Preparations of liposomal fluconazole and their in vitro antifungal activity
Abstract Fluconazole was successfully incorporated into multilamellar (MLV) and large unilamellar liposomes (LUV). Both MLV and LUV were stable up to 72 h in saline but were less stable in the high-resolution medium. The MLV-entrapped fluconazole was found to be four-fold more active than LUV-entrap...
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| Veröffentlicht in: | Journal of microencapsulation 1993, Vol.10 (2), p.229-236 |
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| container_title | Journal of microencapsulation |
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| creator | Singh, M. Singh, M. P. Maiti, S. N. Gandhi, A. Micetich, R. G. Atwal, H. |
| description | Abstract
Fluconazole was successfully incorporated into multilamellar (MLV) and large unilamellar liposomes (LUV). Both MLV and LUV were stable up to 72 h in saline but were less stable in the high-resolution medium. The MLV-entrapped fluconazole was found to be four-fold more active than LUV-entrapped fluconazole against Candida pseudotropicalis and over six-fold more active against C. albicans. The MLV-fluconazole was one-fold less active than free fluconazole in terms of its endpoints (MIC value). However, when compared with free fluconazole, MLV-fluconazole was one-fold more active against two strains of C. albicans and equally active against C. kefyr and C. parapsilosis. In an incubation time-dependent assay against C. tropicalis, MLV-Fluconazole was one-fold more active after 16 h incubation and two-fold less active than fluconazole after 24 or 36 h post-incubation. Our results demonstrate the usefulness of liposomal formulation of the water-soluble azole, fluconazole, in the limited in vitro assay method used. |
| doi_str_mv | 10.3109/02652049309104389 |
| format | Article |
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Fluconazole was successfully incorporated into multilamellar (MLV) and large unilamellar liposomes (LUV). Both MLV and LUV were stable up to 72 h in saline but were less stable in the high-resolution medium. The MLV-entrapped fluconazole was found to be four-fold more active than LUV-entrapped fluconazole against Candida pseudotropicalis and over six-fold more active against C. albicans. The MLV-fluconazole was one-fold less active than free fluconazole in terms of its endpoints (MIC value). However, when compared with free fluconazole, MLV-fluconazole was one-fold more active against two strains of C. albicans and equally active against C. kefyr and C. parapsilosis. In an incubation time-dependent assay against C. tropicalis, MLV-Fluconazole was one-fold more active after 16 h incubation and two-fold less active than fluconazole after 24 or 36 h post-incubation. Our results demonstrate the usefulness of liposomal formulation of the water-soluble azole, fluconazole, in the limited in vitro assay method used.</description><identifier>ISSN: 0265-2048</identifier><identifier>EISSN: 1464-5246</identifier><identifier>DOI: 10.3109/02652049309104389</identifier><identifier>PMID: 8331496</identifier><identifier>CODEN: JOMIEF</identifier><language>eng</language><publisher>Colchester: Informa UK Ltd</publisher><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antifungal agents ; Antifungal Agents - administration & dosage ; Antifungal Agents - pharmacology ; Biological and medical sciences ; Candida - drug effects ; Candida albicans ; Candida albicans - drug effects ; Candida kefyr ; Candida parapsilosis ; Candida pseudotropicalis ; Candida tropicalis ; Culture Media ; Drug Carriers ; Fluconazole - administration & dosage ; Fluconazole - pharmacology ; Indicators and Reagents ; Liposomes ; Medical sciences ; Microbial Sensitivity Tests ; Particle Size ; Pharmacology. Drug treatments</subject><ispartof>Journal of microencapsulation, 1993, Vol.10 (2), p.229-236</ispartof><rights>1993 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1993</rights><rights>1993 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c376t-950aec4a651840a66fa68ec6d682cd6717093ab71e74c19d6f4f1c427154beb3</citedby><cites>FETCH-LOGICAL-c376t-950aec4a651840a66fa68ec6d682cd6717093ab71e74c19d6f4f1c427154beb3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.3109/02652049309104389$$EPDF$$P50$$Ginformahealthcare$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.3109/02652049309104389$$EHTML$$P50$$Ginformahealthcare$$H</linktohtml><link.rule.ids>314,780,784,4024,27923,27924,27925,59647,59753,60436,60542,61221,61256,61402,61437</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=4758291$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8331496$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Singh, M.</creatorcontrib><creatorcontrib>Singh, M. P.</creatorcontrib><creatorcontrib>Maiti, S. N.</creatorcontrib><creatorcontrib>Gandhi, A.</creatorcontrib><creatorcontrib>Micetich, R. G.</creatorcontrib><creatorcontrib>Atwal, H.</creatorcontrib><title>Preparations of liposomal fluconazole and their in vitro antifungal activity</title><title>Journal of microencapsulation</title><addtitle>J Microencapsul</addtitle><description>Abstract
