DEFAR - Departamento de Farmácia
URI permanente desta comunidadehttp://www.hml.repositorio.ufop.br/handle/123456789/530
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12 resultados
Resultados da Pesquisa
Item Nanoemulsion of Ocotea indecora (Shott) Mez essential oil : larvicidal effects against Aedes aegypti .(2023) Machado, Francisco Paiva; Andrade, Diogo Folly Gomes; Salas Enríquez, Jairo Jhonatan; Mello Neto, Cícero Brasileiro de; Esteves, Ricardo dos Santos; Araújo, Raquel Silva; Toledo, Pedro Felipe Seguro de; Mantilla Afanador, Javier Guillermo; Santos, Marcelo Guerra; Oliveira, Eugênio Eduardo de; Ricci Junior, Eduardo; Rocha, Leandro MachadoThe widespread use of insecticide can lead to the resistance of the Aedes aegypti mosquito and adverse effects on non-target organisms, such as humans, other animals, and insects. In this sense, nanotechnology associated with natural products is a promising alternative to obtaining safer and more sustainable insecticide formulations against this vector. Therefore, in this research, we developed and optimized a nanoemulsion with essential oil from Ocotea indecora (Shott) Mez leaves and evaluated its larvicidal properties against Ae. aegypti larvae. In addition, oral toxicity assays were performed to test the nanoemulsion safety of the non-target organism Apis mellifera. The major constituent found was sesquirosefuran (81.4 %). The nanoemulsions were prepared by the low-energy method by phase inversion and characterized by the dynamic light scattering technique. The most suitable surfactant mixture was in hydrophilic-lipophilic balance 14.22, presenting droplets size of 122.8 nm and polydispersity index of 0.262. Then a 23 factorial design was realized to optimize the formulation suggesting the variables conditions of 1:1 of essential oil (5 % w/w) and surfactants at 500 rotations per minute. This led to spherical nanoemulsions with mean size and PdI of 105.3 nm and 0.263, respectively. The optimized nano- emulsion presented stability when stored at room temperature and refrigerated for up to one year. The LC50 values against Ae. aegypti larvae were 61.4, and 26.8 μg/mL after, 48, and 144 h, respectively. Scanning electron micrography showed morphological body alterations on the larvae Ae. aegypti treated with the nanoemulsion. Regarding the ecotoxicological evaluation, the nanoemulsion showed no toxicity against Apis mellifera. There- fore, this work demonstrated a simple method to obtain O. indecora nanoemulsion as an environmental-friendlier alternative to the Aedes aegypti control.Item Copaiba essential oil loaded-nanocapsules film as a potential candidate for treating skin disorders : preparation, characterization, and antibacterial properties.(2023) Pinto, Erveton Pinheiro; Menezes, Rodrigo Prioli; Tavares, Walter de Souza; Ferreira, Adriana Maciel; Sousa, Francisco Fábio Oliveira de; Silva, Gabriel Araújo da; Zamora, Robert Ronald Maguiña; Araújo, Raquel Silva; Souza, Tiago Marcolino deInfections have emerged as a novel target in managing skin and mucosa diseases. Bacterial resistance to anti- microbials and biofilm elimination from surfaces remains a challenge. Because polymeric nanocapsules (NC) can increase antimicrobial activity, this study aimed to produce and characterize NC into chitosan films (CSF). Copaiba essential oil (CO) presents antimicrobial activity and was chosen to load NC. In addition, the antibac- terial activity was evaluated to obtain a new biodegradable polymeric platform system with the potential to treat topical diseases associated with bacterial infections. The CO-NC produced by nanoprecipitation presented par- ticle size lower than 250 nm, negative charge, and encapsulation efficiency higher than 70 %. Direct incorpo- ration of CO into CSF (CO-CSF) by casting method worsened the film’s characteristics. However, incorporating CO-NC into CSF (CO-NC-CSF) avoided these drawbacks demonstrating improved physical, mechanical, morphological, and topographical properties. FTIR results demonstrated possible intermolecular interactions among the polymers and CO. The CO-NC-CSF and CO-CSF presented antibacterial properties against Staphylo- coccus aureus, and Pseudomonas aeruginosa, especially the formulation containing 1 % of CO. These results indicated that CO-NC-CSF is a promising candidate for treating skin disorders.Item PEGylated and functionalized polylactide-based nanocapsules : an overview.