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1.
Adv Healthc Mater ; : e2400506, 2024 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-38712468

RESUMO

Curcumin is a natural product found in the rhizome of Curcuma longa (L) and other Curcuma spp. As a lipophilic molecule, it has greater affinity for polar, non-polar, alkaline or extremely acidic organic solvents. Several studies indicate that curcumin has several benefits for human health, for example, against degenerative diseases, cancer and infectious diseases. To obtain a quality product with nutraceutical properties, it is necessary to know its physicochemical characteristics and preserve it from cultivation until ingestion by the human. However, its low solubility leads to low absorption, in this context, nanotechnological systems can contribute to increase curcumin bioavailability. This review aims to highlight important issues in all stages that curcumin goes through: from aspects related to its extraction, to its association with nanotechnology. Although curcumin extraction process is already well established, it is possible to observe that more and more research focused on increasing yield and being more environmentally friendly. Furthermore, curcumin's low absorption is notable due to its physicochemical characteristics, mainly due to its low aqueous solubility. However, its association with nanotechnology has shown to be promising and an increasingly growing trend, since the use of this "Indian solid gold" is the hope of many patients. This article is protected by copyright. All rights reserved.

2.
Eur J Pharm Biopharm ; 199: 114280, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38588828

RESUMO

Helicobacter pylori (H. pylori) is a microorganism directly linked to severe clinical conditions affecting the stomach. The virulence factors and its ability to form biofilms increase resistance to conventional antibiotics, growing the need for new substances and strategies for the treatment of H. pylori infection. The trans-resveratrol (RESV), a bioactive polyphenol from natural sources, has a potential activity against this gastric pathogen. Here, Chitosan nanoparticles (NP) containing RESV (RESV-NP) were developed for H. pylori management. The RESV-NP were prepared using the ionic gelation method and characterized by Dynamic Light Scattering (DLS), Nanoparticle Tracking Analysis (NTA) and, Cryogenic Transmission Electron Microscopy (Cryo - TEM). The encapsulation efficiency (EE) and in vitro release rate of RESV were quantified using high-performance liquid chromatography (HPLC). RESV-NP performance against H. pylori was evaluated by the quantification of the minimum inhibitory/bactericidal concentrations (MIC/MBC), time to kill, alterations in H. pylori morphology in its planktonic form, effects against H. pylori biofilm and in an in vitro infection model. RESV-NP cytotoxicity was evaluated against AGS and MKN-74 cell lines and by hemolysis assay. Acute toxicity was tested using Galleria mellonella model assays. RESV-NP showed a spherical shape, size of 145.3 ± 24.7 nm, polydispersity index (PDI) of 0.28 ± 0.008, and zeta potential (ZP) of + 16.9 ± 1.81 mV in DLS, while particle concentration was 3.12 x 1011 NP/mL (NTA). RESV-NP EE was 72 %, with full release within the first 5 min. In microbiological assays, RESV-NP presented a MIC/MBC of 3.9 µg/mL, a time to kill of 24 h for complete eradication of H. pylori. At a concentration of 2xMIC (7.8 µg/mL), RESV-NP completely eradicated the H. pylori biofilm, and in an in vitro infection model, RESV-NP (4xMIC - 15.6 µg/mL) showed a significant decrease in bacterial load (1 Log10CFU/mL) when compared to the H. pylori J99 control. In addition, they did not demonstrate a toxic character at MIC concentration for both cell lines. The use of the RESV-NP with mucoadhesion profile is an interesting strategy for oral administration of substances targeting gastric disorders, linked to H. pylori infections.


Assuntos
Antibacterianos , Biofilmes , Quitosana , Infecções por Helicobacter , Helicobacter pylori , Testes de Sensibilidade Microbiana , Nanopartículas , Resveratrol , Resveratrol/administração & dosagem , Resveratrol/farmacologia , Helicobacter pylori/efeitos dos fármacos , Quitosana/química , Nanopartículas/química , Infecções por Helicobacter/tratamento farmacológico , Infecções por Helicobacter/microbiologia , Biofilmes/efeitos dos fármacos , Antibacterianos/farmacologia , Antibacterianos/administração & dosagem , Humanos , Animais , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Estilbenos/farmacologia , Estilbenos/administração & dosagem , Estilbenos/química , Tamanho da Partícula
3.
Int J Biol Macromol ; 263(Pt 1): 130272, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38373560

