Altered chemical and biological activities of all- trans retinoic acid incorporated in solid lipid nanoparticle powders

The principal aim of this study was to investigate whether the solid lipid nanoparticle (SLN) powder formulation of all- trans retinoic acid (ATRA) can favorably alter the chemical stability and biological activities of ATRA. SLN powder formulation of ATRA was obtained by freeze-drying of SLN disper...

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Bibliographic Details
Published in:Journal of controlled release 2004-11, Vol.100 (1), p.53-61
Main Authors: Lim, Soo-Jeong, Lee, Mi-Kyung, Kim, Chong-Kook
Format: Article
Language:English
Subjects:
All- trans retinoic acid
Animals
Antineoplastic Agents - administration & dosage
Biological and medical sciences
Cancer
Cell Line, Tumor
Drug Stability
Female
General pharmacology
Hemolysis - drug effects
Humans
Medical sciences
Mice
Mice, Inbred BALB C
Nanostructures
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Powder
Powders
Solid lipid nanoparticles
Stability
Tretinoin - administration & dosage
Tretinoin - chemistry
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Summary:The principal aim of this study was to investigate whether the solid lipid nanoparticle (SLN) powder formulation of all- trans retinoic acid (ATRA) can favorably alter the chemical stability and biological activities of ATRA. SLN powder formulation of ATRA was obtained by freeze-drying of SLN dispersions. The chemical stability of ATRA was determined by HPLC analysis. The anticancer efficacy of ATRA was determined by evaluating antiproliferative effects of ATRA on cancer cell lines. Hemolytic potential of ATRA was spectrophotometrically determined after incubation with red blood cells (RBCs) in vitro. ATRA could be efficiently incorporated in SLN powder without impairing the physical stability of lipid nanoparticles. After 3 months of storage, >90% ATRA remained intact in SLN powder, indicating that the chemical stability of ATRA was substantially improved by incorporation in SLN powder. The antiproliferative effects of SLN powder formulation of ATRA on a wide range of cancer cell lines were not significantly different from that of free ATRA. Furthermore, the incorporation of ATRA in SLN powder significantly reduced the hemolytic potential of ATRA. Taken together, the molecular characteristics that currently appear to limit the clinical efficacy of ATRA were greatly improved by preparing SLN powder formulation. SLN powder formulation of ATRA may have a potential in enhancing the efficacy of ATRA in cancer chemoprevention and therapeutics.
ISSN:0168-3659
1873-4995
DOI:10.1016/j.jconrel.2004.07.032