Bioavailability of lycopene in the rat: the role of intestinal lymphatic transport

Bioavailability of lycopene in the rat: the role of intestinal lymphatic transport
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DOI:
10.1211/jpp.62.03.0006
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发表时间:
2010-03-01
影响因子:
3.3
通讯作者:
Griffin, Brendan T.
Griffin, Brendan T.
中科院分区:
医学3区
文献类型:
--
作者:
Faisal, Waleed;O'Driscoll, Caitriona M.;Griffin, Brendan T.

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目的番茄红素作为一种天然抗氧化剂,作为一种有效的化学预防剂已引起人们的广泛关注。番茄红素是一种亲脂性极强的化合物,据估计从饮食来源的吸收率很低,而且变化很大。因此,血浆番茄红素浓度与富含番茄红素的食物的膳食摄入量相关性很差。口服制剂的发展仍然是一个挑战,需要更好地了解在肠道吸收的这种compound.Methods的机制番茄红素在模拟生理液体和胆盐混合胶束制剂的溶解度进行了测定。肠淋巴运输的程度和番茄红素的绝对生物利用度从一系列的生物相关媒体进行了评估,在肠系膜淋巴管插管麻醉大鼠model.Results番茄红素的绝对生物利用度后8小时为1.85 +/-0.39%。肠淋巴转运的总体范围为给药剂量的0.6-3.4%。肠内番茄红素含量与肠内甘油三酯含量呈显著正相关(r(2)> 0.9)。结论肠淋巴途径是番茄红素从胃肠道摄取的主要途径。番茄红素在肠淋巴液中的转运与甘油三酯在淋巴液中的转运密切相关。旨在促进肠淋巴吸收的制剂策略,如含有长链脂肪酸(LCFA)或卵磷脂的脂质制剂,可能有助于提高番茄红素的口服生物利用度。
Objectives As a natural antioxidant derived from dietary sources, lycopene has attracted considerable attention as a potent chemopreventative agent. Lycopene is an extremely lipophilic compound and absorption from dietary sources is estimated to be low and highly variable. As a result, plasma lycopene concentrations are poorly correlated with dietary intake of lycopene rich food stuffs. The development of an oral formulation remains a challenge that requires a better understanding of the mechanisms involved in the intestinal absorption of this compound.Methods The solubility of lycopene in simulated physiological fluids and bile salt mixed micelle formulations was determined. The extent of intestinal lymphatic transport and the absolute bioavailability of lycopene from a range of biorelevant media was evaluated in a mesenteric lymph duct cannulated anaesthetised rat model.Results The absolute bioavailability of lycopene after 8 h was 1.85 +/- 0.39%. The overall extent of the intestinal lymphatic transport was in the range of 0.6-3.4% of the administered dose. A strong positive correlation (r(2) > 0.9) between intestinal lycopene levels and intestinal triglyceride levels was demonstrated.Conclusions The intestinal lymphatic route is the major uptake mechanism of lycopene from the gastrointestinal tract. Lycopene transport in intestinal lymph was closely associated with triglyceride transport in the lymph. Formulation strategies designed to promote intestinal lymphatic uptake, such as lipid-based formulations containing long-chain fatty acids (LCFA) or lecithin, may serve to enhance oral bioavailability of lycopene.