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1.
Nanomaterials (Basel) ; 14(12)2024 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-38921890

RESUMO

Solid lipid nanoparticles (SLNs) represent promising nanostructures for drug delivery systems. This study successfully synthesized SLNs containing different proportions of babassu oil (BBS) and copaiba oleoresin (COPA) via the emulsification-ultrasonication method. Before SLN synthesis, the identification and quantification of methyl esters, such as lauric acid and ß-caryophyllene, were performed via GC-MS analysis. These methyl esters were used as chemical markers and assisted in encapsulation efficiency experiments. A 22 factorial design with a center point was employed to assess the impact of stearic acid and Tween 80 on particle hydrodynamic diameter (HD) and polydispersity index (PDI). Additionally, the effects of temperature (8 ± 0.5 °C and 25 ± 1.0 °C) and time (0, 7, 15, 30, 40, and 60 days) on HD and PDI values were investigated. Zeta potential (ZP) measurements were utilized to evaluate nanoparticle stability, while transmission electron microscopy provided insights into the morphology and nanometric dimensions of the SLNs. The in vitro cytotoxic activity of the SLNs (10 µg/mL, 30 µg/mL, 40 µg/mL, and 80 µg/mL) was evaluated using the MTT assay with PC-3 and DU-145 prostate cancer cell lines. Results demonstrated that SLNs containing BBS and COPA in a 1:1 ratio exhibited a promising cytotoxic effect against prostate cancer cells, with a percentage of viable cells of 68.5% for PC-3 at a concentration of 30 µg/mL and 48% for DU-145 at a concentration of 80 µg/mL. These findings underscore the potential therapeutic applications of SLNs loaded with BBS and COPA for prostate cancer treatment.

2.
Int J Nanomedicine ; 19: 5953-5972, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38895147

RESUMO

Background and Purpose: Natural products are potential sources of anticancer components. Among various species, the lipophilic extract of the Viscum album subsp. austriacum (Wiesb.) Vollm. (VALE) has shown promising therapeutic potential. The present work aimed to qualify the plant source and characterize the extract's chemical profile. In addition, a self-nanoemulsifying drug delivery system (SNEDDS) containing VALE (SNEDDS-VALE) was developed. Methods: V. album subsp. austriacum histochemistry was performed, and the chemical profile of VALE was analyzed by GC-MS. After the SNEEDS-VALE development, its morphology was visualized by transmission electron microscopy (TEM), while its stability was evaluated by the average droplet size, polydispersity index (PdI) and pH. Lastly, SNEDDS-VALE chemical stability was evaluated by LC-DAD-MS. Results: The histochemical analysis showed the presence of lipophilic compounds in the leaves and stems. The major compound in the VALE was oleanolic acid, followed by lupeol acetate and ursolic acid. SNEDDS was composed of medium chain triglyceride and Kolliphor® RH 40 (PEG-40 hydrogenated castor oil). A homogeneous, isotropic and stable nanoemulsion was obtained, with an average size of 36.87 ± 1.04 nm and PdI of 0.14 ± 0.02, for 14 weeks. Conclusion: This is the first histochemistry analysis of V. album subsp. austriacum growing on Pinus sylvestris L. which provided detailed information regarding its lipophilic compounds. A homogeneous, isotropic and stable SNEDDS-VALE was obtained to improve the low water solubility of VALE. Further, in vitro and in vivo experiments should be performed, in order to evaluate the antitumoral potential of SNEDDS-VALE.


Assuntos
Emulsões , Extratos Vegetais , Viscum album , Extratos Vegetais/química , Extratos Vegetais/administração & dosagem , Viscum album/química , Emulsões/química , Folhas de Planta/química , Sistemas de Liberação de Medicamentos/métodos , Tamanho da Partícula , Sistemas de Liberação de Fármacos por Nanopartículas/química , Nanopartículas/química
3.
Int J Pharm ; 652: 123765, 2024 Mar 05.
Artigo em Inglês | MEDLINE | ID: mdl-38195032

