Liu Wan-Yi, Hsieh Yun-Shan, Wu Yu-Tse
School of Pharmacy, Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
Pharmaceutics. 2022 Mar 14;14(3):637. doi: 10.3390/pharmaceutics14030637.
The aim of this study was to develop a nanoparticle formulation made of poly (vinyl pyrrolidone) (PVP) and poly (lactic-co-glycolic) acid (PLGA) for the oral delivery of β-carotene (BC). The hybrid nanoparticles were prepared by the interfacial deposition method, and the physicochemical properties of this formulation were characterized in terms of its morphology, particle size, size distribution, encapsulation efficiency, dissolution, intestinal permeability, and in vivo pharmacokinetics. Our results demonstrated that BC-loaded nanoformulation and PLGA nanoparticles (PNP) significantly enhanced a release 6.1 times higher than BC suspension. The fortification of PVP into PLGA nanoparticles, named PLGA-PVP hybrid nanoparticles (PPNP), significantly reduced the particle size, as well as led to an increase 1.9 times higher in the in vitro release of BC, compared with PNP. For the ex vivo intestinal permeability assessment, PNP and PPNP-K15 significantly enhanced the intestinal permeability by 2.7 and 6.5 times at the jejunum, and 2.3 and 4.5 times at the ileum, when compared with unformulated BC. According to the pharmacokinetic study, the optimized hybrid formulation significantly increased the peak plasma concentration (C) and the area under the curve (AUC), and the oral relative bioavailability showed a five-fold enhancement compared with that of the BC suspension. Our results indicate that the hybrid nanoparticulate delivery system is an efficient strategy for the oral delivery of BC.
本研究的目的是开发一种由聚(乙烯基吡咯烷酮)(PVP)和聚(乳酸-乙醇酸)共聚物(PLGA)制成的纳米颗粒制剂,用于β-胡萝卜素(BC)的口服给药。通过界面沉积法制备了混合纳米颗粒,并从其形态、粒径、粒径分布、包封率、溶解性、肠道通透性和体内药代动力学等方面对该制剂的理化性质进行了表征。我们的结果表明,载有BC的纳米制剂和PLGA纳米颗粒(PNP)显著提高了释放率,比BC悬浮液高6.1倍。将PVP强化到PLGA纳米颗粒中,即PLGA-PVP混合纳米颗粒(PPNP),与PNP相比,显著减小了粒径,同时使BC的体外释放增加了1.9倍。对于离体肠道通透性评估,与未配制的BC相比,PNP和PPNP-K15在空肠处显著提高了肠道通透性2.7倍和6.5倍,在回肠处提高了2.3倍和4.5倍。根据药代动力学研究,优化后的混合制剂显著提高了血浆峰浓度(C)和曲线下面积(AUC),口服相对生物利用度与BC悬浮液相比提高了5倍。我们的结果表明,混合纳米颗粒递送系统是BC口服给药的有效策略。