In vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate
Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy o...
Ausführliche Beschreibung
Autor*in: |
Evenbratt, Hanne [verfasserIn] |
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E-Artikel |
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Sprache: |
Englisch |
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2013transfer abstract |
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Umfang: |
6 |
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Übergeordnetes Werk: |
Enthalten in: Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides - Nigolian, H. ELSEVIER, 2022, New York, NY [u.a.] |
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Übergeordnetes Werk: |
volume:452 ; year:2013 ; number:1 ; day:16 ; month:08 ; pages:270-275 ; extent:6 |
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DOI / URN: |
10.1016/j.ijpharm.2013.05.047 |
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ELV021959927 |
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245 | 1 | 0 | |a In vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate |
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520 | |a Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. | ||
520 | |a Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. | ||
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700 | 1 | |a Engström, Sven |4 oth | |
700 | 1 | |a Ericson, Marica B. |4 oth | |
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10.1016/j.ijpharm.2013.05.047 doi GBVA2013012000020.pica (DE-627)ELV021959927 (ELSEVIER)S0378-5173(13)00464-X DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Evenbratt, Hanne verfasserin aut In vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate 2013transfer abstract 6 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. PDT Elsevier ALA Elsevier PG Elsevier GMO Elsevier MAL Elsevier PpIX Elsevier API Elsevier POL Elsevier SAXD Elsevier GME Elsevier Jonsson, Charlotte oth Faergemann, Jan oth Engström, Sven oth Ericson, Marica B. oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:452 year:2013 number:1 day:16 month:08 pages:270-275 extent:6 https://doi.org/10.1016/j.ijpharm.2013.05.047 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 452 2013 1 16 0816 270-275 6 045F 610 |
spelling |
10.1016/j.ijpharm.2013.05.047 doi GBVA2013012000020.pica (DE-627)ELV021959927 (ELSEVIER)S0378-5173(13)00464-X DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Evenbratt, Hanne verfasserin aut In vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate 2013transfer abstract 6 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. PDT Elsevier ALA Elsevier PG Elsevier GMO Elsevier MAL Elsevier PpIX Elsevier API Elsevier POL Elsevier SAXD Elsevier GME Elsevier Jonsson, Charlotte oth Faergemann, Jan oth Engström, Sven oth Ericson, Marica B. oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:452 year:2013 number:1 day:16 month:08 pages:270-275 extent:6 https://doi.org/10.1016/j.ijpharm.2013.05.047 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 452 2013 1 16 0816 270-275 6 045F 610 |
allfields_unstemmed |
10.1016/j.ijpharm.2013.05.047 doi GBVA2013012000020.pica (DE-627)ELV021959927 (ELSEVIER)S0378-5173(13)00464-X DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Evenbratt, Hanne verfasserin aut In vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate 2013transfer abstract 6 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. PDT Elsevier ALA Elsevier PG Elsevier GMO Elsevier MAL Elsevier PpIX Elsevier API Elsevier POL Elsevier SAXD Elsevier GME Elsevier Jonsson, Charlotte oth Faergemann, Jan oth Engström, Sven oth Ericson, Marica B. oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:452 year:2013 number:1 day:16 month:08 pages:270-275 extent:6 https://doi.org/10.1016/j.ijpharm.2013.05.047 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 452 2013 1 16 0816 270-275 6 045F 610 |
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10.1016/j.ijpharm.2013.05.047 doi GBVA2013012000020.pica (DE-627)ELV021959927 (ELSEVIER)S0378-5173(13)00464-X DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Evenbratt, Hanne verfasserin aut In vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate 2013transfer abstract 6 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. PDT Elsevier ALA Elsevier PG Elsevier GMO Elsevier MAL Elsevier PpIX Elsevier API Elsevier POL Elsevier SAXD Elsevier GME Elsevier Jonsson, Charlotte oth Faergemann, Jan oth Engström, Sven oth Ericson, Marica B. oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:452 year:2013 number:1 day:16 month:08 pages:270-275 extent:6 https://doi.org/10.1016/j.ijpharm.2013.05.047 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 452 2013 1 16 0816 270-275 6 045F 610 |
allfieldsSound |
10.1016/j.ijpharm.2013.05.047 doi GBVA2013012000020.pica (DE-627)ELV021959927 (ELSEVIER)S0378-5173(13)00464-X DE-627 ger DE-627 rakwb eng 610 610 DE-600 610 VZ 44.61 bkl Evenbratt, Hanne verfasserin aut In vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate 2013transfer abstract 6 nicht spezifiziert zzz rdacontent nicht spezifiziert z rdamedia nicht spezifiziert zu rdacarrier Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. PDT Elsevier ALA Elsevier PG Elsevier GMO Elsevier MAL Elsevier PpIX Elsevier API Elsevier POL Elsevier SAXD Elsevier GME Elsevier Jonsson, Charlotte oth Faergemann, Jan oth Engström, Sven oth Ericson, Marica B. oth Enthalten in Elsevier Nigolian, H. ELSEVIER Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides 2022 New York, NY [u.a.] (DE-627)ELV008932840 volume:452 year:2013 number:1 day:16 month:08 pages:270-275 extent:6 https://doi.org/10.1016/j.ijpharm.2013.05.047 Volltext GBV_USEFLAG_U GBV_ELV SYSFLAG_U 44.61 Innere Medizin VZ AR 452 2013 1 16 0816 270-275 6 045F 610 |
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Enthalten in Description d’une cohorte française multicentrique de porteurs asymptomatiques d’anticorps anti-phospholipides New York, NY [u.a.] volume:452 year:2013 number:1 day:16 month:08 pages:270-275 extent:6 |
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in vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate |
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In vivo study of an instantly formed lipid–water cubic phase formulation for efficient topical delivery of aminolevulinic acid and methyl-aminolevulinate |
abstract |
Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. |
abstractGer |
Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. |
abstract_unstemmed |
Abstract We demonstrate a rapidly formed cubic liquid crystalline phase, i.e. typically 1g cubic phase in less than 1min confirmed by X-ray diffraction, consisting of an ether lipid, 1-glyceryl monooleyl ether (GME), an aprotic solvent (propylene glycol or pentane-1,5-diol) and water. The efficacy of the cubic formulation was tested in vivo by administrating formulations containing 3% (w/w) of the HCl salts of δ-aminolevulinic acid (ALA) or methylaminolevulinate (MAL) to hairless mice. The endogenous formation of protoporphyrin IX (PpIX) was monitored spectrophotometrically as a marker for cellular uptake of active compound. As reference, a commercial product containing 16% (w/w) MAL in an oil-in-water emulsion (Metvix®), and a cubic phase based on an ester lipid (glyceryl monooleate, GMO), previously shown to facilitate topical delivery of both ALA and MAL, were applied. It was found that in general the cubic phases gave rise to higher fluorescence levels than the mice exposed to the commercial product. The instantly formed cubic formulations based on GME demonstrated the same efficiency as the GMO based formulations. The results imply that instantly formed cubic formulations opens up new opportunities, particularly for transdermal drug delivery of substances subject to stability problems in, e.g. aqueous environments. |
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