Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, Shenyang 110016, PR China.
Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, Shenyang 110016, PR China.
J Colloid Interface Sci. 2018 Feb 1;511:57-66. doi: 10.1016/j.jcis.2017.09.088. Epub 2017 Sep 23.
In this manuscript, the effect of the particle size of polymer-functionalized mesoporous carbon (MPP) nanoparticles on enhancing oral absorption of a water-insoluble drug is first investigated. The insoluble drug, fenofibrate (Fen), was selected as the model drug loaded in the MPP nanoparticles. MPP nanoparticles with different particle sizes were designed for improving the oral bioavailability of drugs, in which the branched polyethyleneimine (PEI) and polyacrylic acid (PAA) were modified on the surfaces of mesoporous carbon nanoparticles (MCNs) with amide bonds. In addition, PEI-functionalized carbon quantum dots (PCA) and radioisotope I were applied to label the MPP nanoparticles to trace in the vivo process. According to the data, the MPP nanoparticles could markedly improve the dissolution rate and oral bioavailability of Fen. Interestingly, the MPP nanoparticle size had a notable effect on Fen oral absorption, and intermediate sized MPP nanoparticles were expected to be more ideal oral drug carriers. The nanoparticles were safe and easily excreted. These findings present the prospect of MPP nanoparticles for oral application, and guides the rational design of an oral delivery system with respect to particle size.
本文首次研究了聚合物功能化介孔碳（MPP）纳米粒子的粒径对提高水不溶性药物口服吸收的影响。将难溶性药物非诺贝特（Fen）作为模型药物负载在 MPP 纳米粒子中。设计了具有不同粒径的 MPP 纳米粒子以提高药物的口服生物利用度，其中支化聚乙烯亚胺（PEI）和聚丙烯酸（PAA）通过酰胺键修饰在介孔碳纳米粒子（MCN）的表面。此外，还应用了 PEI 功能化碳量子点（PCA）和放射性同位素 I 对 MPP 纳米粒子进行标记，以追踪体内过程。结果表明，MPP 纳米粒子可以显著提高 Fen 的溶解速率和口服生物利用度。有趣的是，MPP 纳米粒子的粒径对 Fen 的口服吸收有显著影响，中等粒径的 MPP 纳米粒子有望成为更理想的口服药物载体。这些纳米粒子安全且易于排泄。这些发现为 MPP 纳米粒子的口服应用提供了前景，并指导了基于粒径的口服递药系统的合理设计。
