79 0

Enhanced anti-rheumatic activity of methotrexate-entrapped ultradeformable liposomal gel in adjuvant-induced arthritis rat model

Title
Enhanced anti-rheumatic activity of methotrexate-entrapped ultradeformable liposomal gel in adjuvant-induced arthritis rat model
Author
배옥남
Keywords
Methotrexate; Ultradeformable liposomes; Rheumatoid arthritis; Transdermal delivery; Complete Freund's adjuvant; Inflammation; SOLID LIPID NANOPARTICLES; FOLATE-TARGETED NANOPARTICLES; RHEUMATOID-ARTHRITIS; IN-VIVO; TRANSDERMAL DELIVERY; SKIN DELIVERY; INFLAMMATORY CYTOKINE; POTENTIAL TREATMENT; TOPICAL DELIVERY; DRUG CARRIERS
Issue Date
2017-06
Publisher
ELSEVIER SCIENCE BV
Citation
INTERNATIONAL JOURNAL OF PHARMACEUTICS, v. 525, No. 1, Page. 92-100
Abstract
The aim of this study is to investigate in vivo anti-rheumatic activity of methotrexate-entrapped ultradeformable liposomal gel (MTX-UDLs-gel) in adjuvant-induced arthritis rat model. Methotrexate-entrapped ultradeformable liposomes (MTX-UDLs) with the optimal phosphatidylcholine to Tween 80 ratio (7:3, w/w) were incorporated into 1% Carbopol gel. MTX-UDLs-gel was characterized in terms of appearance, clarity, homogeneity, pH and drug content. The permeation of MTX-UDLs-gel across rat skin was investigated using Franz diffusion cell. In vivo anti-rheumatic activity of MTX-UDLs-gel was assessed in terms of edema volume, paw edema and leukocyte infiltration scores, histopathological analysis and inflammatory cytokines level in complete Freund's adjuvant (CFA)-induced arthritis rat model. MTX-UDLs- gel showed good homogeneity and clarity, neutral pH and about 99.5% drug content. The cumulative amount of MTX permeated for 24 h from MTX-UDLs-gel (164.6 mu g) was 1.5 and 2.15 times higher than that of MTX-CLs-gel (113.3 mu g) and MTX-plain-gel (76.6 mu g), respectively. MTX-UDLs-gel significantly alleviated the severity of inflammation by reducing edema volume, histological scores and accumulation of neutrophils and improving tissue architecture in CFA-induced arthritis rat model. MTXUDLs- gel effectively suppressed the expression of pro-inflammatory cytokines, TNF-alpha and IL-beta, in paw tissues. In conclusion, the developed MTX-UDLs-gel has a great potential for effective delivery of MTX into the inflamed joints in rheumatoid arthritis. (C) 2017 Elsevier B.V. All rights reserved.
URI
https://www.sciencedirect.com/science/article/pii/S0378517317303228http://repository.hanyang.ac.kr/handle/20.500.11754/72161
ISSN
0378-5173; 1873-3476
DOI
10.1016/j.ijpharm.2017.04.032
Appears in Collections:
COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE