Active Loading of Insoluble or Membrane Impermeable Drugs into Liposomal Core


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.


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)

  • 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