Proliposomes for oral delivery of dehydrosilymarin： preparation and evaluation in vitro and in vivo
Aim： To formulate proliposomes with a polyphase dispersed system composed of soybean phospholipids, cholesterol, isopropyl myristate and sodium cholate to improve the oral bioavailability of dehydrosilymarin, an oxidized form of herbal drug silymarin. Methods： Dehydrosilymarin was synthesized from a...
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| Veröffentlicht in: | Acta pharmacologica Sinica 2011-07, Vol.32 (7), p.973-980 |
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| creator | Chu, Chang Tong, Shan-shan Xu, Ying Wang, Li Fu, Min Ge, Yan-ru Yu, Jiang-nan Xu, Xi-ming |
| description | Aim： To formulate proliposomes with a polyphase dispersed system composed of soybean phospholipids, cholesterol, isopropyl myristate and sodium cholate to improve the oral bioavailability of dehydrosilymarin, an oxidized form of herbal drug silymarin. Methods： Dehydrosilymarin was synthesized from air oxidation of silymarin in the presence of pyridine, and proliposomes were prepared by a film dispersion-freeze drying method. Morphological characterization of proliposomes was observed using a transmission electron microscope. Particle size and encapsulation efficiency of proliposomes were measured. The in vitro release of dehydrosilymatin from suspension and proliposomes was evaluated. The oral bioavailability of dehydrosilymarin suspension and proliposomes was investigated in rabbits. Results： The proliposomes prepared under the optimum conditions were spherical and smooth with a mean particle size in the range of 7 to 50 nm. Encapsulation efficiency was 81.59%±0.24%. The in vitro accumulative release percent of dehydrosilymarinloaded proliposomes was stable, which was slow in pH 1.2, and increased continuously in pH 6.8, and finally reached 86.41% at 12 h. After oral administration in rabbits, the relative bioavailability of proliposomes versus suspension in rabbits was 228.85%. Conclusion： Proliposomes may be a useful vehicle for oral delivery of dehydrosilymarin, a drug poorly soluble in water. |
| doi_str_mv | 10.1038/aps.2011.25 |
| format | Article |
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Methods： Dehydrosilymarin was synthesized from air oxidation of silymarin in the presence of pyridine, and proliposomes were prepared by a film dispersion-freeze drying method. Morphological characterization of proliposomes was observed using a transmission electron microscope. Particle size and encapsulation efficiency of proliposomes were measured. The in vitro release of dehydrosilymatin from suspension and proliposomes was evaluated. The oral bioavailability of dehydrosilymarin suspension and proliposomes was investigated in rabbits. Results： The proliposomes prepared under the optimum conditions were spherical and smooth with a mean particle size in the range of 7 to 50 nm. Encapsulation efficiency was 81.59%±0.24%. The in vitro accumulative release percent of dehydrosilymarinloaded proliposomes was stable, which was slow in pH 1.2, and increased continuously in pH 6.8, and finally reached 86.41% at 12 h. After oral administration in rabbits, the relative bioavailability of proliposomes versus suspension in rabbits was 228.85%. Conclusion： Proliposomes may be a useful vehicle for oral delivery of dehydrosilymarin, a drug poorly soluble in water.</description><identifier>ISSN: 1671-4083</identifier><identifier>EISSN: 1745-7254</identifier><identifier>DOI: 10.1038/aps.2011.25</identifier><identifier>PMID: 21666703</identifier><language>eng</language><publisher>London: Nature Publishing Group UK</publisher><subject>Administration, Oral ; Animals ; Biological Availability ; Biomedical and Life Sciences ; Biomedicine ; Immunology ; Internal Medicine ; Liposomes - chemistry ; Liposomes - ultrastructure ; Medical Microbiology ; Original ; original-article ; Pharmacology/Toxicology ; Protective Agents - administration & dosage ; Protective Agents - chemical synthesis ; Protective Agents - pharmacokinetics ; Rabbits ; Silybum marianum - chemistry ; Silymarin - administration & dosage ; Silymarin - analogs & derivatives ; Silymarin - chemical synthesis ; Silymarin - pharmacokinetics ; Vaccine ; 体内 ; 体外释放 ; 口服给药 ; 