<br>负载银杏内酯的大豆磷脂稳定的纳米混悬剂具有改善的储存稳定性和体内生物利用度。,Colloids and Surfaces B: Biointerfaces

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负载银杏内酯的大豆磷脂稳定的纳米混悬剂具有改善的储存稳定性和体内生物利用度。
Colloids and Surfaces B: Biointerfaces ( IF 5.4 ) Pub Date : 2019-06-24 , DOI: 10.1016/j.colsurfb.2019.06.050
Puxiu Wang ₁ , Xiuxiu Cao ₂ , Yang Chu ₁ , Puxiu Wang ₁

Affiliation

本研究的目的是研究大豆磷脂作为空间稳定剂对提高银杏内酯溶出度、储存稳定性和生物利用度的影响。将银杏内酯粗粉、羟丙基甲基纤维素(HPMC)、大豆磷脂和十二烷基硫酸钠(SDS)混合并湿磨制备纳米混悬剂S1。除添加大豆磷脂外，采用相同的方法得到纳米混悬剂S2。粒径结果显示，S1的粒径（D50）从44.25μm显着降低至0.373μm。差示扫描量热法（DSC）、粉末X射线衍射（PXRD）和透射电子显微镜（TEM）结果表明，纳米混悬剂中的银杏内酯仍保持结晶度，纳米粒子均接近圆形且分散均匀。然后，通过将S1和S2分别分层到微晶纤维素(MCC)球体上来制备粒料F1和F2。银杏内酯A（GA）和银杏内酯B（GB）在F1中的溶出率在30分钟内分别为98.3%和97.7%。远高于F2（89.0%和86.5%）和银杏内酯粗粉（22.3%和24.6%）。从稳定性测试结果来看，F1的储存稳定性较F2有所提高。此外，与银杏内酯粗粉相比，F1中GA和GB的相对生物利用度分别高达(221.84±106.67)%和(437.45±336.43)%。上述结果表明，纳米混悬剂中添加大豆磷脂对于提高药物溶出度、储存稳定性和体内生物利用度具有重要作用：（1）两亲性大豆磷脂与药物相互作用，疏水部分吸附在纳米混悬剂表面。难溶性药物和暴露于水介质的亲水部分。这增加了纳米颗粒的润湿性，从而确保了药物颗粒良好的再分散性。 (2)它可以自组装形成界面磷脂膜，包围单个纳米颗粒，产生足够的空间位阻，防止纳米颗粒聚集并保证快速溶解速率。 (3)大豆磷脂及其水解物在体内与胆汁盐形成强胶束增溶载体，刺激银杏内酯的吸收过程。因此，大豆磷脂是纳米混悬给药系统中一种有前途的空间稳定剂。

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Ginkgolides-loaded soybean phospholipid-stabilized nanosuspension with improved storage stability and in vivo bioavailability.

The purpose of this study was to investigate the effects of soybean phospholipid, as a steric stabilizer, on improving dissolution rate, storage stability and bioavailability of ginkgolides. The ginkgolides coarse powder, hydroxypropyl methylcellulose (HPMC), soybean phospholipid and sodium dodecyl sulfate (SDS) were mixed and wet-milled to prepare nanosuspension S1. Nanosuspension S2 was obtained by the same technique except adding the soybean phospholipid. Results of particle size showed that particle size (D50) of S1 significantly decreased from 44.25 μm to 0.373 μm. Results of differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and transmission electron microscope (TEM) showed that ginkgolides in nanosuspension still maintained its crystallinity, and the nanoparticles were all nearly circular and uniformly dispersed. Then, pellets F1 and F2 were prepared by layering S1 and S2 onto the microcrystalline cellulose (MCC) spheres, respectively. The dissolution rate of ginkgolide A (GA) and ginkgolide B (GB) in F1 was 98.3% and 97.7% in 30 min, respectively. It was much higher than F2 (89.0% and 86.5%) and coarse powder of ginkgolides (22.3% and 24.6%). According to the results of stability test, the storage stability of F1 was improved compared with F2. In addition, compared with coarse powder of ginkgolides, the relative bioavailability of GA and GB in F1 were up to (221.84 ± 106.67) % and (437.45 ± 336.43) %, respectively. The above results demonstrated that soybean phospholipid added to the nanosuspension played an important role in improving drug dissolution rate, storage stability and in vivo bioavailability: (1) The amphiphilic soybean phospholipid interacted with the drug, with the hydrophobic part adsorbed on the surface of the poorly soluble drug and the hydrophilic part exposed to the aqueous medium. This increases the wettability of the nanoparticles, which ensure a good redispersibility of the drug particles. (2) It could self-assemble to form an interfacial phospholipid film by surrounding the individual nanoparticles, which can produce enough steric hindrance to prevent nanoparticles from aggregation and ensure a rapid dissolution rate. (3) Soybean phospholipid and its hydrolysate formed strong micellar solubilizing vehicles with bile salts in vivo, stimulated the absorption process of ginkgolides. Thus, soybean phospholipid was a promising steric stabilizer in nanosuspension drug delivery system.

更新日期：2019-06-24

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