Bioavailability of Orally Delivered Alpha-Tocopherol by Poly(Lactic-Co-Glycolic) Acid (PLGA) Nanoparticles and Chitosan Covered PLGA Nanoparticles in F344 Rats.

Q1 Engineering Nanobiomedicine Pub Date : 2016-01-01 DOI:10.5772/63305

Lacey C Simon, Rhett W Stout, Cristina Sabliov

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Abstract

It is hypothesized that the bioavailability of αT (alpha-tocopherol), an antioxidant, can be improved when delivered by poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) and chitosan covered PLGA nanoparticles (PLGA-Chi NPs), and that the mucoadhesive properties of chitosan may enhance absorption of αT. PLGA and PLGA-Chi NPs were characterized by measuring entrapment efficiency, size, polydispersity, and zeta potential. Nanoparticle physical stability, chemical stability of entrapped αT, and release kinetics were also measured. Pharmacokinetic studies were conducted by administering PLGA (αT) NPs, PLGA-Chi (αT) NPs, and free αT via oral gavage in rats. The size and zeta potential of the two particle systems were 97.87 ± 2.63 nm and -36.2 ± 1.31 mV for PLGA(αT) NPs, and 134 ± 2.05 nm and 38.0 ± 2.90 mV for PLGA-Chi (αT) nanoparticles in DI water. The particle systems showed to be stable during various in vitro assays. Bioavailability of nanodelivered αT was improved compared to the free αT, by 170% and 121% for PLGA and PLGA-Chi NPs, respectively. It was concluded that while chitosan did not further improved bioavailability of αT, PLGA NPs protected the entrapped drug from the GI environment degradation and proved to be an effective delivery system for αT.

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聚乳酸-共甘醇酸（PLGA）纳米颗粒和壳聚糖包裹的 PLGA 纳米颗粒口服α-生育酚在 F344 大鼠体内的生物利用率

研究假设，通过聚乳酸-共聚乙醇酸（PLGA）纳米颗粒（NPs）和壳聚糖包覆的 PLGA 纳米颗粒（PLGA-Chi NPs）输送抗氧化剂 αT（α-生育酚），可提高其生物利用率，而且壳聚糖的粘附特性可促进 αT的吸收。PLGA 和 PLGA-Chi NPs 的特性是通过测量包载效率、尺寸、多分散性和 zeta 电位来确定的。此外，还测量了纳米颗粒的物理稳定性、夹带的αT的化学稳定性以及释放动力学。通过给大鼠口服 PLGA（αT）NPs、PLGA-Chi（αT）NPs 和游离 αT 进行了药代动力学研究。在去离子水中，PLGA（αT）NPs和PLGA-Chi（αT）纳米颗粒的粒径和ZETA电位分别为97.87 ± 2.63 nm和-36.2 ± 1.31 mV，PLGA-Chi（αT）纳米颗粒的粒径和ZETA电位分别为134 ± 2.05 nm和38.0 ± 2.90 mV。颗粒系统在各种体外试验中均表现稳定。与游离αT相比，PLGA和PLGA-Chi NPs纳米载体αT的生物利用率分别提高了170%和121%。结论是，壳聚糖不能进一步提高αT的生物利用度，而PLGA NPs则能保护夹带的药物不被消化道环境降解，被证明是一种有效的αT给药系统。

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来源期刊

Nanobiomedicine Biochemistry, Genetics and Molecular Biology-Biotechnology

CiteScore

6.80

自引率

0.00%

发文量

审稿时长

14 weeks

期刊介绍： Nanobiomedicine is an international, peer-reviewed, open access scientific journal that publishes research in nanotechnology as it interfaces with fundamental studies in biology, as well as its application to the fields of medicine. Nanobiomedicine covers all key aspects of this research field, including, but not limited to, bioengineering, biophysics, physical and biological chemistry, and physiology, as well as nanotechnological applications in diagnostics, therapeutic application, preventive medicine, drug delivery, and monitoring of human disease. Additionally, theoretical and modeling studies covering the nanobiomedicine fields will be considered. All submitted articles considered suitable for Nanobiomedicine are subjected to rigorous peer review to ensure the highest levels of quality. The review process is carried out as quickly as possible to minimize any delays in the online publication of articles. Submissions are encouraged on all topics related to nanobiomedicine, and its clinical applications including but not limited to: Nanoscale-structured biomaterials, Nanoscale bio-devices, Nanoscale imaging, Nanoscale drug delivery, Nanobiotechnology, Nanorobotics, Nanotoxicology, Nanoparticles, Nanocarriers, Nanofluidics, Nanosensors (nanowires, nanophotonics), Nanosurgery (dermatology, gastroenterology, ophthalmology, etc), Nanocarriers commercialization of nanobiomedical technologies, Market trends in the nanobiomedicine space, Ethics and regulatory aspects of nanobiomedicine approval, New perspectives of nanobiomedicine in clinical diagnostics, BioMEMS, Nano-coatings, Plasmonics, Nanoscale visualization.