RESUMO

Bevacizumab (BVZ) was the first monoclonal antibody approved by the FDA and has shown an essential advance in the antitumor therapy of colorectal cancer (CRC), however, the systemic action of BVZ administered intravenously can trigger several adverse effects. The working hypothesis of the study was to promote the modulation of the mucoadhesion properties and permeability of the BVZ through the formation of nanoparticles (NPs) with gellan gum (GG) with subsequent surface modification with chitosan (CS). NPs comprising BVZ and GG were synthesized through polyelectrolyte complexation, yielding spherical nanosized particles with an average diameter of 264.0 ± 2.75 nm and 314.0 ± 0.01 nm, polydispersity index of 0.182 ± 0.01 e 0.288 ± 0.01, and encapsulation efficiency of 29.36 ± 0.67 e 60.35 ± 0.27 mV, for NPs without (NP_BVZ) and with surface modification (NP_BVZ + CS). The results showed a good ability of nanoparticles with surface modification to modulate the NPs biological properties.


Assuntos
Quitosana , Nanopartículas , Polissacarídeos Bacterianos , Portadores de Fármacos , Bevacizumab/farmacologia
4.
Pharmaceuticals (Basel) ; 16(12)2023 Nov 29.
Artigo em Inglês | MEDLINE | ID: mdl-38139786

RESUMO

Melanoma, a severe form of skin cancer intricately linked to genetic and environmental factors, is predicted to reach 100,000 new cases worldwide by 2040, underscoring the need for effective and safe treatment options. In this study, we assessed the efficacy of a photosensitizer called Chlorophyll A (Chl-A) incorporated into hydrogels (HGs) made of chitosan (CS) and poloxamer 407 (P407) for Photodynamic Therapy (PDT) against the murine melanoma cell line B16-F10. The HG was evaluated through various tests, including rheological studies, SEM, and ATR-FTIR, along with cell viability assays. The CS- and P407-based HGs effectively released Chl-A and possessed the necessary properties for topical application. The photodynamic activity of the HG containing Chl-A was evaluated in vitro, demonstrating high therapeutic potential, with an IC50 of 25.99 µM-an appealing result when compared to studies in the literature reporting an IC50 of 173.8 µM for cisplatin, used as a positive control drug. The developed formulation of CS and P407-based HG, serving as a thermosensitive system for topical applications, successfully controlled the release of Chl-A. In vitro cell studies associated with PDT exhibited potential against the melanoma cell line.

5.
Crit Rev Anal Chem ; : 1-9, 2023 Nov 22.
Artigo em Inglês | MEDLINE | ID: mdl-37990513

RESUMO

The drug rapamycin is a potent inhibitor of the mTOR complex, acting directly in the signaling cascade of this protein complex; interrupting cell proliferation, in addition to being an extremely efficient immunosuppressant. Currently this drug is being used in several types of cancer. Rapamycin has been a target of great interest within nanomedicine involving nanostructured systems for drug delivery aiming to increase the bioactivity and bioavailability of this drug. In addition, there is a constant search for analytical methods to identify and quantify this drug. Numerous high-performance liquid chromatography analytical techniques, mass spectrometry and immunoassay techniques have been employed efficiently in an attempt to develop increasingly sensitive analytical methods. Thus, this review sought to bring together current and relevant scientific works involving rapamycin and; besides analytical methods more used for quantification of this molecule.

