The efficacy of alginate-glycyl-prednisolone conjugate nanogel (AL-GP-NG) was previously reported to be better than that of prednisolone (PD) alone in arthritic rats. In the present study, novel AL-GP-NG was prepared and its targeting potential was investigated. AL-GP-NG with a PD content of 6.3% (w/w) was obtained and had a slightly larger submicron size and similar zeta potential to that of the previous nanogel. Drug release profiles and pharmacokinetic features were similar to those of the previous nanogel. AL-GP-NG showed prolonged release at weakly acidic and neutral pH and the good systemic retention of total (free + conjugated) PD after an intravenous (i.v.) injection in rats. In animal studies using normal and adjuvant-induced arthritic rats, the distribution of total PD was examined after an i.v. injection. AL-GP-NG achieved a markedly higher drug concentration at inflamed joints than PD alone. Furthermore, ALGP-NG showed specific drug localisation to inflamed joints in arthritic rats, but not in normal rats. Furthermore, specific drug localisation to the joints by AL-GP-NG persisted. Collectively, these results demonstrated the good targeting potential of AL-GP-NG to inflamed joints, suggesting its suitability for the treatment of arthritis.
Keywords: Alginate-glycyl-prednisolone conjugate nanogel; arthritis; drug localisation; inflamed joint; targeting potential.