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Amelioration of lipophilic compounds in regards to bioavailability as self-emulsifying drug delivery system (SEDDS)
Future Journal of Pharmaceutical Sciences ( IF 3.4 ) Pub Date : 2020-06-10 , DOI: 10.1186/s43094-020-00042-0
Pragya Baghel , Amit Roy , Shekhar Verma , Trilochan Satapathy , Sanjib Bahadur

High lipophilicity and poor aqueous solubility are the endemic problems of new drug molecules. Sixty to seventy percent of these drugs are unable to solubilize completely in aqueous media, or have very low permeability. This hampers their oral absorption and further leads to their poor bioavailability. Various researches are in progress to overcome these limitations. Novel technologies like nano-carrier systems have become popular for improving the solubility of drugs. Lipid-based formulations, among nano systems, are taking pace for the enhancement of solubility, oral absorption, and hence the bioavailability of drugs. Among the lipid formulations, self-emulsification systems are gaining popularity by offering various advantages to delivery systems. Self-emulsifying drug delivery systems (SEDDS) are isotropic blends of oil and surfactant/co-surfactants. These ingredients upon gentle agitation in aqueous media results in the formation of o/w emulsion. In spite of many works published in SEDDS, the major concerns of this article are to discuss the various approaches to formulate a good lipid-based carrier system for poorly aqueous soluble drugs, role of various polymers, and their categories used in the formulation along-with the modern technologies used for enhancing the stability of liquid SEDDS. This review majorly focuses upon the problems related to the poor aqueous solubility of the newer lipid molecules and the solutions to overcome their solubility and in addition bioavailability. As per the researches done in formulation and optimization of SEDDS for the enhancement of bioavailability of lipophilic molecules, it can be stated that the aqueous solubility as well as bioavailability can be increased by many folds compared to their marketed or other oral formulations.

中文翻译:

改善亲油性化合物作为自乳化药物递送系统(SEDDS)的生物利用度

高亲脂性和差的水溶性是新药分子的地方性问题。这些药物中有60%至70%无法完全溶解在水性介质中,或者渗透性非常低。这阻碍了它们的口服吸收并进一步导致了它们不良的生物利用度。为了克服这些限制,正在进行各种研究。诸如纳米载体系统之类的新技术已广泛用于改善药物的溶解度。在纳米系统中,基于脂质的制剂正在为提高溶解度,口服吸收以及药物的生物利用度而努力。在脂质制剂中,自乳化系统通过为递送系统提供各种优点而获得普及。自乳化药物输送系统(SEDDS)是油和表面活性剂/助表面活性剂的各向同性混合物。这些成分在水性介质中缓慢搅动会形成o / w乳液。尽管在SEDDS上发表了许多著作,但本文的主要关注点是讨论为难溶于水的药物配制好的基于脂质的载体系统的各种方法,各种聚合物的作用以及在配制过程中使用的类别-以及用于增强液体SEDDS稳定性的现代技术。这篇综述主要集中在与新型脂质分子水溶性差有关的问题以及克服其溶解性和生物利用度的解决方案。
更新日期:2020-06-10
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