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Chitosan Graft Copolymer Nanoparticles for Oral Protein Drug Delivery: Preparation and Characterization

机译：用于口服蛋白质药物递送的壳聚糖接枝共聚物纳米粒子：制备和表征

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摘要

Several novel functionalized graft copolymer nanoparticles consisting of chitosan (CS) and the monomer methyl methacrylate (MMA), N-dimethylaminoethyl methacrylate hydrochloride (DMAEMC), and N-trimethylaminoethyl methacrylate chloride (TMAEMC), which show a higher solubility than chitosan in a broader pH range, have been prepared by free radical polymerization. The nanoparticles were characterized in terms of particle size, zeta potential, TEM, and FT-IR. These nanoparticles were 150-280 nm in size and carried obvious positive surface charges. Protein-loaded nanoparticles were prepared, and their maximal encapsulation efficiency was up to 100%. In vitro release showed that these nanoparticles provided an initial burst release followed by a slowly sustained release for more than 24 h. These graft copolymer nanoparticles enhanced the absorption and improved the bioavailability of insulin via the gastrointestinal (GI) tract of normal male Sprague-Dawley (SD) strain rats to a greater extent than that of the phosphate buffer solution (PBS) of insulin.
机译：由壳聚糖（CS）和单体甲基丙烯酸甲酯（MMA），甲基丙烯酸N-二甲基氨基乙基酯盐酸盐（DMAEMC）和甲基丙烯酸N-三甲基氨基乙基酯氯化物（TMAEMC）组成的几种新型功能化接枝共聚物纳米颗粒，在更广泛的范围内显示出比壳聚糖更高的溶解度pH范围内，已通过自由基聚合制备。根据粒度，ζ电势，TEM和FT-IR表征纳米颗粒。这些纳米粒子的尺寸为150-280 nm，并带有明显的正表面电荷。制备了载有蛋白质的纳米粒子，其最大包封效率高达100％。体外释放表明，这些纳米粒子提供了最初的突释释放，然后缓慢持续释放超过24小时。这些接枝共聚物纳米颗粒通过胰岛素对正常雄性Sprague-Dawley（SD）品系大鼠的胃肠道（GI）的吸收，增强了胰岛素的吸收，并改善了其生物利用度，其程度大于胰岛素的磷酸盐缓冲溶液（PBS）。

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