6.
Curr Drug Deliv ; 2023 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-38013438

RESUMO

Glioblastoma multiforme is the most common and aggressive malignant tumor that affects the central nervous system, with high mortality and low survival. Glioblastoma multiforme treatment includes resection tumor surgery, followed by radiotherapy and chemotherapy adjuvants. However, the drugs used in chemotherapy present some limitations, such as the difficulty of crossing the bloodbrain barrier and resisting the cellular mechanisms of drug efflux. The use of polymeric nanoparticles has proven to be an effective alternative to circumvent such limitations, as it allows the exploration of a range of polymeric structures that can be modified in order to control the biodistribution and cytotoxic effect of the drug delivery systems. Nanoparticles are nanometric in size and allow the incorporation of targeting ligands on their surface, favoring the transposition of the blood-brain barrier and the delivery of the drug to specific sites, increasing the selectivity and safety of chemotherapy. The present review has described the characteristics of chitosan, poly(vinyl alcohol), poly(lactic-coglycolic acid), poly(ethylene glycol), poly(ß-amino ester), and poly(ε-caprolactone), which are some of the most commonly used polymers in the manufacture of nanoparticles for the treatment of glioblastoma multiforme. In addition, some of the main targeting ligands used in these nanosystems are presented, such as transferrin, chlorotoxin, albumin, epidermal growth factor, and epidermal growth factor receptor blockers, explored for the active targeting of antiglioblastoma agents.

7.
Photodiagnosis Photodyn Ther ; 44: 103858, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37898262

RESUMO

Cyclodextrins (CDs) are molecules approved by the FDA and show promise in increasing the solubility of hydrophobic molecules and making them more available to the skin. These CDs have been used to form complexes with some photosensitizers for Photodynamic Therapy (PDT), such as Hypericin (HY). HY is a lipophilic photosensitizer known for its exceptional fluorescence and singlet oxygen quantum yield generation of over 20 % under 590 nm irradiation. In this study, we found a six-fold increase in the release of HY in vitro after complexation with ß-CD. The ß-CDHY assembly also demonstrated better skin retention, which is crucial for the topical application of this photosensitizer. Furthermore, the ß-CD complexation led to a significant increase in the phototoxicity of HY at three different light doses (3, 6, and 10 J cm-2) due to its improved water solubility and higher in vitro accumulation (approximately two times compared with free HY) in HeLa and Vero cell lines.


Assuntos
Perileno , Fotoquimioterapia , Humanos , Fármacos Fotossensibilizantes/uso terapêutico , Fotoquimioterapia/métodos , Perileno/farmacologia , Perileno/química , Células HeLa
8.
Carbohydr Polym ; 320: 121257, 2023 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-37659830

RESUMO

Despite advances in new approaches for colorectal cancer (CRC) therapy, intravenous chemotherapy remains one of the main treatment options; however, it has limitations associated with off-target toxicity, tumor cell resistance due to molecular complexity and CRC heterogeneity, which lead to tumor recurrence and metastasis. In oncology, nanoparticle-based strategies have been designed to avoid systemic toxicity and increase drug accumulation at tumor sites. Hyaluronic acid (HA) has obtained significant attention thanks to its ability to target nanoparticles (NPs) to CRC cells through binding to cluster-determinant-44 (CD44) and hyaluronan-mediated motility (RHAMM) receptors, along with its efficient biological properties of mucoadhesion. This review proposes to discuss the state of the art in HA-based nanoparticulate systems intended for localized treatment of CRC, highlighting the importance of the mucoadhesion and active targeting provided by this polymer. In addition, an overview of CRC will be provided, emphasizing the importance of CD44 and RHAMM receptors in this type of cancer and the current challenges related to this disease, and important concepts about the physicochemical and biological properties of HA will also be addressed. Finally, this review aims to contribute to the advancement of accuracy treatment of CRC by the design of new platforms based on by HA.


Assuntos
Neoplasias Colorretais , Nanopartículas , Humanos , Ácido Hialurônico , Oncologia , Polímeros , Neoplasias Colorretais/tratamento farmacológico
9.
Photodiagnosis Photodyn Ther ; 44: 103739, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37582452

RESUMO

Oral cancer is one of the most prevalent types of cancer head and neck cancers worldwide. Photodynamic therapy (PDT) has demonstrated great potential against cancers, reducing long-term morbidity. In this study, we investigated the incorporation of methylene blue (MB) in a mucoadhesive liquid crystal precursor system (LCPS) for oral cancer treatment. The photostability and the in vitro release, permeation, and retention profile of MB-loaded LCPS (MB-LCPS) were investigated, as well as its in vitro PDT activity against normal (HaCaT) and tumoral (HSC-3) cell lines. LCPS increased the photostability of MB and exhibited a prolonged release profile of MB. In addition, LCPS increased the retention of MB in the porcine esophageal mucosa by around 3 times higher than the MB solution. The retention of MB in LCPS was around 2 times greater than its permeability, which is suitable for guaranteeing the maintenance of the therapy in the oral cavity. In vitro cytotoxicity assay indicated that MB-LCPS increased the antitumoral activity of MB after 20 min of irradiation at 660 nm and 12.5 J/cm2. The results obtained suggest that the developed formulation is an interesting strategy for the potential application in the treatment of oral cancer by PDT.