RESUMO

Despite the successful use of the radiopharmaceutical radium-223 dichloride ([223Ra]RaCl2) for targeted alpha therapy of castration-resistant prostate cancer patients with bone metastases, some short-term side effects, such as diarrhea and vomiting, have been documented, causing patient discomfort. Hence, we prepared a nanosized micellar solution of [223Ra]RaCl2 and evaluated its biodistribution, pharmacokinetics, and induced biochemical changes in healthy mice up to 96 h after intraperitoneal administration as an alternative to overcome the previous limitations. In addition, we evaluated the bone specificity of micellar [223Ra]RaCl2 in patient-derived xenografts in the osteosarcoma model. The biodistribution studies revealed the high bone-targeting properties of the micellar [223Ra]RaCl2. Interestingly, the liver uptake remained significantly low (%ID/g = 0.1-0.02) from 24 to 96 h after administration. In addition, the micellar [223Ra]RaCl2 exhibited a significantly higher uptake in left (%ID/g = 0.85-0.23) and right (%ID/g = 0.76-0.24) kidneys than in small (%ID/g = 0.43-0.06) and large intestines (%ID/g = 0.24-0.09) over time, suggesting its excretion pathway is primarily through the kidneys into the urine, in contrast to the non-micellar [223Ra]RaCl2. The micellar [223Ra]RaCl2 also had low distribution volume (0.055 ± 0.003 L) and longer elimination half-life (28 ± 12 days). This nanosystem was unable to change the enzymatic activities of alanine aminotransferase, aspartate aminotransferase, gamma GT, glucose, and liquiform lipase in the treated mice. Finally, microscopic examination of the animals' osteosarcoma tumors treated with micellar [223Ra]RaCl2 indicated regression of the tumor, with large areas of necrosis. In contrast, in the control group, we observed tumor cellularity and cell anaplasia, mitotic figures and formation of neoplastic extracellular bone matrix, which are typical features of osteosarcoma. Therefore, our findings demonstrated the efficiency and safety of nanosized micellar formulations to minimize the gastrointestinal excretion pathway of the clinical radiopharmaceutical [223Ra]RaCl2, in addition to promoting regression of the osteosarcoma. Further studies must be performed to assess dose-response outcomes and organ/tissue dosimetry for clinical translation.


Assuntos
Neoplasias Ósseas , Osteossarcoma , Neoplasias de Próstata Resistentes à Castração , Humanos , Masculino , Animais , Camundongos , Compostos Radiofarmacêuticos/farmacocinética , Distribuição Tecidual , Eliminação Renal , Neoplasias Ósseas/tratamento farmacológico , Neoplasias Ósseas/radioterapia , Osteossarcoma/tratamento farmacológico , Neoplasias de Próstata Resistentes à Castração/patologia
4.
Molecules ; 28(16)2023 Aug 08.
Artigo em Inglês | MEDLINE | ID: mdl-37630195

RESUMO

Schistosomiasis is a tropical disease transmitted in an aqueous environment by cercariae from the Schistosoma genus. This disease affects 200 million people living in risk areas around the world. The control of schistosomiasis is realized by chemotherapy, wastewater sanitation, health education, and mollusk control using molluscicidal agents. This work evaluates the effects of a nanoemulsion containing essential oil from Myrciaria floribunda leaves as a molluscicidal and cercaricidal agent against Biomphalaria glabrata mollusks and Schistosoma mansoni cercariae. The Myrciaria floribunda essential oil from leaves showed nerolidol, ß-selinene, 1,8 cineol, and zonarene as major constituents. The formulation study suggested the F3 formulation as the most promising nanoemulsion with polysorbate 20 and sorbitan monooleate 80 (4:1) with 5% (w/w) essential oil as it showed a smaller droplet size of approximately 100 nm with a PDI lower than 0.3 and prominent bluish reflection. Furthermore, this nanoemulsion showed stability after 200 days under refrigeration. The Myrciaria floribunda nanoemulsion showed LC50 values of 48.11 µg/mL, 29.66 µg/mL, and 47.02 µg/mL in Biomphalaria glabrata embryos, juveniles, and adult mollusks, respectively, after 48 h and 83.88 µg/mL for Schistosoma mansoni cercariae after 2 h. In addition, a survival of 80% was observed in Danio rerio, and the in silico toxicity assay showed lower overall human toxicity potential to the major compounds in the essential oil compared to the reference molluscicide niclosamide. These results suggest that the nanoemulsion of Myrciaria floribunda leaves may be a promising alternative for schistosomiasis control.


