In-vivo and in-vitro assessment of curcumin loaded bile salt stabilized nanovesicles for oral delivery
Background Bile salts enriched nanovesicles (bilosomes) have been attention worthy in the past few years due to their distinctive effect on the enhancement of drug delivery through various physiological administration routes. Oral delivery of multifunctioning phytochemical curcumin has faced a lot o...
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| creator | Hashem, Fahima M. Elkhateeb, Dalia Ali, Marwa M. Abdel-Rashid, Rania S. |
| description | Background
Bile salts enriched nanovesicles (bilosomes) have been attention worthy in the past few years due to their distinctive effect on the enhancement of drug delivery through various physiological administration routes. Oral delivery of multifunctioning phytochemical curcumin has faced a lot of difficulties due to its scarce solubility and poor oral bioavailability.
Objective
The current investigation aimed to develop curcumin loaded bilosomes for improvement of oral curcumin bioavailability with maximum efficiency and safety.
Methods
The effect of formulation variables (type of span, SDC % to total lipid content Span/Cholesterol molar ratio) on physicochemical characterization and
in vitro
drug release in simulated intestinal fluid was investigated. Furthermore,
in-vivo
protective effect of bilosomes on hepatic and renal functions was also studied.
Results
and conclusion.
The results revealed that the best curcumin loaded bilosomal formulation showed spherical nanovesicular morphology with particle size 145.1 ± 19.42 nm with highly reasonable %EE (93%), Zeta potential (≥ -30mv), prominent controlled
in-vitro
release reaching 55.18 ± 1.10 after 96 h. The formulation also showed good storage stability with negligible differences in physical features and content. The IC50 values of bilosomal, niosomal, and free curcumin were 216.50, 211.44, and 121.63 mmol/ml, respectively revealing that the unencapsulated curcumin displayed high toxicity on Caco2 cell line (nearly 2 folds). Additionally, the prepared bilosomes showed significant
in-vivo
hepatic and renal protection in liver cirrhosis induced rats with conservation to all liver and renal markers and histopathological morphology. The study assumes the effectiveness and safety of oral delivery of curcumin loaded bile salts stabilized nanovesicles and its powerful commandment for further investigations.
Graphical abstract |
| doi_str_mv | 10.1007/s40199-024-00544-9 |
| format | Article |
| fullrecord | <record><control><sourceid>gale_proqu</sourceid><recordid>TN_cdi_proquest_miscellaneous_3148500828</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><galeid>A821138835</galeid><sourcerecordid>A821138835</sourcerecordid><originalsourceid>FETCH-LOGICAL-g2269-990238f2904ee7bd5b37f76ad5c73a6d7c764c81605e6915578ce0cbe7c00e8f3</originalsourceid><addsrcrecordid>eNptkl1rFTEQhoMo9rT6B7yQgCDebM3nJrksRW2h4I1eh2x29jQlm9Rk90D7683pqdSK5CKZ5HmHmcmL0DtKTikh6nMVhBrTESY6QqQQnXmBNowQ3THG6Uu0obInnaZUHqHjWm8I4Vr07DU64kZR0RQbNF2mbhd2Gbs04rA_L6UFtUKtM6QF5wn7tfh1DgnH7EYY8RAi4OriguviWhDu22VyKe-gBh-h4ikXnIuLeIQYdlDu3qBXk4sV3j7uJ-jn1y8_zi-6q-_fLs_PrrotY73pjCGM64kZIgDUMMqBq0n1bpRecdePyqteeE17IqE3VEqlPRA_gPKEgJ74Cfp0yHtb8q8V6mLnUD3E6BLktVpOhZZtQkw39MM_6E1eS2rVPVANEYY9UVsXwYY05aU4v09qzzSjlGvNZaNO_0O1NcIcfE4wtZE9F3z8S3ANbZjXNcd1CTnV5-D7xyrXYYbR3pYwu3Jn__xgA_gBqO0pbaE8tUGJ3fvEHnxim0_sg0-s4b8BKiirEA</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>3148828492</pqid></control><display><type>article</type><title>In-vivo and in-vitro assessment of curcumin loaded bile salt stabilized nanovesicles for oral delivery</title><source>MEDLINE</source><source>Alma/SFX Local Collection</source><source>Free Full-Text Journals in Chemistry</source><source>SpringerLink Journals - AutoHoldings</source><creator>Hashem, Fahima M. ; Elkhateeb, Dalia ; Ali, Marwa M. ; Abdel-Rashid, Rania S.</creator><creatorcontrib>Hashem, Fahima M. ; Elkhateeb, Dalia ; Ali, Marwa M. ; Abdel-Rashid, Rania S.</creatorcontrib><description>Background
Bile salts enriched nanovesicles (bilosomes) have been attention worthy in the past few years due to their distinctive effect on the enhancement of drug delivery through various physiological administration routes. Oral delivery of multifunctioning phytochemical curcumin has faced a lot of difficulties due to its scarce solubility and poor oral bioavailability.
