Effect of cholesterol and ethanol on dermal delivery from DPPC liposomes
The main objective of the present work was to compare the dermal delivery of minoxidil (Mx), a lipophilic drug from ethosomes versus classic liposomes, containing different cholesterol (CHOL) concentrations. All the systems were characterized for shape, lamellarity, particle size and entrapment effi...
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| Veröffentlicht in: | International journal of pharmaceutics 2005-07, Vol.298 (1), p.1-12 |
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| creator | López-Pinto, J.M. González-Rodríguez, M.L. Rabasco, A.M. |
| description | The main objective of the present work was to compare the dermal delivery of minoxidil (Mx), a lipophilic drug from ethosomes versus classic liposomes, containing different cholesterol (CHOL) concentrations. All the systems were characterized for shape, lamellarity, particle size and entrapment efficiency percentage (EE), by transmission electron microscopy (TEM), confocal laser scanning microscopy (CLSM), laser diffraction and ultracentrifugation or dialysis methods, respectively. Multilamellar vesicles (MLVs) were obtained and one to six lamellae were visualized by CLSM. The presence of ethanol in the formulations affects the particle size in terms of reducing this parameter. In addition, it was possible to appreciate the influence of CHOL on the vesicle size, because it was increased, as CHOL concentration was higher. When the EE was determined by two different methods (ultracentrifugation and dialysis methods), a clear losing of entrapped drug by the ultracentrifugation method was observed, because the strong energy transmitted to the samples disrupted vesicles.
Vesicles were non-occlusively applied on rat skin and the permeation pattern of the different systems, depth into the skin and the main permeation pathway were studied by using β-carotene as a fluorescent probe. CLSM studies showed that ethosomal systems were much more efficient at delivering the fluorescent substance into the skin in terms of quantity and depth, than either liposomes or hydroalcoholic solutions. |
| doi_str_mv | 10.1016/j.ijpharm.2005.02.021 |
| format | Article |
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Vesicles were non-occlusively applied on rat skin and the permeation pattern of the different systems, depth into the skin and the main permeation pathway were studied by using β-carotene as a fluorescent probe. CLSM studies showed that ethosomal systems were much more efficient at delivering the fluorescent substance into the skin in terms of quantity and depth, than either liposomes or hydroalcoholic solutions.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2005.02.021</identifier><identifier>PMID: 15896932</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Androstanes - administration & dosage ; Animals ; Biological and medical sciences ; Chemistry, Pharmaceutical ; Cholesterol - administration & dosage ; Confocal laser scanning microscopy ; Drug Stability ; Ethanol - administration & dosage ; Ethosome ; Franz cell ; General pharmacology ; Lamellarity ; Liposome ; Liposomes ; Medical sciences ; Minoxidil ; Minoxidil - administration & dosage ; Minoxidil - pharmacokinetics ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Rats ; Rats, Wistar ; Skin Absorption</subject><ispartof>International journal of pharmaceutics, 2005-07, Vol.298 (1), p.1-12</ispartof><rights>2005 Elsevier B.V.</rights><rights>2005 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c490t-605eff639cab66e8916517197179346a1278d0a49f1a8ae8716468f95bb5ebc73</citedby><cites>FETCH-LOGICAL-c490t-605eff639cab66e8916517197179346a1278d0a49f1a8ae8716468f95bb5ebc73</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517305001389$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=16926898$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15896932$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>López-Pinto, J.M.</creatorcontrib><creatorcontrib>González-Rodríguez, M.L.</creatorcontrib><creatorcontrib>Rabasco, A.M.</creatorcontrib><title>Effect of cholesterol and ethanol on dermal delivery from DPPC liposomes</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The main objective of the present work was to compare the dermal delivery of minoxidil (Mx), a lipophilic drug from ethosomes versus classic liposomes, containing different cholesterol (CHOL) concentrations. All the systems were characterized for shape, lamellarity, particle size and entrapment efficiency percentage (EE), by transmission electron microscopy (TEM), confocal laser scanning microscopy (CLSM), laser diffraction and ultracentrifugation or dialysis methods, respectively. Multilamellar vesicles (MLVs) were obtained and one to six lamellae were visualized by CLSM. The presence of ethanol in the formulations affects the particle size in terms of reducing this parameter. In addition, it was possible to appreciate the influence of CHOL on the vesicle size, because it was increased, as CHOL concentration was higher. When the EE was determined by two different methods (ultracentrifugation and dialysis methods), a clear losing of entrapped drug by the ultracentrifugation method was observed, because the strong energy transmitted to the samples disrupted vesicles.