Assuntos
Moluscocidas , Myrtaceae , Óleos Voláteis , Adulto , Humanos , Óleos Voláteis/farmacologia , Moluscocidas/farmacologia , Eucaliptol , Niclosamida , Alimentos
5.
Curr Med Chem ; 2023 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-37594105

RESUMO

Radiopharmaceuticals are increasingly playing a leading role in diagnosing, monitoring, and treating disease. In comparison with conventional pharmaceuticals, the development of radiopharmaceuticals does follow the principles of medicinal chemistry in the context of imaging-altered physiological processes. The design of a novel radiopharmaceutical has several steps similar to conventional drug discovery and some particularity. In the present work, we revisited the insights of medicinal chemistry in the current radiopharmaceutical development giving examples in oncology, neurology, and cardiology. In this regard, we overviewed the literature on radiopharmaceutical development to study overexpressed targets such as prostate-specific membrane antigen and fibroblast activation protein in cancer; ß-amyloid plaques and tau protein in brain disorders; and angiotensin II type 1 receptor in cardiac disease. The work addresses concepts in the field of radiopharmacy with a special focus on the potential use of radiopharmaceuticals for nuclear imaging and theranostics.

6.
Nutrients ; 15(13)2023 Jun 27.
Artigo em Inglês | MEDLINE | ID: mdl-37447241

RESUMO

Brugmansia suaveolens Bercht. & J. Presl has been widely used due to the presence of different bioactive compounds. This review summarizes the latest advances and perspectives of the B. suaveolens plant species; it is a systematic literature review on aspects of botany, traditional uses, phytochemistry, pharmacology, and toxicology as therapeutic potential. In addition, 120 compounds are described, including alkaloids, flavonoids, terpenoids, steroids, amino acids, aromatics, and aliphatics. As for the therapeutic potential, it is described in extracts and compounds in the antitumor, anti-inflammatory, antioxidant, antimicrobial, antispasmodic, anticoagulant, and analgesic aspects, as well as the effects on the central nervous system. The toxicity of the genus stands out, especially the potential for organ toxicity. Therefore, this review evidenced the knowledge related to the traditional use based on the scientific research of Brugmansia suaveolens, highlighting an overview of bioactive compounds and biological and toxicological activities in order to provide a scientific basis for future studies on the value of this species for the development of new natural products.


Assuntos
Alcaloides , Brugmansia , Fitoterapia , Medicina Tradicional , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Extratos Vegetais/química , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico , Compostos Fitoquímicos/química , Etnofarmacologia
7.
Pharmaceuticals (Basel) ; 16(2)2023 Feb 14.
Artigo em Inglês | MEDLINE | ID: mdl-37259436

RESUMO

Human beings are actively exposed to ultraviolet (UV) radiation, which is associated with skin cancer. This has encouraged the continuous search for more effective and safer photoprotective formulations. Along with the application of traditional organic sunscreens, there is a growing interest in "green products" containing natural compounds such as plant extracts and oils. This trend is combined with the use of nanotechnology as a tool for optimizing the vehicles of such compounds. Nanoemulsions (NEs) are suitable for the encapsulation of natural compounds, which improves topical treatment. Therefore, we have developed oil-in-water (O/W) nanoemulsions containing 3% buriti oil (BO), incorporated in a 10% vegetal extract of Aloe vera (AV) by means of ultrasonic processing to improve the chemical characteristics of this component and, consequently, its efficacy and safety in pharmaceutical and cosmetic formulations. The composition of the formulation was initially defined in a preliminary study on surfactants where the concentrations of Tween® 80 and Span® 20 were evaluated in relation to particle size and the polydispersity index (PDI). The nanoemulsion was prepared and then chemical sunscreens were incorporated with the aim of developing a sunscreen nanoemulsion called NE-A19. This nanoemulsion was found to be the best formulation due to its stability, droplet size (146.80 ± 2.74), and PDI (0.302 ± 0.088), with a monomodal size distribution. The stability was evaluated over 90 days and showed a low growth in particle size at the end of the study. NE-A19 exhibited good viscosity and organoleptic properties, in addition to an occlusion factor indicating an interesting and higher water holding capacity when compared with a NE without AV (p < 0.05). The in vitro efficacy and safety studies of NE-19A were promising. Its average in vitro sun protection factor value was 49, with a critical wavelength (λc) of 369.7 nm, satisfactory UVA protection, and a UVA/UVB ratio of 0.40, indicating broad spectrum protection against UVA and UVB radiation. Furthermore, NE-19A displayed a good safety profile in dermal keratinocytes. It can be concluded that NE-19A is a promising formulation for carrying natural products, such as buriti oil and AV, associated with synthetic filters in lower concentrations.

