Reem Abou Assi, Ibrahim M Abdulbaqi, Siew Mei Tan, Habibah A Wahab, Yusrida Darwis, Siok-Yee Chan
{"title":"打破障碍:双体凝胶电位为三苯氧胺透皮治疗癌症铺平道路。","authors":"Reem Abou Assi, Ibrahim M Abdulbaqi, Siew Mei Tan, Habibah A Wahab, Yusrida Darwis, Siok-Yee Chan","doi":"10.1080/03639045.2023.2256404","DOIUrl":null,"url":null,"abstract":"OBJECTIVE Breast cancer affects women globally, regardless of age or location. On the other hand, Tamoxifen (TXN), a class II biopharmaceutical drug is acting as a prophylactic/treating agent for women at risk of and/or with hormone receptor-positive breast cancer. However, its oral administration has life-threatening side effects, which have led researchers to investigate alternative delivery methods. One such method is transdermal drug delivery utilising bile salts as penetration enhancers, aka Bilosomes. METHODS Bilosomes formulations were optimized statistically for the outcome of vesicle shape, size, and entrapment efficiency using two types of bile, i.e., sodium taurocholate and sodium cholate. These bilosomes were then loaded into HPMC base gel and further characterized for their morphology, drug content, pH, viscosity, spreadability and eventually ex-vivo skin penetration and deposition studies. RESULTS Findings showed that sodium cholate has superiority as a penetration enhancer over sodium taurocholate in terms of morphological characterises, zeta potential, and cumulative amounts of tamoxifen permeated per unit area (15.13 ± 0.71 μg/cm2 and 6.51 ± 0.6 μg/cm2 respectively). In fact, bilosomes designed with sodium cholate provided around 9 folds of skin deposition compared to TXN non-bilosomal gel. CONCLUSION Bilosomes gels could be a promising option for locally delivering tamoxifen to the breast through the skin, offering an encouraging transdermal solution.","PeriodicalId":11263,"journal":{"name":"Drug Development and Industrial Pharmacy","volume":null,"pages":null},"PeriodicalIF":2.4000,"publicationDate":"2023-09-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Breaking barriers: bilosomes gel potentials to pave the way for transdermal breast cancer treatment with Tamoxifen.\",\"authors\":\"Reem Abou Assi, Ibrahim M Abdulbaqi, Siew Mei Tan, Habibah A Wahab, Yusrida Darwis, Siok-Yee Chan\",\"doi\":\"10.1080/03639045.2023.2256404\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"OBJECTIVE Breast cancer affects women globally, regardless of age or location. On the other hand, Tamoxifen (TXN), a class II biopharmaceutical drug is acting as a prophylactic/treating agent for women at risk of and/or with hormone receptor-positive breast cancer. However, its oral administration has life-threatening side effects, which have led researchers to investigate alternative delivery methods. One such method is transdermal drug delivery utilising bile salts as penetration enhancers, aka Bilosomes. METHODS Bilosomes formulations were optimized statistically for the outcome of vesicle shape, size, and entrapment efficiency using two types of bile, i.e., sodium taurocholate and sodium cholate. These bilosomes were then loaded into HPMC base gel and further characterized for their morphology, drug content, pH, viscosity, spreadability and eventually ex-vivo skin penetration and deposition studies. RESULTS Findings showed that sodium cholate has superiority as a penetration enhancer over sodium taurocholate in terms of morphological characterises, zeta potential, and cumulative amounts of tamoxifen permeated per unit area (15.13 ± 0.71 μg/cm2 and 6.51 ± 0.6 μg/cm2 respectively). In fact, bilosomes designed with sodium cholate provided around 9 folds of skin deposition compared to TXN non-bilosomal gel. CONCLUSION Bilosomes gels could be a promising option for locally delivering tamoxifen to the breast through the skin, offering an encouraging transdermal solution.\",\"PeriodicalId\":11263,\"journal\":{\"name\":\"Drug Development and Industrial Pharmacy\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":2.4000,\"publicationDate\":\"2023-09-18\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug Development and Industrial Pharmacy\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/03639045.2023.2256404\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug Development and Industrial Pharmacy","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/03639045.2023.2256404","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Breaking barriers: bilosomes gel potentials to pave the way for transdermal breast cancer treatment with Tamoxifen.
OBJECTIVE Breast cancer affects women globally, regardless of age or location. On the other hand, Tamoxifen (TXN), a class II biopharmaceutical drug is acting as a prophylactic/treating agent for women at risk of and/or with hormone receptor-positive breast cancer. However, its oral administration has life-threatening side effects, which have led researchers to investigate alternative delivery methods. One such method is transdermal drug delivery utilising bile salts as penetration enhancers, aka Bilosomes. METHODS Bilosomes formulations were optimized statistically for the outcome of vesicle shape, size, and entrapment efficiency using two types of bile, i.e., sodium taurocholate and sodium cholate. These bilosomes were then loaded into HPMC base gel and further characterized for their morphology, drug content, pH, viscosity, spreadability and eventually ex-vivo skin penetration and deposition studies. RESULTS Findings showed that sodium cholate has superiority as a penetration enhancer over sodium taurocholate in terms of morphological characterises, zeta potential, and cumulative amounts of tamoxifen permeated per unit area (15.13 ± 0.71 μg/cm2 and 6.51 ± 0.6 μg/cm2 respectively). In fact, bilosomes designed with sodium cholate provided around 9 folds of skin deposition compared to TXN non-bilosomal gel. CONCLUSION Bilosomes gels could be a promising option for locally delivering tamoxifen to the breast through the skin, offering an encouraging transdermal solution.
期刊介绍:
The aim of Drug Development and Industrial Pharmacy is to publish novel, original, peer-reviewed research manuscripts within relevant topics and research methods related to pharmaceutical research and development, and industrial pharmacy. Research papers must be hypothesis driven and emphasize innovative breakthrough topics in pharmaceutics and drug delivery. The journal will also consider timely critical review papers.