Anuar Nurfazreen, Sabri Akmal H, Bustami Effendi Tommy Julianto, Abdul Hamid Khuriah
Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi MARA, Cawangan Selangor, 42300 Puncak Alam, Selangor, Malaysia.
Advanced Materials and Healthcare Technologies Group, School of Pharmacy, The University of Nottingham, NG7 2RD, Nottingham, UK.
Heliyon. 2020 Jul 29;6(7):e04570. doi: 10.1016/j.heliyon.2020.e04570. eCollection 2020 Jul.
Lipophilic compounds constitute a majority of therapeutics in the pipeline of drug discovery. Despite possessing enhanced efficacy and permeability, some of these drugs suffer poor solubility necessitating the need of a suitable drug delivery system. Nanoemulsion is a drug delivery system that provides enhanced solubility for poorly soluble drugs in an attempt to improve the oral bioavailability. The purpose of this study is to develop a nanoemulsion system using ibuprofen as a model drug in order to investigate the potential of this colloidal system to enhance the absorption of poorly water-soluble drugs. Ibuprofen loaded-nanoemulsion with different drug concentrations (1.5, 3 and 6% w/w) were formulated from olive oil, sucrose ester L-1695 and glycerol using D-phase emulsification technique. A pseudoternary phase diagram was utilised to identify the optimal excipient composition to formulate the nanoemulsion system. diffusion chamber studies using rodent intestinal linings highlighted improved absorption profile when ibuprofen was delivered as nanoemulsion in comparison to microemulsions and drug-in-oil systems. This was further corroborated by studies using rat model that highlighted a two-fold increase in ibuprofen absorption when the drug was administered as a nanoemulsion relative to drug-in-oil system. On the other hand, when ibuprofen was administered as microemulsions, only a 1.5-fold increase in absorption was observed relative to drug-in-oil system. Thus, this study highlights the potential of using nanoemulsion as a drug delivery system to enhance the oral bioavailability of hydrophobic drugs.
亲脂性化合物在药物研发的在研治疗药物中占大多数。尽管这些药物具有增强的疗效和渗透性,但其中一些药物的溶解度较差,因此需要合适的药物递送系统。纳米乳剂是一种药物递送系统,它能提高难溶性药物的溶解度,以提高口服生物利用度。本研究的目的是开发一种以布洛芬为模型药物的纳米乳剂系统,以研究这种胶体系统增强难溶性药物吸收的潜力。使用D相乳化技术,由橄榄油、蔗糖酯L-1695和甘油制备了不同药物浓度(1.5%、3%和6%w/w)的载布洛芬纳米乳剂。利用伪三元相图确定制备纳米乳剂系统的最佳辅料组成。使用啮齿动物肠内衬的扩散室研究表明,与微乳剂和油包药系统相比,布洛芬以纳米乳剂形式给药时吸收情况有所改善。使用大鼠模型的研究进一步证实了这一点,该研究表明,与油包药系统相比,当药物以纳米乳剂形式给药时,布洛芬的吸收增加了两倍。另一方面,当布洛芬以微乳剂形式给药时,相对于油包药系统,仅观察到吸收增加了1.5倍。因此,本研究突出了使用纳米乳剂作为药物递送系统来提高疏水性药物口服生物利用度的潜力。