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Biotin-Encoded Pullulan-Retinoic Acid Engineered Nanomicelles: Preparation, Optimization and in Vitro Cytotoxicity Assessment in Mcf-7 Cells Publisher



Hassanzadeh F1 ; Varshosaz J2 ; Khodarahmi GA3 ; Rostami M1 ; Hassanzadeh F1
Authors
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Authors Affiliations
  1. 1. Isfahan Pharmaceutical Sciences Research Center, Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
  2. 2. Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran
  3. 3. Department of Medicinal Chemistry, School of Pharmacy and Pharmaceutical Sciences, Isfahan University of Medical Sciences, Isfahan, Iran

Source: Indian Journal of Pharmaceutical Sciences Published:2016


Abstract

Biotin and retinoic acid grafted pullulan conjugate was synthesized using carbodiimide activation ester bond formation strategy for biotin targeted delivery of doxorubicin in breast cancer chemotherapy using micelle formulation. The conjugate structure was evaluated and confirmed by proton nuclear magnetic resonance and Fourier transform infrared spectroscopy. Critical micelle concentration of final conjugate was determined using the pyrene fluorescence method. Doxorubicin-loaded micelles were prepared using the direct dissolution method. Physical parameters of optimized micelles comprising particle size, zeta potential, drug loading efficacy, and drug release profile were determined. The results reveal that the nanomicelles have formed with mean particle size of 191 nm and zeta potential of -9.45 mv. The drug loading efficacy of 92% and release efficiency of 81% during 24 h, are also obtained. The structure of the micelles was studied by transition electron microscopy technique. The cytotoxicity of doxorubicin-loaded micelles was studied in MCF-7 cells using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. The results of in vitro cell culture cytotoxicity assay showed that the doxorubicin-loaded biotin grafted retinoic acid-pullulan micelles were more cytotoxic in comparison to the non-targeted pullulan and free doxorubicin. © 2016, OMICS International. All rights reserved.
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