Assuntos
Cristais Líquidos , Neoplasias Bucais , Fotoquimioterapia , Animais , Suínos , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes , Azul de Metileno , Neoplasias Bucais/tratamento farmacológico
10.
Microorganisms ; 11(7)2023 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-37512799

RESUMO

Candida auris is an emerging yeast of worldwide interest due to its antifungal resistance and mortality rates. The aim of this study was to analyse the in vitro and in vivo antifungal activity of a nanoemulsion loaded with amphotericin B (NEA) against planktonic cells and biofilm of C. auris clinical isolates belonging to four different clades. In vivo assays were performed using the Galleria mellonella model to analyse antifungal activity and histopathological changes. The in vitro results showed that NEA exhibited better antifungal activity than free amphotericin B (AmB) in both planktonic and sessile cells, with >31% inhibition of mature biofilm. In the in vivo assays, NEA demonstrated superior antifungal activity in both haemolymph and tissue. NEA reduced the fungal load in the haemolymph more rapidly and with more activity in the first 24 h after infection. The histological analysis of infected larvae revealed clusters of yeast, immune cells, melanisation, and granulomas. In conclusion, NEA significantly improved the in vitro and in vivo antifungal activity of AmB and could be considered a promising therapy for C. auris infections.

11.
Photodiagnosis Photodyn Ther ; 43: 103725, 2023 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-37500031

RESUMO

In our previous studies, Chlorin-e6 (Ce6) demonstrated a significant reduction of microorganisms' viability against multi-species biofilm related to periodontitis while irradiated with blue light. However, the conjugation of Ce6 and antimicrobial peptides, and the incorporation of this photosensitizer in a nanocarrier, is still poorly explored. We hypothesized that chlorin-e6 conjugated to the antimicrobial peptide LL-37 loaded nanoemulsion could inhibit a multi-species biofilm related to periodontitis during photodynamic therapy (PDT), the pre-treatment with hydrogen peroxide was also tested. The nanoemulsion (NE) incorporated with Ce6 was characterized regarding the physiochemical parameters. Images were obtained by transmission electron microscopy (TEM) and scanning electron microscopy (SEM). Later, the Ce6 and LL-37 incorporated in NE was submitted to UV-Vis analysis and Reactive Oxygen Species (ROS) assay. Finally, the combined formulation (Ce6+LL-37 in nanoemulsion) was tested against multi-species biofilm related to periodontitis. The formed nanoformulation was kinetically stable, optically transparent with a relatively small droplet diameter (134.2 unloaded and 146.9 loaded), and weak light scattering. The NE system did not impact the standard UV-VIS spectra of Ce6, and the ROS production was improved while Ce6 was incorporated in the NE. The combination of Ce6 and LL-37 in NE was effective to reduce the viability of all bacteria tested. The treatment with hydrogen peroxide previous to PDT significantly impacted bacterial viability. The current aPDT regimen was the best already tested against periodontal biofilm by our research team. Our results suggest that this combined protocol must be exploited for clinical applications in localized infections such as periodontal disease. - Nanoemulsion demonstrated to be an excellent nanocarrier for photodynamic application. - Chlorin-e6 incorporated in nanoemulsion showed great physicochemical and biophotonic parameters. - The combination of chlorin-e6 and LL-37 peptide in nanoemulsion is effective to eliminate periodontal pathogenic bacteria. - The treatment with hydrogen peroxide previous to PDT significantly impacted bacterial viability.


