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采用载有大麻二酚的纳米载体的经皮给药贴剂,体内药代动力学更好。

Key Transdermal Patch Using Cannabidiol-Loaded Nanocarriers with Better Pharmacokinetics in vivo.

机构信息

Department of Chemistry, National Chung Hsing University, Taichung, Taiwan.

Basic Research and Development Department, Powin Biomedical Co. Ltd., Taichung, Taiwan.

出版信息

Int J Nanomedicine. 2024 May 16;19:4321-4337. doi: 10.2147/IJN.S455032. eCollection 2024.

DOI:10.2147/IJN.S455032
PMID:38770103
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11104392/
Abstract

PURPOSE

Cannabidiol (CBD) is a promising therapeutic drug with low addictive potential and a favorable safety profile. However, CBD did face certain challenges, including poor solubility in water and low oral bioavailability. To harness the potential of CBD by combining it with a transdermal drug delivery system (TDDS). This innovative approach sought to develop a transdermal patch dosage form with micellar vesicular nanocarriers to enhance the bioavailability of CBD, leading to improved therapeutic outcomes.

METHODS

A skin-penetrating micellar vesicular nanocarriers, prepared using nano emulsion method, cannabidiol loaded transdermal nanocarriers-12 (CTD-12) was presented with a small particle size, high encapsulation efficiency, and a drug-loaded ratio for CBD. The skin permeation ability used Strat-M™ membrane with a transdermal diffusion system to evaluate the CTD and patch of CTD-12 (PCTD-12) within 24 hrs. PCTD-12 was used in a preliminary pharmacokinetic study in rats to demonstrate the potential of the developed transdermal nanocarrier drug patch for future applications.

RESULTS

In the transdermal application of CTD-12, the relative bioavailability of the formulation was 3.68 ± 0.17-fold greater than in the free CBD application. Moreover, PCTD-12 indicated 2.46 ± 0.18-fold higher relative bioavailability comparing with free CBD patch in the ex vivo evaluation. Most importantly, in the pharmacokinetics of PCTD-12, the relative bioavailability of PCTD-12 was 9.47 ± 0.88-fold higher than in the oral application.

CONCLUSION

CTD-12, a transdermal nanocarrier, represents a promising approach for CBD delivery, suggesting its potential as an effective transdermal dosage form.

摘要

目的

大麻二酚(CBD)是一种很有前途的治疗药物,具有低成瘾性和良好的安全性。然而,CBD 确实面临一些挑战,包括在水中的溶解度差和口服生物利用度低。为了利用 CBD 的潜力,将其与透皮给药系统(TDDS)结合使用。这种创新方法旨在开发一种含有胶束囊泡纳米载体的透皮贴剂剂型,以提高 CBD 的生物利用度,从而改善治疗效果。

方法

采用纳米乳法制备具有透皮性能的胶束囊泡纳米载体,载药胶束纳米载体-12(CTD-12)具有粒径小、包封率高、载药量高等特点。采用 Strat-M™膜透皮扩散系统评价 CTD 和 CTD-12 贴片(PCTD-12)在 24 小时内的皮肤渗透能力。在大鼠初步药代动力学研究中使用 PCTD-12 ,以证明所开发的透皮纳米载体药物贴剂在未来应用中的潜力。

结果

在 CTD-12 的透皮应用中,制剂的相对生物利用度比游离 CBD 应用高 3.68±0.17 倍。此外,PCTD-12 在离体评价中比游离 CBD 贴剂具有 2.46±0.18 倍的相对生物利用度更高。最重要的是,在 PCTD-12 的药代动力学中,PCTD-12 的相对生物利用度比口服应用高 9.47±0.88 倍。

结论

CTD-12 作为一种透皮纳米载体,为 CBD 的传递提供了一种很有前途的方法,表明其作为一种有效的透皮剂型的潜力。

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