Universitas Indonesia Conferences, Asian Federation for Pharmaceutical Sciences (AFPS) 2019

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Preparation and evaluation of elastic liposomes for improved anti-rheumatic agent delivery through skin
Cheol-Ho Lee, Alam Zeb, Yeong-Hwan Choe, Kyoung-Won Kim, Ho-Ik Choi, Jeong-Sook Park, Ok-Nam Bae, Jin-Ki Kim

Last modified: 2019-06-15


Background: MTX is a golden standard anti-rheumatic agent for the treatment of rheumatoid arthritis. Objectives: The aim of this study is to prepare methotrexate-loaded elastic liposomes (MTX-ELs) and to evaluate in vivo anti-rheumatic activity of methotrexate-loaded elastic liposomal gel (MTX-ELs-gel) in adjuvant-induced arthritis rat model. Materials and Methods: MTX-ELs prepared with phosphatidylcholine as a lipid and Tween80 as an edge activator. MTX-ELs were incorporated into 1% Carbopol gel to prepare MTX-ELs-gel. The permeation of MTX-ELs across rat skin was investigated and in vivo anti-rheumatic activity of MTX-ELs was assessed in complete Freund’s adjuvant (CFA)-induced arthritis rat model. Results: The particle size of MTX-ELs was near 100 nm with a narrow size distribu­tion. The deformability of MTX-ELs was 2~5 times greater than that of MTX-CLs. MTX-ELs showed good homogeneity and clarity, neutral pH and 99.5% drug content. The cumulative amount of MTX permeated for 24 h from MTX-ELs was 1.5 and 2.15 times higher than that of MTX-CLs and MTX-plain-gel, respectively. MTX-ELs significantly alleviated the severity of inflammation by reducing edema volume, histological scores and accumulation of neutrophils and improved tissue architecture in CFA-induced arthritis rat model. MTX-ELs effectively suppressed the expression of pro-inflammatory cytokines such as TNF-α and IL-1β in paw tissue. Conclusion: The developed MTX-ELs has a great potential for effective delivery of MTX into the inflamed joints in rheumatoid arthritis.