A Novel Paclitaxel Microemulsion Containing a Reduced Amount of Cremophor EL: Pharmacokinetics, Biodistribution, and <i>In Vivo</i>  Antitumor Efficacy and Safety

Wang, Ying; Wu, Ke-Chun; Zhao, Bing-Xiang; Zhao, Xin; Wang, Xin; Su, Chen; Nie, Song; Pan, Weisan; Zhang, Xuan; Qiang, Zhang

doi:10.1155/2011/854872

Cited by 24 publications

(21 citation statements)

References 27 publications

(23 reference statements)

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“…According to the study, the author concludes that there was no significant difference in the tissue distribution of paclitaxel between the paclitaxel microemulsion group and the paclitaxel injection group (Ying et al, 2011).…”

Section: Discussionmentioning

confidence: 94%

Effect of microemulsion formulation on biodistribution of ^99mTc-Aprotinin in acute pancreatitis models induced rats

et al. 2016

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Background: Aprotinin is a monomeric globular polypeptide, which derived from bovine lung tissue and theoretically attractive molecule in ameliorating the effects of acute pancreatitis. Acute pancreatitis is an inflammatory condition of the pancreas that is painful and at times deadly. Over the following two decades Aprotinin therapeutic potential on pancreatitis is proven experimentally, its clinical therapeutic success is limited due to low targeting to pancreas. Objective: The aim of this study was to evaluate the biodistribution of Technetium-99m ( 99m Tc)-Aprotinin solution ( 99m Tc-Aprotinin-S) and 99m Tc-Aprotinin loaded microemulsion, which was prepared for the aim of treatment for acute pancreatitis. Method: Aprotinin was radiolabeled with 99m Tc. Radiochemical purity was determined with radioactive thin layer chromatography studies.99m Tc-Aprotinin-S and

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Section: Discussionmentioning

confidence: 94%

Effect of microemulsion formulation on biodistribution of ^99mTc-Aprotinin in acute pancreatitis models induced rats

et al. 2016

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“…Weight loss in these animals can largely be associated with the probable process of chemotherapy, in which malnutrition, weight loss, nausea, vomiting, and alopecia are common clinical side effects of PTX. [24][25][26] Nutritional therapy is of the utmost importance to keep the patient prepared for the aggressive nature of treatment and for his or her bodily restructuring after chemotherapy, because by reducing gastrointestinal side effects and changes in weight, it can contribute satisfactorily to the progress of these patients. 27 Signs of cutaneous toxicity such as flaky, inflammatory lesions were observed in the groups treated with commercial PTX from the second cycle of chemotherapy onward.…”

Section: Discussionmentioning

confidence: 99%

Organic effects of associating paclitaxel with a lipid-based nanoparticle system on a nonhuman primate, <em>Cebus apella</em>

Feio¹,

Oliveira²,

Pereira³

et al. 2017

IJN

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Lipid-based nanoparticle systems have been used as vehicles for chemotherapeutic agents in experimental cancer treatments. Those systems have generally been credited with attenuating the severe toxicity of chemotherapeutic agents. This study aimed to investigate the effects of associating paclitaxel (PTX) with a lipid-based nanoparticle system on a nonhuman primate, Cebus apella , documenting the toxicity as measured by serum biochemistry, which is a detailed analysis of blood and tissue. Eighteen C. apella were studied: three animals were treated with cholesterol-rich nanoemulsion (LDE) only, without PTX, administered intravenously every 3 weeks, during six treatment cycles; six animals were treated with PTX associated with LDE at the same administration scheme, three with lower (175 mg/m 2 ) and three with higher (250 mg/m 2 ) PTX doses; and six animals were treated with commercial PTX, three with the lower and three with the higher doses. In the LDE-PTX group, no clinical toxicity appeared, and the weight–food consumption curve was similar to that of the controls. Two animals treated with commercial PTX presented weight loss, nausea and vomiting, diarrhea, skin flaking, 70% loss of body hair, and decreased physical activity. The use of LDE as a carrier at both lower and higher doses reduced the toxicity of the drug in this species, which is closely related to human subjects. This was observed not only by clinical, biochemical, and hematological profiles but also by the histopathological analysis. The results of this study support the assumption that lipid-based nanoparticle systems used as drug carriers can serve as valuable tools to decrease the toxicity and increase the safety of chemotherapeutic agents.