8.
Curr Drug Deliv ; 2023 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-37170995

RESUMO

BACKGROUND: Melanoma is a malignant skin cancer type with a high lethality rate due to active metastasis. Among the risk factors for its development is exposure to ultraviolet radiation (UV) and phenotypical characteristics such as clear skin and eyes. Given the difficulties of the conventional therapy, the high cost of the treatment and the low bioavailability of drugs, it is important to develop new therapeutic methods to circumvent this situation. Nanosystems such as micelles, liposomes and nanoparticles present advantages when compared to conventional treatments. OBJECTIVE: The objective of this paper is to carry out a literature review based on articles that dealt with the use of siRNA-loaded nanosystems for the treatment of melanoma, with trials carried out in vivo to assess tumor size. METHODS: The search was conducted in the Web of Science and PubMed databases considering the last 5 years, that is, the period between January 2017 to December 2021. The "SiRNA and Drug Delivery Systems and Melanoma" keywords were used in both databases, and the articles were analyzed using the inclusion and exclusion criteria established for this paper. RESULTS: The results obtained indicated that using siRNA transported via nanosystems was capable of silencing the BRAF tumor genes and of reducing tumor size and weight, not presenting in vitro and/or in vivo toxicity. CONCLUSION: Such being the case, the development of these systems becomes a non-invasive and promising option for the treatment of melanoma.

9.
Molecules ; 28(8)2023 Apr 13.
Artigo em Inglês | MEDLINE | ID: mdl-37110671

RESUMO

The Aspergillus genus, the etiological agent of aspergillosis, is an important food contaminant and mycotoxin producer. Plant extracts and essential oils are a source of bioactive substances with antimicrobial potential that can be used instead of synthetic food preservatives. Species from the Lauraceae family and the Ocotea genus have been used as traditional medicinal herbs. Their essential oils can be nanoemulsified to enhance their stability and bioavailability and increase their use. Therefore, this study sought to prepare and characterize both nanoemulsion and essential oil from the Ocotea indecora's leaves, a native and endemic species from the Mata Atlântica forest in Brazil, and evaluate the activity against Aspergillus flavus RC 2054, Aspergillus parasiticus NRRL 2999, and Aspergillus westerdjikiae NRRL 3174. The products were added to Sabouraud Dextrose Agar at concentrations of 256, 512, 1024, 2048, and 4096 µg/mL. The strains were inoculated and incubated for up to 96 h with two daily measurements. The results did not show fungicidal activity under these conditions. A fungistatic effect, however, was observed. The nanoemulsion decreased the fungistatic concentration of the essential oil more than ten times, mainly in A. westerdjikiae. There were no significant changes in aflatoxin production.


Assuntos
Aflatoxinas , Ocotea , Óleos Voláteis , Óleos Voláteis/farmacologia , Aspergillus , Aspergillus flavus
10.
Curr Top Med Chem ; 23(15): 1414-1424, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36924101

RESUMO

Ionizing radiation has been used for decades and expanded to several applications in multivariate sectors, becoming an important tool to promote controlled chemical reactions in polymeric structures, according to their chemical properties for developing new materials. In addition, the use of radiation can also be applied in order to reduce or eliminate compounds from solutions that may be harmful or of low interest. In this review, we overviewed the chemistry behind material irradiation and the attractive use of ionizing radiation in scientific and industrial development. In this regard, the review was divided into three main sections titled (1) chemical kinetics intermediated by radiation, (2) chemical bonds intermediated by radiation, and (3) radiation chemistry on polymers. We concluded that graft polymerization, crosslinking and chain scission reactions induced by ionizing radiation are very efficient and green strategies for developing new materials with improved properties. Furthermore, water radiolysis plays a key role in the degradation of several contaminants, including pharmaceuticals and microplastics, in aqueous solutions. However, more studies must be conducted to complement the existing theory about the proposed mechanisms responsible for modifying the chemical, mechanical, thermal, optical, and so forth properties of irradiated materials.


