Development of lipid-based nanoparticles for enhancing the oral bioavailability of paclitaxel

Pandita, Deepti, Ahuja, Alka, Lather, Viney, Benjamin, Biju, Dutta, Tathagata, Velpandian, Thirumurthy and Khar, Roop Krishen (2011) Development of lipid-based nanoparticles for enhancing the oral bioavailability of paclitaxel. AAPS PharmSciTech, 12 2: 712-722. doi:10.1208/s12249-011-9636-8

Author Pandita, Deepti
Ahuja, Alka
Lather, Viney
Benjamin, Biju
Dutta, Tathagata
Velpandian, Thirumurthy
Khar, Roop Krishen
Title Development of lipid-based nanoparticles for enhancing the oral bioavailability of paclitaxel
Journal name AAPS PharmSciTech   Check publisher's open access policy
ISSN 1530-9932
Publication date 2011-06
Sub-type Article (original research)
DOI 10.1208/s12249-011-9636-8
Volume 12
Issue 2
Start page 712
End page 722
Total pages 11
Place of publication New York, NY, U.S.A.
Publisher Springer New York
Collection year 2012
Language eng
Formatted abstract
The current research work investigates the potential of solid lipid nanoparticles (SLNs) in improving the oral bioavailability of paclitaxel. Paclitaxel-loaded SLNs (PTX-SLNs) were prepared by modified solvent injection method using stearylamine as lipid, soya lecithin and poloxamer 188 as emulsifiers. SLNs were characterized in terms of surface morphology, size and size distribution, surface chemistry and encapsulation efficiency. Pharmacokinetics and bioavailability studies were conducted in male Swiss albino mice after oral administration of PTX-SLNs. SLNs exhibited spherical shape with smooth surface as analyzed by transmission electron microscopy (TEM). The mean particle size of SLNs was 96 ± 4.4 nm with a low polydispersity index of 0.162 ± 0.04 and zeta potential of 39.1 ± 0.8 mV. The drug entrapment efficiency was found to be 75.42 ± 1.5% with a loading capacity of 31.5 ± 2.1% (w/w). Paclitaxel showed a slow and sustained in vitro release profile and followed Higuchi kinetic equations. After oral administration of the PTX-SLNs, drug exposure in plasma and tissues was ten- and twofold higher, respectively, when compared with free paclitaxel solution. PTX-SLNs produced a high mean Cmax (10,274 ng/ml) compared with that of free paclitaxel solution (3,087 ng/ml). The absorbed drug was found to be distributed in liver, lungs, kidneys, spleen, and brain. The results suggested that PTX-SLNs dispersed in an aqueous environment are promising novel formulations that enhanced the oral bioavailability of hydrophobic drugs, like paclitaxel and were quite safe for oral delivery of paclitaxel as observed by in vivo toxicity studies.
Keyword Biodistribution
Oral administration
Solid lipid nanoparticles
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2012 Collection
UQ Diamantina Institute Publications
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