Objective
The current investigation aimed to develop curcumin loaded bilosomes for improvement of oral curcumin bioavailability with maximum efficiency and safety.
Methods
The effect of formulation variables (type of span, SDC % to total lipid content Span/Cholesterol molar ratio) on physicochemical characterization and
in vitro
drug release in simulated intestinal fluid was investigated. Furthermore,
in-vivo
protective effect of bilosomes on hepatic and renal functions was also studied.
Results
and conclusion.
The results revealed that the best curcumin loaded bilosomal formulation showed spherical nanovesicular morphology with particle size 145.1 ± 19.42 nm with highly reasonable %EE (93%), Zeta potential (≥ -30mv), prominent controlled
in-vitro
release reaching 55.18 ± 1.10 after 96 h. The formulation also showed good storage stability with negligible differences in physical features and content. The IC50 values of bilosomal, niosomal, and free curcumin were 216.50, 211.44, and 121.63 mmol/ml, respectively revealing that the unencapsulated curcumin displayed high toxicity on Caco2 cell line (nearly 2 folds). Additionally, the prepared bilosomes showed significant
in-vivo
hepatic and renal protection in liver cirrhosis induced rats with conservation to all liver and renal markers and histopathological morphology. The study assumes the effectiveness and safety of oral delivery of curcumin loaded bile salts stabilized nanovesicles and its powerful commandment for further investigations.
Graphical abstract</description><identifier>ISSN: 1560-8115</identifier><identifier>ISSN: 2008-2231</identifier><identifier>EISSN: 2008-2231</identifier><identifier>DOI: 10.1007/s40199-024-00544-9</identifier><identifier>PMID: 39714544</identifier><language>eng</language><publisher>Cham: Springer International Publishing</publisher><subject>Administration, Oral ; Animals ; Bile Acids and Salts - chemistry ; Bioavailability ; Biological Availability ; Biomedical and Life Sciences ; Biomedicine ; Caco-2 Cells ; Curcumin - administration & dosage ; Curcumin - chemistry ; Curcumin - pharmacokinetics ; Curcumin - pharmacology ; Drug Carriers - chemistry ; Drug Delivery Systems ; Drug Liberation ; Drug Stability ; Drugs ; Ethylenediaminetetraacetic acid ; Humans ; Liver - drug effects ; Liver - metabolism ; Liver cirrhosis ; Male ; Medicinal Chemistry ; Morphology ; Nanoparticles - chemistry ; Particle Size ; Pharmaceutical Sciences/Technology ; Pharmacology/Toxicology ; Rats ; Rats, Wistar ; Research Article ; Vehicles</subject><ispartof>Daru, 2024-12, Vol.33 (1), p.9</ispartof><rights>The Author(s), under exclusive licence to Tehran University of Medical Sciences 2024 Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.</rights><rights>2024. The Author(s), under exclusive licence to Tehran University of Medical Sciences.</rights><rights>COPYRIGHT 2024 BioMed Central Ltd.</rights><rights>Copyright Springer Nature B.V. 2024</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><orcidid>0000-0002-0170-1656</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s40199-024-00544-9$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://link.springer.com/10.1007/s40199-024-00544-9$$EHTML$$P50$$Gspringer$$H</linktohtml><link.rule.ids>314,780,784,27924,27925,41488,42557,51319</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/39714544$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hashem, Fahima M.</creatorcontrib><creatorcontrib>Elkhateeb, Dalia</creatorcontrib><creatorcontrib>Ali, Marwa M.</creatorcontrib><creatorcontrib>Abdel-Rashid, Rania S.</creatorcontrib><title>In-vivo and in-vitro assessment of curcumin loaded bile salt stabilized nanovesicles for oral delivery</title><title>Daru</title><addtitle>DARU J Pharm Sci</addtitle><addtitle>Daru</addtitle><description>Background
Bile salts enriched nanovesicles (bilosomes) have been attention worthy in the past few years due to their distinctive effect on the enhancement of drug delivery through various physiological administration routes. Oral delivery of multifunctioning phytochemical curcumin has faced a lot of difficulties due to its scarce solubility and poor oral bioavailability.
Objective
The current investigation aimed to develop curcumin loaded bilosomes for improvement of oral curcumin bioavailability with maximum efficiency and safety.
