In vivo evaluation of lipid nanocapsules as a promising colloidal carrier for paclitaxel

Lacoeuille, Franck; Hindré, François; Moal, F.; Roux, J.; Passirani, Catherine; Couturier, O.; Calès, Paul; Jeune, J. J. Le; Lamprecht, Alf; Benoit, Jean‐Pierre

doi:10.1016/j.ijpharm.2007.06.014

Cited by 71 publications

(44 citation statements)

References 22 publications

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“…Similar results were observed after SC administration in the left flank and behind the neck of the animal (data not shown). The high LNC accumulation in the liver and spleen after IV administration were consistent with the numerous published data using LNC (17,18). In addition, the differences in the LNC biodistribution profiles after IV and SC administration were correlated to the pharmacokinetic profiles, since a very low fraction of LNCs reached systemic circulation after SC administration whereas the total injected dose was in the blood after IV administration (Figure 1).…”

Section: Lnc Biodistribution Vs Injection Sites and Administration Rsupporting

confidence: 88%

Passive and specific targeting of lymph nodes: the influence of the administration route

Pitorre¹,

Bastiat²,

Chatel³

et al. 2015

European Journal of Nanomedicine

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Abstract:Patients diagnosed with an advanced-stage cancer present a dismal prognosis due to the presence of metastases. From the primary tumor, the cancer cells are disseminated via lymphatic circulation; metastases develop initially in lymph nodes. Therefore, the targeting of lymph nodes needs to be improved in the design of future chemotherapy, and one way to ensure this targeting is by using the subcutaneous (SC) route. Using lipid nanocapsules (LNCs) (40 nm and fluorescently-labeled with DiD) as nanocarriers, a correlation between the SC injection site (behind the neck, the right and left flanks, and above the tail) for LNC administration and specific lymph node accumulation (left and right cervical, axillary and inguinal lymph nodes) was achieved for SpragueDawley rats. The pharmacokinetic and biodistribution profiles confirmed the absence of LNCs in systemic circulation after SC administration due to the optimal size of the LNCs. With appropriate SC administration, LNCs can accumulate in specific lymph nodes, whereas IV administration led to a weak accumulation of LNCs in all lymph nodes. Specific accumulation followed the lymph flow: bottom-up from the lower to upper limbs and top down from the head, with two lymph circulation partitions: right upper limb and the rest. Administration above the tail presented high inguinal and axillary lymph node accumulation whereas weak accumulation was observed after administration behind the neck. LNCs administered in the left flank only accumulated in the left inguinal and axillary lymph nodes, whereas left and right inguinal and axillary lymph nodes presented accumulation after administration in the right flank. Cervical lymph nodes, in the opposite direction of lymph flow, were never targeted after SC administration, whatever the injection site.

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Section: Lnc Biodistribution Vs Injection Sites and Administration Rsupporting

confidence: 88%

Passive and specific targeting of lymph nodes: the influence of the administration route

Pitorre¹,

Bastiat²,

Chatel³

et al. 2015

European Journal of Nanomedicine

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“…Hence, many attempts have so far been conducted to replace Cremophor ® EL-based formulations with alternative carriers enable to deliver PTX selectively to the tumor tissues without causing adverse effects to healthy tissues. In this direction, numerous drug delivery carriers including emulsions (4,5), liposomes (6)(7)(8), nanoparticles (9)(10)(11), and polymeric micelles (12)(13)(14)(15) have been extensively studied for delivery of PTX into the cancer cells via parenteral administration. We have recently developed a novel targeted polymeric micelle formulation, through synthesizing tocopherol succinate-chitosan-polyethylene glycol-folate (TS-CS-PEG-FA), for delivering of PTX into cancer cells (16).…”

Section: Introductionmentioning

confidence: 99%

A Rapid and Sensitive HPLC Method for Quantitation of Paclitaxel in Biological Samples using Liquid-Liquid Extraction and UV Detection: Application to Pharmacokinetics and Tissues Distribution Study of Paclitaxel Loaded Targeted Polymeric Micelles in.....

