Abstract
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
Medicinal Chemistry
Title:Poly (D,L-lactic-co-glycolide) Nanoparticles for the Improved Therapeutic Efficacy of All-trans-retinoic Acid: A Study of Acute Myeloid Leukemia (AML) Cell Differentiation In Vitro
Volume: 8 Issue: 5
Author(s): Aswathy Mary Simon, Sankar Jagadeeshan, Emimol Abraham, Ashalatha Akhilandeshwaran, Jisha J. Pillai, Nisha Asok Kumar, Asha Nair Sivakumari and Gopalakrishnapillai Sankaramangalam Vinod Kumar
Affiliation:
Keywords: All-trans-retinoic acid, Controlled release, Nanoparticles, cancer, Myeloid leukemia, HL-60, lactide-co-glycolide, vitamin A, cell, cytochrome P450
Abstract: 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.
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Mary Simon Aswathy, Jagadeeshan Sankar, Abraham Emimol, Akhilandeshwaran Ashalatha, J. Pillai Jisha, Asok Kumar Nisha, Nair Sivakumari Asha and Sankaramangalam Vinod Kumar Gopalakrishnapillai, Poly (D,L-lactic-co-glycolide) Nanoparticles for the Improved Therapeutic Efficacy of All-trans-retinoic Acid: A Study of Acute Myeloid Leukemia (AML) Cell Differentiation In Vitro, Medicinal Chemistry 2012; 8 (5) . https://dx.doi.org/10.2174/157340612802084333
DOI https://dx.doi.org/10.2174/157340612802084333 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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