Hybrid Magnetic Lipid-Based Nanoparticles for Cancer Therapy.

Cancer is one of the major public health problems worldwide. Despite the advances in cancer therapy, it remains a challenge due to the low specificity of treatment and the development of multidrug resistance mechanisms. To overcome these drawbacks, several drug delivery nanosystems have been investigated, among them, magnetic nanoparticles (MNP), especially superparamagnetic iron oxide nanoparticles (SPION), which have been applied for treating cancer. MNPs have the ability to be guided to the tumor microenvironment through an external applied magnetic field. Furthermore, in the presence of an alternating magnetic field (AMF) this nanocarrier can transform electromagnetic energy in heat (above 42 °C) through Néel and Brown relaxation, which makes it applicable for hyperthermia treatment. However, the low chemical and physical stability of MNPs makes their coating necessary. Thus, lipid-based nanoparticles, especially liposomes, have been used to encapsulate MNPs to improve their stability and enable their use as a cancer treatment. This review addresses the main features that make MNPs applicable for treating cancer and the most recent research in the nanomedicine field using hybrid magnetic lipid-based nanoparticles for this purpose.

Polymeric Systems for Colon-specific Mesalazine Delivery in the Intestinal Bowel Diseases Management.

The anti-inflammatory 5-aminosalicylic acid (5-ASA) is the main therapeutic option used to prevent and treat inflammatory bowel diseases. The upper intestinal tract performs rapid and almost complete absorption of this drug when administered orally, making local therapeutic levels of the molecule in the inflamed colonic mucosa difficult to achieve. Micro and nanoparticle systems are promising for 5-ASA incorporation because the reduced dimensions of these structures can improve the drug's pharmacodynamics and contribute to more efficient and localized therapy. Together, the association of these systems with polymers will allow the release of 5-ASA through specific targeting mechanisms to the colon, as demonstrated in the mesalazine modified-release dosage form. This review will summarize and discuss the challenges for the oral administration of 5-ASA and the different colon-specific delivery strategies using polymers.

Development of New Natural Lipid-Based Nanoparticles Loaded with Aluminum-Phthalocyanine for Photodynamic Therapy against Melanoma.

Photodynamic therapy (PDT) mediated by photosensitizers loaded in nanostructures as solid lipid nanoparticles has been pinpointed as an effective and safe treatment against different skin cancers. Amazon butters have an interesting lipid composition when it comes to forming solid lipid nanoparticles (SLN). In the present report, a new third-generation photosensitizing system consisting of aluminum-phthalocyanine associated with Amazon butter-based solid lipid nanoparticles (SLN-AlPc) is described. The SLN was developed using murumuru butter, and a monodisperse population of nanodroplets with a hydrodynamic diameter of approximately 40 nm was obtained. The study of the permeation of these AlPc did not permeate the analyzed skin, but when incorporated into the system, SLN-AlPc allowed permeation of almost 100% with 8 h of contact. It must be emphasized that SLN-AlPc was efficient for carrying aluminum-phthalocyanine photosensitizers and exhibited no toxicity in the dark. Photoactivated SLN-AlPc exhibited a 50% cytotoxicity concentration (IC50) of 19.62 nM when applied to B16-F10 monolayers, and the type of death caused by the treatment was apoptosis. The exposed phospholipid phosphatidylserine was identified, and the treatment triggered a high expression of Caspase 3. A stable Amazon butter-based SLN-AlPc formulation was developed, which exhibits strong in vitro photodynamic activity on melanoma cells.

Targeted Liposomes: A Nonviral Gene Delivery System for Cancer Therapy.

