1, and TGF-ß were identified and further validated in 92 CRC patients. Targeting of PD-L1-TGF-ß inhibited cell growth and migration, associated with modulation of CyclinD1 and MMP9. Furthermore, M7824 inhibited tumor growth via targeting TGF-ß and PD-L1 pathways, resulting in modulation of inflammatory response and fibrosis via TNF-α/IL6/CD4-8 and COL1A1/1A2, respectively. In conclusion, our data illustrated that co-targeting PD-L1 and TGF-ß pathways increased the effect of Fluorouracil (5-FU) and reduced the tumor growth in PD-L1/TGF-ß expressing tumors, providing a new therapeutic option in the treatment of CRC.


Assuntos
Antígeno B7-H1 , Neoplasias Colorretais , Humanos , Antígeno B7-H1/metabolismo , Fator de Crescimento Transformador beta/metabolismo , Neoplasias Colorretais/tratamento farmacológico , Neoplasias Colorretais/genética , Fluoruracila/farmacologia , Fluoruracila/uso terapêutico , Microambiente Tumoral
7.
Photodiagnosis Photodyn Ther ; 42: 103614, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37201772

RESUMO

The future of molecular-level therapy, efficient medical diagnosis, and drug delivery relies on the effective theragnostic function which can be achieved by the synergistic effect of fluorescent carbon dots (FCDs) liposomes (L) and nanoliposomes. FCDs act as the excipient navigation agent while liposomes play the role of the problem-solving agent, thus the term "theragnostic" would describe the effect of LFCDs properly. Liposomes and FCDs share some excellent at-tributes such as being nontoxic and biodegradable and they can represent a potent delivery system for pharmaceutical compounds. They enhance the therapeutic efficacy of drugs via stabilizing the encapsulated material by circumventing barriers to cellular and tissue uptake. These agents facilitate long-term drug biodistribution to the intended locations of action while eliminating systemic side effects. This manuscript reviews recent progress with liposomes, nanoliposomes (collectively known as lipid vesicles) and fluorescent carbon dots, by exploring their key characteristics, applications, characterization, performance, and challenges. An extensive and intensive understanding of the synergistic interaction between liposomes and FCDs sets out a new research pathway to an efficient and theragnostic / theranostic drug delivery and targeting diseases such as cancer.


Assuntos
Lipossomos , Fotoquimioterapia , Carbono , Distribuição Tecidual , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes , Corantes
8.
Crit Rev Food Sci Nutr ; : 1-20, 2023 Mar 23.
Artigo em Inglês | MEDLINE | ID: mdl-36950963

RESUMO

Nowadays, the use of lipid-based nanocarriers for the targeted and controlled delivery of a variety of hydrophobic and hydrophilic bioactive-compounds and drugs has increased significantly. However, challenges such as thermodynamic instability, oxidation, and degradation of lipid membranes, as well as the unintended release of loaded compounds, have limited the use of these systems in the food and pharmaceutical industries. Therefore, the present study reviews the latest achievements in evaluating the characteristics, production methods, challenges, functional, and biological stabilization strategies of lipid-based carriers (including changes in formulation composition, structural modification, membrane-rigidity, and finally monolayer or multilayer coating with biopolymers) in different conditions, as well as molecular dynamics simulations. The scientists' findings indicate the effect of natural biopolymers (such as chitosan, calcium alginate, pectin, dextran, xanthan, caseins, gelatin, whey-proteins, zein, and etc.) in modifying the external structure of lipid-based carriers, improving thermodynamic stability and resistance of membranes to physicochemical and mechanical tensions. However, depending on the type of bioactive compound as well as the design and production goals of the delivery-system, selecting the appropriate biopolymer has a significant impact on the stability of vesicles and maintaining the bioaccessibility of the loaded-compounds due to the stresses caused by the storage-conditions, formulation, processing and gastrointestinal tract.

