Part I: Development and optimization of solid-lipid nanoparticles using Box–Behnken statistical design for ocular delivery of gatifloxacin

Authors

  • Mohd. Abul Kalam,

    1. Nanomedicine Research Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, KSA
    2. Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India
    Search for more papers by this author
  • Yasmin Sultana,

    1. Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India
    Search for more papers by this author
  • Asgar Ali,

    1. Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India
    Search for more papers by this author
  • Mohd. Aqil,

    1. Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), Hamdard Nagar, New Delhi 110062, India
    Search for more papers by this author
  • Anil K. Mishra,

    1. Department of Radiopharmaceuticals, Institute of Nuclear Medicine and Allied Sciences (INMAS), Brig. S. K. Majumdar Road, Delhi 110054, India
    Search for more papers by this author
  • Ibrahim A. Aljuffali,

    1. Nanomedicine Research Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, KSA
    Search for more papers by this author
  • Aws Alshamsan

    Corresponding author
    1. Nanomedicine Research Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, KSA
    • Nanomedicine Research Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, KSA
    Search for more papers by this author

  • How to cite this article: Kalam MA, Sultana Y, Ali A, Aqil M, Mishra AK, Aljuffali IA, Alshamsan A. 2013. Part I: Development and optimization of solid-lipid nanoparticles using Box–Behnken statistical design for ocular delivery of gatifloxacin. J Biomed Mater Res Part A 2013:101A:1813–1827.

Abstract

This study aims to improve gatifloxacin bioavailability to the eye using solid-lipid nanoparticles (SLN). Cationic SLNs were prepared by o/w-microemulsion method using stearylamine. The generated formulations were optimized by three-factor, three-level Box–Behnken statistical design. The independent variables were the lipidmix concentration (X1), poloxamers-188 (X2), and sodium-taurocholate (X3), while the dependent variables were drug release (Y1), encapsulation efficiency (EE) (Y2), and particle size (Y3) with applied constraints of maximizing drug release and EE and minimizing particle size. Response surface plots were drawn, statistical validity of the polynomials was established, optimized formulations were selected by feasibility and grid search, and the optimization process was validated. Particle size, polydispersity index, and zeta-potentials were measured by photon correlation spectroscopy. Particle's morphology was evaluated by transmission electron microscopy. Differential scanning calorimetry (DSC) and wide-angle X-ray diffraction (WXRD) studies were performed to characterize state of drug and lipid modification. SLN size was (250–305 nm) and zeta-potential (29–36 mV) after 3-month storage. Entrapment efficiencies were 46.58 and 78.55%, and loading efficiencies were 29.60 and 20.70 for SLN-C and SLN-D, respectively. DSC and WXRD analyses showed low-crystalline SLN and amorphous drug dispersion in SLN. In vitro release data were fitted to release kinetics equations, where the release pattern was found to follow Korsmeyer–Peppas model. © 2012 Wiley Periodicals, Inc. J Biomed Mater Res Part A, 2013.

Ancillary