Highlighting the Role of Polymer Length, Carbohydrate Size, and Nucleic Acid Type in Potency of Glycopolycation Agents for pDNA and siRNA Delivery
作者： Lian Xue , Nilesh P. Ingle , Theresa M. Reineke
DOI: 10.1021/BM401026N
关键词:
摘要: While nucleic acids such as small interfering RNA (siRNA) and plasmid DNA (pDNA) are promising research tools therapeutic modalities, their potential in medical applications is limited by a fundamental mechanistic understanding inadequate efficiency. Herein, two series of carbohydrate-based polycations were synthesized examined that varied the degree polymerization (n), one containing trehalose [Tr4(n) series: Tr4(23), Tr4(55), Tr4(77)] other β-cyclodextrin [CD4(n) CD4(10), CD4(26), CD4(39), CD4(143), CD4(239)]. In addition, monosaccharide models for comparison contain tartaramidoamine (T4) galactaramidoamine (G4 or Glycofect) repeats. Delivery profiles pDNA compared with those obtained siRNA delivery reveal efficacy differs significantly function carbohydrate type, acid type dose, polymer length, presence excess formulation. The Tr4 polymers yielded higher p...
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