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IL-1Ra and its Delivery Strategies: Inserting the Association in Perspective

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Abstract

Interleukin-1 receptor antagonist (IL-1Ra) is a naturally occurring anti-inflammatory antagonist of interleukin-1 family of pro-inflammatory cytokines. The broad spectrum anti-inflammatory effects of IL-1Ra have been investigated against various auto-immune diseases such as diabetes mellitus, rheumatoid arthritis. Despite of its outstanding broad spectrum anti-inflammatory effects, IL-1Ra has short biological half-life (4–6 h) and to cope with this problem, up till now, many delivery strategies have been applied either to extend the half-life and/or prolong the steady-state sustained release of IL-1Ra from its target site. Here in our present paper, we have provided an overview of all approaches attempted to prolong the duration of therapeutic effects of IL-1Ra either by fusing IL-1Ra using fusion protein technology to extend the half-life and/or development of new dosage forms using various biodegradable polymers to prolong its steady-state sustained release at the site of administration. These approaches have been characterized by their intended impact on either in vitro release characteristics and/or pharmacokinetic and pharmacodynamic parameters of IL-1Ra. We have also compared these delivery strategies with each other on the basis of bioactivity of IL-1Ra after fusion with fusion protein partner and/or encapsulation with biodegradable polymer.

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Abbreviations

AlbudAbs:

Albumin binding human binding domain antibodies

ELP:

Elastin-like peptide

HSA:

Human serum albumin

IL-1Ra:

Interleukin-1 Receptor antagonist

PF127:

Pluronic F127

PLGA:

Poly-lactic-co-glycolic acid

RFVP:

Amino acid residues of Streptococcus gordonii

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Acknowledgments and Disclosures

Authors would like to acknowledge China Scholarship Council to award scholarships for PhDs to Muhammad Sajid Hamid Akash and Kanwal Rehman. One of the authors would like to acknowledge his wife Mrs. Akash for her support in this article. Without her, the writing of this article would not have been possible. Authors declare that they do not have any conflict of interest for this article.

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  1. Institute of Pharmacology, Toxicology and Biochemical Pharmaceutics College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China

    Muhammad Sajid Hamid Akash, Kanwal Rehman & Shuqing Chen

  2. College of Pharmacy, Government College University Faisalabad, Faisalabad, Pakistan

    Muhammad Sajid Hamid Akash

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  1. Muhammad Sajid Hamid Akash
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  2. Kanwal Rehman
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  3. Shuqing Chen
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Correspondence to Muhammad Sajid Hamid Akash or Shuqing Chen.

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Akash, M.S.H., Rehman, K. & Chen, S. IL-1Ra and its Delivery Strategies: Inserting the Association in Perspective. Pharm Res 30, 2951–2966 (2013). https://doi.org/10.1007/s11095-013-1118-0

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