Preparation and Characterization of a Submicron Lipid Emulsion of Docetaxel: Submicron Lipid Emulsion of Docetaxel

Gao, Kun; Sun, Jin; Li, Kai; Liu, Xiaohong; Zhang, He

doi:10.1080/03639040802005057

Cited by 84 publications

(40 citation statements)

References 22 publications

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“…Concerning the oil phase, MCT and SO, as the most widely used oils in the commercially available parenteral lipid emulsions [1,14] were selected, whereas lecithin and polysorbate 80 were used as emulsifiers for the nanoemulsion preparation. The oil-emulsifier ratio was kept constant at 5:1 (w/w) in all formulations.…”

Section: Resultsmentioning

confidence: 99%

“…The mean droplet size of commercial parenteral fat emulsions is usually between 100 and 500 nm and it is generally required to be smaller than 1 µm [14], while the PDI, representing the size distribution width lower than 0.25 represents the acceptable value [16]. In the present study, the PCS particle size analysis (Table 3) confirmed that the mean droplet size (Z-Ave) of all prepared nanoemulsions was in nanometer range (172-208 nm), with a relatively narrow particle size distribution (PDI below 0.15), suggesting that developed nanoemulsions were suitable for parenteral use.…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

Cekić¹,

Đorđević²,

Savić³

et al. 2015

Savr tehnol

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Using the experimental design methodology, we have developed and characterized nanoemulsions for a parenteral delivery using diazepam as a model drug. The formulations containing 20 or 30% (w/w) of medium chain triglycerides or the mixture of medium chain triglycerides and soybean oil as the oil phase, soybean lecithin and polysorbate 80 as emulsifiers, and a phosphate buffer solution as the aqueous phase were prepared by cold high pressure homogenization. The obtained nanoemulsions were evaluated in terms of droplet size, size distribution, surface charge, drug-vehicle interactions and physical stability. To evaluate the effects of the oil phase type, oil content and drug presence, as well as their interactions on critical quality attributes of nanoemulsions, a three-factor two-level full factorial design was applied. After the preparation, all nanoemulsions revealed small spherical droplets in the range 170-210 nm, with the narrow droplet size distribution (< 0.15) and the surface charge about -60 mV. The experimental design results indicated that not only factors alone (oil type, oil content, presence of drug), but their interactions also had a significant effect on the nanoemulsion droplet size, polydispersity index, and zeta potential. During two months of storage at 25 °C, all nanoemulsions formulated with the medium chain triglycerides-soybean oil mixture (4:1, w/w) remained physically stable, without considerable changes in monitored parameters. Physicochemical characteristics and stability of these nanoemulsions demonstrated their suitability for parenteral drug delivery.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

Cekić¹,

Đorđević²,

Savić³

et al. 2015

Savr tehnol

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“…PBS with a pH of 5.5 was selected as the dispersion medium for the micellar formulations to increase DTX stability. 27 Using this method, DTX-loaded micelles based on PEG hybrid polypeptides were prepared successfully. Some characteristics of these micelles -namely, the particle size and size distribution determined by DLS, DLC, and DLE measured by HPLC -are summarized in Table 2.…”

Section: Preparation Of Dtx-loaded Micellesmentioning

confidence: 99%

Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers

Gu¹,

Xu²,

Sui³

et al. 2012

IJN

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Abstract:In this work, racemic hybrid polypeptides poly(ethylene glycol) (PEG)-bpoly(racemic-leucine) (PRL) copolymers with different leucine residues have been synthesized and characterized. Using docetaxel as a model molecule, the high drug-loaded spherical micelles based on PEG-PRL were prepared successfully using dialysis, with a tunable particle size from 170 nm to 250 nm obtained by changing the length of the hydrophobic blocks. Facilitated drugloading behavior (higher drug-loading ability and easier drug-loading process) of PEG-PRL compared with their corresponding levo forms (PEG-b-poly[levo leucine]) was observed and clarified for the first time. With this facilitation, the highest drug-loading content and efficiency of PEG-PRL micelles can achieve 11.2% ± 0.4% and 67.2% ± 2.4%, respectively. All drugloaded PEG-PRL micelles exhibit a similar release behavior with a sustained release up to 72 hours. The PEG-PRL was shown to be nontoxic against MCF-7 and human umbilical vein endothelial cells up to a concentration of 100 μg/mL, displaying a good biocompatibility. Also, the docetaxel-loaded PEG-PRL micelles were more toxic than the free drug against MCF-7 human breast cancer cells -both dose and time dependent. Therefore, these high docetaxel-loaded micelles based on racemic hybrid polypeptides appear to be a novel promising nanomedicine for anticancer therapy.