Vesicles were non-occlusively applied on rat skin and the permeation pattern of the different systems, depth into the skin and the main permeation pathway were studied by using β-carotene as a fluorescent probe. CLSM studies showed that ethosomal systems were much more efficient at delivering the fluorescent substance into the skin in terms of quantity and depth, than either liposomes or hydroalcoholic solutions.</description><subject>Androstanes - administration & dosage</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Chemistry, Pharmaceutical</subject><subject>Cholesterol - administration & dosage</subject><subject>Confocal laser scanning microscopy</subject><subject>Drug Stability</subject><subject>Ethanol - administration & dosage</subject><subject>Ethosome</subject><subject>Franz cell</subject><subject>General pharmacology</subject><subject>Lamellarity</subject><subject>Liposome</subject><subject>Liposomes</subject><subject>Medical sciences</subject><subject>Minoxidil</subject><subject>Minoxidil - administration & dosage</subject><subject>Minoxidil - pharmacokinetics</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Skin Absorption</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1LJDEQhsOi6Oj6E1b64t56THW683FaltFVQdCDew7pdIXJkO6MyYzgvzcyDR6FgsrhqcrLU4T8AroECvx6s_Sb7dqkcdlQ2i1pUwp-kAVIwWrWCn5EFpQJWXcg2Ck5y3lDKeUNsBNyCp1UXLFmQe5vnUO7q6Kr7DoGzDtMMVRmGircrc1U3nGqBkyjCaUF_4bpvXIpjtXN8_OqCn4bcxwx_yTHzoSMF3M_J___3b6s7uvHp7uH1d_H2raK7mpOO3SOM2VNzzlKBbwEBCVAKNZyA42QAzWtcmCkQSmAt1w61fV9h70V7Jz8Puzdpvi6L3n16LPFEMyEcZ81F6qTvKHfgkWLaAWwAnYH0KaYc0Knt8mPJr1roPrTtd7o2bX-dK1pUwrK3OX8wb4fcfiamuUW4GoGTLYmuGQm6_MXx1XDpZKF-3PgsHh785h0th4ni4NP5TZ6iP6bKB84iZ4j</recordid><startdate>20050714</startdate><enddate>20050714</enddate><creator>López-Pinto, J.M.</creator><creator>González-Rodríguez, M.L.</creator><creator>Rabasco, A.M.</creator><general>Elsevier B.V</general><general>Elsevier</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>P64</scope><scope>7X8</scope></search><sort><creationdate>20050714</creationdate><title>Effect of cholesterol and ethanol on dermal delivery from DPPC liposomes</title><author>López-Pinto, J.M. ; González-Rodríguez, M.L. ; Rabasco, A.M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c490t-605eff639cab66e8916517197179346a1278d0a49f1a8ae8716468f95bb5ebc73</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Androstanes - administration & dosage</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Chemistry, Pharmaceutical</topic><topic>Cholesterol - administration & dosage</topic><topic>Confocal laser scanning microscopy</topic><topic>Drug Stability</topic><topic>Ethanol - administration & dosage</topic><topic>Ethosome</topic><topic>Franz cell</topic><topic>General pharmacology</topic><topic>Lamellarity</topic><topic>Liposome</topic><topic>Liposomes</topic><topic>Medical sciences</topic><topic>Minoxidil</topic><topic>Minoxidil - administration & dosage</topic><topic>Minoxidil - pharmacokinetics</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Skin Absorption</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>López-Pinto, J.M.</creatorcontrib><creatorcontrib>González-Rodríguez, M.L.</creatorcontrib><creatorcontrib>Rabasco, A.M.</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>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>López-Pinto, J.M.</au><au>González-Rodríguez, M.L.</au><au>Rabasco, A.M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of cholesterol and ethanol on dermal delivery from DPPC liposomes</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2005-07-14</date><risdate>2005</risdate><volume>298</volume><issue>1</issue><spage>1</spage><epage>12</epage><pages>1-12</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The main objective of the present work was to compare the dermal delivery of minoxidil (Mx), a lipophilic drug from ethosomes versus classic liposomes, containing different cholesterol (CHOL) concentrations. All the systems were characterized for shape, lamellarity, particle size and entrapment efficiency percentage (EE), by transmission electron microscopy (TEM), confocal laser scanning microscopy (CLSM), laser diffraction and ultracentrifugation or dialysis methods, respectively. Multilamellar vesicles (MLVs) were obtained and one to six lamellae were visualized by CLSM. The presence of ethanol in the formulations affects the particle size in terms of reducing this parameter. In addition, it was possible to appreciate the influence of CHOL on the vesicle size, because it was increased, as CHOL concentration was higher. When the EE was determined by two different methods (ultracentrifugation and dialysis methods), a clear losing of entrapped drug by the ultracentrifugation method was observed, because the strong energy transmitted to the samples disrupted vesicles.
Vesicles were non-occlusively applied on rat skin and the permeation pattern of the different systems, depth into the skin and the main permeation pathway were studied by using β-carotene as a fluorescent probe. CLSM studies showed that ethosomal systems were much more efficient at delivering the fluorescent substance into the skin in terms of quantity and depth, than either liposomes or hydroalcoholic solutions.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>15896932</pmid><doi>10.1016/j.ijpharm.2005.02.021</doi><tpages>12</tpages></addata></record> |
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| subjects | Androstanes - administration & dosage Animals Biological and medical sciences Chemistry, Pharmaceutical Cholesterol - administration & dosage Confocal laser scanning microscopy Drug Stability Ethanol - administration & dosage Ethosome Franz cell General pharmacology Lamellarity Liposome Liposomes Medical sciences Minoxidil Minoxidil - administration & dosage Minoxidil - pharmacokinetics Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Rats Rats, Wistar Skin Absorption |
| title | Effect of cholesterol and ethanol on dermal delivery from DPPC liposomes |
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