水飞蓟素 ; 生物利用度 ; 电子显微镜观察 ; 肉豆蔻酸异丙酯 ; 评价</subject><ispartof>Acta pharmacologica Sinica, 2011-07, Vol.32 (7), p.973-980</ispartof><rights>CPS and SIMM 2011</rights><rights>Copyright Nature Publishing Group Jul 2011</rights><rights>Copyright © 2011 CPS and SIMM 2011 CPS and SIMM</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c470t-895bb8d3aa3c1035c1b5cff052e4a2e5af16991b1a55478110d176c4968c53853</citedby><cites>FETCH-LOGICAL-c470t-895bb8d3aa3c1035c1b5cff052e4a2e5af16991b1a55478110d176c4968c53853</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Uhttp://image.cqvip.com/vip1000/qk/95561A/95561A.jpg</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4003120/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4003120/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21666703$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chu, Chang</creatorcontrib><creatorcontrib>Tong, Shan-shan</creatorcontrib><creatorcontrib>Xu, Ying</creatorcontrib><creatorcontrib>Wang, Li</creatorcontrib><creatorcontrib>Fu, Min</creatorcontrib><creatorcontrib>Ge, Yan-ru</creatorcontrib><creatorcontrib>Yu, Jiang-nan</creatorcontrib><creatorcontrib>Xu, Xi-ming</creatorcontrib><title>Proliposomes for oral delivery of dehydrosilymarin： preparation and evaluation in vitro and in vivo</title><title>Acta pharmacologica Sinica</title><addtitle>Acta Pharmacol Sin</addtitle><addtitle>Acta Pharmacologica Sinica</addtitle><description>Aim： To formulate proliposomes with a polyphase dispersed system composed of soybean phospholipids, cholesterol, isopropyl myristate and sodium cholate to improve the oral bioavailability of dehydrosilymarin, an oxidized form of herbal drug silymarin. Methods： Dehydrosilymarin was synthesized from air oxidation of silymarin in the presence of pyridine, and proliposomes were prepared by a film dispersion-freeze drying method. Morphological characterization of proliposomes was observed using a transmission electron microscope. Particle size and encapsulation efficiency of proliposomes were measured. The in vitro release of dehydrosilymatin from suspension and proliposomes was evaluated. The oral bioavailability of dehydrosilymarin suspension and proliposomes was investigated in rabbits. Results： The proliposomes prepared under the optimum conditions were spherical and smooth with a mean particle size in the range of 7 to 50 nm. Encapsulation efficiency was 81.59%±0.24%. The in vitro accumulative release percent of dehydrosilymarinloaded proliposomes was stable, which was slow in pH 1.2, and increased continuously in pH 6.8, and finally reached 86.41% at 12 h. After oral administration in rabbits, the relative bioavailability of proliposomes versus suspension in rabbits was 228.85%. Conclusion： Proliposomes may be a useful vehicle for oral delivery of dehydrosilymarin, a drug poorly soluble in water.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Biological Availability</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Immunology</subject><subject>Internal Medicine</subject><subject>Liposomes - chemistry</subject><subject>Liposomes - ultrastructure</subject><subject>Medical Microbiology</subject><subject>Original</subject><subject>original-article</subject><subject>Pharmacology/Toxicology</subject><subject>Protective Agents - administration & dosage</subject><subject>Protective Agents - chemical synthesis</subject><subject>Protective Agents - pharmacokinetics</subject><subject>Rabbits</subject><subject>Silybum marianum - chemistry</subject><subject>Silymarin - administration & dosage</subject><subject>Silymarin - analogs & derivatives</subject><subject>Silymarin - chemical synthesis</subject><subject>Silymarin - pharmacokinetics</subject><subject>Vaccine</subject><subject>体内</subject><subject>体外释放</subject><subject>口服给药</subject><subject>水飞蓟素</subject><subject>生物利用度</subject><subject>电子显微镜观察</subject><subject>肉豆蔻酸异丙酯</subject><subject>评价</subject><issn>1671-4083</issn><issn>1745-7254</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><recordid>eNptUctO3DAUtRAIKLBij0K3JYOvX3E2SAi1BQmpLGBtOYkzY5Sxg52JNL_Sb-k_9RfqYYYBpK58H8fnnnsPQqeAJ4CpvNR9nBAMMCF8Bx1CwXheEM52UywKyBmW9AB9ifEZY0oolPvogIAQosD0EJmH4Dvb--jnJmatD5kPussa09nRhGXm2xTPlk3w0XbLuQ7W_f3zO-uD6XXQg_Uu067JzKi7xTq1LhvtEPxr_TUZ_THaa3UXzcnmPUJPP74_3tzm979-3t1c3-c1K_CQy5JXlWyo1rROq_EaKl63LebEME0M1y2IsoQKNOeskAC4gULUrBSy5lRyeoSu1rz9opqbpjZuSNuoPtikfKm8tupzx9mZmvpRsXQbIDgRfN0QBP-yMHFQz34RXNKsZCE54QSvQN_WoDpdJQbTbgcAVitLVLJErSxRZKXp7KOmLfbNgwS4WANiarmpCe8z_893vpk-8276kn5sKakUpcCC0X98UqR5</recordid><startdate>20110701</startdate><enddate>20110701</enddate><creator>Chu, 