10.
Biomedicines ; 11(1)2023 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-36672732

RESUMO

Cancer is one of the main causes of death worldwide. There are several different types of cancer recognized thus far, which can be treated by different approaches including surgery, radiotherapy, chemotherapy or a combination thereof. However, these approaches have certain drawbacks and limitations. Photodynamic therapy (PDT) is regarded as an alternative noninvasive approach for cancer treatment based on the generation of toxic oxygen (known as reactive oxygen species (ROS)) at the treatment site. PDT requires photoactivation by a photosensitizer (PS) at a specific wavelength (λ) of light in the vicinity of molecular oxygen (singlet oxygen). The cell death mechanisms adopted in PDT upon PS photoactivation are necrosis, apoptosis and stimulation of the immune system. Over the past few decades, the use of natural compounds as a photoactive agent for the selective eradication of neoplastic lesions has attracted researchers' attention. Many reviews have focused on the PS cell death mode of action and photonanomedicine approaches for PDT, while limited attention has been paid to the photoactivation of phytocompounds. Photoactivation is ever-present in nature and also found in natural plant compounds. The availability of various laser light setups can play a vital role in the discovery of photoactive phytocompounds that can be used as a natural PS. Exploring phytocompounds for their photoactive properties could reveal novel natural compounds that can be used as a PS in future pharmaceutical research. In this review, we highlight the current research regarding several photoactive phytocompound classes (furanocoumarins, alkaloids, poly-acetylenes and thiophenes, curcumins, flavonoids, anthraquinones, and natural extracts) and their photoactive potential to encourage researchers to focus on studies of natural agents and their use as a potent PS to enhance the efficiency of PDT.

11.
Crit Rev Food Sci Nutr ; 63(19): 3362-3385, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-34661483

RESUMO

Anthocyanins (ACNs) are notable hydrophilic compounds that belong to the flavonoid family, which are available in plants. They have excellent antioxidants, anti-obesity, anti-diabetic, anti-inflammatory, anticancer activity, and so on. Furthermore, ACNs can be used as a natural dye in the food industry (food colorant). On the other hand, the stability of ACNs can be affected by processing and storage conditions, for example, pH, temperature, light, oxygen, enzymes, and so on. These factors further reduce the bioavailability (BA) and biological efficacy of ACNs, as well as limit ACNs application in both food and pharmaceutics field. The stability and BA of ACNs can be improved via loading them in encapsulation systems including nanoemulsions, liposomes, niosomes, biopolymer-based nanoparticles, nanogel, complex coacervates, and tocosomes. Among all systems, biopolymer-based nanoparticles, nanohydrogels, and complex coacervates are comparatively suitable for improving the stability and BA of ACNs. These three systems have excellent functional properties such as high encapsulation efficiency and well-stable against unfavorable conditions. Furthermore, these carrier systems can be used for coating of other encapsulation systems (such as liposome). Additionally, tocosomes are a new system that can be used for encapsulating ACNs. ACNs-loaded encapsulation systems can improve the stability and BA of ACNs. However, further studies regarding stability, BA, and in vivo work of ACNs-loaded micro/nano-encapsulation systems could shed a light to evaluate the therapeutic efficacy including physicochemical stability, target mechanisms, cellular internalization, and release kinetics.


Assuntos
Antocianinas , Nanopartículas , Antocianinas/química , Disponibilidade Biológica , Nanopartículas/química , Antioxidantes/química , Lipossomos/química
12.
Biomedicines ; 10(12)2022 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-36551830

RESUMO

Severe acute respiratory syndrome (SARS)-CoV-2 from the family Coronaviridae is the cause of the outbreak of severe pneumonia, known as coronavirus disease 2019 (COVID-19), which was first recognized in 2019. Various potential antiviral drugs have been presented to hinder SARS-CoV-2 or treat COVID-19 disease. Side effects of these drugs are among the main complicated issues for patients. Natural compounds, specifically primary and secondary herbal metabolites, may be considered as alternative options to provide therapeutic activity and reduce cytotoxicity. Phenolic materials such as epigallocatechin gallate (EGCG, polyphenol) and quercetin have shown antibacterial, antifungal, antiviral, anticancer, and anti-inflammatory effects in vitro and in vivo. Therefore, in this study, molecular docking was applied to measure the docking property of epigallocatechin gallate and quercetin towards the transmembrane spike (S) glycoprotein of SARS-CoV-2. Results of the present study showed Vina scores of -9.9 and -8.3 obtained for EGCG and quercetin by CB-Dock. In the case of EGCG, four hydrogen bonds of OG1, OD2, O3, and O13 atoms interacted with the Threonine (THR778) and Aspartic acid (ASP867) amino acids of the spike glycoprotein (6VSB). According to these results, epigallocatechin gallate and quercetin can be considered potent therapeutic compounds for addressing viral diseases.