Assuntos
Clorofilídeos , Periodontite , Fotoquimioterapia , Porfirinas , Humanos , Fármacos Fotossensibilizantes/farmacologia , Catelicidinas , Fotoquimioterapia/métodos , Peptídeos Antimicrobianos , Espécies Reativas de Oxigênio/metabolismo , Peróxido de Hidrogênio , Periodontite/tratamento farmacológico , Biofilmes , Linhagem Celular Tumoral
12.
Artigo em Inglês | MEDLINE | ID: mdl-37282638

RESUMO

BACKGROUND: Ruthenium complexes have shown promise in treating many cancers, including breast cancer. Previous studies of our group have demonstrated the potential of the trans-[Ru(PPh3)2(N,N-dimethylN'-thiophenylthioureato-k2O,S)(bipy)]PF6 complex, the Ru(ThySMet), in the treatment of breast tumor cancers, both in 2D and 3D culture systems. Additionally, this complex presented low toxicity when tested in vivo. AIMS: Improve the Ru(ThySMet) activity by incorporating the complex into a microemulsion (ME) and testing its in vitro effects. METHODS: The ME-incorporated Ru(ThySMet) complex, Ru(ThySMet)ME, was tested for its biological effects in two- (2D) and three-dimensional (3D) cultures using different types of breast cells, MDA-MB-231, MCF-10A, 4T1.13ch5T1 and Balb/C 3T3 fibroblasts. RESULTS: An increased selective cytotoxicity of the Ru(ThySMet)ME for tumor cells was found in 2D cell culture, compared with the original complex. This novel compound also changed the shape of tumor cells and inhibited cell migration with more specificity. Additional 3D cell culture tests using the non-neoplastic S1 and the triple-negative invasive T4-2 breast cells have shown that Ru(ThySMet)ME presented increased selective cytotoxicity for tumor cells compared with the 2D results. The morphology assay performed in 3D also revealed its ability to reduce the size of the 3D structures and increase the circularity in T4-2 cells. CONCLUSION: These results demonstrate that the Ru(ThySMet)ME is a promising strategy to increase its solubility, delivery, and bioaccumulation in target breast tumors.

13.
Expert Opin Drug Deliv ; 20(6): 831-849, 2023 06.
Artigo em Inglês | MEDLINE | ID: mdl-37259517

RESUMO

INTRODUCTION: Skin cancer is the most common form of cancer worldwide, with increasing incidence rates in recent years. Although conventional chemotherapy and radiation therapy have been used for its treatment, these therapies have several limitations such as lack of selectivity and significant side effects. Targeted nanocarriers have emerged as a promising approach for the treatment of skin cancer. AREAS COVERED: This review article provides an overview of targeted nanocarriers for skin cancer treatment. It covers the various types of targeted nanocarriers, including liposomes, polymeric nanoparticles, dendrimers, and inorganic nanoparticles. EXPERT OPINION: There are still several challenges that need to be addressed before the clinical translation of targeted nanoparticles, such as optimization of their properties, development of reliable and robust characterization methods, and evaluation of their safety and efficacy in clinical trials. Another key aspect for the advancement of these studies is the need to improve regulatory aspects related to the toxicity and regulation of nanomedicines targeting skin cancer. Overall, targeted nanocarriers hold great potential for the development of safe and effective treatments for skin cancer, which can contribute to a better prognosis and overall patients' life quality.


Assuntos
Nanopartículas , Neoplasias Cutâneas , Humanos , Portadores de Fármacos , Sistemas de Liberação de Medicamentos , Neoplasias Cutâneas/tratamento farmacológico , Pele , Lipossomos
14.
Mater Today Bio ; 20: 100671, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37273792

RESUMO

Gliomas are the most common type of brain cancer, and among them, glioblastoma multiforme (GBM) is the most prevalent (about 60% of cases) and the most aggressive type of primary brain tumor. The treatment of GBM is a major challenge due to the pathophysiological characteristics of the disease, such as the presence of the blood-brain barrier (BBB), which prevents and regulates the passage of substances from the bloodstream to the brain parenchyma, making many of the chemotherapeutics currently available not able to reach the brain in therapeutic concentrations, accumulating in non-target organs, and causing considerable adverse effects for the patient. In this scenario, nanocarriers emerge as tools capable of improving the brain bioavailability of chemotherapeutics, in addition to improving their biodistribution and enhancing their uptake in GBM cells. This is possible due to its nanometric size and surface modification strategies, which can actively target nanocarriers to elements overexpressed by GBM cells (such as transmembrane receptors) related to aggressive development, drug resistance, and poor prognosis. In this review, an overview of the most frequently overexpressed receptors in GBM cells and possible approaches to chemotherapeutic delivery and active targeting using nanocarriers will be presented.

