Methotrexate loading in chitosan nanoparticles at a novel pH: Response surface modeling, optimization and characterization

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• 作者：Rania A. Hashad^a ; ^{Dr.Rania@pharma.asu.edu.eg" class="auth_mail" title="E-mail the corresponding author} ; Rania A.H. Ishak^a ; ^{raniaaziz@pharma.asu.edu.eg" class="auth_mail" title="E-mail the corresponding author} ; ^{raniaaziz77@yahoo.com" class="auth_mail" title="E-mail the corresponding author} ; Ahmed S. Geneidi^a ; ^{Ahmed.Gnedy@pharma.asu.edu.eg" class="auth_mail" title="E-mail the corresponding author} ; Samar Mansour^a ; ^b ; ^{samar_holayel@yahoo.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Chitosan (PubChem CID ; 71853) ; Tripolyphosphate (PubChem CID ; 24455) ; Methotrexate sodium (PubChem CID ; 11329481)
• 刊名：International Journal of Biological Macromolecules
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：91
• 期：Complete
• 页码：630-639
• 全文大小：2866 K

文摘

The aim of this study was to assess the feasibility of employing a novel but critical formulation pH (6.2) to encapsulate an anionic model drug (methotrexate, MTX) into chitosan(Cs)-tripolyphosphate nanoparticles(NPs). A response surface methodology using a three-level full factorial design was applied studying the effects of two independent variables namely; Cs concentration and MTX concentration. The responses investigated were the entrapment efficiency (EE%), mean hydrodynamic particle size (PS), polydispersity index (PDI) and zeta potential (ZP). In order to simultaneously optimize the series of models obtained, the desirability function approach was applied with a goal to produce high percent of MTX encapsulated into highly charged Cs-TPP NPs of homogenous optimum PS. MTX-loaded CsNPs were successfully prepared at the novel pH applied. The suggested significant models were found quadratic for EE, PS and ZP responses, while 2-factor interaction model for PDI. The optimization overlay graph showed that the maximum global desirability, D = 0.856, was reached when the conditions were set at high Cs and MTX concentration. Thus, the use of such optimized conditions, at this novel pH, achieved a maximum drug EE% (73.38%) into NPs characterized by optimum PS (232.6 nm), small PDI value (0.195) and highly surface charged (+18.4 mV).