13.
Foods ; 11(23)2022 Dec 04.
Artigo em Inglês | MEDLINE | ID: mdl-36496721

RESUMO

Hydrocolloids are known as natural hydrophilic biopolymers that can contribute viscosity and gelation in solution, as well as nutritional benefits, thus, they are widely used in the food industry. In our work, hydrocolloid was isolated by aqueous extraction of Sesamum indicum seed at 80 °C and pH 8.0. The chemical composition and functional properties of Sesamum indicum seed hydrocolloid (SISH) were characterized, and the effects of concentration including 1%, 2%, and 3% as well as heating/cooling rate (1, 5, and 10 °C/min) on the rheological behavior of SISH dispersions in aqueous solution were investigated. The viscoelastic properties of SISH dispersions were characterized by small-amplitude oscillatory shear measurement. The resultant SISH consisted of 60.95% carbohydrate and 23.32% protein, and was thus endowed with a relatively high water-holding capacity, solubility, appropriate emulsifying and foaming properties. Rheological results revealed that the aqueous dispersion of SISH exhibited a non-Newtonian shear-thinning flow behavior. The viscoelastic moduli changes were found to be dependent on SISH concentration, temperature, and heating/cooling rate. Increasing SISH concentrations from 1% to 3% promoted the development of stronger cross-link network. The mechanical spectra derived from strain and frequency sweep measurements showed that the storage moduli were always higher than the loss moduli, and the loss tangent was calculated to be above 0.1 and below 1.0. Furthermore, both moduli had slight frequency dependency, and the complex viscosity exhibited an almost linear reduction with the increase of frequency. Therefore, SISH dispersion behaved as a weak gel-like system. The hysteresis of viscoelastic moduli during heating and cooling reduced with decreasing the heating-cooling rates from 10 to 1 °C/min, suggesting that SISH molecules had enough time to develop a stable and thermally irreversible network. Overall, SISH can be regarded as an acceptable hydrocolloid for generating natural food components with intriguing functional and rheological qualities in the formulation of microstructured goods.

16.
Nutrients ; 14(3)2022 Jan 20.
Artigo em Inglês | MEDLINE | ID: mdl-35276810

RESUMO

Iron deficiency in pregnancy is a major public health problem that causes maternal complications. The objective of this randomized, controlled trial was to examine the bioavailability, efficacy, and safety of oral ferrous bisglycinate plus folinic acid supplementation in pregnant women with iron deficiency. Subjects (12−16 weeks of gestation, n = 120) were randomly allocated to receive oral iron as ferrous bisglycinate (equiv. iron 24 mg) in supplement form with folinic acid and multivitamins (test group, n = 60) or as ferrous fumarate (equiv. iron 66 mg iron, control group, n = 60) after breakfast daily. Iron absorption was assessed by measuring fasted serum iron levels at 1 and 2 h immediately after supplementation. Hematological biomarkers and iron status were assessed before intervention, and at 3 and 6 months. Side effects were monitored throughout the intervention. A significant increase in serum iron was seen in both groups (p < 0.001) during the bioavailability assessment; however, the test group increases were comparatively higher than the control values at each timepoint (p < 0.001). Similarly, both test and control groups demonstrated a statistically significant increases in hemoglobin (Hb) (p < 0.001), erythrocytes (p < 0.001), reticulocytes (p < 0.001), mean corpuscular volume (MCV) (p < 0.001), mean corpuscular hemoglobin (MCH) (p < 0.001), mean corpuscular hemoglobin concentration (MCHC) (p < 0.001), % transferrin saturation (p < 0.001), and ferritin (p < 0.001) at 3 and 6 months after supplementation. However, in all cases, the test group increases were numerically larger than the control group increases at each timepoint. The test intervention was also associated with significantly fewer reports of nausea, abdominal pain, bloating, constipation, or metallic taste (p < 0.001). In conclusion, ferrous bisglycinate with folinic acid as a multivitamin nutraceutical format is comparable to standard ferrous fumarate for the clinical management of iron deficiency during pregnancy, with comparatively better absorption, tolerability, and efficacy and with a lower elemental iron dosage.


Assuntos
Anemia Ferropriva , Compostos Ferrosos , Deficiências de Ferro , Complicações na Gravidez , Anemia Ferropriva/sangue , Anemia Ferropriva/tratamento farmacológico , Biomarcadores/sangue , Feminino , Compostos Ferrosos/uso terapêutico , Glicina/uso terapêutico , Humanos , Deficiências de Ferro/sangue , Deficiências de Ferro/tratamento farmacológico , Leucovorina/uso terapêutico , Gravidez , Complicações na Gravidez/sangue , Complicações na Gravidez/tratamento farmacológico
17.
Food Chem ; 382: 132411, 2022 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-35158271

RESUMO

Recently, there has been a growing interest in novel food formulations and packaging materials using controlled release systems in order to enhance the functional performance of food bioactive ingredients and to prolong the shelf-life of food products. Correspondingly, numerous types of matrices (polymers, biopolymers, synthetic materials) could be implemented as carriers based on their compatibility with the bioactive ingredients and the type of releasing medium. A plethora of applications of controlled release can be identified in the pharmaceutical, agriculture, cosmetics, and particularly the food industries. Moreover, several physical and chemical stimuli are applied to regulate the release behavior of a bioactive molecule in the desired medium, which is under development. This review highlights the strategies applied to regulate the release rate of biopolymeric networks mainly including mixing of biopolymers, physical and chemical crosslinkers along with encapsulation systems, furthermore, the future prospects of release concept are discussed.