Methods
The effect of formulation variables (type of span, SDC % to total lipid content Span/Cholesterol molar ratio) on physicochemical characterization and
in vitro
drug release in simulated intestinal fluid was investigated. Furthermore,
in-vivo
protective effect of bilosomes on hepatic and renal functions was also studied.
Results
and conclusion.
The results revealed that the best curcumin loaded bilosomal formulation showed spherical nanovesicular morphology with particle size 145.1 ± 19.42 nm with highly reasonable %EE (93%), Zeta potential (≥ -30mv), prominent controlled
in-vitro
release reaching 55.18 ± 1.10 after 96 h. The formulation also showed good storage stability with negligible differences in physical features and content. The IC50 values of bilosomal, niosomal, and free curcumin were 216.50, 211.44, and 121.63 mmol/ml, respectively revealing that the unencapsulated curcumin displayed high toxicity on Caco2 cell line (nearly 2 folds). Additionally, the prepared bilosomes showed significant
in-vivo
hepatic and renal protection in liver cirrhosis induced rats with conservation to all liver and renal markers and histopathological morphology. The study assumes the effectiveness and safety of oral delivery of curcumin loaded bile salts stabilized nanovesicles and its powerful commandment for further investigations.
Graphical abstract</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Bile Acids and Salts - chemistry</subject><subject>Bioavailability</subject><subject>Biological Availability</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Caco-2 Cells</subject><subject>Curcumin - administration & dosage</subject><subject>Curcumin - chemistry</subject><subject>Curcumin - pharmacokinetics</subject><subject>Curcumin - pharmacology</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Delivery Systems</subject><subject>Drug Liberation</subject><subject>Drug Stability</subject><subject>Drugs</subject><subject>Ethylenediaminetetraacetic acid</subject><subject>Humans</subject><subject>Liver - drug effects</subject><subject>Liver - metabolism</subject><subject>Liver cirrhosis</subject><subject>Male</subject><subject>Medicinal Chemistry</subject><subject>Morphology</subject><subject>Nanoparticles - chemistry</subject><subject>Particle Size</subject><subject>Pharmaceutical Sciences/Technology</subject><subject>Pharmacology/Toxicology</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Research Article</subject><subject>Vehicles</subject><issn>1560-8115</issn><issn>2008-2231</issn><issn>2008-2231</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNptkl1rFTEQhoMo9rT6B7yQgCDebM3nJrksRW2h4I1eh2x29jQlm9Rk90D7683pqdSK5CKZ5HmHmcmL0DtKTikh6nMVhBrTESY6QqQQnXmBNowQ3THG6Uu0obInnaZUHqHjWm8I4Vr07DU64kZR0RQbNF2mbhd2Gbs04rA_L6UFtUKtM6QF5wn7tfh1DgnH7EYY8RAi4OriguviWhDu22VyKe-gBh-h4ikXnIuLeIQYdlDu3qBXk4sV3j7uJ-jn1y8_zi-6q-_fLs_PrrotY73pjCGM64kZIgDUMMqBq0n1bpRecdePyqteeE17IqE3VEqlPRA_gPKEgJ74Cfp0yHtb8q8V6mLnUD3E6BLktVpOhZZtQkw39MM_6E1eS2rVPVANEYY9UVsXwYY05aU4v09qzzSjlGvNZaNO_0O1NcIcfE4wtZE9F3z8S3ANbZjXNcd1CTnV5-D7xyrXYYbR3pYwu3Jn__xgA_gBqO0pbaE8tUGJ3fvEHnxim0_sg0-s4b8BKiirEA</recordid><startdate>20241223</startdate><enddate>20241223</enddate><creator>Hashem, Fahima M.</creator><creator>Elkhateeb, Dalia</creator><creator>Ali, Marwa M.</creator><creator>Abdel-Rashid, Rania S.</creator><general>Springer International Publishing</general><general>BioMed Central Ltd</general><general>Springer Nature B.V</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>K9.</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0002-0170-1656</orcidid></search><sort><creationdate>20241223</creationdate><title>In-vivo and in-vitro assessment of curcumin loaded bile salt stabilized nanovesicles for oral delivery</title><author>Hashem, Fahima M. ; Elkhateeb, Dalia ; Ali, Marwa M. ; Abdel-Rashid, Rania S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-g2269-990238f2904ee7bd5b37f76ad5c73a6d7c764c81605e6915578ce0cbe7c00e8f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Bile Acids and Salts - chemistry</topic><topic>Bioavailability</topic><topic>Biological Availability</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Caco-2 Cells</topic><topic>Curcumin - administration & dosage</topic><topic>Curcumin - chemistry</topic><topic>Curcumin - pharmacokinetics</topic><topic>Curcumin - pharmacology</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Delivery Systems</topic><topic>Drug Liberation</topic><topic>Drug Stability</topic><topic>Drugs</topic><topic>Ethylenediaminetetraacetic acid</topic><topic>Humans</topic><topic>Liver - drug effects</topic><topic>Liver - metabolism</topic><topic>Liver cirrhosis</topic><topic>Male</topic><topic>Medicinal Chemistry</topic><topic>Morphology</topic><topic>Nanoparticles - chemistry</topic><topic>Particle Size</topic><topic>Pharmaceutical Sciences/Technology</topic><topic>Pharmacology/Toxicology</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Research Article</topic><topic>Vehicles</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hashem, Fahima M.