Zhang Yanzhuo, Zhao Qinfu, Zhu Wufu, Zhang Lihua, Han Jin, Lin Qisi, Ai Fengwei
Jiangsu Key Laboratory of New Drug Research and Clinical Pharmacy, Xuzhou Medical College, P.O. Box 62, No. 209, Tongshan Road, Xuzhou, 221004, China,
Pharm Res. 2015 Jul;32(7):2372-83. doi: 10.1007/s11095-015-1630-5. Epub 2015 Jan 22.
A novel mesoporous carbon/lipid bilayer nanocomposite (MCLN) with a core-shell structure was synthesized and characterized as an oral drug delivery system for poorly water-soluble drugs. The objective of this study was to investigate the potential of MCLN-based formulation to modulate the in vitro release and in vivo absorption of a model drug, nimodipine (NIM).
NIM-loaded MCLN was prepared by a procedure involving a combination of thin-film hydration and lyophilization. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), specific surface area analysis, differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were employed to characterize the NIM-loaded MCLN formulation. The effect of MCLN on cell viability was assessed using the MTT assay. In addition, the oral bioavailability of NIM-loaded MCLN in beagle dogs was compared with that of the immediate-release formulation, Nimotop®.
Our results demonstrate that the NIM-loaded MCLN formulation exhibited a typical sustained release pattern. The NIM-loaded MCLN formulation achieved a greater degree of absorption and longer lasting plasma drug levels compared with the commercial formulation. The relative bioavailability of NIM for NIM-loaded MCLN was 214%. MCLN exhibited negligible toxicity.
The data reported herein suggest that the MCLN matrix is a promising carrier for controlling the drug release rate and improving the oral absorption of poorly water-soluble drugs.
合成了一种具有核壳结构的新型介孔碳/脂质双层纳米复合材料（MCLN），并将其表征为用于难溶性药物的口服给药系统。本研究的目的是研究基于MCLN的制剂调节模型药物尼莫地平（NIM）体外释放和体内吸收的潜力。
通过薄膜水化和冻干相结合的方法制备了载NIM的MCLN。采用扫描电子显微镜（SEM）、透射电子显微镜（TEM）、比表面积分析、差示扫描量热法（DSC）和X射线衍射（XRD）对载NIM的MCLN制剂进行表征。使用MTT法评估MCLN对细胞活力的影响。此外，将载NIM的MCLN在比格犬体内的口服生物利用度与速释制剂尼莫通®进行了比较。
我们的结果表明，载NIM的MCLN制剂呈现出典型的缓释模式。与市售制剂相比，载NIM的MCLN制剂实现了更高程度的吸收和更长时间的血浆药物水平。载NIM的MCLN中NIM的相对生物利用度为214%。MCLN表现出可忽略不计的毒性。
本文报道的数据表明，MCLN基质是一种有前景的载体，可用于控制药物释放速率并改善难溶性药物的口服吸收。
