The purpose of the present research was to compare the skin permeation and study the antifungal efficacy of Terbinafine hydrochloride (TH) transfersome, menthosome and ethosome formulations under non-occlusive conditions. Terbinafine hydrochloride is an antifungal drug for onychomycosis. Poor permeability of its external preparation leads to poor curative effect. Preparation of TH transfersome utilized the mixture component model to determine the optimized desirable formula using different concentrations of nonionic surfactant, Span and Tween (X1 & X2 respectively) were investigated. The results revealed that both X1 and X2 had a pronounced effect on vesicle size (Y1) and entrapment efficiency (EE) of the drug (Y2). The vesicles were prepared and characterized for shape, size, zeta potential and entrapment efficiency. Ex vivo study via Franz diffusion cells was used for the percutaneous absorption studies. The optimum desirable formula of transfersome, menthosome and ethosome formulations were showed vesicle size (78.7, 122.8 and 67.8 nm), zeta potential (-8.28, 8.77 and 11.30 mV) and encapsulation efficiency (92.67, 93.86 and 95.75%), respectively. Ex vivo permeation of the drug-loaded nanovesicle showed more than two to three folds higher permeation rate compared with drug suspension. Deformability verified elasticity of the preparation. Finally, TH nanovesicle formulations improved drug delivery with greater improvement in skin permeation and antifungal activity. Our selected formulae showed potent antifungal effect against Aspergillus niger for the treatment of fingernails or toenails. Keywords; Terbinafine Hydrochloride, Transfersome, Menthosome, Ethosome, Nanovesicles
{"title":"COMPARATIVE STUDY OF TERBINAFINE HYDROCHLORIDE TRANSFERSOME, MENTHOSOME AND ETHOSOME NANOVESICLE FORMULATIONS VIA SKIN PERMEATION AND ANTIFUNGAL EFFICACY","authors":"A. Zaky","doi":"10.21608/AJPS.2018.6631","DOIUrl":"https://doi.org/10.21608/AJPS.2018.6631","url":null,"abstract":"The purpose of the present research was to compare the skin permeation and study the antifungal efficacy of Terbinafine hydrochloride (TH) transfersome, menthosome and ethosome formulations under non-occlusive conditions. Terbinafine hydrochloride is an antifungal drug for onychomycosis. Poor permeability of its external preparation leads to poor curative effect. Preparation of TH transfersome utilized the mixture component model to determine the optimized desirable formula using different concentrations of nonionic surfactant, Span and Tween (X1 & X2 respectively) were investigated. The results revealed that both X1 and X2 had a pronounced effect on vesicle size (Y1) and entrapment efficiency (EE) of the drug (Y2). The vesicles were prepared and characterized for shape, size, zeta potential and entrapment efficiency. Ex vivo study via Franz diffusion cells was used for the percutaneous absorption studies. The optimum desirable formula of transfersome, menthosome and ethosome formulations were showed vesicle size (78.7, 122.8 and 67.8 nm), zeta potential (-8.28, 8.77 and 11.30 mV) and encapsulation efficiency (92.67, 93.86 and 95.75%), respectively. Ex vivo permeation of the drug-loaded nanovesicle showed more than two to three folds higher permeation rate compared with drug suspension. Deformability verified elasticity of the preparation. Finally, TH nanovesicle formulations improved drug delivery with greater improvement in skin permeation and antifungal activity. Our selected formulae showed potent antifungal effect against Aspergillus niger for the treatment of fingernails or toenails. Keywords; Terbinafine Hydrochloride, Transfersome, Menthosome, Ethosome, Nanovesicles","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"27 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2016-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83557909","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Macrophage–epithelial interactions play a crucial role in breast cancer progression and metastasis. Tumor associated macrophages (TAMs) provide the tumor microenvironment with multiple inflammatory mediators that stimulate several signaling pathways which participate in survival and growth of cancer cells, thus they have become an attractive target for chemotherapeutic agents. Sulindac Sulfide is one of NSAIDs and its anticancer activity in prevention of tumor incidence and progression has been documented in several types of cancer. The aim of this study was to test the effects of media conditioned by U937 human monocytes (U937-CM) as well as the effect of Sulindac Sulfide on the survival oncogenic expression and apoptosis of MCF-7 cells. The results showed that U937-CM enhanced MCF-7 survival and proliferation through significant increase in Ras expression which resulted in upregulation of anti-apoptotic protein Bcl-2 and down regulation of tumor suppressor Par-4. Sulindac Sulfide treatment inhibited the growth of induced cells by inhibition of Ras expression and its downstream signaling. Suppression of Ras is accompanied by activation of apoptotic machinery through down regulation of Bcl-2 and upregulation of Par-4 that resulted in significant activation of caspase-3.The current data demonstrate that Sulindac Sulfide succeeded in suppressing the paracrine effect of TAMs on breast cancer cells suggesting the promising role in breast cancer treatment.