(2023) Oliveira, Maria Alice de; Araújo, Raquel Silva; Mosqueira, Vanessa Carla FurtadoPolymeric nanocapsules (NC) are versatile mixed vesicular nanocarriers, generally containing a lipid core with a polymeric wall. They have been first developed over four decades ago with outstanding applicability in the cosmetic and pharmaceutical fields. Biodegradable polyesters are frequently used in nanocapsule preparation and among them, polylactic acid (PLA) derivatives and copolymers, such as PLGA and amphiphilic block co- polymers, are widely used and considered safe for different administration routes. PLA functionalization stra- tegies have been developed to obtain more versatile polymers and to allow the conjugation with bioactive ligands for cell-targeted NC. This review intends to provide steps in the evolution of NC since its first report and the recent literature on PLA-based NC applications. PLA-based polymer synthesis and surface modifications are included, as well as the use of NC as a novel tool for combined treatment, diagnostics, and imaging in one de- livery system. Furthermore, the use of NC to carry therapeutic and/or imaging agents for different diseases, mainly cancer, inflammation, and infections is presented and reviewed. Constraints that impair translation to the clinic are discussed to provide safe and reproducible PLA-based nanocapsules on the market. We reviewed the entire period in the literature where the term “nanocapsules” appears for the first time until the present day, selecting original scientific publications and the most relevant patent literature related to PLA-based NC. We presented to readers a historical overview of these Sui generis nanostructures.Item Comparing the nanoscale topography and interface properties of chitosan films containing free and nano-encapsulated copaiba essential oil : an atomic force microscopy (AFM) and fractal geometry study.(2023) Pinto, Erveton Pinheiro; Menezes, Rodrigo Prioli; Pires, Marcelo Amanajás; Zamora, Robert Ronald Maguiña; Araújo, Raquel Silva; Souza, Tiago Marcolino deThis article compared chitosan films containing copaiba essential oil (CO) and nano-encapsulated CO using nanoscaled topographic characteristics and interface properties. The CO-loaded nanocapsules (CO-NC) were prepared by the polymer nanoprecipitation method, whereas the composite films were produced by the casting method. The films’ surface was evaluated by atomic force microscopy (AFM) and scanning electron microscopy (SEM). Wettability and adhesion were also investigated by measuring the contact angle and AFM. The results suggested that the film’s surface containing CO-NC presented characteristics that favor interface interactions at the nanoscale. Furthermore, these films showed greater interaction with water and superior adhesion force than the control and CO-loaded chitosan films. Thus, considering the surface characteristics and the evaluated properties, CO-NC seems to be a promising alternative for incorporating CO in chitosan films.Item Poly-ε-caprolactone nanocapsules loaded with copaiba essential oil reduce inflammation and pain in mice.(2023) Pinto, Erveton Pinheiro; Costa, Sarah Olivia Alves Mendes da; D’Haese, Cecile; Nysten, Bernard; Machado, Francisco Paiva; Rocha, Leandro Machado; Souza, Tiago Marcolino de; Beloqui, Ana; Machado, Renes Resende; Araújo, Raquel SilvaDiverse drugs have been used for the management of inflammation disorders and pain. However, they present many side effects and stimulate the search for new pharmacotherapeutic alternatives. Plant-derived products such as copaiba essential oil (CO) offer beneficial pharmacological effects. On the other hand, essential oil’s low water solubility and physical instability hinder its in vivo application. Thus, poly-ε-caprolactone (PCL)-based nanocarriers have been used to increase their stability and efficacy. This work aimed to encapsulate CO in PCL nanocapsules and evaluate their effect on inflammation models and pain. The polymeric nanocapsules loading CO (CO-NC) were prepared by nanoprecipitation technique, characterized, and analyzed for their anti- inflammatory effect in vitro and in vivo. The results showed that CO-NC presented a spherical shape, 229.3 ± 1.5 nm diameter, and a negative zeta potential (approximately − 23 mV). CO and CO-NC presented anti- inflammatory and antioxidant effects by LPS-activated macrophages (J774 cells). In addition, CO-NC signifi- cantly reduced TNF-α secretion (3-fold) compared to CO. In vivo, pre-treatment with CO or CO-NC (50, 100, 200 mg/kg, intraperitoneal; i.p) reduced the mechanical allodynia, paw edema, and pro-inflammatory cytokines induced by intraplantar (i.pl) injection of carrageenan in mice. Specifically, CO-NC (200 mg/kg; i.p.) reduced the production of TNF-α similar to the control group. Our results support using polymeric nanocapsules for CO delivery in inflammatory conditions.Item Lecithin-based nanocapsule loading sucupira (Pterodon emarginatus) oil effects in experimental mucositis.