Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, China.
Int J Pharm. 2012 Dec 15;439(1-2):307-16. doi: 10.1016/j.ijpharm.2012.09.017. Epub 2012 Sep 16.
Highly efficient nanomedicines were successfully fabricated by the indomethacin (IND) directed self-assembly of β-cyclodextrin (β-CD)-conjugated polyethyleneimine (PEI-CD), taking advantage of the multiple interactions between drug and polymer. These nanoscaled assemblies exhibited spherical shape and positively charged surface. Compared with the commercial tablet, the relative oral bioavailability of IND-nanomedicines was significantly enhanced. Evaluation based on either carrageenan-induced paw edema or complete Freund's adjuvant (CFA)-induced arthritis suggested the newly developed nanomedicines were more effective than raw IND or IND tablet in terms of prophylactic effect and therapeutic activity. Even the low dose of nanomedicines offered the comparable results to those of control groups at the high dosage in most cases. Moreover, the nanoformulation exhibited ameliorated gastrointestinal stimulation. All these positive results indicated that this type of nanomedicines might serve as a highly efficient and effective delivery nanoplatform for the oral delivery of water-insoluble therapeutics.
高效的纳米药物是通过吲哚美辛(IND)引导的β-环糊精(β-CD)-接枝聚乙烯亚胺(PEI-CD)的自组装成功制备的,利用药物和聚合物之间的多种相互作用。这些纳米级组装体呈现球形和带正电荷的表面。与商业片剂相比,IND-纳米药物的相对口服生物利用度显著提高。基于角叉菜胶诱导的足肿胀或完全弗氏佐剂(CFA)诱导的关节炎的评估表明,与原料药 IND 或 IND 片剂相比,新开发的纳米药物在预防效果和治疗活性方面更有效。即使在大多数情况下,纳米药物的低剂量也能提供与对照组高剂量相当的结果。此外,该纳米制剂显示出改善的胃肠道刺激。所有这些积极的结果表明,这种类型的纳米药物可能作为一种高效、有效的水不溶性治疗药物口服递药的纳米载体。