دورية أكاديمية

Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design.

التفاصيل البيبلوغرافية
العنوان: Nanoemulsions containing a synthetic chalcone as an alternative for treating cutaneous leshmaniasis: optimization using a full factorial design.
المؤلفون: de Mattos CB; Faculdade de Farmácia, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil., Argenta DF; Faculdade de Farmácia, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil., Melchiades Gde L; Faculdade de Farmácia, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil., Cordeiro MN; Departamento de Química, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brazil., Tonini ML; Departamento de Microbiologia, Imunologia e Parasitologia, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brazil., Moraes MH; Departamento de Microbiologia, Imunologia e Parasitologia, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brazil., Weber TB; Departamento de Ciências Biológicas, Universidade Regional Integrada do Alto Uruguai e das Missões, Erechim, Rio Grande do Sul, Brazil., Roman SS; Departamento de Ciências Biológicas, Universidade Regional Integrada do Alto Uruguai e das Missões, Erechim, Rio Grande do Sul, Brazil., Nunes RJ; Departamento de Química, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brazil., Teixeira HF; Faculdade de Farmácia, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil., Steindel M; Departamento de Microbiologia, Imunologia e Parasitologia, Universidade Federal de Santa Catarina, Florianópolis, Santa Catarina, Brazil., Koester LS; Faculdade de Farmácia, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Rio Grande do Sul, Porto Alegre, Rio Grande do Sul, Brazil.
المصدر: International journal of nanomedicine [Int J Nanomedicine] 2015 Sep 01; Vol. 10, pp. 5529-42. Date of Electronic Publication: 2015 Sep 01 (Print Publication: 2015).
نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't
اللغة: English
بيانات الدورية: Publisher: DOVE Medical Press Country of Publication: New Zealand NLM ID: 101263847 Publication Model: eCollection Cited Medium: Internet ISSN: 1178-2013 (Electronic) Linking ISSN: 11769114 NLM ISO Abbreviation: Int J Nanomedicine Subsets: MEDLINE
أسماء مطبوعة: Original Publication: Auckland : DOVE Medical Press,
مواضيع طبية MeSH: Drug Delivery Systems*, Antiparasitic Agents/*pharmacology , Chalcone/*pharmacology , Leishmaniasis, Cutaneous/*drug therapy , Nanostructures/*chemistry, Administration, Cutaneous ; Antiparasitic Agents/chemistry ; Cell Line, Tumor ; Chalcone/chemistry ; Chemical Phenomena ; Emulsions ; Humans ; Hydrogen-Ion Concentration ; Inhibitory Concentration 50 ; Lecithins/chemistry ; Lecithins/pharmacology ; Particle Size ; Polysorbates/chemistry ; Polysorbates/pharmacology ; Skin/drug effects ; Skin/parasitology ; Solubility ; Structure-Activity Relationship ; Surface-Active Agents/chemistry ; Surface-Active Agents/pharmacology ; Viscosity
مستخلص: Nanoemulsions are drug delivery systems that may increase the penetration of lipophilic compounds through the skin, enhancing their topical effect. Chalcones are compounds of low water solubility that have been described as promising molecules for the treatment of cutaneous leishmaniasis (CL). In this context, the aim of this work was to optimize the development of a nanoemulsion containing a synthetic chalcone for CL treatment using a 2(2) full factorial design. The formulations were prepared by spontaneous emulsification and the experimental design studied the influence of two independent variables (type of surfactant - soybean lecithin or sorbitan monooleate and type of co-surfactants - polysorbate 20 or polysorbate 80) on the physicochemical characteristics of the nanoemulsions, as well as on the skin permeation/retention of the synthetic chalcone in porcine skin. In order to evaluate the stability of the systems, the antileishmanial assay was performed against Leishmania amazonensis 24 hours and 60 days after the preparation of the nanoemulsions. The formulation composed of soybean lecithin and polysorbate 20 presented suitable physicochemical characteristics (droplet size 171.9 nm; polydispersity index 0.14; zeta potential -39.43 mV; pH 5.16; and viscosity 2.00 cP), drug content (91.09%) and the highest retention in dermis (3.03 µg·g(-1)) - the main response of interest - confirmed by confocal microscopy. This formulation also presented better stability of leishmanicidal activity in vitro against L. amazonensis amastigote forms (half maximal inhibitory concentration value 0.32±0.05 µM), which confirmed the potential of the nanoemulsion soybean lecithin and polysorbate 20 for CL treatment.
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فهرسة مساهمة: Keywords: chalcone; full factorial; leishmaniasis; nanoemulsion; skin permeation
المشرفين على المادة: 0 (Antiparasitic Agents)
0 (Emulsions)
0 (Lecithins)
0 (Polysorbates)
0 (Surface-Active Agents)
5S5A2Q39HX (Chalcone)
تواريخ الأحداث: Date Created: 20150915 Date Completed: 20160909 Latest Revision: 20240520
رمز التحديث: 20240520
مُعرف محوري في PubMed: PMC4562752
DOI: 10.2147/IJN.S83929
PMID: 26366075
قاعدة البيانات: MEDLINE
الوصف
تدمد:1178-2013
DOI:10.2147/IJN.S83929