15.
J Funct Biomater ; 14(6)2023 Jun 11.
Artigo em Inglês | MEDLINE | ID: mdl-37367283

RESUMO

Piperine (PIP), a compound found in Piper longum, has shown promise as a potential chemotherapeutic agent for breast cancer. However, its inherent toxicity has limited its application. To overcome this challenge, researchers have developed PIP@MIL-100(Fe), an organic metal-organic framework (MOF) that encapsulates PIP for breast cancer treatment. Nanotechnology offers further treatment options, including the modification of nanostructures with macrophage membranes (MM) to enhance the evasion of the immune system. In this study, the researchers aimed to evaluate the potential of MM-coated MOFs encapsulated with PIP for breast cancer treatment. They successfully synthesized MM@PIP@MIL-100(Fe) through impregnation synthesis. The presence of MM coating on the MOF surface was confirmed through SDS-PAGE analysis, which revealed distinct protein bands. Transmission electron microscopy (TEM) images demonstrated the existence of a PIP@MIL-100(Fe) core with a diameter of around 50 nm, surrounded by an outer lipid bilayer layer measuring approximately 10 nm in thickness. Furthermore, the researchers evaluated the cytotoxicity indices of the nanoparticles against various breast cancer cell lines, including MCF-7, BT-549, SKBR-3, and MDA. The results demonstrated that the MOFs exhibited between 4 and 17 times higher cytotoxicity (IC50) in all four cell lines compared to free PIP (IC50 = 193.67 ± 0.30 µM). These findings suggest that MM@PIP@MIL-100(Fe) holds potential as an effective treatment for breast cancer. The study's outcomes highlight the potential of utilizing MM-coated MOFs encapsulated with PIP as an innovative approach for breast cancer therapy, offering improved cytotoxicity compared to free PIP alone. Further research and development are warranted to explore the clinical translation and optimize the efficacy and safety of this treatment strategy.

16.
Nanomedicine (Lond) ; 18(7): 633-647, 2023 03.
Artigo em Inglês | MEDLINE | ID: mdl-37183804

RESUMO

Nanomedicines have been investigated for delivering drugs to tumors due to their ability to accumulate in the tumor tissues. 2D in vitro cell culture has been used to investigate the antitumoral potential of nanomedicines. However, a 2D model cannot adequately mimic the in vivo tissue conditions because of the lack of cell-cell interaction, a gradient of nutrients and the expression of genes. To overcome this limitation, 3D cell culture models have emerged as promising platforms that better replicate the complexity of native tumors. For this purpose, different techniques can be used to produce 3D models, including scaffold-free, scaffold-based and microfluidic-based models. This review addresses the principles, advantages and limitations of these culture methods for evaluating the antitumoral efficacy of nanomedicines.


Assuntos
Neoplasias , Esferoides Celulares , Humanos , Nanomedicina , Neoplasias/tratamento farmacológico , Neoplasias/patologia , Técnicas de Cultura de Células/métodos , Microfluídica
17.
Nanomedicine (Lond) ; 18(10): 789-801, 2023 04.
Artigo em Inglês | MEDLINE | ID: mdl-37199266

RESUMO

Aims: The development of rapamycin (RAP) and resveratrol (RSV) coloaded liposomes (RAP-RSV-LIP) for breast cancer therapy. Materials & methods: Liposomes were prepared using a high-pressure homogenization technique and evaluated according to their physicochemical characteristics, cellular uptake and cytotoxicity against tumoral and normal cells. Results & conclusion: The RAP-RSV-LIP showed negative surface charge, size around 100 nm, low polydispersity and high encapsulation efficiency for RAP and RSV (58.87 and 63.22%, respectively). RAP-RSV-LIP showed great stability over 60 days and a prolonged drug-release profile. In vitro studies indicated that RAP-RSV-LIP were internalized in an estrogen receptor-positive human breast cancer cell line (MCF-7, 34.2%) and improved cytotoxicity when compared with free drugs. Therefore RAP-RSV-LIP showed great antitumoral potential against breast cancer cells.