Assuntos
Polímeros , Biopolímeros/química , Composição de Medicamentos
18.
Int J Prev Med ; 12: 71, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34447513

RESUMO

BACKGROUND: The basis of prevention of non-communicable diseases is the identification of primary risk factors and the prevention and control of these factors. The purpose is to prevent the spread of the disease and to control it as much as possible. If population growth continues at this rate, by 2030, 52 million people will die from these diseases each year. The aim of this study was to evaluate the challenges of preventing non-communicable diseases. METHODS: The present study was a systematic review that conducted in July 2020 and the articles related to prevention of non-communicable diseases on databases of web of science, PubMed, Scopus, science direct, Ovid, Pro Quest and Google Scholar. Strategy for searching and selecting the articles was PRISMA Guidelines. RESULTS: Challenges of non-communicable disease prevention, in 4 main codes, including infrastructure, economic, demographic and management and 12 sub-codes that include, lack of preventive infrastructure, restrictions on access to medicine, restrictions on primary health care, restrictions on access to Technology, disease-oriented disease, unsustainable financial resources, failure to implement poverty reduction projects, increase in aging population, migration, rapid and unplanned urban planning, hasty planning and lack of internal and external coordination were classified. CONCLUSIONS: To reduce non-communicable diseases, strengthen global capacities, reduce risk factors for NCDs and place social determinants by creating health-promoting environments, strengthen health systems to implement prevention and control of NCDs, and place determinants Social can play an effective role through people-centered primary health care.

20.
Nanomaterials (Basel) ; 11(7)2021 Jun 29.
Artigo em Inglês | MEDLINE | ID: mdl-34209471

RESUMO

Resistance to temozolomide (TMZ) is the main cause of death in glioblastoma multiforme (GBM). The use of nanocarriers for drug delivery applications is one of the known approaches to overcome drug resistance. This study aimed to investigate the possible effect of selenium-chitosan nanoparticles loaded with TMZ on the efficacy of TMZ on the expression of MGMT, E2F6, and RELA genes and the rate of apoptosis in the C6 cell line. Selenium nanoparticles (SNPs) were loaded with TMZ and then they were coated by Eudragit® RS100 (Eud) and chitosan (CS) to prepare Se@TMZ/Eud-Cs. Physicochemical properties were determined by scanning electron microscope (SEM), energy-dispersive X-ray spectroscopy (EDAX), thermal gravimetric analysis (TGA), Fourier-transform infrared spectroscopy (FTIR), and dynamic light scattering (DLS) methods. Se@TMZ/Eud-Cs was evaluated for loading and release of TMZ by spectrophotometric method. Subsequently, SNPs loaded with curcumin (as a fluorophore) were analyzed for in vitro uptake by C6 cells. Cytotoxicity and apoptosis assay were measured by MTT assay and Annexin-PI methods. Finally, real-time PCR was utilized to determine the expression of MGMT, E2F6, and RELA genes. Se@TMZ/Eud-Cs was prepared with an average size of 200 nm as confirmed by the DLS and microscopical methods. Se@TMZ/Eud-Cs presented 82.77 ± 5.30 loading efficiency with slow and pH-sensitive release kinetics. SNPs loaded with curcumin showed a better uptake performance by C6 cells compared with free curcumin (p-value < 0.01). Coated nanoparticles loaded with TMZ showed higher cytotoxicity, apoptosis (p-value < 0.0001), and down-regulation of MGMT, E2F6, and RELA and lower IC50 value (p-value < 0.0001) than free TMZ and control (p-value < 0.0001) groups. Using Cs as a targeting agent in Se@TMZ/Eud-Cs system improved the possibility for targeted drug delivery to C6 cells. This drug delivery system enhanced the apoptosis rate and decreased the expression of genes related to TMZ resistance. In conclusion, Se@TMZ/Eud-Cs may be an option for the enhancement of TMZ efficiency in GBM treatment.

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