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“…18 In brief, to prepare a concentrated CLA-PTX microemulsion, CLA-PTX was dissolved in dehydrated alcohol and then mixed with Lipoid E 80, CrEL, and soybean oil. The concentration of CLA-PTX in the microemulsion was 80 mg/mL.…”

Section: Preparation Of Cla-ptx Microemulsionmentioning

confidence: 99%

“…Recently, a novel paclitaxel microemulsion was developed for intravenous administration in our laboratory. 18 In addition, considering that conjugated linoleic acid is a mixture of positional and geometric isomers of octadecadienoic acid, which is a component of some conjugated linoleic acid-rich soy oils, we hypothesized that the solubility of conjugated linoleic acid in oil would be high. We believed that the compatibility of CLA-PTX in oil, like conjugated linoleic acid, would be acceptable, and that development of a CLA-PTX microemulsion would be very feasible.…”

Section: Introductionmentioning

confidence: 99%

Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings

Li¹,

Yang²,

Li³

et al. 2012

IJN

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Background: Considering the observations that linoleic acid conjugated with paclitaxel (CLA-PTX) possesses antitumor activity against brain tumors, is able to cross the blood-brain barrier, but has poor water solubility, the purpose of this study was to prepare a novel CLA-PTX microemulsion and evaluate its activity against brain tumors in vitro and in vivo. Methods: The in vitro cytotoxicity of a CLA-PTX microemulsion was investigated in C6 glioma cells. The in vivo antitumor activity of the CLA-PTX microemulsion was evaluated in tumorbearing nude mice and rats. The pharmacokinetics of the CLA-PTX microemulsion were investigated in rats, and its safety was also evaluated in mice. Results: The average droplet size of the CLA-PTX microemulsion was approximately 176.3 ± 0.8 nm and the polydispersity index was 0.294 ± 0.024. In vitro cytotoxicity results showed that the IC 50 of the CLA-PTX microemulsion was 1.61 ± 0.83 µM for a C6 glioma cell line, which was similar to that of free paclitaxel and CLA-PTX solution (P . 0.05). The antitumor activity of the CLA-PTX microemulsion against brain tumors was confirmed in our in vivo C6 glioma tumor-bearing nude mice as well as in a rat model. In contrast, Taxol ® had almost no significant antitumor effect in C6 glioma tumor-bearing rats, but could markedly inhibit growth of C6 tumors in C6 glioma tumor-bearing nude mice. The pharmacokinetic results indicated that CLA-PTX in solution has a much longer circulation time and produces higher drug plasma concentrations compared with the CLA-PTX microemulsion. The results of the acute toxicity study showed that the LD 50 of CLA-PTX solution was 103.9 mg/kg. In contrast, the CLA-PTX microemulsion was well tolerated in mice when administered at doses up to 200 mg/kg. Conclusion: CLA-PTX microemulsion is a novel formulation with significant antitumor efficacy in the treatment of brain tumors, and is safer than CLA-PTX solution.

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A Novel Paclitaxel Microemulsion Containing a Reduced Amount of Cremophor EL: Pharmacokinetics, Biodistribution, and In Vivo Antitumor Efficacy and Safety

Cited by 24 publications

References 27 publications

Effect of microemulsion formulation on biodistribution of ^99mTc-Aprotinin in acute pancreatitis models induced rats

Effect of microemulsion formulation on biodistribution of ^99mTc-Aprotinin in acute pancreatitis models induced rats

Organic effects of associating paclitaxel with a lipid-based nanoparticle system on a nonhuman primate, <em>Cebus apella</em>

Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings

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A Novel Paclitaxel Microemulsion Containing a Reduced Amount of Cremophor EL: Pharmacokinetics, Biodistribution, and In Vivo Antitumor Efficacy and Safety

Cited by 24 publications

References 27 publications

Effect of microemulsion formulation on biodistribution of 99mTc-Aprotinin in acute pancreatitis models induced rats

Effect of microemulsion formulation on biodistribution of 99mTc-Aprotinin in acute pancreatitis models induced rats

Organic effects of associating paclitaxel with a lipid-based nanoparticle system on a nonhuman primate, <em>Cebus apella</em>

Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings

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Effect of microemulsion formulation on biodistribution of ^99mTc-Aprotinin in acute pancreatitis models induced rats

Effect of microemulsion formulation on biodistribution of ^99mTc-Aprotinin in acute pancreatitis models induced rats