Abstract
Objective: The present research was designed to produce methylprednisolone containing chitosan-based nanoparticles using Box-Behnken Design (BBD) and Response Surface Methodology (RSM) for optimization.
 Methods: Nanostructures were prepared using the ionic gelation method with screened process parameters. According to the design, methylprednisolone chitosan-based nanoparticles (MCSNPs) were optimized using factors like methylprednisolone concentration, stirring speed and temperature whereas particle size, zeta potential and % encapsulation efficiency as responses. From the observed values of responses with confirmation location and desirability, the predicted values were very close to the observed values.
 Results: Observed values for the optimized formulation have a particle size of 243±2.33 nm with an encapsulation efficiency of 79.3±7.2%. Morphology of the particles using scanning electron microscopy reveals nearly spherical shaped particles. Methylprednisolone was released in vitro in a sustained manner for about 24 h in simulated colonic fluid pH 7, pH 7.8 (Fasted state) and phosphate buffer pH 7.4, when compared to simulated colonic fluid at pH 6 (Fed state). Optimized MCSNPs followed Korsmeyer peppas kinetics with drug release mechanism as anomalous transport.
 Conclusion: Application of Box-Behnken design and Response Surface Methodology using Design Expert software was successfully used in the optimization of methylprednisolone loaded chitosan-based nanoparticles with high encapsulation efficiency.
Highlights
Methylprednisolone is a potent anti-inflammatory agent used in the short-term and long-term treatment of Crohn’s disease (CD) [1, 2]
Blank chitosan nanoparticles were formulated to optimize the concentration of chitosan, TPP and acetic acid based on the dependent variables like particle size, zeta potential and polydispersity index (PDI)
Observed values for the confirmation location were close to the predicted values showing that Box-Behnken Design can be considered being the best tool in formulating methylprednisolone chitosan nanoparticles
Summary
Methylprednisolone is a potent anti-inflammatory agent used in the short-term and long-term treatment of Crohn’s disease (CD) [1, 2]. Methylprednisolone nanoparticles were prepared to target the drug into the colon. For this intention, chitosan was selected as a polymer because of its biodegradability, biocompatibility and ability to sustain the drug release in colonic pH [7]. The presence of primary amine at C-2 position of glucosamine residue made chitosan as an important polysaccharide for the fabrication of functional drug delivery. Ability of chitosan to release the drug in a sustained manner is because of the deprotonation of amines that undergo inter-polymer associations leading to film and gel formation [8, 9]. It was found that methylprednisolone nanoparticles were prepared using albumin [11], inulin [12], cyclodextrin polymer [13] etc
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