Assuntos
Plásticos , Polímeros , Polímeros/química , Cinética , Radiação Ionizante , Água
11.
Colloids Surf B Biointerfaces ; 223: 113174, 2023 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-36746067

RESUMO

The use of targeted alpha therapy (TAT) for bone cancer is increasing each year. Among the alpha radionuclides, radium [223Ra]Ra+2 is the first one approved for bone cancer metastasis therapy. The development of novel radiopharmaceutical based on [223Ra]Ra+2 is essential to continuously increase the arsenal of new TAT drugs. In this study we have developed, characterized, and in vitro evaluated [223Ra] Ra-nano-hydroxyapatite. The results showed that [223Ra] Ra-nano-hydroxyapatite has a dose-response relationship for osteosarcoma cells and a safety profile for human fibroblast cells, corroborating the application as a radiopharmaceutical.


Assuntos
Neoplasias Ósseas , Nanoestruturas , Osteossarcoma , Rádio (Elemento) , Humanos , Compostos Radiofarmacêuticos , Rádio (Elemento)/química , Rádio (Elemento)/uso terapêutico , Neoplasias Ósseas/tratamento farmacológico , Osteossarcoma/tratamento farmacológico
12.
Cells ; 12(3)2023 01 31.
Artigo em Inglês | MEDLINE | ID: mdl-36766793

RESUMO

The use of alpha-particle (α-particle) radionuclides, especially [223Ra]RaCl2 (radium dichloride), for targeted alpha therapy is steadily increasing. Despite the positive clinical outcomes of this therapy, very little data are available about the effect on the ultrastructure of cells. The purpose of this study was to evaluate the nanomechanical and ultrastructure effect of [223Ra] RaCl2 on cancer cells. To analyze the effect of [223Ra]RaCl2 on tumor cells, human breast cancer cells (lineage MDA-MB-231) were cultured and treated with the radiopharmaceutical at doses of 2 µCi and 0.9 µCi. The effect was evaluated using atomic force microscopy (AFM) and transmission electron microscopy (TEM) combined with Raman spectroscopy. The results showed massive destruction of the cell membrane but preservation of the nucleus membrane. No evidence of DNA alteration was observed. The data demonstrated the formation of lysosomes and phagosomes. These findings help elucidate the main mechanism involved in cell death during α-particle therapy.


Assuntos
Neoplasias , Rádio (Elemento) , Humanos , Compostos Radiofarmacêuticos , Rádio (Elemento)/uso terapêutico , Radioisótopos , Partículas alfa/uso terapêutico , Membrana Celular , Neoplasias/tratamento farmacológico
13.
Rev Bras Farmacogn ; 33(1): 73-88, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36466145

RESUMO

The use of nanotechnological products is increasing steadily. In this scenario, the application of nanotechnology in food science and as a technological platform is a reality. Among the several applications, the main use of this technology is for the development of foods and nutraceuticals with higher bioavailability, lower toxicity, and better sustainability. In the health field, nano-nutraceuticals are being used as supplementary products to treat an increasing number of diseases. This review summarizes the main concepts and applications of nano-nutraceuticals for health, with special focus on treating cancer and inflammation. Supplementary Information: The online version contains supplementary material available at 10.1007/s43450-022-00338-7.

14.
Braz. J. Pharm. Sci. (Online) ; 59: e21425, 2023. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1429965

RESUMO

Abstract The University Pharmacy Program (FU), from the Federal University of Rio de Janeiro (UFRJ), was created based on the need to offer a curricular internship to students of the Undergraduate Course at the Faculty of Pharmacy. Currently, it is responsible for the care of about 200 patients/day, offering vacancies for curricular internships for students in the Pharmacy course, it has become a reference in the manipulation of many drugs neglected by the pharmaceutical industry and provides access to medicines for low-income users playing an important social function. Research is one of the pillars of FU-UFRJ and several master and doctoral students use the FU research laboratory in the development of dissertations and theses. As of 2002, the Pharmaceutical Care extension projects started to guarantee a rational and safe pharmacotherapy for the medicine users. From its beginning in 1982 until the current quarantine due to the COVID-19 pandemic, FU-UFRJ has been adapting to the new reality and continued to provide patient care services, maintaining its teaching, research, and extension activities. The FU plays a relevant social role in guaranteeing the low-income population access to special and neglected medicines, and to pharmaceutical and education services in health promotion.


