Pharmacodelivery Research Group, School of Pharmacy, University College Cork, Ireland.
Int J Pharm. 2013 Sep 10;453(2):307-14. doi: 10.1016/j.ijpharm.2013.06.027. Epub 2013 Jun 21.
Lycopene is a potent anti-oxidant, which has been widely reported for its potential benefits at reducing the risks of certain types of cancer e.g. prostate cancer. The oral bioavailability of this highly lipophilic carotenoid is low and highly influenced by the extent of intestinal lymphatic uptake. The aim of this study was to develop an optimised formulation, which allows for efficient absorption following oral administration. A self-emulsifying drug delivery system (SEDDS) and solid dispersion of Lycopene were developed initially. Subsequently, a novel lipid based solid dispersion (LBSD) was designed. Processing via a solid dispersion approach was found to alter the solid state characteristics of Lycopene, as determined by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The bioavailability of Lycopene was significantly increased after oral administration of LBSD to fasted pigs, relative to the commercial product (Lycovit(®)). A clear distinction in terms of Cmax and AUC was observed between Lycovit(®) and LBSD. In conclusion, a novel LBSD formulation was developed to enhance the oral bioavailability of the model lipophilic compound, Lycopene, by enhancing dissolution in the gastrointestinal tract and promoting intestinal lymphatic uptake utilising digestible lipid excipients.
番茄红素是一种有效的抗氧化剂，已广泛报道其具有降低某些类型癌症（如前列腺癌）风险的潜力。这种高度亲脂性类胡萝卜素的口服生物利用度较低，并且高度受肠道淋巴摄取程度的影响。本研究旨在开发一种优化的配方，使口服后能够有效地吸收。最初开发了自乳化药物递送系统（SEDDS）和番茄红素固体分散体。随后，设计了一种新型基于脂质的固体分散体（LBSD）。通过固体分散体方法进行处理被发现会改变番茄红素的固态特性，如差示扫描量热法（DSC）和 X 射线衍射（XRD）所确定的那样。与商业产品（Lycovit®）相比，LBSD 口服给予禁食猪后，番茄红素的生物利用度显著增加。在 Lycovit®和 LBSD 之间观察到 Cmax 和 AUC 的明显差异。总之，开发了一种新型 LBSD 配方，通过增强在胃肠道中的溶解并利用可消化的脂质赋形剂促进肠道淋巴摄取，来提高模型亲脂性化合物番茄红素的口服生物利用度。
