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Sci. Pharm. 2014, 82(4), 873-888; doi:10.3797/scipharm.1401-10

Low Density Lipid Nanoparticles for Solid Tumor Targeting

1
Pharmaceutics Research Project Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar (M. P.), India
2
Defense Research and Development Establishment, Gwalior (M. P), India
*
Author to whom correspondence should be addressed.
Received: 13 January 2014 / Accepted: 28 August 2014 / Published: 28 August 2014
Download PDF [597 KB, uploaded 28 September 2016]

Abstract

One of the most significant characteristics of cancer cells is their rapid dividing ability and overexpression of LDL receptors, which offers an opportunity for the selective targeting of these cells. 5-Fluorouracil (5-FU)-encapsulated low density lipid nanoparticles (LDLN) were prepared by the emulsion congealing method which mimics the plasma-derived LDL by acquiring the apolipoprotein B-100 from the blood. The average particle size, transmission electron microscope (TEM), and drug content of the prepared LDLN dispersion were found to be 161±3.5 nm, with spherical shape, and 0.370±0.05 mg/mL, respectively. In vitro release studies revealed a sustained profile which decrea-sed with a lapse of time. In vivo studies of 5-FU serum concentration and biodistribution revealed a 5-FU serum concentration of 8.5% in tumor cells and about 2.1% in the liver at the end of 24 hr from LDLN. Tumor growth suppres-sion studies showed 185.42% average tumor growth and 89.76% tumor height as compared to the control exhibiting tumor growth at 1166.47% and tumor height at 176.07%. On the basis of these collective data, it is suggested that a higher accumulation of LDLN, when given as an IV, in solid tumors is attributed to the active uptake of LDLN via LDL receptors via apolipoprotein B-100.
Keywords: LDL receptors; Lipoproteins; Apo protein 100; 5-Fluorouracil LDL receptors; Lipoproteins; Apo protein 100; 5-Fluorouracil
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

SHRIVASTAVA, M.; JAIN, A.; GULBAKE, A.; HURKAT, P.; JAIN, N.; VIJAYRAGHWAN, R.; JAIN, S.K. Low Density Lipid Nanoparticles for Solid Tumor Targeting. Sci. Pharm. 2014, 82, 873-888.

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