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Docetaxel-loaded-lipid-based-nanosuspensions (DTX-LNS): preparation, pharmacokinetics, tissue distribution and antitumor activity.
- Source :
-
International journal of pharmaceutics [Int J Pharm] 2011 Jul 15; Vol. 413 (1-2), pp. 194-201. Date of Electronic Publication: 2011 Apr 21. - Publication Year :
- 2011
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Abstract
- The purpose of the study was to design lipid-based-nanosuspensions (LNS) for Docetaxel (DTX) without Tween 80 for clinical intravenous administration (i.v.). DTX-LNS were prepared by high pressure homogenization method, and then lyophilization was carried out to improve the stability. The physical-chemical properties in terms of particle size, size distribution, zeta potential and morphology were evaluated, respectively. The in vitro cytotoxic activity was assessed by MTT against SKOV-3 and malignant melanoma B16 cells. The in vivo pharmacokinetics, tissue distribution as well as antitumor efficacy were investigated in B16 melanoma-bearing Kunming mice. The particle size and zeta potential of DTX-LNS were (200.0 ± 3.42)nm and (-11.15 ± 0.99)mV, respectively. Compared with Duopafei, it was shown that DTX-LNS exhibited higher antitumor efficacy by reducing tumor volume (P<0.05) and increasing survival rate in B16 melanoma-bearing mice and strongly reduced the anticancer drug toxicity. The results of biodistribution studies clearly indicated the superiority of DTX-LNS to Duopafei in increasing the accumulation of DTX within tumor and the organs rich in macrophages (liver, lungs and spleen), while, the drug concentration in heart and kidney decreased. Together these results suggested that DTX-LNS could effectively inhibit tumor growth, reduce toxicity during the therapeutic procedure and hold the potential to be an appropriate choice for the clinical administration of DTX.<br /> (Copyright © 2011 Elsevier B.V. All rights reserved.)
- Subjects :
- Animals
Antineoplastic Agents pharmacokinetics
Antineoplastic Agents pharmacology
Cell Line, Tumor
Docetaxel
Drug Compounding
Excipients chemistry
Female
Formazans metabolism
Humans
Lecithins chemistry
Lipids chemistry
Melanoma
Mice
Nanoparticles chemistry
Neoplasms
Ovarian Neoplasms
Particle Size
Suspensions chemistry
Taxoids pharmacokinetics
Taxoids pharmacology
Tetrazolium Salts metabolism
Tissue Distribution
Antineoplastic Agents chemistry
Drug Carriers chemistry
Drug Delivery Systems
Taxoids chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1873-3476
- Volume :
- 413
- Issue :
- 1-2
- Database :
- MEDLINE
- Journal :
- International journal of pharmaceutics
- Publication Type :
- Academic Journal
- Accession number :
- 21540085
- Full Text :
- https://doi.org/10.1016/j.ijpharm.2011.04.023