Fluconazole was successfully incorporated into multilamellar (MLV) and large unilamellar liposomes (LUV). Both MLV and LUV were stable up to 72 h in saline but were less stable in the high-resolution medium. The MLV-entrapped fluconazole was found to be four-fold more active than LUV-entrapped fluconazole against Candida pseudotropicalis and over six-fold more active against C. albicans. The MLV-fluconazole was one-fold less active than free fluconazole in terms of its endpoints (MIC value). However, when compared with free fluconazole, MLV-fluconazole was one-fold more active against two strains of C. albicans and equally active against C. kefyr and C. parapsilosis. In an incubation time-dependent assay against C. tropicalis, MLV-Fluconazole was one-fold more active after 16 h incubation and two-fold less active than fluconazole after 24 or 36 h post-incubation. Our results demonstrate the usefulness of liposomal formulation of the water-soluble azole, fluconazole, in the limited in vitro assay method used.</description><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antifungal agents</subject><subject>Antifungal Agents - administration & dosage</subject><subject>Antifungal Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Candida - drug effects</subject><subject>Candida albicans</subject><subject>Candida albicans - drug effects</subject><subject>Candida kefyr</subject><subject>Candida parapsilosis</subject><subject>Candida pseudotropicalis</subject><subject>Candida tropicalis</subject><subject>Culture Media</subject><subject>Drug Carriers</subject><subject>Fluconazole - administration & dosage</subject><subject>Fluconazole - pharmacology</subject><subject>Indicators and Reagents</subject><subject>Liposomes</subject><subject>Medical sciences</subject><subject>Microbial Sensitivity Tests</subject><subject>Particle Size</subject><subject>Pharmacology. 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G.</creator><creator>Atwal, H.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><general>Informa</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>M7N</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>1993</creationdate><title>Preparations of liposomal fluconazole and their in vitro antifungal activity</title><author>Singh, M. ; Singh, M. P. ; Maiti, S. N. ; Gandhi, A. ; Micetich, R. G. ; Atwal, H.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c376t-950aec4a651840a66fa68ec6d682cd6717093ab71e74c19d6f4f1c427154beb3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antifungal agents</topic><topic>Antifungal Agents - administration & dosage</topic><topic>Antifungal Agents - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Candida - drug effects</topic><topic>Candida albicans</topic><topic>Candida albicans - drug effects</topic><topic>Candida kefyr</topic><topic>Candida parapsilosis</topic><topic>Candida pseudotropicalis</topic><topic>Candida tropicalis</topic><topic>Culture Media</topic><topic>Drug Carriers</topic><topic>Fluconazole - administration & dosage</topic><topic>Fluconazole - pharmacology</topic><topic>Indicators and Reagents</topic><topic>Liposomes</topic><topic>Medical sciences</topic><topic>Microbial Sensitivity Tests</topic><topic>Particle Size</topic><topic>Pharmacology. Drug treatments</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Singh, M.</creatorcontrib><creatorcontrib>Singh, M. P.</creatorcontrib><creatorcontrib>Maiti, S. N.</creatorcontrib><creatorcontrib>Gandhi, A.</creatorcontrib><creatorcontrib>Micetich, R. G.</creatorcontrib><creatorcontrib>Atwal, H.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of microencapsulation</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Singh, M.</au><au>Singh, M. P.</au><au>Maiti, S. N.</au><au>Gandhi, A.</au><au>Micetich, R. G.</au><au>Atwal, H.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparations of liposomal fluconazole and their in vitro antifungal activity</atitle><jtitle>Journal of microencapsulation</jtitle><addtitle>J Microencapsul</addtitle><date>1993</date><risdate>1993</risdate><volume>10</volume><issue>2</issue><spage>229</spage><epage>236</epage><pages>229-236</pages><issn>0265-2048</issn><eissn>1464-5246</eissn><coden>JOMIEF</coden><abstract>Abstract
Fluconazole was successfully incorporated into multilamellar (MLV) and large unilamellar liposomes (LUV). Both MLV and LUV were stable up to 72 h in saline but were less stable in the high-resolution medium. The MLV-entrapped fluconazole was found to be four-fold more active than LUV-entrapped fluconazole against Candida pseudotropicalis and over six-fold more active against C. albicans. The MLV-fluconazole was one-fold less active than free fluconazole in terms of its endpoints (MIC value). However, when compared with free fluconazole, MLV-fluconazole was one-fold more active against two strains of C. albicans and equally active against C. kefyr and C. parapsilosis. In an incubation time-dependent assay against C. tropicalis, MLV-Fluconazole was one-fold more active after 16 h incubation and two-fold less active than fluconazole after 24 or 36 h post-incubation. Our results demonstrate the usefulness of liposomal formulation of the water-soluble azole, fluconazole, in the limited in vitro assay method used.</abstract><cop>Colchester</cop><pub>Informa UK Ltd</pub><pmid>8331496</pmid><doi>10.3109/02652049309104389</doi><tpages>8</tpages></addata></record> |
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| ispartof | Journal of microencapsulation, 1993, Vol.10 (2), p.229-236 |
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| source | MEDLINE; Taylor & Francis:Master (3349 titles); Taylor & Francis Medical Library - CRKN |
| subjects | Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Antifungal Agents - administration & dosage Antifungal Agents - pharmacology Biological and medical sciences Candida - drug effects Candida albicans Candida albicans - drug effects Candida kefyr Candida parapsilosis Candida pseudotropicalis Candida tropicalis Culture Media Drug Carriers Fluconazole - administration & dosage Fluconazole - pharmacology Indicators and Reagents Liposomes Medical sciences Microbial Sensitivity Tests Particle Size Pharmacology. Drug treatments |
| title | Preparations of liposomal fluconazole and their in vitro antifungal activity |
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