A lipophilic paclitaxel derivative incorporated in a lipid emulsion for parenteral administration

Lundberg, Bo; Risovic, Verica; Ramaswamy, Manisha; Wasan, Kishor M.

doi:10.1016/s0168-3659(02)00323-1

Cited by 119 publications

(86 citation statements)

References 15 publications

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“…Because of their hydrophobic core, the nLDLs are expected to provide a mechanism for the transport of hydrophobic drugs. In addition, hydrophilic drugs can be converted to hydrophobic pro-drugs by chemical modifications as suggested by several laboratories (Lundberg et al, 2003, Firestone et al, 1984, Dubowchik and Firestone, 1995 thus increasing the arsenal of drugs that can be potentially targeted to GBM via nLDL.…”

Section: Discussionmentioning

confidence: 99%

Synthetic nano-low density lipoprotein as targeted drug delivery vehicle for glioblastoma multiforme

Nikanjam

Blakely

Bjornstad

et al. 2007

International Journal of Pharmaceutics

108

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The low density lipoprotein (LDL) receptor has been shown to be upregulated in GBM tumor cells and is therefore a potential molecular target for the delivery of therapeutic agents. A synthetic nano-LDL (nLDL) particle was developed and tested to determine its utility as a drug Collectively these data strongly suggest that the synthetic nano-LDLs described here are taken up by LDLR and can serve as a drug delivery vehicle for targeting GBM tumors via the LDLR.3

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Section: Discussionmentioning

confidence: 99%

Synthetic nano-low density lipoprotein as targeted drug delivery vehicle for glioblastoma multiforme

Nikanjam

Blakely

Bjornstad

et al. 2007

International Journal of Pharmaceutics

108

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“…Other poorly water-soluble drugs have been formulated in o/w emulsions and are currently being extensively studied, including such drugs as paclitaxel [8][9][10] and cyclosporin A [11]. Emulsions with phosphatidylcholine as the major emulsifier have also been widely used as a source of energy in parenteral nutrition (fat emulsions).…”

Section: Introductionmentioning

confidence: 99%

Emulsions of oil from Adenanthera pavonina L. seeds and their protective effect

Jaromin

Żarnowski

Kozubek

2006

Cellular and Molecular Biology Letters

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Abstract:In our previous study, we developed very stable formulations of submicron oil-in-water emulsions from Adenanthera pavonina L. (family Leguminosae, subfamily Mimosoideae) seed oil, stabilised with soybean lecithin (SPC). Continuing our research, we introduced an additional co-emulsifier, Tween 80, to those formulations in order to decrease the size of the emulsion particles and improve their stability. Formulations with a mean particle size ranging from 43.6 to 306.5 nm and a negative surface charge from -45.3 to -28.5 mV were obtained. Our stability experiments also revealed that most of the tested formulations had a very good degree of stability over a 3-month storage period, both at 4ºC and at room temperature. Since many intravenous injectable drugs exhibit lytic activity against erythrocytes, we examined this activity for the emulsion form of cardol, a natural compound with already proven hemolytic properties. The incorporation of this agent into the emulsion caused an evident decrease in hemolytic activity (97-99%). This highly protective effect, observed against sheep erythrocytes, was independent of both the composition and the particle size of the emulsions used. Our studies suggest that nonionic surfactant/phospholipid-based emulsions containing this edible oil of A. pavonina L. may be useful as an alternative formulation matrix for pharmaceutical, nutritional or cosmetic applications of otherwise membrane-acting components.

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“…42 This attenuated drug release suggests potential applicability of polymeric micelles as a controlled drug delivery system that could result in a more favorable pharmacokinetic profile in vivo and minimize exposure of healthy tissues, while increasing accumulation of drug at the tumor site. [43][44][45] An in vitro cytotoxicity study showed that GA-mPEG 2000 micelles retain the cytotoxicity of gambogic acid to B16-F10, C26, and HUVECs, indicating that polymeric prodrugs do not lose the anticancer and antiangiogenetic activity of gambogic acid. However, compared with free gambogic acid, the IC 50 values for the GA-mPEG 2000 micelles were increased by 2.7-3.0-fold.…”

Section: Discussionmentioning

confidence: 99%

Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles

Cai¹,

Qiu²,

Xiang³

et al. 2013

IJN

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The clinical application of gambogic acid, a natural component with promising antitumor activity, is limited due to its extremely poor aqueous solubility, short half-life in blood, and severe systemic toxicity. To solve these problems, an amphiphilic polymer-drug conjugate was prepared by attachment of low molecular weight (ie, 2 kDa) methoxy poly(ethylene glycol) methyl ether (mPEG) to gambogic acid (GA-mPEG 2000 ) through an ester linkage and characterized by 1 H nuclear magnetic resonance. The GA-mPEG 2000 conjugates self-assembled to form nanosized micelles, with mean diameters of less than 50 nm, and a very narrow particle size distribution. The properties of the GA-mPEG 2000 micelles, including morphology, stability, molecular modeling, and drug release profile, were evaluated. MTT (3-(4,5-dimethylthiazo l-2-yl)-2,5 diphenyl tetrazolium bromide) tests demonstrated that the GA-mPEG 2000 micelle formulation had obvious cytotoxicity to tumor cells and human umbilical vein endothelial cells. Further, GA-mPEG 2000 micelles were effective in inhibiting tumor growth and prolonged survival in subcutaneous B16-F10 and C26 tumor models. Our findings suggest that GA-mPEG 2000 micelles may have promising applications in tumor therapy.

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A lipophilic paclitaxel derivative incorporated in a lipid emulsion for parenteral administration

Cited by 119 publications

References 15 publications

Synthetic nano-low density lipoprotein as targeted drug delivery vehicle for glioblastoma multiforme

Synthetic nano-low density lipoprotein as targeted drug delivery vehicle for glioblastoma multiforme

Emulsions of oil from Adenanthera pavonina L. seeds and their protective effect

Improving aqueous solubility and antitumor effects by nanosized gambogic acid-mPEG2000 micelles

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