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chemical synthesis</topic><topic>Protective Agents - pharmacokinetics</topic><topic>Rabbits</topic><topic>Silybum marianum - chemistry</topic><topic>Silymarin - administration & dosage</topic><topic>Silymarin - analogs & derivatives</topic><topic>Silymarin - chemical synthesis</topic><topic>Silymarin - pharmacokinetics</topic><topic>Vaccine</topic><topic>体内</topic><topic>体外释放</topic><topic>口服给药</topic><topic>水飞蓟素</topic><topic>生物利用度</topic><topic>电子显微镜观察</topic><topic>肉豆蔻酸异丙酯</topic><topic>评价</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chu, Chang</creatorcontrib><creatorcontrib>Tong, Shan-shan</creatorcontrib><creatorcontrib>Xu, Ying</creatorcontrib><creatorcontrib>Wang, Li</creatorcontrib><creatorcontrib>Fu, Min</creatorcontrib><creatorcontrib>Ge, Yan-ru</creatorcontrib><creatorcontrib>Yu, Jiang-nan</creatorcontrib><creatorcontrib>Xu, 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Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chu, Chang</au><au>Tong, Shan-shan</au><au>Xu, Ying</au><au>Wang, Li</au><au>Fu, Min</au><au>Ge, Yan-ru</au><au>Yu, Jiang-nan</au><au>Xu, Xi-ming</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Proliposomes for oral delivery of dehydrosilymarin： preparation and evaluation in vitro and in vivo</atitle><jtitle>Acta pharmacologica Sinica</jtitle><stitle>Acta Pharmacol Sin</stitle><addtitle>Acta Pharmacologica Sinica</addtitle><date>2011-07-01</date><risdate>2011</risdate><volume>32</volume><issue>7</issue><spage>973</spage><epage>980</epage><pages>973-980</pages><issn>1671-4083</issn><eissn>1745-7254</eissn><abstract>Aim： To formulate proliposomes with a polyphase dispersed system composed of soybean phospholipids, cholesterol, isopropyl myristate and sodium cholate to improve the oral bioavailability of dehydrosilymarin, an oxidized form of herbal drug silymarin. Methods： Dehydrosilymarin was synthesized from air oxidation of silymarin in the presence of pyridine, and proliposomes were prepared by a film dispersion-freeze drying method. Morphological characterization of proliposomes was observed using a transmission electron microscope. Particle size and encapsulation efficiency of proliposomes were measured. The in vitro release of dehydrosilymatin from suspension and proliposomes was evaluated. The oral bioavailability of dehydrosilymarin suspension and proliposomes was investigated in rabbits. Results： The proliposomes prepared under the optimum conditions were spherical and smooth with a mean particle size in the range of 7 to 50 nm. Encapsulation efficiency was 81.59%±0.24%. The in vitro accumulative release percent of dehydrosilymarinloaded proliposomes was stable, which was slow in pH 1.2, and increased continuously in pH 6.8, and finally reached 86.41% at 12 h. After oral administration in rabbits, the relative bioavailability of proliposomes versus suspension in rabbits was 228.85%. Conclusion： Proliposomes may be a useful vehicle for oral delivery of dehydrosilymarin, a drug poorly soluble in water.</abstract><cop>London</cop><pub>Nature Publishing Group UK</pub><pmid>21666703</pmid><doi>10.1038/aps.2011.25</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Administration, Oral Animals Biological Availability Biomedical and Life Sciences Biomedicine Immunology Internal Medicine Liposomes - chemistry Liposomes - ultrastructure Medical Microbiology Original original-article Pharmacology/Toxicology Protective Agents - administration & dosage Protective Agents - chemical synthesis Protective Agents - pharmacokinetics Rabbits Silybum marianum - chemistry Silymarin - administration & dosage Silymarin - analogs & derivatives Silymarin - chemical synthesis Silymarin - pharmacokinetics Vaccine 体内 体外释放 口服给药 水飞蓟素 生物利用度 电子显微镜观察 肉豆蔻酸异丙酯 评价 |
| title | Proliposomes for oral delivery of dehydrosilymarin： preparation and evaluation in vitro and in vivo |
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