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开发稳定的纳米级传递体作为直肠胶体以增强大麻二酚的递送。

Development of Stable Nano-Sized Transfersomes as a Rectal Colloid for Enhanced Delivery of Cannabidiol.

作者信息

Moqejwa Thope, Marimuthu Thashree, Kondiah Pierre P D, Choonara Yahya E

机构信息

Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, Faculty of Health Sciences, School of Therapeutic Science, University of the Witwatersrand, 7 York Road, Parktown, Johannesburg 2193, South Africa.

出版信息

Pharmaceutics. 2022 Mar 25;14(4):703. doi: 10.3390/pharmaceutics14040703.

Abstract

Current cannabidiol (CBD) formulations are challenged with unpredictable release and absorption. Rational design of a rectal colloid delivery system can provide a practical alternative In this study the inherent physiochemical properties of transferosomes were harnessed for the development of a nano-sized transfersomes to yield more stable release, absorption, and bioavailability of CBD as a rectal colloid. Transfersomes composed of soya lecithin, cholesterol, and polysorbate 80 were synthesized via thin film evaporation and characterized for size, entrapment efficiency (%), morphology, CBD release, ex vivo permeation, and physicochemical stability. The optimized formulation for rectal delivery entrapped up to 80.0 ± 0.077% of CBD with a hydrodynamic particle size of 130 nm, a PDI value of 0.285, and zeta potential of -15.97 mV. The morphological investigation via SEM and TEM revealed that the transfersomes were spherical and unilamellar vesicles coinciding with the enhanced ex vivo permeation across the excised rat colorectal membrane. Furthermore, transfersomes improved the stability of the encapsulated CBD for up to 6 months at room temperature and showed significant promise that the transfersomes promoted rectal tissue permeation with superior stability and afforded tunable release kinetics of CBD as a botanical therapeutic with inherent poor bioavailability.

摘要

目前的大麻二酚(CBD)制剂面临着不可预测的释放和吸收问题。合理设计直肠胶体递送系统可以提供一种切实可行的替代方案。在本研究中,利用传递体的固有物理化学性质开发了一种纳米级传递体,以实现CBD作为直肠胶体更稳定的释放、吸收和生物利用度。通过薄膜蒸发法合成了由大豆卵磷脂、胆固醇和聚山梨酯80组成的传递体,并对其粒径、包封率(%)、形态、CBD释放、离体渗透和物理化学稳定性进行了表征。用于直肠给药的优化制剂包封了高达80.0±0.077%的CBD,流体动力学粒径为130nm,PDI值为0.285,zeta电位为-15.97mV。通过扫描电子显微镜(SEM)和透射电子显微镜(TEM)进行的形态学研究表明,传递体为球形单层囊泡,这与在切除的大鼠结肠直肠膜上增强的离体渗透相一致。此外,传递体在室温下可将包封的CBD稳定性提高长达6个月,并显示出显著的前景,即传递体可促进直肠组织渗透,具有卓越的稳定性,并能提供具有固有低生物利用度的植物治疗剂CBD的可调释药动力学。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a19b/9032849/4e2edadb96f2/pharmaceutics-14-00703-g001.jpg

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