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Characterization and Evaluation of 5-Fluorouracil-Loaded Solid Lipid Nanoparticles Prepared via a Temperature-Modulated Solidification Technique

  • Research Article
  • Theme: Translational Application of Nano Delivery Systems: Emerging Cancer Therapy
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Abstract

The aim of this research was to advance solid lipid nanoparticle (SLN) preparation methodology by preparing glyceryl monostearate (GMS) nanoparticles using a temperature-modulated solidification process. The technique was reproducible and prepared nanoparticles without the need of organic solvents. An anticancer agent, 5-fluorouracil (5-FU), was incorporated in the SLNs. The SLNs were characterized by particle size analysis, zeta potential analysis, differential scanning calorimetry (DSC), infrared spectroscopy, atomic force microscopy (AFM), transmission electron microscopy (TEM), drug encapsulation efficiency, in vitro drug release, and in vitro cell viability studies. Particle size of the SLN dispersion was below 100 nm, and that of redispersed lyophilizates was ~500 nm. DSC and infrared spectroscopy suggested that the degree of crystallinity did not decrease appreciably when compared to GMS. TEM and AFM images showed well-defined spherical to oval particles. The drug encapsulation efficiency was found to be approximately 46%. In vitro drug release studies showed that 80% of the encapsulated drug was released within 1 h. In vitro cell cultures were biocompatible with blank SLNs but demonstrated concentration-dependent changes in cell viability to 5-FU-loaded SLNs. The 5-FU-loaded SLNs can potentially be utilized in an anticancer drug delivery system.

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Acknowledgments

This research was performed with support from start-up funds made available by the Department of Pharmacy Practice at the University of Toledo College of Pharmacy and Pharmaceutical Sciences. We are grateful to Dr. Joseph Lawrence, Center for Sensor and Materials Characterization, University of Toledo College of Engineering, for his assistance during the TEM work. We thank Ms. Charisse Montgomerry, Scientific Editor and College Communicator, College of Pharmacy and Pharmaceutical Sciences, University of Toledo, for her review and comments.

Conflict of Interest

The authors report no conflict of interest.

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Authors and Affiliations

  1. Department of Pharmacy Practice, College of Pharmacy and Pharmaceutical Sciences, University of Toledo, 3000 Arlington Avenue, MS1013, Toledo, Ohio, 43614, USA

    Meghavi N. Patel, Sushant Lakkadwala, Mohamed S. Majrad, Sai Hanuman Sagar Boddu & Jerry Nesamony

  2. Department of Pharmaceutical Sciences, School of Pharmacy, Cedarville University, 251N. Main St., Cedarville, Ohio, 45314, USA

    Elisha R. Injeti

  3. Department of Science and Mathematics, College of Arts and Sciences, Cedarville University, 251 N. Main St., Cedarville, Ohio, 45314, USA

    Steven M. Gollmer

  4. Department of Medicinal and Biological Chemistry, College of Pharmacy and Pharmaceutical Sciences, University of Toledo, 3000 Arlington Avenue, MS1013, Toledo, Ohio, 43614, USA

    Zahoor A. Shah

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  1. Meghavi N. Patel
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  2. Sushant Lakkadwala
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Correspondence to Jerry Nesamony.

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Guest Editors: Mahavir B. Chougule and Chalet Tan

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Patel, M.N., Lakkadwala, S., Majrad, M.S. et al. Characterization and Evaluation of 5-Fluorouracil-Loaded Solid Lipid Nanoparticles Prepared via a Temperature-Modulated Solidification Technique. AAPS PharmSciTech 15, 1498–1508 (2014). https://doi.org/10.1208/s12249-014-0168-x

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  • DOI: https://doi.org/10.1208/s12249-014-0168-x

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