Noelia Pérez-González, José A Morales-Molina, Ana C Calpena-Campmany, Lyda Halbaut, María J Rodríguez-Lagunas, Nuria Bozal-de Febrer, Eliana B Souto, Mireia Mallandrich, Beatriz Clares-Naveros
{"title":"用于颊黏膜和舌下黏膜抗真菌感染的卡泊芬净制剂:理化特性、流变分析、释放和体内外渗透性概况。","authors":"Noelia Pérez-González, José A Morales-Molina, Ana C Calpena-Campmany, Lyda Halbaut, María J Rodríguez-Lagunas, Nuria Bozal-de Febrer, Eliana B Souto, Mireia Mallandrich, Beatriz Clares-Naveros","doi":"10.1080/10837450.2024.2415545","DOIUrl":null,"url":null,"abstract":"<p><strong>Aim: </strong>Oral candidiasis is often challenging due to limited effectiveness of topical treatments. This study aimed to develop novel caspofungin formulations for administration onto the oral mucosa to enhance drug retention and efficacy.</p><p><strong>Method: </strong>Five caspofungin (2%, w/v) formulations were developed to assess their permeability, retention and mucoadhesiveness. <i>Ex vivo</i> permeability assays were performed on buccal and sublingual mucosae, and histological analyses conducted to evaluate tissue tolerance.</p><p><strong>Results: </strong>Formulation composed of chitosan demonstrated the highest retention in both buccal (5183.24 ± 587.32 µg/cm<sup>2</sup>) and sublingual (1090.72 ± 110.26 µg/cm<sup>2</sup>) mucosae. Other formulations exhibited significantly lower retention, ranging from 7.53 ± 0.81 to 1852.10 ± 193.24 µg/cm<sup>2</sup> in buccal mucosa and 1.64 ± 0.14 to 317.74 ± 31.78 µg/cm<sup>2</sup> in sublingual mucosa. Chitosan-based formulation exhibited the highest mucoadhesive strength, with values of 5179.05 ± 31.99 mN/cm<sup>2</sup> for buccal and 7026.10 ± 123.41 mN/cm<sup>2</sup> for sublingual mucosae, and also superior extensibility, which facilitates application in the oral cavity. All formulations showed antifungal activity against <i>Candida</i> spp., and histological analyses revealed minor epithelial alterations.</p><p><strong>Conclusion: </strong>The developed formulations offer distinct advantages for treating oral candidiasis, with chitosan formulation emerging as the most promising due to its superior retention, mucoadhesion force, and spreadability, making it a potential candidate for further clinical investigation.</p>","PeriodicalId":20004,"journal":{"name":"Pharmaceutical Development and Technology","volume":" ","pages":"1042-1063"},"PeriodicalIF":2.6000,"publicationDate":"2024-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Caspofungin formulations for buccal and sublingual mucosae anti-fungal infections: physicochemical characterization, rheological analysis, release and <i>ex vivo</i> permeability profiles.\",\"authors\":\"Noelia Pérez-González, José A Morales-Molina, Ana C Calpena-Campmany, Lyda Halbaut, María J Rodríguez-Lagunas, Nuria Bozal-de Febrer, Eliana B Souto, Mireia Mallandrich, Beatriz Clares-Naveros\",\"doi\":\"10.1080/10837450.2024.2415545\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Aim: </strong>Oral candidiasis is often challenging due to limited effectiveness of topical treatments. This study aimed to develop novel caspofungin formulations for administration onto the oral mucosa to enhance drug retention and efficacy.</p><p><strong>Method: </strong>Five caspofungin (2%, w/v) formulations were developed to assess their permeability, retention and mucoadhesiveness. <i>Ex vivo</i> permeability assays were performed on buccal and sublingual mucosae, and histological analyses conducted to evaluate tissue tolerance.</p><p><strong>Results: </strong>Formulation composed of chitosan demonstrated the highest retention in both buccal (5183.24 ± 587.32 µg/cm<sup>2</sup>) and sublingual (1090.72 ± 110.26 µg/cm<sup>2</sup>) mucosae. Other formulations exhibited significantly lower retention, ranging from 7.53 ± 0.81 to 1852.10 ± 193.24 µg/cm<sup>2</sup> in buccal mucosa and 1.64 ± 0.14 to 317.74 ± 31.78 µg/cm<sup>2</sup> in sublingual mucosa. Chitosan-based formulation exhibited the highest mucoadhesive strength, with values of 5179.05 ± 31.99 mN/cm<sup>2</sup> for buccal and 7026.10 ± 123.41 mN/cm<sup>2</sup> for sublingual mucosae, and also superior extensibility, which facilitates application in the oral cavity. All formulations showed antifungal activity against <i>Candida</i> spp., and histological analyses revealed minor epithelial alterations.</p><p><strong>Conclusion: </strong>The developed formulations offer distinct advantages for treating oral candidiasis, with chitosan formulation emerging as the most promising due to its superior retention, mucoadhesion force, and spreadability, making it a potential candidate for further clinical investigation.</p>\",\"PeriodicalId\":20004,\"journal\":{\"name\":\"Pharmaceutical Development and Technology\",\"volume\":\" \",\"pages\":\"1042-1063\"},\"PeriodicalIF\":2.6000,\"publicationDate\":\"2024-11-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutical Development and Technology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1080/10837450.2024.2415545\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2024/10/17 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical Development and Technology","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1080/10837450.2024.2415545","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2024/10/17 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Caspofungin formulations for buccal and sublingual mucosae anti-fungal infections: physicochemical characterization, rheological analysis, release and ex vivo permeability profiles.
Aim: Oral candidiasis is often challenging due to limited effectiveness of topical treatments. This study aimed to develop novel caspofungin formulations for administration onto the oral mucosa to enhance drug retention and efficacy.
Method: Five caspofungin (2%, w/v) formulations were developed to assess their permeability, retention and mucoadhesiveness. Ex vivo permeability assays were performed on buccal and sublingual mucosae, and histological analyses conducted to evaluate tissue tolerance.
Results: Formulation composed of chitosan demonstrated the highest retention in both buccal (5183.24 ± 587.32 µg/cm2) and sublingual (1090.72 ± 110.26 µg/cm2) mucosae. Other formulations exhibited significantly lower retention, ranging from 7.53 ± 0.81 to 1852.10 ± 193.24 µg/cm2 in buccal mucosa and 1.64 ± 0.14 to 317.74 ± 31.78 µg/cm2 in sublingual mucosa. Chitosan-based formulation exhibited the highest mucoadhesive strength, with values of 5179.05 ± 31.99 mN/cm2 for buccal and 7026.10 ± 123.41 mN/cm2 for sublingual mucosae, and also superior extensibility, which facilitates application in the oral cavity. All formulations showed antifungal activity against Candida spp., and histological analyses revealed minor epithelial alterations.
Conclusion: The developed formulations offer distinct advantages for treating oral candidiasis, with chitosan formulation emerging as the most promising due to its superior retention, mucoadhesion force, and spreadability, making it a potential candidate for further clinical investigation.
期刊介绍:
Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology.
Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as:
-Preformulation and pharmaceutical formulation studies
-Pharmaceutical materials selection and characterization
-Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation
-QbD in the form a risk assessment and DoE driven approaches
-Design of dosage forms and drug delivery systems
-Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies
-Drug delivery systems research and quality improvement
-Pharmaceutical regulatory affairs
This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.