Assuntos
Farmácia/classificação , Educação em Farmácia , COVID-19/classificação , Pacientes/classificação , Assistência Farmacêutica/história , Ensino/ética , Preparações Farmacêuticas/provisão & distribuição , Assistência ao Paciente/ética
15.
Braz. J. Pharm. Sci. (Online) ; 59: e23011, 2023. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1505852

RESUMO

Abstract Oil-in-water photoprotective nanoemulsions (NEs) were developed using Babassu (BBS) lipophilic extract, nonionic surfactants, and low concentrations of organic sunscreens by ultrasonic processing. BBS extract was chosen due to its suitable physicochemical properties (acidity index, peroxide index, refraction index, and relative density) and predominance of saturated fatty acids, identified by gas chromatography-mass spectrometry (GC-MS), which promote biological activities and high oxidative stability. NEs were characterized by mean droplet size, morphology, polydispersity index (PdI), pH, and organoleptic properties, and the physical stability of the NEs was evaluated for 120 days at room temperature. The sun protection factor (SPF) was determined, and the photostability and in vitro cytotoxicity assays were performed for NEs. All NEs remained stable for 120 days, with a droplet size <150 nm and a monomodal distribution profile. The pH values were compatible with the skin's pH. NE3 showed a spherical morphology, with a mean droplet size of 125.15 ± 0.16 nm and PdI of 0.145 ± 0.032. NE3 containing BBS extract and sunscreens presented an SPF of 35.5 ± 3.0, was photostable after 6 h of radiation and was non-cytotoxic to fibroblast cells. Thus, NE3 could be considered a promising formulation for developing synergic plant-extract sunscreen photoprotective products for the market


Assuntos
Plantas/efeitos adversos , Protetores Solares/farmacologia , Extratos Vegetais/agonistas , Arecaceae/classificação , Gorduras Vegetais , Técnicas In Vitro/métodos , Fator de Proteção Solar/classificação , Cromatografia Gasosa-Espectrometria de Massas/métodos
16.
Braz. J. Pharm. Sci. (Online) ; 59: e201090, 2023. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1439513

RESUMO

Abstract Hydrogels are used for wound treatment, as they may contain one or more active components and protect the wound bed. Papain is one of the active substances that have been used with this purpose, alongside urea. In this paper, carboxypolymethylene hydrogels containing papain (2% and 10% concentrations) and urea (5% concentration) were produced. Physical-chemical stability was performed at 0, 7, 15 and 30 days at 2-8ºC, 25ºC and 40ºC, as well as the rheological aspects and proteolytic activity of papain by gel electrophoresis. Clinical efficacy of the formulations in patients with lower limb ulcers was also evaluated in a prospective, single-center, randomized, double-blind and comparative clinical trial. The results showed 7-day stability for the formulations under 25ºC, in addition to approximately 100% and 15% of protein activity for 10% and 2% papain hydrogel, respectively. The rheological profile was non-Newtonian for the 10% papain hydrogel tested. There were no significant differences regarding the mean time for healing of the lesions, although 10% papain presented a better approach to be used in all types of tissue present in the wound bed.


Assuntos
Ureia/efeitos adversos , Cicatrização/efeitos dos fármacos , Papaína/efeitos adversos , Hidrogéis/análise , Ferimentos e Lesões/classificação , Eletroforese/instrumentação
17.
Braz. J. Pharm. Sci. (Online) ; 59: e201150, 2023. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1513810

RESUMO

Abstract The objective of this paper was to develop and evaluate two semi-solid pharmaceutical forms containing 0.1% tacrolimus: cream (CRT01) and gel (GLT01). For the evaluation of physicochemical stability, at times 0, 30, 60 and 90 days, at 23°C and at 40°C, High Performance Liquid Chromatography coupled with a Diode Array Detector (HPLC-DAD) was employed. This method was developed and validated for tacrolimus quantification. The occlusivity test and skin permeation assay were also performed, using an animal model (Wistar rats), and the CRT01 and GLT01 were compared to the 0.1% tacrolimus ointment (PFU01) obtained from the University Pharmacy, Federal University of Rio de Janeiro, Brazil. CRT01 and GLT01 presented a homogeneous aspect and consistency adequate for topical products, along with sensory characteristics above PFU01. They also presented adequate physicochemical stability for 90 days and a lower occlusive effect than PFU01 (p<0.05). CRT01 showed greater affinity for the skin when compared to PFU01 and GLT01, with low systemic absorption. The CRT01 semi-solid formulation was considered the most adequate one to treat patients with atopic dermatitis or other dermatologic inflammatory diseases, promoting rational use of tacrolimus


