关键词: Absorption enhancer CBD LBDDS SNEDDS THC bioavailability cannabinoids chylomicrons cyclosporine first pass metabolism lymphatic absorption piperine Absorption enhancer CBD LBDDS SNEDDS THC bioavailability cannabinoids chylomicrons cyclosporine first pass metabolism lymphatic absorption piperine

Mesh : Administration, Oral Biological Availability Cannabinoids Drug Delivery Systems Emulsions Humans Nanoparticles Particle Size Solubility

来  源:   DOI:10.1080/17425255.2022.2099837

Abstract:
UNASSIGNED: Oral administration of cannabinoids is a convenient route of administration in many cases. To enhance the poor and variable bioavailability of cannabinoids, selected strategies utilizing proper delivery systems have been designed. Low solubility in the GI aqueous media is the first and most critical barrier. Thereafter, cannabinoids can reach the systemic blood circulation via the portal vein that is associated with significant hepatic first pass metabolism (FPM) or bypass it via lymphatic absorption.
UNASSIGNED: The solubility obstacle of cannabinoids is mainly addressed with lipid-based formulations such as self-nanoemulsifying drug delivery systems (SNEDDS). Certain lipids are used to overcome the solubility issue. Surfactants and other additives in the formulation have additional impact on several barriers, including dictating the degree of lymphatic bioavailability and hepatic FPM. Gastro-retentive formulation is also plausible.
UNASSIGNED: Comparison of the role of the same SNEDDS formulation, cyclosporine vs. cannabinoids, when used to elevate the oral bioavailability of different compounds, is presented. It illustrates some similarities and major mechanistic differences obtained by the same SNEDDS. Thus, the different influence over the absorption pathway illuminates the importance of understanding the absorption mechanism and its barriers to properly select appropriate strategies to achieve enhanced oral bioavailability.
摘要:
在许多情况下,口服大麻素是一种方便的给药途径。为了增强大麻素的不良和可变的生物利用度,已经设计了利用适当输送系统的选定策略。在GI水性介质中的低溶解度是第一和最关键的屏障。此后,大麻素可以通过与重要的肝首过代谢(FPM)相关的门静脉到达全身血液循环,或通过淋巴吸收绕过它。
大麻素的溶解度障碍主要通过基于脂质的制剂如自纳米乳化药物递送系统(SNEDDS)来解决。某些脂质用于克服溶解度问题。配方中的表面活性剂和其他添加剂对几种屏障有额外的影响,包括决定淋巴生物利用度和肝FPM的程度。胃滞留制剂也是合理的。
相同SNEDDS配方的作用比较,环孢菌素vs.大麻素,当用于提高不同化合物的口服生物利用度时,是presented。它说明了相同SNEDDS获得的一些相似性和主要机械差异。因此,对吸收途径的不同影响说明了了解吸收机制及其障碍对正确选择适当策略以提高口服生物利用度的重要性。
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