{"title":"SULINDAC SULFIDE INDUCES APOPTOSIS OF BREAST CANCER CELLS ACTIVATED BY CO-CULTURE MODEL: A MECHANISM MEDIATED BY RAS SIGNALING PATHWAY.","authors":"N. A. Thabet","doi":"10.21608/AJPS.2018.6638","DOIUrl":"https://doi.org/10.21608/AJPS.2018.6638","url":null,"abstract":"Macrophage–epithelial interactions play a crucial role in breast cancer progression and metastasis. Tumor associated macrophages (TAMs) provide the tumor microenvironment with multiple inflammatory mediators that stimulate several signaling pathways which participate in survival and growth of cancer cells, thus they have become an attractive target for chemotherapeutic agents. Sulindac Sulfide is one of NSAIDs and its anticancer activity in prevention of tumor incidence and progression has been documented in several types of cancer. The aim of this study was to test the effects of media conditioned by U937 human monocytes (U937-CM) as well as the effect of Sulindac Sulfide on the survival oncogenic expression and apoptosis of MCF-7 cells. The results showed that U937-CM enhanced MCF-7 survival and proliferation through significant increase in Ras expression which resulted in upregulation of anti-apoptotic protein Bcl-2 and down regulation of tumor suppressor Par-4. Sulindac Sulfide treatment inhibited the growth of induced cells by inhibition of Ras expression and its downstream signaling. Suppression of Ras is accompanied by activation of apoptotic machinery through down regulation of Bcl-2 and upregulation of Par-4 that resulted in significant activation of caspase-3.The current data demonstrate that Sulindac Sulfide succeeded in suppressing the paracrine effect of TAMs on breast cancer cells suggesting the promising role in breast cancer treatment.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2016-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81359470","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
The present study was conducted to evaluate the ameliorative role of pumpkin seed oil (PSO) against potential adverse effects of bisphenol-A (BPA) in male mice. BPA was administered to the mice orally at a dose of 50 mg/kg body weight once a day for 28 successive days. While, PSO was administered to the mice orally at 1 mL/kg b.w. either before, with or after treatment of BPA, once a day for 28 successive days. The studied parameters were DNA damage evaluation using comet assay in liver and testes cells and micronucleus test in bone marrow; and histopathological examination of liver and testes tissues. Results revealed that BPA induced DNA damage in tested cells and marked histopathological alterations in liver and testes. In contrast, PSO treatments alleviated DNA damage and improved the histopathological alterations in liver and testes tissues. Furthermore, administration of mice with the PSO before BPA treatment was the best regimen in the alleviation of the adverse effects of BPA, followed by administration of PSO after then with treatment of BPA. It can be concluded that PSO may has a protective role against BPA genotoxicity and histopathological alterations in male mice.
{"title":"AMELIORATIVE EFFECT OF PUMPKIN SEED OIL AGAINST THE BISPHENOL-A ADVERSE EFFECTS IN MALE MICE.","authors":"O. Elhamalawy","doi":"10.21608/AJPS.2018.6641","DOIUrl":"https://doi.org/10.21608/AJPS.2018.6641","url":null,"abstract":"The present study was conducted to evaluate the ameliorative role of pumpkin seed oil (PSO) against potential adverse effects of bisphenol-A (BPA) in male mice. BPA was administered to the mice orally at a dose of 50 mg/kg body weight once a day for 28 successive days. While, PSO was administered to the mice orally at 1 mL/kg b.w. either before, with or after treatment of BPA, once a day for 28 successive days. The studied parameters were DNA damage evaluation using comet assay in liver and testes cells and micronucleus test in bone marrow; and histopathological examination of liver and testes tissues. Results revealed that BPA induced DNA damage in tested cells and marked histopathological alterations in liver and testes. In contrast, PSO treatments alleviated DNA damage and improved the histopathological alterations in liver and testes tissues. Furthermore, administration of mice with the PSO before BPA treatment was the best regimen in the alleviation of the adverse effects of BPA, followed by administration of PSO after then with treatment of BPA. It can be concluded that PSO may has a protective role against BPA genotoxicity and histopathological alterations in male mice.","PeriodicalId":7603,"journal":{"name":"Al-Azhar Journal of Pharmaceutical Sciences","volume":"2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2016-03-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79426697","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
京公网安备 11010802042870号
京ICP备2023020795号-1
扫码关注我们
求助内容：
应助结果提醒方式：