Surface Functionalization of Piperine-Loaded Liposomes with Sophorolipids Improves Drug Loading and Stability
Surface Functionalization of Piperine-Loaded Liposomes with Sophorolipids Improves Drug Loading and Stability
复制标题
槐糖脂负载胡椒碱的脂质体的表面功能化提高了药物负载量和稳定性
DOI：
10.1007/s12247-022-09687-1
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发表时间：
2022-09-28
影响因子：
2.6
通讯作者：
Zhang, Qianyu
中科院分区：
文献类型：
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作者：
Chen, Huali;Zhang, Qianyu
目的近年来，两亲性生物表面活性剂在药物释放系统中的应用引起了人们的兴趣。在这项研究中，胡椒碱负载脂质体与生物表面活性剂槐脂修饰，以更好地稳定和分散的脂质体制剂和性能的脂质体进行了evaluated.MethodsSophorolipid修饰的脂质体制备和胡椒碱的粒径和包封率（EEs）进行了测定。还分别在血清中、在4 °C储存下以及在各种NaCl浓度和pH条件下评价脂质体的稳定性。胡椒碱的体外释放曲线也investigated.ResultsSophorolipids帮助稳定和分散脂质体证明了由粒径减小，降低的PDI，并增加血清稳定性后，此外。它们还提高了胡椒碱进入脂质体的EE，并在4 °C储存期间稳定了装载胡椒碱的脂质体。在高NaCl浓度以及各种pH条件下，槐脂修饰的脂质体在粒径和EE方面表现出良好的体外稳定性。槐脂功能化的胡椒碱加载的脂质体也表现出持续的体外药物释放profiles.ConclusionThis初步研究验证了接枝脂质体与两亲性生物表面活性剂槐脂制剂稳定的可行性，证明其适用于改善脂质体载量的疏水性营养品，如胡椒碱。
PurposeThe application of amphiphilic biosurfactants in drug delivery systems has sparked interest in recent years. In this study, piperine-loaded liposomes were modified with the biosurfactant sophorolipids to better stabilize and disperse the liposomal formulation and the properties of the liposomes were evaluated.MethodsSophorolipid-modified liposomes were prepared and the particle sizes and entrapment efficiencies (EEs) of piperine were measured. The stability of liposomes was also evaluated in serum, under 4 °C storage and under various NaCl concentrations and pH conditions respectively. The in vitro release profile of piperine was also investigated.ResultsSophorolipids helped stabilize and disperse liposomes as evidenced by the decreased particle sizes, lowered PDIs, and increased serum stability after the addition. They also elevated the EEs of piperine into liposomes and stabilized piperine-loaded liposomes during 4 °C storage. Under high NaCl concentrations as well as various pH conditions, sophorolipid-modified liposomes showed favorable in vitro stability in terms of particle sizes and EEs. Sophorolipid-functionalized piperine-loaded liposomes also exhibited sustained in vitro drug release profiles.ConclusionThis preliminary study validated the feasibility of grafting liposomes with amphiphile biosurfactant sophorolipids for formulation stabilization, demonstrating their applicability in improving the liposomal loading of hydrophobic nutraceuticals such as piperine.