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“…The initial typical formula was selected based on previous literature on parenteral lipid emulsions (Gao et al, 2008;Venkateshwarlu et al, 2010). Control emulsion (docetaxel lipid nanoemulsion (DLNE)) consisted of 10% (w/v) olive oil as the oil core, 1.2% (w/v) EPC-80 as a phospholipid emulsifier, oleic acid (0.3%) as a negative charge inducer, a-tocopherol (0.25%) as antioxidant and glycerol (2.25%) was included to maintain the isotonicity of the formulation for iv administration (Table 1).…”

Section: Resultsmentioning

confidence: 99%

“…The enhanced uptake of albumin-based drug delivery systems in tumors is mediated by hyper vasculature, enhanced permeability of vascular tissue and enhanced retention in tumor tissue, primarily due to lack of or the impaired lymphatic system (Sinha et al, 2006;Kratz, 2008). Nontargeted docetaxel lipid nanoemulsions were reported (Gao et al, 2008;Venkateshwarlu et al, 2010), which were easy to formulate and no albumin ligand attached lipid emulsions were reported. However, folate-decorated docetaxel-loaded human serum albumin nanoparticles were reported (Shougang et al, 2015) for effective targeted activity on human hepatoma cell lines and better in vivo antitumor activity.…”

Section: Introductionmentioning

confidence: 99%

Albumin anchored docetaxel lipid nanoemulsion for improved targeting efficiency – preparation, characterization, cytotoxic, antitumor and in vivo imaging studies

et al. 2015

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The aim was to develop albumin anchored docetaxel lipid nanoemulsion (ALNE) for improving tumor targeted delivery. The O/W lipid nanoemulsion, LNEs were prepared by homogenization and ultrasonication processes. The size of globules and zeta potential were measured by Malvern Zetasizer. Albumin was coupled to stearylamine containing lipid nanoemulsion (SALNE) globules using water soluble EDC reaction. The drug content and entrapment efficiencies for the LNEs were determined by the high-performance liquid chromatography. The in vitro cytotoxic studies of the delivery systems were performed on MCF-7 and Hela cells. The IC 50 values of ALNE on both the cell lines were statistically significant. The in vivo antitumor activity was tested on solid tumors induced in C57BL/6 mice. This study revealed that the percentage tumor inhibition for the groups treated with DLNE, SALNE and ALNE when compared with untreated control was found to be 55.62 ± 5.41%, 54.27 ± 4.85% and 80.01 ± 2.74%, respectively. Furthermore, in vivo distribution studies were carried out in breast cancer MDA-MB231 xenografted Balb/c mice. The LNEs were loaded with fluorescent DiD oil and the distribution in different organs after 6 h was tracked using Caliper life sciences in vivo imaging system. The studies revealed that ALNE was superior in tumor targeting activity when compared with DLNE and SALNE by 3.04 and 2.26 folds, respectively. The average radiance values of ALNE on the tumor tissue were statistically significant when compared with DLNE, SALNE at p50.01. In addition, this strategy can become a platform technology for other lipophilic drugs to target tumors. KeywordsAlbumin tagged docetaxel lipid emulsion, antitumor study, fluorescent imaging study, improved tumor delivery, tumor targeting History

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Preparation and Characterization of a Submicron Lipid Emulsion of Docetaxel: Submicron Lipid Emulsion of Docetaxel

Cited by 84 publications

References 22 publications

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

A full factorial design in the formulation of diazepam parenteral nanoemulsions: Physicochemical characterization and stability evaluation

Polymeric micelles based on poly(ethylene glycol) block poly(racemic amino acids) hybrid polypeptides: conformation-facilitated drug-loading behavior and potential application as effective anticancer drug carriers

Albumin anchored docetaxel lipid nanoemulsion for improved targeting efficiency – preparation, characterization, cytotoxic, antitumor and in vivo imaging studies

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