Journal
INTERNATIONAL JOURNAL OF PHARMACEUTICS
Volume 490, Issue 1-2, Pages 324-333Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ijpharm.2015.05.070
Keywords
Paclitaxel; Nanosuspension; Emulsification; Dissolution; Bioavailability
Categories
Funding
- National Natural Science Foundation of China [21473023]
- Ph.D. Independent Innovation Foundation Project of Northeast Forestry University [2572014AB10]
Ask authors/readers for more resources
The aim of this study was to develop an alternative, more bio-available, better tolerated paclitaxel nanosuspension (PTXNS) for intravenous injection in comparison with commercially available Taxol (R) formulation. In this study, PTXNS was prepared by emulsification method through combination of high speed homogenizer and high pressure homogenization, followed by lyophilization process for intravenous administration. The main production parameters including volume ratio of organic phase in water and organic phase (V-o: Vw+o), concentration of PTX, content of PTX and emulsification time (E-t), homogenization pressure (HP) and passes (P-s) for high pressure homogenization were optimized and their effects on mean particle size (MPS) and particle size distribution (PSD) of PTXNS were investigated. The characteristics of PTXNS, such as, surface morphology, physical status of paclitaxel (PTX) in PTXNS, redispersibility of PTXNS in purified water, in vitro dissolution study and bioavailability in vivo were all investigated. The PTXNS obtained under optimum conditions had an MPS of 186.8 nm and a zeta potential (ZP) of -6.87 mV. The PTX content in PTXNS was approximately 3.42%. Moreover, the residual amount of chloroform was lower than the International Conference on Harmonization limit (60 ppm) for solvents. The dissolution study indicated PTXNS had merits including effect to fast at the side of raw PTX and sustained-dissolution character compared with Taxol (R) formulation. Moreover, the bioavailability of PTXNS increased 14.38 and 3.51 times respectively compared with raw PTX and Taxol (R) formulation. (C) 2015 Elsevier B.V. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available