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Part I: Development and optimization of solid‐lipid nanoparticles using Box–Behnken statistical design for ocular delivery of gatifloxacin
Author(s) -
Kalam Mohd. Abul,
Sultana Yasmin,
Ali Asgar,
Aqil Mohd.,
Mishra Anil K.,
Aljuffali Ibrahim A.,
Alshamsan Aws
Publication year - 2013
Publication title -
journal of biomedical materials research part a
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.849
H-Index - 150
eISSN - 1552-4965
pISSN - 1549-3296
DOI - 10.1002/jbm.a.34453
Subject(s) - box–behnken design , materials science , solid lipid nanoparticle , differential scanning calorimetry , zeta potential , particle size , dispersity , microemulsion , chemical engineering , nanoparticle , chromatography , response surface methodology , nanotechnology , polymer chemistry , chemistry , pulmonary surfactant , physics , thermodynamics , engineering
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 lipid mix concentration ( X 1 ), poloxamers‐188 ( X 2 ), and sodium‐taurocholate ( X 3 ), while the dependent variables were drug release ( Y 1 ), encapsulation efficiency (EE) ( Y 2 ), and particle size ( Y 3 ) 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.