RESUMO
The objective of this study was to develop and evaluate nanoemulsion system for transdermal delivery of granisetron hydrochloride. Pseudo-ternary phase diagram was constructed to ascertain the concentration range of components of nanoemulsion composed of isopropyl myristate (IPM) as an oil phase, tween 85 as surfactant, ethanol as cosurfactant, water as aqueous phase. The effects of the content of IPM as an oil phase and n-methyl pyrrolidone (NMP) as transdermal enhancer on rat skin permeation of granisetron hydrochloride nanoemulsion were studied in vitro. The results showed that the mean particle size of nanoemulsion ranged from 50.4+/-1.5 to 82.4+/-0.9 nm with homogeneous size distribution. The resulted optimum formulation composed of 2.5% granisetron hydrochloride, 4% IPM, 40% tween 85/ethanol (1 : 1) and 10% NMP showed that the skin permeation rate was the highest (85.39+/-2.90 microg/cm(2)/h) and enhancement of drug permeability was 4.1-fold for transdermal delivery of granisetron hydrochloridein comparison with the control group (20% of tween 85 and 20% of ethanol micelle solution containing 2.5% of granisetron hydrochloride without IPM), and cumulative permeation amount was the highest (891.8+/-2.86 microg/cm(2)) with the shortest lag time (0.11+/-0.02 h) and was stable for at least 12 months. Therefore, the nanoemulsion system developed in this study offers a promising vehicle for the transdermal delivery system of granisetron hydrochloride, which may be as effective as oral or intravenous dosage forms and avoid some difficulties associated with these dosage forms.
Assuntos
Granisetron/administração & dosagem , Granisetron/farmacocinética , Nanopartículas/administração & dosagem , Absorção Cutânea , Administração Cutânea , Animais , Estabilidade de Medicamentos , Emulsões , Granisetron/química , Micelas , Nanopartículas/química , Tamanho da Partícula , Ratos , Solubilidade , Tensão SuperficialRESUMO
OBJECTIVE: To investigate the effects of tetrandrine on nuclear factor-kappaB (NF-kappaB) activity and proliferation of Diabetes Mellitus (DM) rats vascular smooth muscle cells (VSMCs). METHODS: DM models were established,the culture of DM and normal VSMCs were done by modified tissue-piece incoculztion; Inhibitory effect of Tetrandrine was determined by cell counting kit (CCK-8). Immunofluorescence laser confocal microscopy was used to estimate the effect of NF-kappaB in DM VSMCs with Tet. RESULTS: Tetrandrine inhibited the proliferation of DM and normal VSMCs,the IC50 value was (11.35 +/- 1.24) micromol/L and (28.01 +/- 4.35) micromol/L, respectively. Furthermore, Tetrandrine strongly inhibited the activation of NF-kappaB in DM VSMCs and reduced the nuclear translocation of NF-kappaB. CONCLUSION: Tetrandrine inhibits the proliferation of DM VSMCs more effectively than that of normal, the mechanism may be related to reducing NF-kappaB nuclear translocation.
Assuntos
Benzilisoquinolinas/farmacologia , Bloqueadores dos Canais de Cálcio/farmacologia , Proliferação de Células/efeitos dos fármacos , Diabetes Mellitus Experimental/patologia , Músculo Liso Vascular/efeitos dos fármacos , Stephania tetrandra/química , Animais , Células Cultivadas , Diabetes Mellitus Experimental/metabolismo , Masculino , Músculo Liso Vascular/metabolismo , NF-kappa B/efeitos dos fármacos , NF-kappa B/metabolismo , Plantas Medicinais/química , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , EstreptozocinaRESUMO
OBJECTIVE: To observe the effect of asiaticoside (AS) on IL-6,TNF-alpha, IL-10 of bronchoaliveolar lavage fluid (BALF) of acute lung injury (ALI) induced by lipopolysaccharides (LPS). METHODS: 56 Balb/c mice were randomly divided into control, model, sham operation,vehicle, model + asiaticoside 5, 15, 45 mg/kg groups. Model of ALI were established by intratracheal instillation of LPS 20 microl ( 2.5 mg/kg), mice were killed 24 hours later, the content of IL-6 ,TNF-alpha, IL-10 of BALF was detected by enzyme-linked immunosorbentassay (ELISA). RESULTS: AS could reduce the content of IL-6, TNF-alpha and increase IL-10 of BALF in dose-dependent manner. CONCLUSION: The protective effects against ALL induced by LPS on AS are related to reducing the content of IL-6, TNF-alpha, increasing secretion IL-10 and keeping the balance between inflammatory factors and anti-inflammatory factors.
Assuntos
Lesão Pulmonar Aguda/metabolismo , Líquido da Lavagem Broncoalveolar/química , Centella/química , Interleucinas/metabolismo , Triterpenos/farmacologia , Lesão Pulmonar Aguda/induzido quimicamente , Lesão Pulmonar Aguda/patologia , Animais , Anti-Inflamatórios/farmacologia , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Ensaio de Imunoadsorção Enzimática , Interleucina-10/metabolismo , Interleucina-6/metabolismo , Lipopolissacarídeos , Camundongos , Camundongos Endogâmicos BALB C , Distribuição Aleatória , Fator de Necrose Tumoral alfa/metabolismoRESUMO
OBJECTIVE: To observe effect of Xue Hanjing oral fluid on mice immunological function. METHOD: The weight of thymus gland and spleen and the function of abdominal cavity macrophage were measured. Production of the hemolysin antibody, the immunoglobulin of blood serum and complement and the proliferation of T lymphocytes were observed respectively by means of microblood, immune-turbidimetry and MTT staining. RESULT: Xue Hanjing oral fluid could enhance index of the thymus gland and spleen and the phago-percent of abdominal cavity macrophage, increase the immunoglobulin of blood serum(IgG and IgM), and accelerate production of the hemolysin antibody and the proliferation of T lymphocytes. CONCLUSIONS: Xue Hanjing oral can reinforce immunological function in mice.