蟾蜍抗菌肽脂质体的制备及抗菌研究
Preparation and Antibacterial of Toad Antibacterial Peptide Liposomes
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摘要: 目的 筛选制备蟾蜍抗菌肽脂质体最佳处方，延长其抑菌疗效，提高其安全稳定性。方法 采用水提法提取蟾蜍多肽，薄膜分散法制备蟾蜍抗菌肽脂质体，以包封率为考察指标，Box-Behnken Design-响应面优化法（BBD-RSM）分析筛选处方，Design Export 8.0.6 Trial软件进行回归分析得出最优处方，透皮吸收实验验证蟾蜍抗菌肽脂质体吸收情况，溶出性抗菌产品抑菌性能试验测定抗菌效果。结果 通过响应面法优化的蟾蜍抗菌肽脂质体最佳处方为：磷脂含量为40 mg，磷脂与胆固醇比例为4∶1，脂药比为4∶1，最佳条件下制备的蟾蜍抗菌肽脂质体的药物包封率为（79.14±0.5）%；透皮吸收实验结果显示，在12 h时，表面存留率为94%，提高了蟾蜍抗菌肽的安全稳定性；抗菌结果表明，蟾蜍抗菌肽脂质体有效地延长了蟾蜍抗菌肽的药效时间。结论 改良后的蟾蜍抗菌肽剂型有效地提高了药效时间及安全稳定性。Abstract: OBJECTIVE To optimize the preparation of the toad antibacterial peptide liposomes， to prolong its antibacterial effect and improve its safety and stability. METHODS The toad antibacterial peptide was extracted by water extraction method， and the liposomes were prepared by thin-film dispersion. The Box-Behnken Design-response surface optimization method (BBD-RSM) was applied to analyze and screen the prescription， in which the encapsulation efficiency was used as an index. Design Export 8.0.6 Trial software was used to conduct experimental regression analysis to obtain the optimal prescription. Transdermal absorption experiments were used to verify the absorption of liposome. The antibacterial effect was determinated by dissolution inhibition test. RESULTS The optimal parameters for preparing the toad antibacterial peptide liposomes was that the mass of phospholipid was 40 mg， the ratio of phospholipid and cholesterol was 4∶1， the ratio of lipid phase to drug was 4∶1. And the highest encapsulation efficiency of the toad antibacterial peptide was (79.14±0.5)%. After 12 h， their surface retention rate were appropriate 94.0%， possessing high surface retention， which improved the safety and stability of the antibacterial. The antibacterial results showed that the antibacterial time was effectively prolonged by antibacterial peptide liposomes. CONCLUSION The antibacterial effect is effectively improved and the antibacterial time is effectively prolonged by toad antibacterial peptide liposomes.
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