Assuntos
Animais , Masculino , Feminino , Ratos , Preparações Farmacêuticas/análise , Físico-Química/classificação , Tacrolimo/agonistas , Pomadas/análise , Doença/classificação , Cromatografia Líquida de Alta Pressão/métodos , Dermatite Atópica/patologia , Absorção Fisiológica/efeitos dos fármacos
18.
Eur J Pharm Biopharm ; 180: 91-100, 2022 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-36154904

RESUMO

The use of graphene quantum dots as biomedical devices and drug delivery systems has been increasing. The nano-platform of pure carbon has shown unique properties and is approved to be safe for human use. In this study, we successfully produced and characterized folic acid-functionalized graphene quantum dots (GQD-FA) to evaluate their antiviral activity against Zika virus (ZIKV) infection in vitro, and for radiolabeling with the alpha-particle emitting radionuclide radium-223. The in vitro results exhibited the low cytotoxicity of the nanoprobe GQD-FA in Vero E6 cells and the antiviral effect against replication of the ZIKV infection. In addition, our findings demonstrated that functionalization with folic acid doesn't improve the antiviral effect of graphene quantum dots against ZIVK replication in vitro. On the other hand, the radiolabeled nanoprobe 223Ra@GQD-FA was also produced as confirmed by the Energy Dispersive X-Ray Spectroscopy analysis. 223Ra@GQD-FA might expand the application of alpha targeted therapy using radium-223 in folate receptor-overexpressing tumors.


Assuntos
Grafite , Pontos Quânticos , Infecção por Zika virus , Zika virus , Humanos , Pontos Quânticos/química , Grafite/química , Ácido Fólico/química , Antivirais/farmacologia
19.
Eur J Pharm Biopharm ; 176: 180-187, 2022 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-35640783

RESUMO

Graphene and its derivatives are in the edge of technology with a wide and diverse range of applications. In the last years, especially graphene quantum dots (GQDs) have had their biomedical application expanded in scope, mainly focused on cancer therapy, drug delivery and imaging. Although many studies have evaluated the application of this nanomaterial in biomedical field, only a few studies aimed to understand their biological impact in human health. In this regard, here we evaluated the impact of high doses of GQDs on the microcirculation of a healthy animal model to better assess risks of its use in humans. Our data show that successive applications of GQDs cause irreversible damage to the microcirculation. After seven days, a complete destruction of the microcirculation has been observed. In addition, GQDs showed substantial activity in human erythrocytes. Our findings suggest that risks associated with the use of GQDs, as well as all graphene derivatives, must be better understood, especially concerning biomedical application. A greater understanding of how GQDs impact body circulation, including the context of environmental and engineered nanosystems, is of paramount importance.


Assuntos
Grafite , Nanoestruturas , Pontos Quânticos , Animais , Microcirculação
20.
EJNMMI Radiopharm Chem ; 7(1): 8, 2022 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-35467307

RESUMO

BACKGROUND: Recent advances in nanotechnology have offered new hope for cancer detection, prevention, and treatment. Nanomedicine, a term for the application of nanotechnology in medical and health fields, uses nanoparticles for several applications such as imaging, diagnostic, targeted cancer therapy, drug and gene delivery, tissue engineering, and theranostics. RESULTS: Here, we overview the current state-of-the-art of radiolabeled nanoparticles for molecular imaging and radionuclide therapy. Nanostructured radiopharmaceuticals of technetium-99m, copper-64, lutetium-177, and radium-223 are discussed within the scope of this review article. CONCLUSION: Nanoradiopharmaceuticals may lead to better development of theranostics inspired by ingenious delivery and imaging systems. Cancer nano-theranostics have the potential to lead the way to more specific and individualized cancer treatment.

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