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Updated: Jun 18, 2025

Preparation, Administration, and Assessment of In Vivo Tissue-Specific Cellular Uptake of Fluorescent Dye-Labeled Liposomes
Published on: July 30, 2020
Comparative study on pharmacokinetics of extract from Bufonis venenum and its liposomes
Yun Liu1, Yizhu Luo2, Ming Li2
1School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai, China; National Innovation Platform for medical industry-education integration, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
Bufonis venenum extract-liposomes (BVE-LP) enhance drug exposure and reduce clearance of active compounds compared to traditional Bufonis venenum extract (BVE). This liposomal formulation offers a promising therapeutic option for improved delivery of Bufonis venenum components.
Area of Science:
- Pharmacology and Pharmaceutics
- Drug Delivery Systems
- Natural Product Chemistry
Background:
- Bufonis venenum contains bufadienolides and indolealkylamines with rapid clearance and low bioavailability.
- These active components are associated with significant adverse effects.
- Challenges exist in simultaneously loading lipophilic and hydrophilic compounds from Bufonis venenum extract.
Purpose of the Study:
- To develop and characterize Bufonis venenum extract-liposomes (BVE-LP) for improved drug delivery.
- To compare the pharmacokinetic profiles of BVE-LP against traditional Bufonis venenum extract (BVE).
- To evaluate the potential of BVE-LP in reducing toxicity and enhancing therapeutic efficacy.
Main Methods:
- Preparation and characterization of Bufonis venenum extract-liposomes (BVE-LP).
- Development of an ultra-high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) assay for simultaneous detection of 12 chemical components.
- Pharmacokinetic studies in Sprague-Dawley (SD) rats comparing BVE-LP and BVE groups.
Main Results:
- BVE-LP significantly increased the area under the plasma concentration-time curve (AUC0-t) for 5-hydroxytryptamine by 72.36% compared to BVE.
- Exposure (AUC0-t) of key bufadienolides (desacetylcinobufotalin, desacetylcinobufagin, arenobufagin, telocinobufagin) was notably higher in the BVE-LP group.
- Liposomal formulation resulted in decreased clearance and increased terminal half-life (t1/2) for several bufadienolides and indolealkylamines.
Conclusions:
- BVE-LP demonstrates a slower elimination rate and enhanced systemic exposure of active Bufonis venenum components.
- The liposomal formulation effectively addresses the bioavailability and toxicity challenges associated with traditional Bufonis venenum extract.
- BVE-LP presents a viable therapeutic strategy for effective delivery and improved clinical outcomes of Bufonis venenum.
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