All-trans-retinoic acid reverses malignant cell growth and induces cell differentiation and apoptosis. Poor aqueous
solubility and uncertain bioavailability are the limiting factors for using all-trans-retinoic acid for tumor therapy. The
objective of present study was to encapsulate the hydrophobic drug all-trans-retinoic acid in the polymer poly (lactide-coglycolide).
The encapsulation was expected to improve the bioavailability and solubility of the drug. Oil in water single
emulsion solvent evaporation technique used for the preparation efficiently encapsulated about 60% of the drug. The drug
release profile showed a biphasic pattern with 70% of the drug being released in first 48 hrs and the residual drug showing
a slow controlled release reaching up to 8 days. The particle size of 150-200 nm as determined with TEM was ideal for
tumor targeting. All-trans-retinoic acid loaded nanoparticles were efficient to induce differentiation and blocked the proliferation
of HL-60 cells invitro. These studies also revealed that the dosage of drug required for the therapeutic effects
have been reduced efficiently. Our studies thereby demonstrate that Poly (lactide-co-glycolide) based nanoparticles may
be efficient for parenteral administration of the drug.
Keywords: All-trans-retinoic acid, Controlled release, Nanoparticles, cancer, Myeloid leukemia, HL-60, lactide-co-glycolide, vitamin A, cell, cytochrome P450
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Published on: 22 July, 2012
Page: [805 - 810]