Introduction
The technique of including a solubilizing agent or coupling agent during the process of active loading has shown to significantly increase the encapsulation of water-insoluble drugs into lipid-based nanoparticles.
Figure 1. Schematic diagram of the mechanism of active loading of water-insoluble drugs
Figure 2. Cryo-TEM images of the drug free lipid-based nanoparticles (left) and the Staurosporine lipid-based nanoparticles in the presence of 5% DMSO during the Staurosporine loading. Scale bar represents 100 nm.
Applications
A Simple and Improved Active Loading Method to Efficiently Encapsulate Staurosporine into Lipid-Based Nanoparticles for Enhanced Therapy of Multidrug Resistant Cancer (Tang et al., 2016) https://link.springer.com/article/10.1007/s11095-015-1854-4
- Increase solubility
- Prolong pharmacokinetics of drugs
- Enhance efficacy of drugs
Other Applications
- Develop rapidly dissolvable pediatric formulation with complete taste masking, as measured by E-tongue
- Sustained drug release for prolonged effect