Khanum Ramona, Thevanayagam Haema
School of Postgraduate Studies, International Medical University (IMU), 126, Jalan Jalil Perkasa 19, Bukit Jalil, Kuala Lumpur 57000, Malaysia.
Asian J Pharm Sci. 2017 Sep;12(5):401-411. doi: 10.1016/j.ajps.2017.05.003. Epub 2017 May 6.
Pharmaceutical delivery systems are developed to improve the physicochemical properties of therapeutic compounds. Emulsions are one of these drug delivering systems formulated using water, oils and lipids as main ingredients. Extensive data are usually generated on the physical and chemical characteristics of these oil-in-water and lipid emulsions. However, the oxidative tendency of emulsions is often overlooked. Oxidation impacts the overall quality and safety of these pharmaceutical emulsions. Additionally, introducing oxidatively unstable emulsions into biological systems further promotes oxidation . Products of these reactions then continue to pose serious harm to cells and fuel other physiological oxidation reactions. Consequently, the increase of oxidation products leads to oxidative damage to biological systems. Thus, emulsions with lower lipid peroxidation are more stable and will reduce the negative effects of oxidation . Preventive measures during the formulation of emulsions are important. Many naturally occurring and cost effective substances possess low oxidation tendencies and confer oxidative protection when used in emulsions. Additionally, certain preparatory methods should be employed to reduce or better control lipid peroxidation. Finally, emulsions must be evaluated for their oxidation susceptibility using the various techniques available. Careful attention to the preparation of emulsions and assessment of their oxidative stability will help produce safer emulsions without compromising efficacy.
药物递送系统的开发旨在改善治疗性化合物的物理化学性质。乳剂是这些药物递送系统之一,它以水、油和脂质作为主要成分配制而成。通常会生成大量关于这些水包油型和脂质乳剂物理和化学特性的数据。然而,乳剂的氧化倾向常常被忽视。氧化会影响这些药物乳剂的整体质量和安全性。此外,将氧化不稳定的乳剂引入生物系统会进一步促进氧化。这些反应的产物随后会继续对细胞造成严重损害,并引发其他生理氧化反应。因此,氧化产物的增加会导致对生物系统的氧化损伤。因此,脂质过氧化程度较低的乳剂更稳定,并且会减少氧化的负面影响。乳剂配方过程中的预防措施很重要。许多天然存在且具有成本效益的物质具有较低的氧化倾向,并且在用于乳剂时能提供氧化保护。此外,应采用某些制备方法来减少或更好地控制脂质过氧化。最后,必须使用各种可用技术评估乳剂的氧化敏感性。仔细关注乳剂的制备及其氧化稳定性评估将有助于生产出更安全的乳剂,同时不影响疗效。