PH-sensitive liposomes for colonic co-delivery of mesalazine and curcumin for the treatment of ulcerative colitis

Abstract

The ineffectiveness of the current management of ulcerative colitis (UC) demands novel pharmaceutical techniques and advance therapeutic strategies to facilitate safe and efficacious treatment of the disease. In this quest, mesalazine (MZ), a 5-aminosalicylate with anti-inflammatory and potent antioxidant activities, along with curcumin (CM), a natural anti-inflammatory and antioxidant polyphenol, were found to produce a synergistic efficacy to efficiently alleviate UC. In the present study, we have formulated pH-sensitive liposomes (LS) containing a low-dose combination of MZ and CM as a potential therapy for UC. It was hypothesized that the synergistic action of the two drugs, pH-dependent colon-specific delivery, and use of LS as a nano-technological drug carrier system could diminish drug-associated side effects, reduce the dose and provide effective treatment strategy for UC. The guinea pig model of UC was used to evaluate the in vivo efficacy of pH sensitive MZ-CM co-loaded LS and found to be more efficacious than single-drug LS or drug solution. Furthermore, both drugs exhibited high antioxidant activity and mitigated the oxidative stress present along UC; resulting in an effective treatment of UC. In conclusion, eudragit-S100 coated MZ-CM liposomes is a promising treatment strategy for the effective oral therapy of UC.