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1.
Int J Pharm ; 633: 122608, 2023 Feb 25.
Artigo em Inglês | MEDLINE | ID: mdl-36642350

RESUMO

Infections have emerged as a novel target in managing skin and mucosa diseases. Bacterial resistance to antimicrobials 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 antibacterial 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 particle size lower than 250 nm, negative charge, and encapsulation efficiency higher than 70 %. Direct incorporation 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 Staphylococcus 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.


Assuntos
Anti-Infecciosos , Quitosana , Nanocápsulas , Óleos Voláteis , Óleos Voláteis/farmacologia , Antibacterianos/farmacologia , Polímeros
2.
Biomed Pharmacother ; 134: 111109, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33341050

RESUMO

Cutaneous 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 resistance. 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 intraperitoneal meglumine antimoniate reduced lesion size by 41 % and tissue regeneration was proven by histopathological 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.


Assuntos
Fabaceae , Leishmania mexicana/efeitos dos fármacos , Leishmaniose Cutânea/tratamento farmacológico , Extratos Vegetais/farmacologia , Pele/efeitos dos fármacos , Tripanossomicidas/farmacologia , Administração Tópica , Animais , Citocinas/metabolismo , Modelos Animais de Doenças , Composição de Medicamentos , Quimioterapia Combinada , Emulsões , Fabaceae/química , Feminino , Interações Hospedeiro-Parasita , Leishmania mexicana/crescimento & desenvolvimento , Leishmaniose Cutânea/parasitologia , Leishmaniose Cutânea/patologia , Antimoniato de Meglumina/farmacologia , Mesocricetus , Camundongos Endogâmicos BALB C , Nanopartículas , Carga Parasitária , Extratos Vegetais/isolamento & purificação , Pele/parasitologia , Pele/patologia , Tripanossomicidas/isolamento & purificação
3.
Pharmaceuticals (Basel) ; 12(4)2019 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-31801207

RESUMO

The plant species Libidibia ferrea (Mart. ex Tul.) LP Queiroz var. ferrea basionym of Caesalpinia ferrea (Mart. ex Tul.) is used in various regions of Brazil in folk medicine in the treatment of several health problems, especially in acute and chronic inflammatory processes. Most of the preparations employed are alcoholic. Therefore, this study aimed to evaluate the acute toxicity of the hydroethanolic extract of fruits of Libidibia ferrea (EHEFLf) in zebrafish, emphasizing the possible changes in the organic-cellular level of the gills, liver, kidneys, and intestine and on embryos. The result obtained by LC-M/MS from EHEFLf indicated a high concentration of possible polyhydroxylated substances. EHEFLf, at a dose of 2 g/kg orally, produced non-significant alterations of the analyzed organs. However, for embryos, the treatment with different concentrations demonstrated heart toxicity that was concentration-dependent. There is no evidence of a correlation of the observed effects with the phytochemical composition, and considering the species of animal used, it can be suggested that the oral use of L. ferrea hydroethanolic extract has an acceptable degree of safety for use as an oral medicinal product. and embryo results have shown significant affinity to the heart; however, it is perceived to be related to the concentrations used.

4.
Molecules ; 22(11)2017 Nov 17.
Artigo em Inglês | MEDLINE | ID: mdl-29149027

RESUMO

Baccharis reticularia DC. is a plant species from the Asteraceae family that is endemic to Brazil. Despite the great importance of Baccharis genus, no study has been carried out regarding either the phytochemical composition of B. reticularia or the evaluation of its larvicidal potential. Considering the intrinsic immiscibility of essential oils, this study shows larvicidal nanoemulsions containing the B. reticularia phytochemically characterized essential oil and its main constituent against Aedes aegypti. The major compound found was d-limonene (25.7%). The essential oil inhibited the acetylcholinesterase, one of the main targets of insecticides. The required hydrophile-lipophile balance of both nanoemulsions was 15.0. The mean droplet sizes were around 90.0 nm, and no major alterations were observed after 24 h of preparation for both formulations. After 48 h of treatment, the estimated LC50 values were 118.94 µg mL-1 and 81.19 µg mL-1 for B. reticularia essential oil and d-limonene nanoemulsions, respectively. Morphological alterations evidenced by scanning electron micrography were observed on the larvae treated with the d-limonene nanoemulsion. This paper demonstrated a simple and ecofriendly method for obtaining B. reticularia essential oil and d-limonene aqueous nanoemulsions by a non-heating and solvent-free method, as promising alternatives for Aedes aegypti control.


Assuntos
Baccharis/química , Cicloexenos/química , Cicloexenos/farmacologia , Inseticidas/química , Inseticidas/farmacologia , Terpenos/química , Terpenos/farmacologia , Aedes/efeitos dos fármacos , Animais , Brasil , Cromatografia Gasosa-Espectrometria de Massas , Larva/efeitos dos fármacos , Limoneno , Controle de Mosquitos , Óleos Voláteis/química , Óleos Voláteis/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia
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