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聚(D,L-乳酸)纳米粒的制备及其作为 L-茶氨酸的缓释给药系统。

Fabrication of poly(D, L-lactic acid) nanoparticles as delivery system for sustained release of L-theanine.

机构信息

Department of Biotechnology, School of Bio Sciences and Technology, Vellore Institute of Technology, Vellore - 632014, TN, India.

University Institute of Biotechnology, Chandigarh University, NH-95 Chandigarh-Ludhiana Highway, Mohali, Punjab, India.

出版信息

IET Nanobiotechnol. 2019 Sep;13(7):742-747. doi: 10.1049/iet-nbt.2018.5248.

Abstract

L-theanine is present in tea as a unique, free, non-protein amino acid. Due to various beneficial effects on brain activity, it is widely used as a nutraceutical. After consumption, it is rapidly absorbed and metabolised followed by excretion through urine. Therefore, the authors developed an L-theanine delivery system by encapsulating into polymeric nanoparticles to release it slowly and make it available for a longer period of time. Poly(D, L-lactic acid) nanoparticle (PLANP) was fabricated by the double emulsion method and L-theanine was encapsulated into it (PLANP-T). Spherical nanoparticles with a hydrodynamic diameter of 247 and 278 nm and surface charge of -14.5 and -25.7 mV for PLANP and PLANP-T, respectively, were fabricated. The Fourier transform infrared spectroscopic data indicated encapsulation of L-theanine into PLANP. The PLANP showed high L-theanine encapsulation capacity (71.65%) with a sustained release character. The maximum release (66.3%) of L-theanine was recorded in pH 7.3 at 48 h. The release kinetics followed the Higuchi model and the release mechanism was determined as super case-II transport (erosion). This slow release will make it available to the target tissue for a longer period of time (sustain release effect) and will also avoid immediate metabolism and clearance from the circulation.

摘要

L-茶氨酸是一种独特的、游离的、非蛋白质氨基酸,存在于茶中。由于其对大脑活动有多种有益的影响,因此被广泛用作营养保健品。摄入后,它会迅速被吸收和代谢,然后通过尿液排出体外。因此,作者通过将其包裹在聚合物纳米颗粒中,开发了一种 L-茶氨酸递释系统,以使其缓慢释放,并延长其有效作用时间。采用双乳液法制备聚(D,L-乳酸)纳米颗粒(PLANP),并将 L-茶氨酸包封于其中(PLANP-T)。制备出的纳米颗粒呈球形,水动力直径分别为 247nm 和 278nm,表面电荷分别为-14.5mV 和-25.7mV。傅里叶变换红外光谱数据表明 L-茶氨酸已被包封于 PLANP 中。PLANP 对 L-茶氨酸具有较高的包封率(71.65%)和持续释放特性。在 48 小时时,在 pH 7.3 下,L-茶氨酸的最大释放量(66.3%)。释放动力学符合 Higuchi 模型,释放机制被确定为超 II 型(侵蚀)传递。这种缓慢释放将使其在更长的时间内(持续释放效应)到达靶组织,并避免立即被代谢和从循环中清除。

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