Cancer is the second most frequent cause of death worldwide, with 28.4 million new cases expected for 2040. Despite de advances in the treatment, it remains a challenge because of the tumor heterogenicity and the increase in multidrug resistance mechanisms. Thus, gene therapy has been a potential therapeutic approach owing to its ability to introduce, silence, or change the content of the human genetic code for inhibiting tumor progression, angiogenesis, and metastasis. For the proper delivery of genes to tumor cells, it requires the use of gene vectors for protecting the therapeutic gene and transporting it into cells. Among these vectors, liposomes have been the nonviral vector most used because of their low immunogenicity and low toxicity. Furthermore, this nanosystem can have its surface modified with ligands (e.g., antibodies, peptides, aptamers, folic acid, carbohydrates, and others) that can be recognized with high specificity and affinity by receptor overexpressed in tumor cells, increasing the selective delivery of genes to tumors. In this context, the present review address and discuss the main targeting ligands used to functionalize liposomes for improving gene delivery with potential application in cancer treatment.

Characteristics, Properties and Analytical/Bioanalytical Methods of 5-Aminosalicylic Acid: A Review.

Five-aminosalicylic acid (5-ASA) is an anti-inflammatory drug indicated in the treatment of inflammatory bowel diseases such as ulcerative colitis and Crohn's disease. Among the analytical methods of quantification of 5-ASA described in the literature, the High Efficiency Liquid Chromatography stands out, a sensitive technique but with a high cost. In recent years, alternative methods have been developed, presenting efficiency and reduced cost, such as UV/visible spectrophotometric, spectrofluorescent, and electrochemical methods, techniques recommended for the application in quality control and quantification of 5-ASA in pharmaceutical forms and biological fluids. This article aims to review the physicochemical characteristics, pharmacokinetics, mechanisms of action, controlled release systems, and the different analytical and bioanalytical methods for the quantification of 5-ASA.

Highlights in targeted nanoparticles as a delivery strategy for glioma treatment.

Glioma is the most common type of Central Nervous System (CNS) neoplasia and it arises from glial cells. As glial cells are formed by different types of cells, glioma can be classified according to the cells that originate it or the malignancy grade. Glioblastoma multiforme is the most common and aggressive glioma. The high lethality of this tumor is related to the difficulty in performing surgical removal, chemotherapy, and radiotherapy in the CNS. To improve glioma treatment, a wide range of chemotherapeutics have been encapsulated in nanosystems to increase their ability to overcome the blood-brain barrier (BBB) and specifically reach the tumoral cells, reducing side effects and improving drug concentration in the tumor microenvironment. Several studies have investigated nanosystems covered with targeting ligands (e.g., proteins, peptides, aptamers, folate, and glucose) to increase the ability of drugs to cross the BBB and enhance their specificity to glioma through specific recognition by receptors on BBB and glioma cells. This review addresses the main targeting ligands used in nanosystems to overcome the BBB and promote the active targeting of drugs for glioma. Furthermore, the advantages of using these molecules in glioma treatment are discussed.

Highlights in poloxamer-based drug delivery systems as strategy at local application for vaginal infections.

Infectious diseases related to the vagina include diseases caused by the imbalance of the vaginal flora and by sexually transmitted infections. Some of these present themselves as a public health problem due to the lack of efficient treatment that leads to their complete cure, and others due to the growing resistance to drugs used in therapy. In this sense, new treatment strategies are desirable, with vaginal administration rout being a great choice since can bypass first-pass metabolism and decrease drug interactions and adverse effects. However, it is worth highlighting limitations related to patient's discomfort at application time. Thereby, the use of poloxamer-based drug delivery systems is desirable due its stimuli-sensitive characteristic. Therefore, the present review reports a brief overview of poloxamer properties, biological behavior and advances in poloxamer applications in controlled drug release systems for infectious diseases related to the vagina treatment and prevention.

Nanosystem functionalization strategies for prostate cancer treatment: a review.

Prostate cancer (PC) has a high morbidity and mortality rate worldwide, and the current clinical guidelines can vary depending on the stage of the disease. Drug delivery nanosystems (DDNs) can improve biopharmaceutical properties of encapsulated anti-cancer drugs by modulating their release kinetics, improving physicochemical stability and reducing toxicity. DDN can also enhance the ability of specific targeting through surface modification by coupling ligands (antibodies, nucleic acids, peptides, aptamer, proteins), thus favouring the cell internalisation process by endocytosis. The purposes of this review are to describe the limitations in the treatment of PC, explore different functionalization such as polymeric, lipid and inorganic nanosystems aimed at the treatment of PC, and demonstrate the improvement of this modification for an active target, as alternative and promising candidates for new therapies.

