Back to Journals » International Journal of Nanomedicine » Volume 6

Formulation and pharmacokinetic evaluation of a paclitaxel nanosuspension for intravenous delivery

Authors Wang YL, Li XM, Wang LY, Xu YL, Cheng XD, Wei P

Published 13 July 2011 Volume 2011:6 Pages 1497—1507

DOI https://doi.org/10.2147/IJN.S21097

Review by Single-blind

Peer reviewer comments 3

Yonglu Wang1,4, Xueming Li1,2*, Liyao Wang3, Yuanlong Xu1, Xiaodan Cheng1, Ping Wei4
1
College of Pharmacy, Nanjing University of Technology, Nanjing; 2State Key Laboratory of Materials-Oriented Chemical Engineering, Nanjing University of Technology, Nanjing; 3College of Life Science, Anhui Agricultural University, Hefei; 4College of Biotechnology and Pharmaceutical Engineering, Nanjing University of Technology, Nanjing, People’s Republic of China
*These authors contributed equally to this work.

Abstract: Paclitaxel is a diterpenoid isolated from Taxus brevifolia. It is effective for various cancers, especially ovarian and breast cancer. Due to its aqueous insolubility, it is administered dissolved in ethanol and Cremophor® EL (BASF, Ludwigshafen, Germany), which can cause serious allergic reactions. In order to eliminate Cremophor EL, paclitaxel was formulated as a nanosuspension by high-pressure homogenization. The nanosuspension was lyophilized to obtain the dry paclitaxel nanoparticles (average size, 214.4 ± 15.03 nm), which enhanced both the physical and chemical stability of paclitaxel nanoparticles. Paclitaxel dissolution was also enhanced by the nanosuspension. Differential scanning calorimetry showed that the crystallinity of paclitaxel was preserved during the high-pressure homogenization process. The pharmacokinetics and tissue distribution of paclitaxel were compared after intravenous administration of paclitaxel nanosuspension and paclitaxel injection. In rat plasma, paclitaxel nanosuspension exhibited a significantly (P < 0.01) reduced area under the concentration curve (AUC)0–∞ (20.343 ± 9.119 µg · h · mL−1 vs 5.196 ± 1.426 µg · h · mL−1), greater clearance (2.050 ± 0.616 L · kg−1 · h−1 vs 0.556 ± 0.190 L · kg−1 · h−1), and shorter elimination half-life (5.646 ± 2.941 vs 3.774 ± 1.352 hours) compared with the paclitaxel solution. In contrast, the paclitaxel nanosuspension resulted in a significantly greater AUC0–∞ in liver, lung, and spleen (all P < 0.01), but not in heart or kidney.

Keywords: high-pressure homogenization, tissue distribution, surfactant

Creative Commons License This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

Download Article [PDF]  View Full Text [HTML][Machine readable]

 

Readers of this article also read:

Real-world evaluation of compliance and preference in Alzheimer’s disease treatment

Pai MC, Aref H, Bassil N, Kandiah N, Lee JH, Srinivasan AV, diTommaso S, Yuksel O

Clinical Interventions in Aging 2015, 10:1779-1788

Published Date: 3 November 2015

Effects of a hybrid micro/nanorod topography-modified titanium implant on adhesion and osteogenic differentiation in rat bone marrow mesenchymal stem cells

Zhang WJ, Li ZH, Huang QF, Xu L, Li JH, Jin YQ, Wang GF, Liu XY, Jiang XQ

International Journal of Nanomedicine 2013, 8:257-265

Published Date: 11 January 2013

Gemcitabine-loaded liposomes: rationale, potentialities and future perspectives

Federico C, Morittu VM, Britti D, Trapasso E, Cosco D

International Journal of Nanomedicine 2012, 7:5423-5436

Published Date: 1 November 2012

Sustained-release G-CSF microspheres using a novel solid-in-oil-in-oil-in-water emulsion method

Liu G, Hong X, Jiang M, Yuan W

International Journal of Nanomedicine 2012, 7:4559-4569

Published Date: 17 August 2012

Liver cell specific targeting by the preS1 domain of hepatitis B virus surface antigen displayed on protein nanocages

Murata M, Narahara S, Umezaki K, Toita R, Tabata S, Piao JS, Abe K, Kang JH, Ohuchida K, Cui L, Hashizume M

International Journal of Nanomedicine 2012, 7:4353-4362

Published Date: 9 August 2012

Corrigendum

Biazar E, Heidari M, Asefnejad A, Montazeri N

International Journal of Nanomedicine 2011, 6:1141-1142

Published Date: 2 June 2011

Zinc oxide nanoparticles as selective killers of proliferating cells

Taccola L, Raffa V, Riggio C, Vittorio O, Iorio MC, Vanacore R, Pietrabissa A, Cuschieri A

International Journal of Nanomedicine 2011, 6:1129-1140

Published Date: 30 May 2011

Nanovaccine for leishmaniasis: preparation of chitosan nanoparticles containing Leishmania superoxide dismutase and evaluation of its immunogenicity in BALB/c mice

Danesh-Bahreini MA, Shokri J, Samiei A, Kamali-Sarvestani E, Barzegar-Jalali M, Mohammadi-Samani S

International Journal of Nanomedicine 2011, 6:835-842

Published Date: 20 April 2011