title: Assembled nanomedicines as efficient and safe therapeutics for articular inflammation.
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.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, Third Military Medical University, Chongqing 400038, China.
authors.forename: Ling
authors.initials: L
authors.lastname: Che
authors.forename: Jianzhi
authors.initials: J
authors.lastname: Zhou
authors.forename: Shuhui
authors.initials: S
authors.lastname: Li
authors.forename: Hongmei
authors.initials: H
authors.lastname: He
authors.forename: Yuxuan
authors.initials: Y
authors.lastname: Zhu
authors.forename: Xing
authors.initials: X
authors.lastname: Zhou
authors.forename: Yi
authors.initials: Y
authors.lastname: Jia
authors.forename: Yao
authors.initials: Y
authors.lastname: Liu
authors.forename: Jianxiang
authors.initials: J
authors.lastname: Zhang
authors.forename: Xiaohui
authors.initials: X
authors.lastname: Li
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D001169:Arthritis, Experimental / Q000188:drug therapy* / Q000473:pathology; D002351:Carrageenan; D005620:Freund's Adjuvant; D007213:Indomethacin / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D007249:Inflammation / Q000139:chemically induced* / Q000188:drug therapy / Q000473:pathology; D007422:Intestines / Q000187:drug effects / Q000473:pathology; D008297:Male; D049329:Nanostructures / Q000008:administration & dosage* / Q000737:chemistry; D036103:Nanotechnology; D011094:Polyethyleneimine / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013270:Stomach / Q000187:drug effects / Q000473:pathology; D014018:Tissue Distribution; D047392:beta-Cyclodextrins / Q000737:chemistry
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D047392:beta-Cyclodextrins; D002351:Carrageenan; D011094:Polyethyleneimine; D005620:Freund's Adjuvant; C031215:betadex; D007213:Indomethacin