</creatorcontrib><creatorcontrib>Elkhateeb, Dalia</creatorcontrib><creatorcontrib>Ali, Marwa M.</creatorcontrib><creatorcontrib>Abdel-Rashid, Rania S.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>MEDLINE - Academic</collection><jtitle>Daru</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hashem, Fahima M.</au><au>Elkhateeb, Dalia</au><au>Ali, Marwa M.</au><au>Abdel-Rashid, Rania S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In-vivo and in-vitro assessment of curcumin loaded bile salt stabilized nanovesicles for oral delivery</atitle><jtitle>Daru</jtitle><stitle>DARU J Pharm Sci</stitle><addtitle>Daru</addtitle><date>2024-12-23</date><risdate>2024</risdate><volume>33</volume><issue>1</issue><spage>9</spage><pages>9-</pages><issn>1560-8115</issn><issn>2008-2231</issn><eissn>2008-2231</eissn><abstract>Background
Bile salts enriched nanovesicles (bilosomes) have been attention worthy in the past few years due to their distinctive effect on the enhancement of drug delivery through various physiological administration routes. Oral delivery of multifunctioning phytochemical curcumin has faced a lot of difficulties due to its scarce solubility and poor oral bioavailability.
Objective
The current investigation aimed to develop curcumin loaded bilosomes for improvement of oral curcumin bioavailability with maximum efficiency and safety.
Methods
The effect of formulation variables (type of span, SDC % to total lipid content Span/Cholesterol molar ratio) on physicochemical characterization and
in vitro
drug release in simulated intestinal fluid was investigated. Furthermore,
in-vivo
protective effect of bilosomes on hepatic and renal functions was also studied.
Results
and conclusion.
The results revealed that the best curcumin loaded bilosomal formulation showed spherical nanovesicular morphology with particle size 145.1 ± 19.42 nm with highly reasonable %EE (93%), Zeta potential (≥ -30mv), prominent controlled
in-vitro
release reaching 55.18 ± 1.10 after 96 h. The formulation also showed good storage stability with negligible differences in physical features and content. The IC50 values of bilosomal, niosomal, and free curcumin were 216.50, 211.44, and 121.63 mmol/ml, respectively revealing that the unencapsulated curcumin displayed high toxicity on Caco2 cell line (nearly 2 folds). Additionally, the prepared bilosomes showed significant
in-vivo
hepatic and renal protection in liver cirrhosis induced rats with conservation to all liver and renal markers and histopathological morphology. The study assumes the effectiveness and safety of oral delivery of curcumin loaded bile salts stabilized nanovesicles and its powerful commandment for further investigations.
Graphical abstract</abstract><cop>Cham</cop><pub>Springer International Publishing</pub><pmid>39714544</pmid><doi>10.1007/s40199-024-00544-9</doi><orcidid>https://orcid.org/0000-0002-0170-1656</orcidid></addata></record> |
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| subjects | Administration, Oral Animals Bile Acids and Salts - chemistry Bioavailability Biological Availability Biomedical and Life Sciences Biomedicine Caco-2 Cells Curcumin - administration & dosage Curcumin - chemistry Curcumin - pharmacokinetics Curcumin - pharmacology Drug Carriers - chemistry Drug Delivery Systems Drug Liberation Drug Stability Drugs Ethylenediaminetetraacetic acid Humans Liver - drug effects Liver - metabolism Liver cirrhosis Male Medicinal Chemistry Morphology Nanoparticles - chemistry Particle Size Pharmaceutical Sciences/Technology Pharmacology/Toxicology Rats Rats, Wistar Research Article Vehicles |
| title | In-vivo and in-vitro assessment of curcumin loaded bile salt stabilized nanovesicles for oral delivery |
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