Nanotechnology as a tool for detection and treatment of arbovirus infections.

Arboviruses are medically important viruses that cause high rates of infection all over the world. In addition, the severity of the symptoms and the inadequate diagnostic methods represent a challenge far beyond eradicating the vector. The lack of specific treatments for arbovirus infections reflects the imminent need for new research for safe and efficient medicines to treat these infections. Nanotechnology is an innovative approach currently used as a platform for developing new treatments, thus improving the biopharmaceutical properties of drugs. It can also be applied to the development of diagnostic devices, improving their detection capacity. The purpose of this paper is to review recent research on the use of nanotechnology for developing new treatments and detection devices for arbovirus infections. Interestingly, it was found that only a few studies report on the use of nanotechnology to treat arbovirus infections and that most of these reports focus on the fabrication of diagnostic tools. Also, some papers report on the use of nanotechnology for the development of vaccines, which in association with mosquito eradication programs could effectively reduce the high rates of infections by these viruses.

Drug Delivery Nanosystems in Glioblastoma Multiforme Treatment: Current State of the Art.

Glioblastoma multiforme (GBM) is the most common primary malignant Central Nervous System cancer, responsible for about 4% of all deaths associated with neoplasia, characterized as one of the fatal human cancers. Tumor resection does not possess curative character, thereby radio and/or chemotherapy are often necessary for the treatment of GBM. However, drugs used in GBM chemotherapy present some limitations, such as side effects associated with non-specific drug biodistribution as well as limited bioavailability, which limits their clinical use. To attenuate the systemic toxicity and overcome the poor bioavailability, a very attractive approach is drug encapsulation in drug delivery nanosystems. The main focus of this review is to explore the actual cancer global problem, enunciate barriers to overcome in the pharmacological treatment of GBM, as well as the most updated drug delivery nanosystems for GBM treatment and how they influence biopharmaceutical properties of anti-GBM drugs. The discussion will approach lipid-based and polymeric nanosystems, as well as inorganic nanoparticles, regarding their technical aspects as well as biological effects in GBM treatment. Furthermore, the current state of the art, challenges to overcome and future perspectives in GBM treatment will be discussed.

Antimicrobial effect of anacardic acid-loaded zein nanoparticles loaded on Streptococcus mutans biofilms.

Bacterial biofilms play a key role in the pathogenesis of major oral diseases. Nanoparticles open new paths for drug delivery in complex structures such as biofilms. This study evaluated the antimicrobial effect of zein nanoparticles containing anacardic acid (AA) extracted from cashew shells of Anacardium occidentale on in vitro Streptococcus mutans biofilm formation and mature biofilms. The minimum inhibitory concentration (MIC), minimum bacterial concentration (MBC), and antibiofilm assays were performed. Streptococcus mutans UA159 biofilms were formed on saliva-coated hydroxyapatite disk for 5 days. To evaluate the preventive effect on biofilm formation, before contact with the inoculum, the disks were immersed once for 2 min in (1) hydroethanolic solution; (2) blank zein nanoparticles; (3) zein nanoparticles containing AA; and (4) 0.12% chlorhexidine gluconate. To determine the effect against mature biofilms, the disks containing 5-day preformed biofilms were further treated using the same procedure. The bacterial viability and dry weight were determined for both assays and used to compare the groups using ANOVA followed by Tukey's test (p < 0.05). Both MIC and MBC for AA-loaded zein nanoparticles were 0.36 µg/mL. Groups 3 and 4 were very effective in inhibiting S. mutans biofilm formation, as no colony-forming units were detected. In contrast, for mature biofilms, no difference in bacterial viability (p = 0.28) or dry weight (p = 0.09) was found between the treatments. Therefore, the AA-based nanoformulation presented very high inhibitory and bactericidal activities against planktonic S. mutans, and the results indicate a strong antiplaque effect. However, the formulation showed no antimicrobial effect on the established biofilm.