Engineering tenofovir loaded chitosan nanoparticles to maximize microbicide mucoadhesion.
Engineering tenofovir loaded chitosan nanoparticles to maximize microbicide mucoadhesion.
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DOI：
10.1016/j.ejps.2011.06.007
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发表时间：
2011-09-18
影响因子：
4.6
通讯作者：
Youan, Bi-Botti C.
中科院分区：
文献类型：
--
作者：
Meng, Jianing;Sturgis, Timothy F.;Youan, Bi-Botti C.
本研究的目的是设计一种模型抗HIV杀微生物剂（替诺福韦）负载基于壳聚糖的纳米颗粒（NPs）。Box-Behnken设计允许评估制剂变量对分别通过动态光散射和UV光谱分析的NP尺寸和药物包封效率（EE%）的影响。分别通过细胞毒性测定和荧光测定法评估NPs对阴道上皮细胞和卷曲乳杆菌活力及其对猪阴道组织的粘膜粘附的影响。在最佳水相条件下，纳米粒子的粒径为207.97nm，EE%为5.83%。用50%（v/v）乙醇/水作为替代溶剂，这两个响应分别增加到20%和602 nm。中等尺寸（281 nm）和大尺寸（602 nm）纳米粒的药物释放分别符合Higuchi（r2=0.991）和一级释放（r2=0.999）模型。这些NP在48小时内对阴道上皮细胞系和乳杆菌都没有细胞毒性。当纳米颗粒的直径从900 nm减小到188 nm时，粘膜粘附力从6%增加到12%。然而，对于较大尺寸的NP，EE% ×粘膜粘附的组合效应最高。总的来说，大尺寸的，杀菌剂加载壳聚糖纳米颗粒似乎是有前途的纳米药物，用于预防艾滋病毒的传播。
The objective of this study was to engineer a model anti-HIV microbicide (Tenofovir) loaded chitosan based nanoparticles (NPs). Box-Behnken design allowed to assess the influence of formulation variables on the size of NPs and drug encapsulation efficiency (EE%) that were analyzed by dynamic light scattering and UV spectroscopy, respectively. The effect of the NPs on vaginal epithelial cells and Lactobacillus crispatus viability and their mucoadhesion to porcine vaginal tissue were assessed by cytotoxicity assays and fluorimetry, respectively. In the optimal aqueous conditions, the EE% and NPs size was 5.83% and 207.97nm, respectively. With 50% (v/v) ethanol/water as alternative solvent, these two responses increased to 20% and 602 nm, respectively. Drug release from medium (281 nm) and large size (602 nm)-sized NPs fitted the Higuchi (r2=0.991) and first-order release (r2=0.999) models, respectively. These NPs were not cytotoxic to both the vaginal epithelial cell line and Lactobacillus for 48 hours. When the diameter of the NPs decreased from 900 nm to 188 nm, the mucoadhesion increased from 6% to 12%. However, the combinatorial effect of EE% × mucoadhesion for larger size NPs was the highest. Overall, large-size, microbicide loaded chitosan NPs appeared to be promising nanomedicines for the prevention of HIV transmission.
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