RESUMO
OBJECTIVE: The purpose of this study was to formulate stable Ganoderma lucidum (GLT) nanogels suitable for topical delivery with a view to improve the therapeutic effect for frostbite. METHODS: GLT nanosuspensions were formulated using the high-pressure homogenization technique and then suitably gelled for characterized. In order to confirm the advantages of GLT nanogel for dermal application, skin permeation studies in vitro and pharmacodynamic evaluation in vivo were studied and compared with GLT-carbopol gel. RESULTS: The particle size analysis and SEM studies revealed that GLT nanosuspensions were still stably kept their particle size after suitably gelled by carbopol preparation. The drug content, pH, and spreadability of the GLT nanogel was found to be 99.23 ± 1.8%, 6.07 ± 0.1, and 26.42 (g·cm)/s, which were within acceptable limits. In vitro permeation studies through rat skin indicated that the amount of GLT permeated through skin of GLT nanogel after 24 h was higher than GLT-carbopol gel, and GLT nanogel increased the accumulative amount of GLT in epidermis five times than GLT-carbopol gel. No oedema and erythema were observed after administration of GLT nanogel on the rabbits' skin. Pharmacodynamic study showed that GLT nanogel was more effective than GLT-carbopol gel in treatment of frostbite. CONCLUSION: The GLT nanogel possess superior therapeutic effect for frostbite compared with the GLT-carbopol gel, which indicates that nanogels are eligible for the use as a suitable nanomedicine for dermal delivery of poorly soluble drugs such as GLT.
Assuntos
Congelamento das Extremidades/tratamento farmacológico , Nanopartículas , Reishi/química , Pele/efeitos dos fármacos , Triterpenos/administração & dosagem , Resinas Acrílicas/química , Administração Cutânea , Animais , Modelos Animais de Doenças , Composição de Medicamentos , Estabilidade de Medicamentos , Excipientes/química , Congelamento das Extremidades/patologia , Géis , Concentração de Íons de Hidrogênio , Masculino , Microscopia Eletrônica de Varredura , Nanotecnologia , Tamanho da Partícula , Permeabilidade , Fitoterapia , Plantas Medicinais , Pressão , Coelhos , Ratos Sprague-Dawley , Pele/metabolismo , Pele/patologia , Absorção Cutânea , Propriedades de Superfície , Tecnologia Farmacêutica/métodos , Triterpenos/química , Triterpenos/isolamento & purificação , Triterpenos/farmacocinética , ViscosidadeRESUMO
The purpose of this paper was to study the influence of drug physicochemical characteristics on in vitro transdermal absorption of hydrophobic drug nanosuspensions. Four drug nanosuspensions were produced by high-pressure homogenization technique, which were the same in stabilizer and similar in particle size. Differential scanning calorimetry and powder X-ray diffraction analysis showed that the crystalline state of the nanocrystals did not change. In vitro permeation study demonstrated that the drug nanosuspensions have a higher rate of permeation that ranged from 1.69- to 3.74-fold compared to drug microsuspensions. Correlation analysis between drug physicochemical properties and Jss revealed that log P and pKa were factors that influenced the in vitro transdermal absorption of hydrophobic drug nanosuspensions, and drugs with a log P value around 3 and a higher pKa value (when pKa < pH+2) would gain higher Jss in this paper.