et al. 2015

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-A simple, rapid, and sensitive reversed-phase HPLC method was developed and validated for determination of paclitaxel (PTX) in plasma, various organs and tumor tissues of tumor-bearing mice. Tissue specimens of liver, kidneys, spleen, lungs, heart and tumor were separately homogenized in normal saline. Plasma or tissue homogenate (250 µl) containing PTX and internal standard (diazepam) were extracted by diethyl ether (6 ml). The separation was achieved on a µ-Bondapak C 18 HPLC column using sodium acetate buffer solution (0.01 M)/acetonitrile (58/42 v/v) at pH 5 ± 0.1 and flow rate of 1.9 mL/min. The effluent was monitored at 227 nm and column temperature was adjusted at 58 º C. The internal standard and PTX were eluted at 4.2 and 5.2 min, respectively and no interfering peaks were observed. Calibration curves were linear over the concentration range of 0.25-10 µg/ml of PTX in plasma and 0.3-20 µg/ml PTX in tissue homogenates with acceptable precision and accuracy (<15%). The mean recoveries of the drug after plasma extraction was 87.4% ± 3.6 while those of tissue homogenates ranged from 62.1± 4.5 to 75.5± 3.2 depending on the type of tissues studied. PTX was stable in samples with no evidence of degradation during 3 freeze-thaw cycles and 3 months storage at −70 °C. The developed HPLC method was applied to quantify PTX in the mouse plasma and tissues after intravenous administration of 10 mg equivalent PTX/Kg dose of PTX-loaded tocopherol succinate-chitosan-polyethylene glycol-folate (TS-CS-PEG-FA) micelles formulation or Anzatax ® (Cremophor ®

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“…They are prepared by a solvent-free, simple phase inversion technique and are composed of rigid surfactant shell surrounding an oily liquid core. 20 They have shown potential for the delivery of many drugs by different routes, mainly parenteral 21 as well as pulmonary 22 and more interestingly, the oral route. 23 Their gastrointestinal stability 24 and their P-gp inhibiting properties are attributed to Solutol ® HS15 (BASF, Ludwigshafen, Germany), which is a key excipient in their composition.…”

Section: Introductionmentioning

confidence: 99%

Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study

Ramadan¹,

Lagarce²,

Tessier-Marteau³

et al. 2011

IJN

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Abstract:Oral anticoagulant therapy could be advanced using lipid-based nanoparticulate systems. This study examined lipid nanocapsules for their oral absorption potential as the first step in developing oral fondaparinux (Fp) novel carriers. Using phase inversion method and cationic surfactants such as hexadecyltrimethyl ammonium bromide (CTAB) or stearylamine (SA), cationic lipid nanocapsules (cLNCs), loaded with Fp on their surface, were prepared and characterized (zeta potential, size and Fp association efficiency and content). In vivo studies were conducted after single oral increasing doses of Fp-loaded cLNCs (0.5 to 5 mg/kg of Fp) in rats and the concentration of Fp in the plasma was measured by anti-factor Xa activity assay. The monodisperse, (∼50 nm), positively charged Fp-cLNCs with high drug loadings demonstrated linear pharmacokinetic profiles of the drug with an increased oral absolute bioavailability (up to ∼21%) compatible with therapeutic anticoagulant effect (.0.2 µg/mL).

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In vivo evaluation of lipid nanocapsules as a promising colloidal carrier for paclitaxel

Cited by 71 publications

References 22 publications

Passive and specific targeting of lymph nodes: the influence of the administration route

Passive and specific targeting of lymph nodes: the influence of the administration route

A Rapid and Sensitive HPLC Method for Quantitation of Paclitaxel in Biological Samples using Liquid-Liquid Extraction and UV Detection: Application to Pharmacokinetics and Tissues Distribution Study of Paclitaxel Loaded Targeted Polymeric Micelles in.....

Oral fondaparinux: use of lipid nanocapsules as nanocarriers and in vivo pharmacokinetic study

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