Novel approaches circumventing blood-ocular barriers in systemic drug delivery are lacking. We hypothesize receptor-mediated delivery of curcumin (CUR) across intestinal and ocular barriers leads to decreased inflammation in a model of lens-induced uveitis. CUR was encapsulated in double-headed polyester nanoparticles using gambogic acid (GA)–coupled polylactide-co-glycolide (PLGA). Orally administered PLGA-GA2-CUR led to notable aqueous humor CUR levels and was dosed (10 mg/kg twice daily) to adult male beagles (n = 8 eyes) with induced ocular inflammation. Eyes were evaluated using a semiquantitative preclinical ocular toxicology scoring (SPOTS) and compared to commercial anti-inflammatory treatment (oral carprofen 2.2 mg/kg twice daily) (n = 8) and untreated controls (n = 8). PLGA-GA2-CUR offered improved protection compared with untreated controls and similar protection compared with carprofen, with reduced aqueous flare, miosis, and chemosis in the acute phase (<4 hours). This study highlights the potential of PLGA-GA2 nanoparticles for systemic drug delivery across ocular barriers.

The present study aimed to investigate the potential anti-inflammatory and anti-nociceptive activities of glycyrrhizin (GL) in mice and to explore the possible related mechanisms. Xylene-induced ear edema, carrageenan-induced paw edema and acetic acid-induced vascular permeability test were used to investigate the anti-inflammatory activities of GL in mice. Anti-nociceptive effects of GL were assessed by using acetic acid-induced writhing, hot plate test and formalin test, as well as evaluation of spontaneous locomotor activity and motor performance. The mRNA expression of pro-inflammatory cytokines (such as TNF-α, IL-6 and iNOS) and the protein expression of cyclooxygenase-2 (COX-2) were explored by using real-time fluorogenic PCR and Western blot, respectively. The results showed that GL significantly reduced xylene-induced ear edema, carrageenan-induced paw edema, and acetic acid-induced vascular permeation. Additionally, GL significantly inhibited the nociceptions induced by acetic acid and formalin. However, the nociceptions could not be decreased by GL in the hot plate test, and GL did not affect spontaneous locomotor activity and motor performance. The expression levels of TNF-α, IL-6, iNOS and COX-2 were significantly downregulated by GL. In conclusion, GL exerts significant anti-inflammatory and analgesic activities by attenuating the expression levels of TNF-α, IL-6, iNOS and COX-2.

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This study was to investigate the anti-inflammatory and anti-nociceptive activities of indigo in mice and to explore the possible related mechanisms. Xylene-induced ear edema, carrageenan-induced paw edema and acetic acid-induced...