Chaturvedi Shashank, Verma Anurag, Saharan Vikas Anand
Department of Pharmaceutics, Institute of Pharmaceutical Research, GLA University, Mathura, Uttar Pradesh, India.
Department of Pharmaceutics, School of Pharmaceutical Sciences, IFTM University, Moradabad, Uttar Pradesh, India.
Adv Pharm Bull. 2020 Sep;10(4):524-541. doi: 10.34172/apb.2020.064. Epub 2020 Aug 9.
In the treatment of cancer, chemotherapy plays an important role though the efficacy of anti-cancer drug administered orally is limited, due to their poor solubility in physiological medium, inability to cross biological membrane, high Para-glycoprotein (P-gp) mediated drug efflux, and pre-systemic metabolism. These all factors cumulatively reduce drug exposure at the target site leading to multidrug resistance (MDR). Lipid based carriers systems has been explored to overcome solubility and permeability related issues of anti-cancer drugs. The lipid based formulations have also been reported to circumvent the effect of P-gp and CYP3A4. Further long chain triglycerides (LCT) has shown their ability to access Lymphatic route over Medium Chain Triglycerides, as the former has been extensively used for targeting anti-cancer drugs at proliferating cells through lymphatic route. Therefore this review tries to reflect the usefulness of lipid based drug carriers systems (viz. liposome, solid lipid nanoparticle, nano-lipid carriers, self-emulsifying, lipidic pro-drugs) in targeting lymphatic system and overcoming issues related to solubility and permeability of anti-cancer drugs. Moreover, we have also tried to reflect how critically lipid based carriers are important in maximizing therapeutic safety and efficacy of anti-cancer drugs.
在癌症治疗中,化疗起着重要作用,尽管口服抗癌药物的疗效有限,这是由于它们在生理介质中的溶解度差、无法穿过生物膜、高P-糖蛋白(P-gp)介导的药物外排以及首过代谢。所有这些因素共同降低了药物在靶部位的暴露,导致多药耐药性(MDR)。基于脂质的载体系统已被用于克服抗癌药物的溶解度和渗透性相关问题。据报道,基于脂质的制剂还能规避P-gp和CYP3A4的影响。此外,长链甘油三酯(LCT)已显示出其比中链甘油三酯更能进入淋巴途径的能力,因为前者已被广泛用于通过淋巴途径将抗癌药物靶向增殖细胞。因此,本综述试图反映基于脂质的药物载体系统(即脂质体、固体脂质纳米粒、纳米脂质载体、自乳化制剂、脂质前药)在靶向淋巴系统以及克服抗癌药物的溶解度和渗透性相关问题方面的有用性。此外,我们还试图反映基于脂质的载体在最大化抗癌药物的治疗安全性和疗效方面的关键重要性。