Yin Juntao, Xiang Cuiyu, Wang Peiqing, Yin Yuyun, Hou Yantao
Department of Pharmaceutics, Huaihe Hospital Affiliated to Henan University, Kaifeng.
Department of Physiochemical Analysis, Henan Provincial Institute for Food and Drug Control, Zhengzhou.
Int J Nanomedicine. 2017 Apr 10;12:2923-2931. doi: 10.2147/IJN.S131167. eCollection 2017.
Baicalein (BCL) possesses high pharmacological activities but low solubility and stability in the intestinal tract. This study aimed to probe the potential of nanoemulsions (NEs) consisting of hemp oil and less surfactants in ameliorating the oral bioavailability of BCL. BCL-loaded NEs (BCL-NEs) were prepared by high-pressure homogenization technique to reduce the amount of surfactants. BCL-NEs were characterized by particle size, entrapment efficiency (EE), in vitro drug release, and morphology. Bioavailability was studied in Sprague-Dawley rats following oral administration of BCL suspensions, BCL conventional emulsions, and BCL-NEs. The obtained NEs were ~90 nm in particle size with an EE of 99.31%. BCL-NEs significantly enhanced the oral bioavailability of BCL, up to 524.7% and 242.1% relative to the suspensions and conventional emulsions, respectively. BCL-NEs exhibited excellent intestinal permeability and transcellular transport ability. The cytotoxicity of BCL-NEs was documented to be low and acceptable for oral purpose. Our findings suggest that such novel NEs and preparative process provide a promising alternative to current formulation technologies and suitable for oral delivery of drugs with bioavailability issues.
黄芩苷(BCL)具有较高的药理活性,但在肠道中的溶解度和稳定性较低。本研究旨在探究由大麻油和较少表面活性剂组成的纳米乳剂(NEs)改善BCL口服生物利用度的潜力。采用高压均质技术制备负载BCL的纳米乳剂(BCL-NEs)以减少表面活性剂的用量。通过粒径、包封率(EE)、体外药物释放和形态对BCL-NEs进行表征。在口服给予BCL混悬液、BCL常规乳剂和BCL-NEs后,在Sprague-Dawley大鼠中研究生物利用度。所制备的纳米乳剂粒径约为90 nm,包封率为99.31%。BCL-NEs显著提高了BCL的口服生物利用度,相对于混悬液和常规乳剂分别高达524.7%和242.1%。BCL-NEs表现出优异的肠道通透性和跨细胞转运能力。BCL-NEs的细胞毒性被证明较低,对于口服给药而言是可接受的。我们的研究结果表明,这种新型纳米乳剂及其制备工艺为当前的制剂技术提供了一种有前景的替代方案,适用于口服递送存在生物利用度问题的药物。