Docetaxel-loaded-lipid-based-nanosuspensions (DTX-LNS): Preparation, pharmacokinetics, tissue distribution and antitumor activity

Wang, Lili; Liu, Zhihong; Liu, Donghua; Liu, Chunxi; Zhang, Juan; Zhang, Na

doi:10.1016/j.ijpharm.2011.04.023

Cited by 86 publications

(60 citation statements)

References 36 publications

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“…61 Our group has prepared a DTX-loaded-LNS(DTX-LNS), a poly(ethylene glycol)-modified docetaxel-lipid-based nanosuspension (pLNS), and a folate-targeted docetaxel-lipid-based nanosuspension (tLNS) by high pressure homogenization for DTX delivery. 59,62 The particle sizes of the nanosuspensions were about 200 nm and they are physically stable over 3 months at 4°C ± 2°C and 25°C ± 2°C. The folate-targeted DTX-LNS showed high antitumor efficacy, prolonged blood circulation, and much less toxicity in B16 tumor-bearing mice than Duopafei ® (Qilu Pharmaceutical Co, Ltd , Jinan, People's Republic of China).…”

Section: Lipid-based Nanoformulationsmentioning

confidence: 99%

“…58 LNSs, first developed by our group, are colloidal dispersions with dispersed nanosized drug particles ranging between 100 and 500 nm in an aqueous medium and stabilized against self-aggregation by lipid-derived surfactants. 59 Compared with other lipid-based nanocarriers, LNSs have no drug leakage problems, are easily produced on a large-scale, have a high drug-loading capacity, are physically stable over the long-term, have low toxicity, and are suitable for drugs that are insoluble in both water and oil. As such, LNSs are one of the most potential nanoformulations.…”

Section: Lipid-based Nanoformulationsmentioning

confidence: 99%

“…As such, LNSs are one of the most potential nanoformulations. 59 They can be produced through high pressure homogenization, precipitation, emulsion/microemulsion template, media milling, and dry co-grinding. 60 In nanosuspensions, drugs are in crystalline state and have a nanoscale particle size, thereby increasing the saturation solubility and dissolution rate of poorly soluble drugs, and improving bioavailability.…”

Section: Lipid-based Nanoformulationsmentioning

confidence: 99%

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How nanotechnology can enhance docetaxel therapy

Zhang¹,

Zhang²

2013

IJN

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Docetaxel has been recognized as one of the most efficient anticancer drugs over the past decade; however, its poor water solubility and systemic toxicity have greatly limited its clinical application. In recent decades, the emergence of nanotechnology has provided new drug delivery systems for docetaxel, which can improve its water solubility, minimize the side effects and increase the tumor-targeting distribution by passive or active targeting. This review focuses on the research progress in nanoformulations related to docetaxel delivery -such as polymer-based, lipid-based, and lipid-polymer hybrid nanocarriers, as well as inorganic nanoparticles -addressing their structures, characteristics, preparation, physicochemical properties, methods by which drugs are loaded into them, and their in vitro and in vivo efficacies. Further, the targeted ligands used in the docetaxel nanoformulations, such as monoclonal antibodies, peptides, folic acid, transferrin, aptamers and hyaluronic acid, are described. The issues to overcome before docetaxel nanoformulations can be used in clinical and commercial applications are also discussed.

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Section: Lipid-based Nanoformulationsmentioning

confidence: 99%

Section: Lipid-based Nanoformulationsmentioning

confidence: 99%

Section: Lipid-based Nanoformulationsmentioning

confidence: 99%

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How nanotechnology can enhance docetaxel therapy

Zhang¹,

Zhang²

2013

IJN

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“…4 Samples were chromatographed on a 4.6 × 250 mm reverse phase stainless steel column packed with 5 µm particles (Venusil XBP C18; Bonna-Agela, Tianjin, China) eluted with a mobile phase consisting of acetonitrile/water (55/45 volume/volume) at a flow rate of 1 mL/minute. The column was maintained at room temperature.…”

Section: Preparation Of Plns and Tlnsmentioning

confidence: 99%

“…4 The mice were subcutaneously injected at the right axillary space with 0.1 mL of cell suspension containing 5 × 10 4 B16 cells. 26 Treatments started 8-10 days after implantation in mice with a tumor volume of ∼100 mm 3 .…”

Section: In Vivo Antitumor Efficacymentioning

confidence: 99%

Folate-targeted docetaxel-lipid-based-nanosuspensions for active-targeted cancer therapy

Wang¹,

Li²,

Zhang³

2012

IJN

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Abstract:The purpose of this study was to develop two novel drug delivery systems based on biodegradable docetaxel-lipid-based-nanosuspensions. The first one was poly(ethylene glycol)-modified docetaxel-lipid-based-nanosuspensions (pLNS). It was developed to increase the cycle time of the drug within the body and enhance the accumulation of the drug at the tumor site. The second one was targeted docetaxel-lipid-based-nanosuspensions (tLNS) using folate as the target ligand. The tLNS could target the tumor cells that overexpressed folate receptor (FR). The morphology, particle size, and zeta potential of pLNS and tLNS were characterized, respectively. The in vitro cytotoxicity evaluation of Duopafei ® , pLNS, and tLNS were performed in human hepatocellular liver carcinoma HepG2 (FR-) and B16 (FR+) cells, respectively. The in vivo antitumor efficacy and pharmacokinetics, as well as the drug tissue distribution, were evaluated in Kunming mice bearing B16 cells. The particle size of pLNS was 204.2 ± 6.18 nm and tLNS had a mean particle size of 220.6 ± 9.54 nm. Cytotoxicity of tLNS against B16 (FR+) cell lines was superior to pLNS (P , 0.05), while there was no significant difference in the half maximum inhibitory concentration values for HepG2 (FR-) cells between pLNS and tLNS. The results of the in vivo antitumor efficacy evaluation showed that tLNS exhibited higher antitumor efficacy by reducing tumor volume (P , 0.01) compared with Duopafei and pLNS, respectively. The results of the in vivo biodistribution study indicate that the better antitumor efficacy of tLNS was attributed to the increased accumulation of the drug in the tumor.

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