Fail-safe nano-formulation of prodrug of sulfapyridine: Preparation and evaluation for treatment of rheumatoid arthritis.

Abstract

Aim of the present study was to give a second life to the long-abandoned drug, sulfapyridine (SP) for its anti-arthritic potential by design of nano-vesicular delivery system. For this, intra-articular delivery of its liposomal formulation was tried. As the prepared formulation exhibited rapid drug leakage, an arthritis responsive prodrug of SP showing lability towards synovial enzymes was synthesized to exploit the over-expression of arthritis specific enzymes. Prodrug (SP-PD) exhibited better retention in liposomes as compared to the drug, preventing its escape from synovium. Hydrolysis of SP-PD in human plasma and synovial fluid indicated its high susceptibility to enzymes. The liposomes of SP-PD exhibited larger mean size, less PDI and higher zeta potential as compared to those for SP liposomes. In arthritic rats, prodrug liposomes were found to reverse the symptoms of inflammation, including the levels of biochemical markers. Liposomes of bio-responsive prodrug, therefore, offer a revolutionary approach in the treatment of rheumatoid arthritis.

• Authors: Bhupinder Kapoor, Monica Gulati, Sachin K Singh, Gopal L Khatik, Reena Gupta, Rakesh Kumar, Rajan Kumar, K Gowthamarajan, Sanjeev Mahajan, Som Gupta
• Journal: Materials science & engineering. C, Materials for biological applications (Mater Sci Eng C Mater Biol Appl) Vol. 118 Pg. 111332 (Jan 2021) ISSN: 1873-0191 [Electronic] Netherlands
• PMID: 33254964 (Publication Type: Journal Article)
• Copyright: Copyright © 2020 Elsevier B.V. All rights reserved.

Chemical References

• Liposomes
• Prodrugs
• Sulfapyridine

Topics

• Animals
• Arthritis, Rheumatoid (drug therapy)
• Liposomes
• Prodrugs (pharmacology)
• Rats
• Sulfapyridine
• Synovial Membrane