Oral Delivery Platform for Lipophilic Drugs Based on Pro-Nano Lipospheres
Cluster9 Dispersible Concentrate Lipospheres for the Delivery of Agents (PNL) Project ID : 6-2017-4492
Summary of the technology
Dispersible Concentrate Lipospheres for the Delivery of Agents (PNL)
Project ID : 6-2017-4492
Description of the technology
Categories: Life Science & Biotechnology Technology Keywords: Formulation, drug delivery, increased bioavailability Development Stage: POC in Human
Life Science & Biotechnology
Formulation, drug delivery, increased bioavailability
POC in Human
The P-gp efflux and oxidative Phase I metabolism are major predicaments in drug absorption and oral delivery of small molecules. The Pro-Nano Lipospheresvehicle serves as a platform for the successful oral delivery of lipophilic drugs. The proposed formulation improves the oral administration of clinically relevant molecules, which are otherwise prone to low oral bioavailability.
The poorly absorbed drug is dissolved in the oily formulation. Upon contact with water, the formulation forms nano particles. Theses nano particles trap the lipophilic components in their lipid core. Thus, the lipophilic drug is solubilized in the aqueous environment of the GI. When reaching the intestine monolayer, the formulation’s excipients (surfactants and medium chain triglyceride) diminishes the drug’s metabolism and efflux from the enterocytes.
Figure 1: Clear o/w nano-emulsion formation upon PNL dilution with water
Many of today’s leading compounds and drugs in pipeline fail to reach clinical stages due to poor oral bioavailability. This formulation presents an ideal, simple solution for the optimal oral delivery of these compounds and a direct to clinic development.
Increase in oral bioavailability leads a lower inter and intra subject variability
 GRAS - Generally Recognized As Safe