Sustained-Release Curcumin Microparticles for Effective Prophylactic Treatment of Exocrine Dysfunction of Pancreas: A Preclinical Study on Cerulein-Induced Acute Pancreatitis

被引:26
作者
Anchi, Pratibha [1 ]
Khurana, Amit [1 ]
Swain, Debasish [2 ]
Samanthula, Gananadhamu [2 ]
Godugu, Chandraiah [1 ]
机构
[1] Natl Inst Pharmaceut Educ & Res, Dept Regulatory Toxicol, Hyderabad 500037, Telangana, India
[2] Natl Inst Pharmaceut Educ & Res, Dept Pharmaceut Anal, Hyderabad 500037, Telangana, India
关键词
acute pancreatitis; cerulein; curcumin microparticles; oxidative stress; sustained release; NF-KAPPA-B; OXIDATIVE STRESS; DIETARY CURCUMIN; NANOPARTICLES; BIOAVAILABILITY; PROGRESSION; ACTIVATION; MECHANISMS; INHIBITION; LUNG;
D O I
10.1016/j.xphs.2018.07.009
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
Acute pancreatitis (AP) is a serious inflammatory disorder of the pancreas with considerable mortality. The clinical therapy is hampered due to lack of any approved drug for AP. In this study, we developed curcumin (cur)-loaded poly (lactic-co-glycolic acid) cur microparticles (CuMPs) for sustained release. CuMPs were prepared by emulsion solvent evaporation method and characterized for shape, size, compatibility, and entrapment efficiency. The in vitro drug release and in vivo pharmacokinetic studies confirmed sustained release pattern of cur from CuMPs. The pharmacodynamic study was conducted in cerulein induced AP model. Prophylactic treatment was planned with single dose of CuMPs (equivalent to 7.5 mg/kg of cur) and compared with free cur given orally (100 mg/kg) and intraperitoneally (7.5 mg/kg) daily for 7 days. Interestingly, the effects of CuMPs were superior compared to the free drug administered either orally or intraperitoneally through repeated administrations. CuMPs showed significant decrease of serum amylase and lipase levels, oxidative and nitrosative stress was also significantly decreased. Moreover, CuMPs impressively decreased inflammatory cytokines. Our results may pave a way to propose similar strategy for many of promising natural products to combat several oxidative stressemediated disorders via sustained release microparticle approaches. (c) 2018 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
引用
收藏
页码:2869 / 2882
页数:14
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