Preparation and application of a purified synthetic phospholipid-monoterpene traditional Chinese medicine penetration enhancer associated composition

By reacting acid anhydrides with monoterpene chemical penetration enhancers to generate active esters, which are then combined with phosphatidylethanolamine, modified phospholipid-monoterpene lipid carriers are prepared. This solves the problems of easy volatility and low modification rate of monoterpene traditional Chinese medicine penetration enhancers, and realizes efficient transdermal drug delivery and brain-targeted application.

CN122404401APending Publication Date: 2026-07-17INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
Filing Date
2025-01-17
Publication Date
2026-07-17

AI Technical Summary

Technical Problem

Existing monoterpenoid-based traditional Chinese medicine penetration enhancers are volatile, and the physical modification rate of lipid carriers is not high, making it difficult to effectively improve their penetration effect in transdermal drug delivery.

Method used

An active ester is generated by reacting anhydride with a monoterpene chemical penetration enhancer in an organic solvent. This ester is then combined with phosphatidylethanolamine (PE) and modified phospholipid-monoterpene lipid carriers are prepared by thin-film dispersion or reverse evaporation to form solid lipid nanoparticles or ethanol bodies. Surfactants are added to improve film-forming properties.

Benefits of technology

It improved the modification rate of monoterpenoid traditional Chinese medicine penetration enhancers, enhanced the permeability of transdermal drug delivery, reduced cell toxicity at high concentrations, and improved the potential for brain-targeted applications.

✦ Generated by Eureka AI based on patent content.

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Abstract

本发明将纯化的合成磷脂和含羟基单萜类中药促渗剂通过酸酐连接形成新化合物,并公开了新化合物的使用方法和使用范围,通过该合成方法,稳定易挥发的中药促渗剂,同时起到促进药物跨膜吸收的效果。本发明中的化合物合成方法成功合成出了BO‑DOPE,通过简单的纯化步骤即可明显提高合成产物纯度,并考察了BO‑DOPE制备的纳米粒的细胞摄取效率,相比于无修饰的纳米粒和游离药物,BO‑DOPE的修饰能够明显增加药物的细胞摄取速率和累积量。所制备新化合物可用于制备纳米粒或醇质体等脂质载体,所得载体的粒径均较小且较为均一,并降低了细胞毒性,具有良好的促进渗透过生物屏障的应用前景。
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