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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Preparation of aminoglycoside-loaded chitosan nanoparticles using dextran sulphate as a counterion
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Preparation of aminoglycoside-loaded chitosan nanoparticles using dextran sulphate as a counterion

机译：以硫酸葡聚糖为抗衡离子制备氨基糖苷负载的壳聚糖纳米粒

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Purpose. To prepare aminoglycoside (AG) (streptomycin, gentamicin and tobramycin) loaded chitosan nanoparticles with high drug incorporation efficiency and test the in vivo oral efficacy of streptomycin (SM) loaded chitosan nanoparticles in a Mycobacterium tuberculosis (TB) chronic infection mouse model.Method. Dextran sulphate (a polyanion) was used to shield the positive charge of AG and increase the drug incorporation in the chitosan nanoparticle. By varying the concentration of each component, the formulation of SM-loaded chitosan nanoparticle was optimized by monitoring the drug incorporation efficacy and particle size. The mechanism of the nanoparticle formation was suggested and the preparation method was applied to two other aminoglycosides (AG): gentamicin (GM) and tobramycin (TM). The resulting nanoparticles were characterized by particle diameter, drug incorporation efficacy, drug loading efficacy and zeta potential. The in vitro drug release from these nanoparticles was carried out in pH 1.2 and pH 7.4 buffer. Preliminary in vivo oral efficacy studies of SM-loaded chitosan nanoparticles was performed in a Mycobacterium tuberculosis (TB) chronic infection mouse model.Results. The optimal concentration of streptomycin (SM)/dextran sulphate/chitosan/tripolyphosphate (TPP) for SM nanoparticles preparation was 2/1.2/2/0.8 mg mL~(-1). Through calculation, the optimal concentrations of dextran sulphate are 2.5mg mL~(-1) and 2.4mg mL~(-1) for 2mg mL~(-1) gentamicin and tobramycin, respectively (Table 1).The resulting AG chitosan nanoparticles had a high drug incorporation efficacy with particle sizes in the nanometre range. The in vitro drug release studies showed that more than 60% drug is retained inside the nanoparticles in pH 1.2 buffer after 6 h. The preliminary in vivo results indicated that oral SM chitosan nanoparticles induced one log 10 reduction (p<0.01) in growth of the bacilli and were as effective as subcutaneously injected aqueous SM solution at the same concentration (100 mg kg~(-1)).Conclusion. Dextran sulphate can significantly increase AG incorporation into the chitosan nanoparticles. The concentration of each component was critical in preparing AG-loaded chitosan nanoparticles. The chitosan nanoparticles designed in this study may provide a promising oral drug delivery formulation for AG which usually, in tuberculosis treatment, is administrated as an injectible preparation.
机译：目的。为了制备具有高药物掺入效率的氨基糖苷（AG）（链霉素，庆大霉素和妥布霉素）负载的壳聚糖纳米颗粒，并在结核分枝杆菌（TB）慢性感染小鼠模型中测试负载链霉素（SM）的壳聚糖纳米颗粒的体内口服功效。硫酸葡聚糖（一种聚阴离子）用于屏蔽AG的正电荷，并增加药物在壳聚糖纳米颗粒中的掺入。通过改变每种成分的浓度，通过监测药物掺入功效和粒径来优化负载SM的壳聚糖纳米颗粒的配方。提出了纳米粒子的形成机理，并将其制备方法应用于另外两种氨基糖苷类化合物（AG）：庆大霉素（GM）和妥布霉素（TM）。所得纳米颗粒通过粒径，药物掺入功效，药物负载功效和ζ电位来表征。从这些纳米颗粒的体外药物释放是在pH 1.2和pH 7.4缓冲液中进行的。在结核分枝杆菌（TB）慢性感染小鼠模型中进行了SM负载的壳聚糖纳米颗粒的体内初步口服功效研究。制备SM纳米颗粒的最佳链霉素（SM）/硫酸葡聚糖/壳聚糖/三聚磷酸酯（TPP）浓度为2 / 1.2 / 2 / 0.8 mg mL〜（-1）。通过计算，硫酸葡聚糖的最佳浓度分别为2mg mL〜（-1）的庆大霉素和妥布霉素为2.5mg mL〜（-1）和2.4mg mL〜（-1）（表1）。具有在纳米范围内的粒径的高药物掺入功效。体外药物释放研究表明6小时后，pH 1.2缓冲液中60％以上的药物保留在纳米颗粒中。体内初步研究结果表明，口服SM壳聚糖纳米颗粒可诱导细菌生长减少1 log 10（p <0.01），并且与相同浓度（100 mg kg〜（-1））的皮下注射SM水溶液一样有效。 。结论。硫酸葡聚糖可显着增加AG掺入壳聚糖纳米颗粒的过程。每种组分的浓度对于制备载有AG的壳聚糖纳米颗粒至关重要。在这项研究中设计的壳聚糖纳米粒子可能为AG提供有希望的口服药物递送制剂，该制剂通常在结核病治疗中以注射剂的形式给药。

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