Assembled nanomedicines as efficient and safe therapeutics for articular inflammation

Int J Pharm. 2012 Dec 15;439(1-2):307-16. doi: 10.1016/j.ijpharm.2012.09.017. Epub 2012 Sep 16.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Arthritis, Experimental / drug therapy*
  • Arthritis, Experimental / pathology
  • Carrageenan
  • Freund's Adjuvant
  • Indomethacin / administration & dosage*
  • Indomethacin / chemistry
  • Indomethacin / pharmacokinetics
  • Inflammation / chemically induced*
  • Inflammation / drug therapy
  • Inflammation / pathology
  • Intestines / drug effects
  • Intestines / pathology
  • Male
  • Nanostructures / administration & dosage*
  • Nanostructures / chemistry
  • Nanotechnology
  • Polyethyleneimine / chemistry
  • Rats
  • Rats, Sprague-Dawley
  • Stomach / drug effects
  • Stomach / pathology
  • Tissue Distribution
  • beta-Cyclodextrins / chemistry

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • beta-Cyclodextrins
  • Carrageenan
  • Polyethyleneimine
  • Freund's Adjuvant
  • betadex
  • Indomethacin