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
- 김진기
- 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/S0378517317303228https://repository.hanyang.ac.kr/handle/20.500.11754/72163
- ISSN
- 0378-5173; 1873-3476
- DOI
- 10.1016/j.ijpharm.2017.04.032
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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