(2022) Di Miceli, Jeruza Ferraz Filgueiras; Andrade, Maria Emília Rabelo; Carvalho, Paula Lopes Armond; Santos, Elandia Aparecida; Oliveira, Anna Eliza Maciel de Faria Mota; Fernandes, Caio Pinho; Cruz, Rodrigo Alves Soares; Garrett, Rafael; Mosqueira, Vanessa Carla Furtado; Cassali, Geovanni Dantas; D’Haese, Cecile; Nysten, Bernard; Leite, Jacqueline Isaura Alvarez; Cardoso, Valbert Nascimento; Araújo, Raquel SilvaIntestinal mucositis (IM) is a frequent adverse effect in anticancer therapy without standard treatment. The oil obtained from sucupira (Pterodon emarginatus) has anti-inflammatory properties, and the soybean lecithin re- duces the intestinal toxicity of several xenobiotics. However, their water insolubility impairs the in vivo appli- cation. For this reason, we evaluated if the nanoencapsulation of sucupira oil (SO) in lecithin-based nanocapsules (SO-NC) could be a therapeutically effective system for the treatment of IM in murine cisplatin (CDDP)-induced intestinal mucositis model. SO was analyzed by LC-HRMS/MS and HPLC. SO-NC was prepared by nano- precipitation and characterized using DLS, HPLC, and AFM. Mice body weight and food consumption were assessed daily during experimental mucositis induced by CDDP. The animals were euthanized, and intestinal permeability, inflammatory mediators, and intestinal histology were performed. SO-NC demonstrated adequate characteristics for oral administration as size under 300 nm, IP < 0.3, high EE, and spherical shape. In vitro cytotoxicity performed against RAW 264.7 cell lines resulted in cell viability above 80 % confirming the non- cytotoxic profile of SO (IC50 268 μg/mL) and SO-NC (IC50 118.5 μg/mL) up to 117.2 μg/mL. The untreated mice showed intestinal toxicity after i.p. of CDDP, principally weight loss, increased intestinal permeability, and MPO and TNF-α levels. Surprisingly, the administration of SO to CDDP-mucositis animals did not circumvent the CDDP effects and increased intestinal permeability. However, SO-NC proved efficient in mitigating the experi- mental intestinal mucositis by improving intestinal epithelium architecture, reducing intestinal permeability, and improving the MPO levels. In conclusion, SO-NC can positively impact intestinal mucositis by promoting mucosal recovery. This is a promising strategy for developing a new treatment for intestinal mucositis.Item Efficacy of nanoemulsion with Pterodon emarginatus Vogel oleoresin for topical treatment of cutaneous leishmaniasis.(2021) Kawakami, Monique Yoko Martins; Zamora, Lisset Ortiz; Araújo, Raquel Silva; Fernandes, Caio Pinho; Ricotta, Tiago Queiroga Nery; Oliveira, Leandro G. de; Queiroz Júnior, Celso Martins; Fernandes, Ana Paula Salles Moura; Conceição, Edemilson Cardoso da; Ferreira, Lucas Antônio Miranda; Barros, André Luís Branco de; Aguiar, Marta Marques Gontijo de; Oliveira, Anna Eliza Maciel de Faria MotaCutaneous leishmaniasis (CL) is a neglected tropical skin disease caused by the protozoan genus Leishmania. The treatment is restricted to a handful number of drugs that exhibit toxic effects, limited efficacy, and drug resis- tance. Additionally, developing an effective topical treatment is still an enormous unmet medical challenge. Natural oils, e.g. the oleoresin from P. emarginatus fruits (SO), contain various bioactive molecules, especially terpenoid compounds such as diterpenes and sesquiterpenes. However, its use in topical formulations can be impaired due to the natural barrier of the skin for low water solubility compounds. Nanoemulsions (NE) are drug delivery systems able to increase penetration of lipophilic compounds throughout the skin, improving their topical effect. In this context, we propose the use of SO-containing NE (SO-NE) for CL treatment. The SO-NE was produced by a low energy method and presented suitable physicochemical characteristic: average diameter and polydispersity index lower than 180 nm and 0.2, respectively. Leishmania (Leishmania) amazonensis-infected BALB/c mice were given topical doses of SO or SO-NE. The topical use of a combination of SO-NE and intra- peritoneal meglumine antimoniate reduced lesion size by 41 % and tissue regeneration was proven by histo- pathological analyses. In addition, a reduction in the parasitic load and decreased in the level of IFN-γ in the lesion may be associated, as well as a lower level of the cytokine IL-10 may be associated with a less intense inflammatory process. The present study suggests that SO-NE in combination meglumine antimoniate represents a promising alternative for the topical treatment of CL caused by L. (L.) amazonensis.Item Nano-emulsions of the essential oil of Baccharis reticularia and its constituents as eco-friendly repellents against Tribolium castaneum.