Pulmonary Targeting of Liposomal Triamcinolone Acetonide Phosphate.
| Title: | Pulmonary Targeting of Liposomal Triamcinolone Acetonide Phosphate. |
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| Authors: | Gonzalez-Rothi, Ricardo, Suarez, Sandra, Hochhaus, Guenther, Schreier, Hans, Lukyanov, Anatoly, Derendorf, Hartmut, Dalla Costa, Teresa |
| Source: | Pharmaceutical Research; Nov1996, Vol. 13 Issue 11, p1699-1703, 5p |
| Abstract: | Purpose. To explore the use of triamcinolone acetonide phosphate liposomes as a pulmonary targeted drug delivery system. Methods. Triamcinolone acetonide phosphate liposomes composed of 1,2-distearoyl phosphatidylcholine and 1,2-distearoyl phosphatidyl glycerol and triamcinolone acetonide 21-phosphate dipotassium salt were prepared by dispersion and extruded through polycarbonate membranes. Encapsulation efficiency and in vitro stability at 37°C were assessed after size exclusion chromatography. TAP liposomes (TAP-lip) or TAP in solution (TAP-sol) were delivered to rats either by intratracheal instillation (IT) or intravenous (IV) administration. Pulmonary targeting was assessed by simultaneous monitoring of glucocorticoid receptor occupancy over time in lung (local organ) and liver (systemic organ) using an ex vivo receptor binding assay as a pharmacodynamic measure of glucocorticoid action. Results. In vitro studies in different fluids over 24 hours, showed that more than 75% of the TAP remained encapsulated in liposomes. Cumulative pulmonary effects after IT administration of TAP-lip were 1.6 times higher than liver receptor occupancy. In contrast, there was no difference in the pulmonary and hepatic receptor occupancy time profiles when TAP was administered intratracheally as a solution. No preferential lung targeting was observed when TAP-lip was administered IV. As indicated by the mean effect times, lung receptor occupancy was sustained only when TAP-lip was administered IT. Conclusions. Intratracheal administration of TAP-lip provided sustained receptor occupancy, and increased pulmonary targeting which was superior to IT administration of TAP-sol or IV administration of TAP-lip. The use of liposomes may represent a valuable approach to optimize sustained delivery of glucocorticoids to the lungs via topical administration. [ABSTRACT FROM AUTHOR] |
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| Database: | Complementary Index |
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| Items | – Name: Title Label: Title Group: Ti Data: Pulmonary Targeting of Liposomal Triamcinolone Acetonide Phosphate. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Gonzalez-Rothi%2C+Ricardo%22">Gonzalez-Rothi, Ricardo</searchLink><br /><searchLink fieldCode="AR" term="%22Suarez%2C+Sandra%22">Suarez, Sandra</searchLink><br /><searchLink fieldCode="AR" term="%22Hochhaus%2C+Guenther%22">Hochhaus, Guenther</searchLink><br /><searchLink fieldCode="AR" term="%22Schreier%2C+Hans%22">Schreier, Hans</searchLink><br /><searchLink fieldCode="AR" term="%22Lukyanov%2C+Anatoly%22">Lukyanov, Anatoly</searchLink><br /><searchLink fieldCode="AR" term="%22Derendorf%2C+Hartmut%22">Derendorf, Hartmut</searchLink><br /><searchLink fieldCode="AR" term="%22Dalla+Costa%2C+Teresa%22">Dalla Costa, Teresa</searchLink> – Name: TitleSource Label: Source Group: Src Data: Pharmaceutical Research; Nov1996, Vol. 13 Issue 11, p1699-1703, 5p – Name: Abstract Label: Abstract Group: Ab Data: Purpose. To explore the use of triamcinolone acetonide phosphate liposomes as a pulmonary targeted drug delivery system. Methods. Triamcinolone acetonide phosphate liposomes composed of 1,2-distearoyl phosphatidylcholine and 1,2-distearoyl phosphatidyl glycerol and triamcinolone acetonide 21-phosphate dipotassium salt were prepared by dispersion and extruded through polycarbonate membranes. Encapsulation efficiency and in vitro stability at 37°C were assessed after size exclusion chromatography. TAP liposomes (TAP-lip) or TAP in solution (TAP-sol) were delivered to rats either by intratracheal instillation (IT) or intravenous (IV) administration. Pulmonary targeting was assessed by simultaneous monitoring of glucocorticoid receptor occupancy over time in lung (local organ) and liver (systemic organ) using an ex vivo receptor binding assay as a pharmacodynamic measure of glucocorticoid action. Results. In vitro studies in different fluids over 24 hours, showed that more than 75% of the TAP remained encapsulated in liposomes. Cumulative pulmonary effects after IT administration of TAP-lip were 1.6 times higher than liver receptor occupancy. In contrast, there was no difference in the pulmonary and hepatic receptor occupancy time profiles when TAP was administered intratracheally as a solution. No preferential lung targeting was observed when TAP-lip was administered IV. As indicated by the mean effect times, lung receptor occupancy was sustained only when TAP-lip was administered IT. Conclusions. Intratracheal administration of TAP-lip provided sustained receptor occupancy, and increased pulmonary targeting which was superior to IT administration of TAP-sol or IV administration of TAP-lip. The use of liposomes may represent a valuable approach to optimize sustained delivery of glucocorticoids to the lungs via topical administration. [ABSTRACT FROM AUTHOR] – Name: Abstract Label: Group: Ab Data: <i>Copyright of Pharmaceutical Research is the property of Springer Nature and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
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| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1023/A:1016448908909 Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 5 StartPage: 1699 Titles: – TitleFull: Pulmonary Targeting of Liposomal Triamcinolone Acetonide Phosphate. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Gonzalez-Rothi, Ricardo – PersonEntity: Name: NameFull: Suarez, Sandra – PersonEntity: Name: NameFull: Hochhaus, Guenther – PersonEntity: Name: NameFull: Schreier, Hans – PersonEntity: Name: NameFull: Lukyanov, Anatoly – PersonEntity: Name: NameFull: Derendorf, Hartmut – PersonEntity: Name: NameFull: Dalla Costa, Teresa IsPartOfRelationships: – BibEntity: Dates: – D: 01 M: 11 Text: Nov1996 Type: published Y: 1996 Identifiers: – Type: issn-print Value: 07248741 Numbering: – Type: volume Value: 13 – Type: issue Value: 11 Titles: – TitleFull: Pharmaceutical Research Type: main |
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