Assuntos
Neoplasias da Mama , Lipossomos , Humanos , Feminino , Resveratrol/farmacologia , Lipossomos/uso terapêutico , Sirolimo/farmacologia , Sirolimo/uso terapêutico , Neoplasias da Mama/tratamento farmacológico , Antioxidantes/uso terapêutico , Linhagem Celular Tumoral
18.
Colloids Surf B Biointerfaces ; 226: 113309, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-37054466

RESUMO

Glioblastoma multiforme is the most common and most aggressive human brain cancer. GBM treatment is still a challenge because many drugs are not able to cross the blood-brain barrier, in addition to the increasing resistance to currently available chemotherapy. New therapeutic alternatives are emerging, and, in this context, we highlight kaempferol, a flavonoid with remarkable anti-tumor activity but with limited bioavailability due to its strong lipophilic property. A promising tool to improve the biopharmaceutical properties of molecules such as kaempferol is the use of drug-delivery nanosystems, such as nanostructured lipid carriers (NLC), which can facilitate the dispersion and delivery of highly lipophilic molecules. The present work aimed at the development and characterization of kaempferol-loaded NLC (K-NLC) and the evaluation of its biological properties using in vitro models. The K-NLC showed an average size of 120 nm, zeta potential of - 21 mV, and polydispersity index of 0.099. The K-NLC presented high kaempferol encapsulation efficiency (93%), a drug loading of 3.58%, and a sustained kaempferol release profile for up to 48 h. In addition to presenting a 7-fold increase in kaempferol cytotoxicity, its encapsulation in NLC promoted a cellular uptake of 75%, which corroborates with increased cytotoxicity in U-87MG cells, as observed. Together, these data reinforce the promising antineoplastic properties of kaempferol in addition to the key role of NLC as a platform for the efficient delivery of lipophilic drugs to neoplastic cells, which improved their uptake and therapeutic efficacy in glioblastoma multiforme cells.


Assuntos
Glioblastoma , Nanoestruturas , Humanos , Lipídeos , Glioblastoma/tratamento farmacológico , Quempferóis/farmacologia , Portadores de Fármacos , Tamanho da Partícula
19.
Pharmaceutics ; 15(3)2023 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-36986612

RESUMO

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.

20.
Photodiagnosis Photodyn Ther ; 42: 103322, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-36773754

RESUMO

New therapies involving natural products and nanobiotechnology open additional perspectives to reduce endodontic infections. Curcumin is a natural polyphenol extracted from the dry rhizome of curcuma long Linn with therapeutic properties for application in nanobiotechnology and as a photosensitizer for photodynamic therapy. This study aimed to synthesize a novel polymeric nanoparticle of poly (lactic-co-glycolic acid) (PLGA) loaded with curcumin (NP+Cur), and evaluate its antimicrobial activity against endodontic biofilms. Additionally, its biocompatibility using oral keratinocytes was assessed. The polymeric NP+Cur was prepared by the nanoprecipitation method. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) were calculated for the three endodontic bacteria (Enterococcus faecalis, Streptococcus oralis and Actinomyces viscosus). Antibacterial activity of NP+Cur against single- and multispecies biofilm pre-formed on the botton 24-well plate and into dentin tubules of bovine teeth were evaluated by colony forming units and confocal laser scanning microscopy. The pre-irradiation time was 5 min followed by exposure to blue light-emitting diode at 450 nm for the photodynamic treatment. Cell viability using oral keratinocytes was assessed by Alamar Blue assay. MIC and MBC showed antibacterial activity of NP+Cur against endodontic bacteria. A treatment of pre-formed biofilms of endodontic bacteria with NP+Cur also significantly decreased bacterial viability. The concentration of 325 µg/mL of photoactivated NP+Cur was the one that most reduced the viability of the endodontic bacteria evaluated. Regarding biocompatibility, NP+Cur 325 µg/mL and pure nanoparticles showed a cell viability greater than 80%. The novel polymeric nanoparticles loaded with curcumin may be a promising adjunct use to treatment of endodontic infections.


Assuntos
Curcumina , Nanopartículas , Fotoquimioterapia , Animais , Bovinos , Fotoquimioterapia/métodos , Fármacos Fotossensibilizantes/farmacologia , Curcumina/farmacologia , Antibacterianos/farmacologia , Biofilmes , Polímeros
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