(2021) Lima, Luana A.; Sá, Paula S. Ferreira; Garcia Júnior, Manoel Daltro Nunes; Pereira, Vera Lúcia P.; Carvalho, José Carlos Tavares; Rocha, Leandro; Fernandes, Caio Pinho; Souto, Raimundo Nonato Picanço; Araújo, Raquel Silva; Botas, Gisele da Silva; Cruz, Rodrigo Alves SoaresNanoproducts based on natural products have been studied as ecologically and economically sustainable alter- natives for crop pest control. Baccharis reticularia DC. is a shrub endemic to Brazil, which leaves are traditionally used in aromatic medicinal baths. This study aims to evaluate the repellent activities of nano-emulsions con- taining the B. reticularia phytochemically characterized essential oil and some of its monoterpene constituents (limonene, α-pinene, and β-pinene) against Tribolium castaneum (Herbst). Essential oil was obtained by hydro- distillation of fresh leaves and stems and yielded 0.28 % (w/w). The main constituents of the essential oil were: limonene (14.6 %), β-myrcene (12.6 %), and bicyclogermacrene (12.5 %). The required hydrophile-lipophile balance (rHLB) of the nano-emulsions were: 13 (α-pinene) and 15 (essential oil, limonene, and β-pinene). All nano-emulsions showed mean droplet sizes bellow 200 nm and remain stable, at least, for 28 days (limonene), 90 days (β-pinene), or 150 days (essential oil and α-pinene). All nano-emulsions exhibited repellent activity against T. castaneum at 8.8 μg/cm2 . Limonene and α-pinene were the most active nano-emulsions, showing significant repellent action at 1.1 μg/cm2 , which indicates that these compounds contribute to the repellent action of the essential oil of B. reticularia. The present study opens perspectives for the utilization of B. reticularia essential oil and its constituents as raw material of new promising nanopesticides produced using a low energy, solvent-free and ecofriendly method. Thus, this work contributes significantly to the search for new ecologically correct strategies for the control of T. castaneum.Item Recent progress in micro and nano-encapsulation of bioactive derivatives of the Brazilian genus Pterodon.(2021) Lemos, Janaina de Alcantara; Oliveira, Anna Eliza M. F. M.; Araújo, Raquel Silva; Townsend, Danyelle M.; Ferreira, Lucas Antônio Miranda; Barros, André Luís Branco deIn the last few decades, utilization of medicinal plants by the pharmaceutical industry has led to the identifi- cation of many new bioactive compounds. The genus Pterodon, native of the Brazilian Flora, is known for the therapeutic properties attributed to its species, which are widely used in popular medicine for their anti- inflammatory, anti-rheumatic, tonic, and depurative properties. The intrinsic low water solubility of the plant derivatives from the genus, including diterpenes with vouacapane skeletons that are partially associated with the pharmacological activities, impairs the bioavailability of these bioactive compounds. Recent studies have aimed to encapsulate Pterodon products to improve their water solubility, achieve stability, increase their efficacy, and allow clinical applications. The purpose of this paper is to review recent research on the use of nanotechnology for the development of new products from plant derivatives of the Pterodon genus in different types of micro- and nanocarriers. Therapeutic properties of their different products are also presented. Finally, an update about the current and future applications of encapsulated formulations is provided.Item Lacunarity exponent and Moran index : a complementary methodology to analyze AFM images and its application to chitosan films.(2021) Pinto, Erveton Pinheiro; Pires, Marcelo Amanajás; Matos, Robert Saraiva; Zamora, Robert Ronald Maguiña; Menezes, Rodrigo Prioli; Araújo, Raquel Silva; Souza, Tiago Marcolino deIn this work, we developed new scripts to calculate the lacunarity exponent and Moran’s index of Atomic Force Microscopy (AFM) images. The lacunarity exponent was estimated by combining the Otsu binarization and gliding-box algorithm, and Moran index was introduced to evaluate the surfaces’ spatial autocorrelation. Developed scripts were first validated using numerical simulation of self-similar fractal and self-affine isotropic surfaces. Then, we successfully synthesized chitosan films with different glycerol con- centrations and used the lacunarity and Moran’s index for a thorough characterization. The validation of the proposed scripts using simulated Sierpinski Carpets and 3D artificial surfaces showed promising potential for analyzing AFM images. Finally, the methodology application to AFM images of chitosan films suggested that lacunarity analysis and Moran index determination could complement thin films’ quality processing control.