New nasal nanocomplex self-assembled from charged biomacromolecules: N,N,N-Trimethyl chitosan and dextran sulfate

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• 作者：Abhijeet D. Kulkarni<sup>asup> ; Yogesh H. Vanjari<sup>asup> ; Karan H. Sancheti<sup>asup> ; Harun M. Patel<sup>bsup> ; Veena S. Belgamwar<sup>csup> ; Sanjay J. Surana<sup>asup> ; Chandrakantsing V. Pardeshi<sup>asup><sup> ; sup><sup>chandrakantpardeshi11@gmail.com" class="auth_mail" title="E-mail the corresponding authorsup>
• 关键词：Chitosan ; N ; N ; N-Trimethyl chitosan ; Reductive methylation ; Dextran sulfate ; Polyelectrolyte nanocomplex ; Nasal delivery
• 刊名：International Journal of Biological Macromolecules
• 出版年：2016
• 出版时间：July 2016
• 年：2016
• 卷：88
• 期：Complete
• 页码：476-490
• 全文大小：4725 K

文摘

Although chitosan (CHT, a linear cationic polysaccharide) is biodegradable, biocompatible, non-toxic, and mucoadhesive in nature, the low solubility of CHT in aqueous and alkaline media limits its applicability in pharmaceutical and biomedical field. This necessitate the introduction of new chemically-modified derivatives of CHT those can surmount the solubility barrier. Herein, N,N,N-trimethyl chitosan (TMC), a quaternized hydrophilic derivative of CHT, was synthesized by two-step reductive methylation of CHT and characterized for <sup>1sup>H NMR and zeta potential measurements. Polyelectrolyte complexes (PECs) based on TMC and dextran sulfate (DS) were prepared via ionic interactions between charged functional groups of former polysaccharides at different pH conditions (pH 5, 8, 10, and 12) and characterized for physicochemical (particle size and zeta potential) and solid- state characterizations (HR-TEM, SEM, FTIR, TGA and XRD). At alkaline pH conditions, the participant polymer chains (TMC and DS) are sufficiently close to form more stable PECs. The release efficiency was assessed after loading a model drug into optimized PEC formulation. Data indicated that the PECs fabricated at alkaline pH presents a reliable formulation for pharmaceutical and biomedical applications.