Interaction of cremophor el with human plasma

Kongshaug, Magne; Cheng, Long; Moan, Johan Emelian; Rimington, C.

doi:10.1016/0020-711x(91)90176-n

Cited by 66 publications

(21 citation statements)

References 19 publications

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“…The mechanisms underlying this effect are not apparent, although they are probably related to the modality of interaction between the individual 60- lipoprotein classes and the lipophilic vehicle. Thus, Cremophor has been found to alter the density of lipoproteins (Kongshaug et al, 1991), indicating that at least a partial fusion between the oil emulsion and the lipid moiety of the phospholipid bilayer of the lipoproteins must occur. Similarly, the fluidity and composition of the phospholipid bilayer of liposomal vesicles influences both the interlipoprotein distribution of phthalocyanines and the kinetics of photosensitiser release to lipoproteins (L Polo, E Reddi and G Jori, unpublished observations).…”

Section: Discussionmentioning

confidence: 99%

Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines

Soncin

Polo²,

Reddi³

et al. 1995

Br J Cancer

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Summary Four Ge(IV)-octabutoxy-phthalocyanines (GePcs) bearing two alkyl-type axial ligands were assayed for their pharmacokinetic properties and phototherapeutic efficiency in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The GePcs were i.v. injected at a dose of 0.351imolkg-' body weight after incorporation into either Cremophor emulsions or small unilamellar liposomes of dipalmitoyl-phosphatidylcholine (DPPC). Both the nature of the delivery system and the chemical structure of the phthalocyanine were found to affect the behaviour of the GePcs in vivo. Thus, Cremophor-administered GePcs invariably yielded a more prolonged serum retention and a larger association with low-density lipoproteins (LDLs) as compared with the corresponding liposome-delivered phthalocyanines. This led to a greater efficiency and selectivity of tumour targeting. These effects were more pronounced for those GePcs having relatively long alkyl chains (hexyl to decyl) in the axial ligands. Maximal tumour accumulation (0.67 nmol per g of tissue) was found for Ge-Pc(hexyl)2 at 24 h after injection. Consistently, the Ge-Pc(hexyl)2, administered via Cremophor, showed the highest phototherapeutic activity towards the MS-2 fibrosarcoma.

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Section: Discussionmentioning

confidence: 99%

Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines

Soncin

Polo²,

Reddi³

et al. 1995

Br J Cancer

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“…In Taxol®, the first paclitaxel formulation used in clinical practice, paclitaxel, is solubilised by a surfactant in an organic medium, Cremophor®EL (polyethoxylated castor oil), and dehydrated ethanol in a 1:1 (vol/vol) ratio. Cremophor®EL is an excipient with notorious effects on humans, such as life-threatening anaphylaxis (4)(5)(6), hyperlipidaemia (7), abnormal lipoprotein patterns (8,9), the aggregation of erythrocytes (10), and peripheral neuropathy (11)(12)(13). Some studies indicate that Cremophor®EL may trigger complement activation (14)(15)(16).…”

Section: Introductionmentioning

confidence: 98%

Toxicological Study and Efficacy of Blank and Paclitaxel-Loaded Lipid Nanocapsules After i.v. Administration in Mice

et al. 2010

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“…Recently, we have observed that the selectivity and efficiency of phthalocyanine accumulation in the MS-2 fibrosarcoma increases with an increasing degree of hydrophobicity of the dye and the extent of phthalocyanine associated with serum LDL (Soncin et al, 1995a). In particular, Cremophor appears to promote a greater selectivity of tumour targeting by a given phthalocyanine compared with liposomal vesicles (Soncin et al, 1995b), since it determines a larger release of the incorporated photosensitiser to LDL, probably owing to a specific interaction leading to an alteration of this component of the lipoprotein family (Kongshaug et al, 1991;Woodburn et al, 1994). On these bases, the extremely high selectivity of ZnODPc uptake in the tumour can be related to its unusually high affinity for LDL, which is clearly expressed by the data on the distribution of this phthalocyanine among serum proteins (see Table I).…”

Section: Discussionmentioning

confidence: 99%

Tumour-localising and -photosensitising properties of a novel zinc(II) octadecylphthalocyanine

Ometto

Fabris²,

Milanesi³

et al. 1996

Br J Cancer

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Summary 1,4,8,11,15,18,22,, ZnODPc, incorporated into a Cremophor emulsion, was assayed for its pharmacokinetic and phototherapeutic properties in Balb/c mice bearing an intramuscularly transplanted MS-2 fibrosarcoma. The phthalocyanine was injected intravenously (i.v.) in three doses, i.e. 1.46, 0.73 and 0.37 ttmol kg-' body weight. In all cases, the octadecyl-substituted phthalocyanine showed an unusually high affinity for serum low-density lipoproteins (LDLs) and a high efficiency and selectivity of tumour targeting: the maximum accumulation in the tumour occurred at 24 h after injection, whereas no detectable amount of phthalocyanine was recovered from the muscle, i.e. the peritumoral tissue, between I h and 1 week after injection. At the same time, low amounts of phthalocyanine were recovered from skin and then only at short times after injection, with skin photosensitivity rapidly disappearing and the phthalocyanine present in the serum only. Tumour photosensitisation studies were carried out at 24 h after administration of 1.46 ,umol kg-' ZnODPc and showed that this phthalocyanine has a very high phototherapeutic efficiency; this is probably a consequence of the multiple mechanisms by which the phthalocyanine induces tumour damage, involving both direct modification of malignant cells and impairment of blood flow, as well as the alteration of a variety of subcellular components, such as mitochondria, the rough endoplasmic reticulum, the perinuclear membrane and, occasionally, cell nuclei. Tumour necrosis appears to be the consequence of both random cell death and apoptosis.

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Interaction of cremophor el with human plasma

Cited by 66 publications

References 19 publications

Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines

Effect of axial ligation and delivery system on the tumour-localising and -photosensitising properties of Ge(IV)-octabutoxy-phthalocyanines

Toxicological Study and Efficacy of Blank and Paclitaxel-Loaded Lipid Nanocapsules After i.v. Administration in Mice

Tumour-localising and -photosensitising properties of a novel zinc(II) octadecylphthalocyanine

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