Physical and Pharmacokinetic Characterizations of trans-Resveratrol (t-Rev) Encapsulated with Self-Assembling Lecithin-based Mixed Polymeric Micelles (saLMPMs).
Physical and Pharmacokinetic Characterizations of trans-Resveratrol (t-Rev) Encapsulated with Self-Assembling Lecithin-based Mixed Polymeric Micelles (saLMPMs).
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DOI：
10.1038/s41598-017-11320-y
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发表时间：
2017-09-06
影响因子：
4.6
通讯作者：
Sheu MT
中科院分区：
文献类型：
--
作者：
Li TP;Wong WP;Chen LC;Su CY;Chen LG;Liu DZ;Ho HO;Sheu MT
本研究涉及反式白藜芦醇（t-Rev）负载的saLMPM的物理和药代动力学表征，试图改善t-Rev的药代动力学特征和生物利用度，解决限制其潜在健康益处的障碍。最佳制剂由t-Rev、卵磷脂和Pluronic® P123以5：2：20（t-Rev负载的PP 123 saLMPM）组成，提供平均粒径<200 nm，包封效率> 90%，并且药物负载> 15%。与用HP-β-CD增溶的t-Rev相比，负载t-Rev的PP 123 saLMPM增强了t-Rev在室温、4 °C和37 °C下在PBS中以及在37 °C下在FBS中的稳定性，并且延迟了体外释放。静脉内给予负载t-Rev的PP 123 saLMPM能够提高40%的绝对生物利用度，并且发现更大部分的t-Rev优选分布到外周室中，可能在靶向部位建立治疗水平。口服给药，t-Rev负载LMPM增加2.17倍的绝对生物利用度，并提供了3小时的时间，其中血浆浓度保持在化学预防的理想浓度以上，并实现了更高的剂量标准化曲线下面积值，用于潜在地在靶部位建立有效水平。因此，用PP 123 saLMPM包封的t-Rev的静脉内和口服药代动力学特征表明，t-Rev可以转化为临床上有用的治疗剂。
This study involved physical and pharmacokinetic characterizations of trans-resveratrol (t-Rev)-loaded saLMPMs which attempted to improve t-Rev’s pharmacokinetic profiles and bioavailability resolving hurdles limiting its potential health benefits. The optimal formulation consisted of t-Rev, lecithin, and Pluronic® P123 at 5:2:20 (t-Rev-loaded PP123 saLMPMs) provided mean particle size <200 nm, encapsulation efficiency >90%, and drug loading >15%. Compared to t-Rev solubilized with HP-β-CD, t-Rev-loaded PP123 saLMPMs enhanced t-Rev’s stability in PBS at RT, 4 °C, and 37 °C and in FBS at 37 °C, and retarded the in vitro release. Intravenous administration of t-Rev-loaded PP123 saLMPMs was able to enhance 40% absolute bioavailability and a greater portion of t-Rev was found to preferably distribute into peripheral compartment potentially establishing a therapeutic level at the targeted site. With oral administration, t-Rev-loaded LMPMs increases 2.17-fold absolute bioavailability and furnished a 3-h period of time in which the plasma concentration maintained above the desirable concentration for chemoprevention and accomplished a higher value of the dose-normalized area under the curve for potentially establishing an effective level at the target site. Therefore, intravenous and oral pharmacokinetic characteristics of t-Rev encapsulated with PP123 saLMPMs indicate that t-Rev can be translated into a clinically useful therapeutic agent.
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影响因子：
4.6
作者：
Meng J;Guo F;Xu H;Liang W;Wang C;Yang XD
通讯作者：
Yang XD
影响因子：
6
作者：
Singh, Gurinder;Pai, Roopa S.
通讯作者：
Pai, Roopa S.
DOI：
10.1124/jpet.102.033340
发表时间：
2002-07-01
影响因子：
3.5
作者：
Marier, JF;Vachon, P;Ducharme, MP
通讯作者：
Ducharme, MP
DOI：
10.1111/j.1749-6632.2010.05851.x
发表时间：
2011-01-01
期刊：
RESVERATROL AND HEALTH
影响因子：
--
作者：
Ndiaye, Mary;Kumar, Raj;Ahmad, Nihal
通讯作者：
Ahmad, Nihal
DOI：
10.2147/dddt.s95905
发表时间：
2016
期刊：
Drug design, development and therapy
影响因子：
--
作者：
Balata GF;Essa EA;Shamardl HA;Zaidan SH;Abourehab MA
通讯作者：
Abourehab MA