A. Gowri Nath, Klaudi K. Vaiphei, Ankaj Kumar, Sargun Basrani, Ashwini Jadhav, Rudra Chakravarti, Dipanjan Ghosh, Kuldeep K. Bansal, Arvind Gulbake
{"title":"针对白色念珠菌的双药外用立方体凝胶:体外和体内概念验证","authors":"A. Gowri Nath, Klaudi K. Vaiphei, Ankaj Kumar, Sargun Basrani, Ashwini Jadhav, Rudra Chakravarti, Dipanjan Ghosh, Kuldeep K. Bansal, Arvind Gulbake","doi":"10.1208/s12249-025-03070-2","DOIUrl":null,"url":null,"abstract":"<div><p>Dual drug approaches are gaining research interest owing to the reduction of drug resistance and additive or synergistic effects in treating fungal infections caused by <i>Candida albicans</i>. The present study includes the combination of ketoconazole (KTC) and eugenol (EGN) co-embedded cubosomes (KTC-EGN-CBs) for the effective treatment of candidiasis.The bio-membrane-typical framework of the cubic phase in CBs can help retain both drugs leading to enhancement of antifungal activity. KTC-EGN-CBs were developed by high-speed homogenization, followed by the probe sonication. The optimized KTC-EGN-CBs depicted lower particle size (138.8 ± 1.03 nm) and PdI (0.260 ± 0.006) with a high entrapment efficiency of KTC (79.73 ± 1.21%) and EGN (90.92 ± 2.53%). Further, KTC-EGN-CBs were loaded into the hydrogel system for ease of topical application. The <i>ex vivo</i> diffusion study depicted the CBs helping the KTC and EGN to exhibit significantly higher permeation and retention owing to the resemblance in cubic structure with the skin. Additionally, the <i>in vitro</i> antifungal study of KTC-EGN-CBs resulted in a higher zone of inhibition when compared to the plain drugs against <i>Candida albicans</i>. Furthermore, the effectiveness of cubosomal formulation was observed in the inhibition of planktonic growth, yeast to hyphal formation, biofilm formation, and ROS production. The antifungal activity of KTC-EGN-CBs was found to be more prominent in the infected silkworm model than the plain KTC-EGN. The cell cytotoxicity study on human keratinocyte cells and the irritation study on the hen's egg test-chorioallantoic membrane assay revealed the non-cytotoxic and non-irritant nature of the prepared cubosomes. In a nutshell, these findings demonstrated CBs as a promising carrier for KTC and EGN to effectively treat candidiasis.</p></div>","PeriodicalId":6925,"journal":{"name":"AAPS PharmSciTech","volume":"26 3","pages":""},"PeriodicalIF":3.4000,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Dual Drug Loaded Topical Cubosomal Gel Against Candida Albicans: An In Vitro and In Vivo Proof of Concept\",\"authors\":\"A. Gowri Nath, Klaudi K. Vaiphei, Ankaj Kumar, Sargun Basrani, Ashwini Jadhav, Rudra Chakravarti, Dipanjan Ghosh, Kuldeep K. Bansal, Arvind Gulbake\",\"doi\":\"10.1208/s12249-025-03070-2\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>Dual drug approaches are gaining research interest owing to the reduction of drug resistance and additive or synergistic effects in treating fungal infections caused by <i>Candida albicans</i>. The present study includes the combination of ketoconazole (KTC) and eugenol (EGN) co-embedded cubosomes (KTC-EGN-CBs) for the effective treatment of candidiasis.The bio-membrane-typical framework of the cubic phase in CBs can help retain both drugs leading to enhancement of antifungal activity. KTC-EGN-CBs were developed by high-speed homogenization, followed by the probe sonication. The optimized KTC-EGN-CBs depicted lower particle size (138.8 ± 1.03 nm) and PdI (0.260 ± 0.006) with a high entrapment efficiency of KTC (79.73 ± 1.21%) and EGN (90.92 ± 2.53%). Further, KTC-EGN-CBs were loaded into the hydrogel system for ease of topical application. The <i>ex vivo</i> diffusion study depicted the CBs helping the KTC and EGN to exhibit significantly higher permeation and retention owing to the resemblance in cubic structure with the skin. Additionally, the <i>in vitro</i> antifungal study of KTC-EGN-CBs resulted in a higher zone of inhibition when compared to the plain drugs against <i>Candida albicans</i>. Furthermore, the effectiveness of cubosomal formulation was observed in the inhibition of planktonic growth, yeast to hyphal formation, biofilm formation, and ROS production. The antifungal activity of KTC-EGN-CBs was found to be more prominent in the infected silkworm model than the plain KTC-EGN. The cell cytotoxicity study on human keratinocyte cells and the irritation study on the hen's egg test-chorioallantoic membrane assay revealed the non-cytotoxic and non-irritant nature of the prepared cubosomes. In a nutshell, these findings demonstrated CBs as a promising carrier for KTC and EGN to effectively treat candidiasis.</p></div>\",\"PeriodicalId\":6925,\"journal\":{\"name\":\"AAPS PharmSciTech\",\"volume\":\"26 3\",\"pages\":\"\"},\"PeriodicalIF\":3.4000,\"publicationDate\":\"2025-03-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"AAPS PharmSciTech\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1208/s12249-025-03070-2\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"AAPS PharmSciTech","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1208/s12249-025-03070-2","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Dual Drug Loaded Topical Cubosomal Gel Against Candida Albicans: An In Vitro and In Vivo Proof of Concept
Dual drug approaches are gaining research interest owing to the reduction of drug resistance and additive or synergistic effects in treating fungal infections caused by Candida albicans. The present study includes the combination of ketoconazole (KTC) and eugenol (EGN) co-embedded cubosomes (KTC-EGN-CBs) for the effective treatment of candidiasis.The bio-membrane-typical framework of the cubic phase in CBs can help retain both drugs leading to enhancement of antifungal activity. KTC-EGN-CBs were developed by high-speed homogenization, followed by the probe sonication. The optimized KTC-EGN-CBs depicted lower particle size (138.8 ± 1.03 nm) and PdI (0.260 ± 0.006) with a high entrapment efficiency of KTC (79.73 ± 1.21%) and EGN (90.92 ± 2.53%). Further, KTC-EGN-CBs were loaded into the hydrogel system for ease of topical application. The ex vivo diffusion study depicted the CBs helping the KTC and EGN to exhibit significantly higher permeation and retention owing to the resemblance in cubic structure with the skin. Additionally, the in vitro antifungal study of KTC-EGN-CBs resulted in a higher zone of inhibition when compared to the plain drugs against Candida albicans. Furthermore, the effectiveness of cubosomal formulation was observed in the inhibition of planktonic growth, yeast to hyphal formation, biofilm formation, and ROS production. The antifungal activity of KTC-EGN-CBs was found to be more prominent in the infected silkworm model than the plain KTC-EGN. The cell cytotoxicity study on human keratinocyte cells and the irritation study on the hen's egg test-chorioallantoic membrane assay revealed the non-cytotoxic and non-irritant nature of the prepared cubosomes. In a nutshell, these findings demonstrated CBs as a promising carrier for KTC and EGN to effectively treat candidiasis.
期刊介绍:
AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.