吉他霉素纳米凝胶制备与评价

Preparation and Evaluation of Kitasamycin Nanogel

【目的】制备一种可局部递送吉他霉素用于皮肤创口感染的纳米凝胶。【方法】以京尼平为交联剂在希夫碱作用下,通过凝胶材料之间的静电作用制备壳聚糖/明胶/聚乙烯醇纳米凝胶,并载入药物吉他霉素,对其包封率、载药量、溶胀性能、纳米粒径、Zeta电位、微观结构扫描等表征结构及生物安全性进行测试,评估纳米凝胶的体外释放效果和伤口愈合活性。【结果】本研究制备的吉他霉素纳米凝胶,在其组方为每25 mL凝胶中含吉他霉素0.25 g、壳聚糖0.4 g、明胶0.3 g、聚乙烯醇0.2 g,京尼平0.2 g,其余量为去离子水时外观性状为淡蓝色纳米凝胶,无沉淀与药物析出,溶胀度高,载药量为13.6%,包封率为83.1%;扫描电镜下可见该纳米凝胶形成孔隙致密且分布均匀的三维网状结构;平均粒径为28.56 nm,Zeta电位为16.33 mV;生物安全性良好;纳米凝胶在体外释放药物可维持48 h,明显长于吉他霉素溶液的释放时间。此外,纳米凝胶还能使小鼠伤口缩小96%,有助于伤口愈合。【结论】本研究成功制备了吉他霉素纳米凝胶,通过体内体外试验评估证明了其潜在的药物控释与促进皮肤伤口愈合的能力。

【Objective】The aim of the experiment was to prepare a nanogel for topical delivery of kitasamycin for skin wound infections.【Method】Chitosan/gelatin/poly(vinyl alcohol)nanogel were developed by electrostatic interaction between the gel materials under the action of Schiff base using genipin as cross-linking agent and loaded with the drug kitasamycin.The encapsulation rate,drug loading,swelling properties,nanoparticle size,Zeta potential,microstructure scanning,and other characterisation structures and biosafety were tested.The in vitro release effect and wound healing activity of nanogel were evaluated.【Result】In the present study,the kitasamycin nanogel was prepared in the composition of 0.25 g of kitasamycin,0.4 g of chitosan,0.3 g of gelatin,0.2 g of polyvinyl alcohol,and 0.2 g genipin per 25 mL of the gel,and the remaining amount of deionized water,the appearance properties were light blue nanogel,without precipitation and drug precipitation,the swelling degree was high,the drug loading was 13.6%,and the encapsulation rate was 83.1%.Scanning electron microscopy showed that the nanogel formed a three-dimensional mesh structure with dense and uniformly distributed pores.The average particle size was 28.56 nm,Zeta potential was 16.33 mV,with good biological safety.The nanogel could release the drug in vitro for 48 h,which was significantly longer than that of the kitasamycin solution.In addition,the nanogel could reduce the wound size of mice by 96%,which was helpful for wound healing.【Conclusion】In this study,kitasamycin nanogels were successfully prepared,and their potential ability to control drug release and promote skin wound healing was demonstrated by in vitro and in vivo evaluations.