Ma Tongtong, Wang Lianyan, Wang Dong, Ma Guanghui, Wang Siling
Department of Pharmaceutics, Shenyang Pharmaceutical University, P.O. Box 23, 103 Wenhua Road, Shenhe District, Shenyang, Liaoning 110016, PR China; National Key Laboratory of Biochemical Engineering, PLA Key Laboratory of Biopharmaceutical Production & Formulation Engineering, Institute of Process Engineering, Chinese Academy of Sciences, P.O. Box 353 No. 1 Bei-Er-Tiao Street, Haidian District, Beijing 100190, PR China.
National Key Laboratory of Biochemical Engineering, PLA Key Laboratory of Biopharmaceutical Production & Formulation Engineering, Institute of Process Engineering, Chinese Academy of Sciences, P.O. Box 353 No. 1 Bei-Er-Tiao Street, Haidian District, Beijing 100190, PR China.
Colloids Surf B Biointerfaces. 2014 May 1;117:512-9. doi: 10.1016/j.colsurfb.2014.02.039. Epub 2014 Mar 2.
The main challenge in the oral delivery of protein drugs is to enhance their oral bioavailability. Herein, we report the uniform-sized liposphere prepared by premix membrane emulsification combined with W1/O/W2 double-emulsion method as a potential oral carrier for proteins. The protein-loaded liposphere was composed of a hydrophobic poly (D, L-lactide-co-glycolide) (PLGA) core and the lipid molecules self-assembled at the interface of W1/O and O/W2. During the preparation, the protein structure was effectively maintained. Compared with PLGA microsphere, the liposphere achieved a higher loading capacity (LC, 20.18%), entrapment efficiency (EE, 90.82%) and a lower initial burst (24.73%). Importantly, the lipospheres also showed high transcytotic efficiency with human microfold cell (M cell) model, leading to a potential enhancement of intestinal absorption. This result, together with the above studies supported that the PLGA-lipid liposphere could be a promising platform for enhancing the proteins oral bioavailability.
蛋白质药物口服给药的主要挑战在于提高其口服生物利用度。在此，我们报道了通过预混膜乳化结合W1/O/W2双乳液法制备的尺寸均匀的脂质体，作为蛋白质的潜在口服载体。负载蛋白质的脂质体由疏水性聚（D，L-丙交酯-共-乙交酯）（PLGA）核以及在W1/O和O/W2界面处自组装的脂质分子组成。在制备过程中，蛋白质结构得到有效维持。与PLGA微球相比，脂质体具有更高的载药量（LC，20.18%）、包封率（EE，90.82%）和更低的初始突释（24.73%）。重要的是，脂质体在人微褶细胞（M细胞）模型中也表现出高转胞吞效率，从而有可能增强肠道吸收。这一结果与上述研究共同支持PLGA-脂质脂质体可能是提高蛋白质口服生物利用度的一个有前景的平台。
