N-乙酰-D-半乳糖胺修饰头孢克洛-壳聚糖纳米乳的制备及释药性能研究

Preparation and Drug Release Performance of N-Acetyl-D-galactosamine Modified Cefaclor-chitosan Nanoemulsion

采用低能乳化法制备了N-乙酰-D-半乳糖胺修饰头孢克洛-壳聚糖纳米乳,测定了纳米乳的粒径和Zeta电位,通过比较纳米乳和头孢克洛混悬液的累积释药率、考察释放介质和乳化剂用量对纳米乳累积释药率的影响初步研究了其释药性能。结果表明,纳米乳的粒径在60~250 nm范围内,Zeta电位为(3.63±0.32)mV;相较于头孢克洛混悬液,纳米乳的释药性能更优,但纳米乳不适合在偏碱性环境(pH≥7.3)中释药;在3~8 g范围内,随着乳化剂用量的增加,纳米乳的累积释药率逐渐升高,当乳化剂用量为8 g时,24 h累积释药率最高达到72.43%;纳米乳的释药行为符合一级释药模型。

We prepared N-acetyl-D-galactosamine modified Cefaclor-chitosan nanoemulsion by a low-energy emulsification method,and determined the particle size and Zeta potential of the nanoemulsion.Moreover,we preliminarily studied the drug release performance of the nanoemulsion through the comparison of the cumulative drug release rates of the nanoemulsion and Cefaclor suspension,and the investigation of the effects of release medium and emulsifier dosage on the cumulative drug release rate of the nanoemulsion.The results show that the particle size of the nanoemulsion is in the range of 60-250 nm,and the Zeta potential is(3.63±0.32)mV.Compared with Cefaclor suspension,the nanoemulsion has better drug release performance,but which is not suitable for drug release in alkaline environment(pH≥7.3).In the range of 3-8 g,with the increase of emulsifier dosage,the cumulative drug release rate of the nanoemulsion gradually increases.When the emulsifier dosage is 8 g,the cumulative drug release rate reaches the highest of 72.43%at 24 h.The drug release behavior of the nanoemulsion conforms to the first-order drug release model.