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用于将抗菌精油特异性递送至动物肠道的颗粒制剂。

Formulation of Granules for Site-Specific Delivery of an Antimicrobial Essential Oil to the Animal Intestinal Tract.

作者信息

Ma Yin-Hing, Wang Qi, Gong Joshua, Wu Xiao Yu

机构信息

Guelph Food Research Centre, Agriculture and Agri-Food Canada, Guelph, Ontario, Canada N1G 5C9; Advanced Pharmaceutics and Drug Delivery Laboratory, Leslie Dan Faculty of Pharmacy, University of Toronto, Toronto, Ontario, Canada M5S 3M2.

Guelph Food Research Centre, Agriculture and Agri-Food Canada, Guelph, Ontario, Canada N1G 5C9.

出版信息

J Pharm Sci. 2016 Mar;105(3):1124-33. doi: 10.1016/j.xphs.2015.10.001. Epub 2015 Dec 23.

Abstract

Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal feed has limited practicality due to their high volatility, odor, fast decomposition, and poor availability in the lower intestines. To solve these problems, we formulated trans-cinnamaldehyde (CIN) with an adsorbent powder and fatty acid via a melt-solidification technique. Core granules of an optimized composition contained up to 48% wt/wt CIN. The granules were then coated with an enteric polymer to impart site-specific release of CIN. CIN was mostly retained in simulated gastric fluid and released rapidly (>80% under 2 h) in simulated intestinal fluids. Rapid CIN autoxidation into cinnamic acid was inhibited by adding 1% vol/vol eugenol, which maintained CIN stability for at least 1 y. The granule formulation increased the antimicrobial activity of CIN against Escherichia coli K88 slightly with a minimum bactericidal concentration of 450 μg/mL for CIN in lauric acid-based granules compared with 550-600 μg/mL for palmitic acid-based granules and free CIN, respectively. These results encourage the potential use of encapsulated CIN for control of animal enteric pathogens by oral in-feed administration.

摘要

由于抗生素耐药菌的扩散,许多国家已禁止使用抗生素促进家畜生长,因此需要饲料用抗生素的替代品。肉桂精油具有很强的体外抗菌活性;然而,由于其高挥发性、气味、快速分解以及在小肠下段的低利用率,直接将精油添加到动物饲料中的实用性有限。为了解决这些问题,我们通过熔融固化技术将反式肉桂醛(CIN)与吸附剂粉末和脂肪酸进行配方。优化组成的核心颗粒含有高达48%(重量/重量)的CIN。然后用肠溶聚合物包衣颗粒,以实现CIN的定点释放。CIN在模拟胃液中大部分保留,并在模拟肠液中迅速释放(2小时内>80%)。通过添加1%(体积/体积)丁香酚抑制CIN快速自动氧化为肉桂酸,这使CIN的稳定性维持至少1年。颗粒制剂使CIN对大肠杆菌K88的抗菌活性略有增加,基于月桂酸的颗粒中CIN的最低杀菌浓度为450μg/mL,而基于棕榈酸的颗粒和游离CIN的最低杀菌浓度分别为550 - 600μg/mL。这些结果鼓励了通过口服饲料给药使用包封CIN来控制动物肠道病原体的潜在应用。

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