Folate-conjugated liposomes target and deliver therapeutics to immune cells in a rat model of rheumatoid arthritis

Nanomedicine (Lond). 2017 Oct;12(20):2441-2451. doi: 10.2217/nnm-2017-0166. Epub 2017 Sep 20.

Abstract

Aim: We endeavored to create a folate-targeted liposome (Fol-liposome) that could selectively target areas of inflammation.

Materials & methods: Fol-liposomes were prepared with encapsulated DiD fluorophore or betamethasone (BM) to image and treat an adjuvant-induced rat model of rheumatoid arthritis.

Results: Fol-liposomes selectively accumulated in arthritic rat paws to a greater extent than nontargeted liposomes. When these Fol-liposomes were used to encapsulate BM and administered to arthritic rats, animals exhibited less paw swelling, lower arthritis scores, a reduction in bone erosion, less splenomegaly and better maintenance of body weight when compared with nontreated or nontargeted BM-containing liposome groups.

Conclusion: Fol-liposomes can selectively deliver imaging and therapeutic agents to sites of inflammation in a rat model of rheumatoid arthritis.

Keywords: activated macrophages; arthritis; folate liposome; folate receptor; folate targeting; inflammatory disease; liposome.

MeSH terms

  • Adjuvants, Immunologic / metabolism
  • Animals
  • Arthritis, Experimental / drug therapy
  • Arthritis, Experimental / immunology
  • Arthritis, Experimental / pathology
  • Arthritis, Rheumatoid / drug therapy*
  • Arthritis, Rheumatoid / immunology
  • Arthritis, Rheumatoid / pathology
  • Drug Liberation
  • Female
  • Fluorescent Dyes / chemistry
  • Folic Acid / chemistry*
  • Folic Acid / metabolism*
  • Folic Acid Transporters / metabolism
  • Inflammation / drug therapy
  • Liposomes / chemistry*
  • Macrophages
  • Molecular Targeted Therapy / methods*
  • Optical Imaging / methods
  • Particle Size
  • Rats
  • Rats, Inbred Lew
  • Surface Properties

Substances

  • Adjuvants, Immunologic
  • Fluorescent Dyes
  • Folic Acid Transporters
  • Liposomes
  • Folic Acid