Research Articles

2019  |  Vol: 5(3)  |  Issue: 3 (May- June)  |  https://doi.org/10.31024/ajpp.2019.5.3.10
Chondroitin sulphate mediated targeted delivery of methotrexate and aceclofenac to the joints for effective management of rheumatoid arthritis

Satish Shilpi*, Shikha Upadhaye, Roshni Shivvedi, Ekta Gurnany, Pranali Chimaniya, Amrita Singh, Megha Chouhan, Shikha Jain, Sunil K. Yagnik, Kapil Khatri

Pharmaceutics Research Laboratory, Department of Pharmaceutics, Ravishankar College of Pharmacy, Bhopal, MP, India

*Address for Corresponding Authors:

Dr. Satish Shilpi

Pharmaceutics Research Laboratory,

Department of Pharmaceutics, Ravishankar College of Pharmacy, Bhopal, MP, India

Abstract

Objective: Rheumatoid arthritis (RA) is an autoimmune disease in which immune system of body mistakenly attacks the joints. This creates inflammation and severe pain around the joints due to thickening or degeneration of synovial fluid. Frequent high dosing of drug may precipitate side effect.  Purpose of this work was site specific and simultaneously delivery of methotrexate and aceclofenac by chondroitin sulphate conjugated lipid nanocarrier i.e. solid lipid nanoparticles (SLNs) for the effective management of RA. Method and Material: The SLNs were prepared by solvent injection method and further they were surface engineered with Chondroitin sulphate. They were further characterized for size and its size distribution, shape and surface morphology, zeta potential, % entrapment efficiency and in vitro drug release profile. Anti-inflammatory activity and in vivo performance was also predicted. Result: The particle size of the unconjugated SLNs and chondroitin sulphate conjugated-SLNs (CS-SLNs) were found to be 127.9 ± 5.3 nm and 131.2 ± 4.6 nm, respectively. SLNs showed matrix diffusion sustained drug release pattern. In vitro aceclofenac release was found 61.35 ± 1.08% and 58.97 ± 2.30%  and release of methotrexate was found to be 58.08 ± 0.93% and 56.18 ± 1.27 in 24 h for chondroitin uncoupled and coupled SLNs. Conclusion: Highest uptake of SLNs by the knee joint due to highly expressed receptors associated with chondroitin sulphate. Targeting efficiency of prepared chondroitin sulphate conjugated lipidic nanoparticles were potential nanocarrier for the effective management of RA.

Keywords: Rheumatoid arthritis, SLNs, Chondroitin sulphate, immunosuppressant

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