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Published on: February 9, 2019
Long circulating lipid nanocapsules for drug detoxification
Anand Babu Dhanikula1, Nabil Mohamed Khalid, Stephen D Lee
1Canada Research Chair in Drug Delivery, Faculty of Pharmacy, C.P. 6128 Succ. Centre-ville, Montreal, QC, Canada H3C 3J7.
Biomaterials
|November 28, 2006
Summary
Lipid nanocapsules (NC) can sequester drugs like haloperidol and docetaxel, reducing free drug levels and increasing blood drug concentrations. These findings suggest NCs are effective parenteral detoxifying colloids.
Area of Science:
- Nanotechnology
- Pharmacology
- Drug Delivery
Background:
- Lipid nanocapsules (NC) are investigated as potential drug delivery systems.
- Poly(ethylene glycol) (PEG)-decorated NC offer modified properties for drug sequestration.
- Medium chain triglycerides form the core of these nanocapsules.
Purpose of the Study:
- To evaluate uncoated and PEG-decorated lipid nanocapsules (NC) as parenteral detoxifying colloids.
- To assess the in vitro and in vivo ability of NC to sequester haloperidol, docetaxel, and paclitaxel.
- To determine the impact of NC on drug distribution and efficacy.
Main Methods:
- In vitro studies of drug uptake by NC based on drug nature and NC composition.
- Inclusion of complexing fatty acids to enhance haloperidol affinity.
- Plasma lipoprotein distribution studies.
- Cytotoxicity assays to assess drug-carrier interactions.
- In vivo studies in mice using docetaxel and different administration sequences (NC-DTX, PEG(NC)-DTX, DTX-PEG(NC)).
Main Results:
- In vitro drug uptake varied with drug type and NC composition; maximal haloperidol affinity was achieved with a complexing fatty acid.
- NC significantly increased the association of haloperidol and docetaxel with triglyceride-rich lipoproteins.
- NC reduced free drug concentrations, leading to decreased antiproliferative activity of docetaxel in cytotoxicity studies.
- In vivo, NC increased blood levels of docetaxel regardless of administration sequence due to in situ sequestration.
Conclusions:
- Lipid nanocapsules demonstrate potential as parenteral detoxifying colloids.
- NC can effectively sequester drugs with high lipophilicity, modulating their distribution and efficacy.
- The findings support the use of lipid NC for managing drug levels and toxicity.
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