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Oral Delivery Platform for Lipophilic drugs based on Pro-Nano Lipospheres

Domb Abraham, HUJI, School of Medicine - IMRIC, School of Pharmacy- Institute for Drug Research
Hoffman Amnon, HUJI, School of Medicine - IMRIC, School of Pharmacy- Institute for Drug Research

 

Categories:

Life Science & Biotechnology

Technology Keywords:

Formulation, drug delivery, increased bioavailability

Development Stage:

POC in Human

 

Highlights

The P-gp efflux and oxidative Phase I metabolism are major predicaments in drug absorption and oral delivery of small molecules. The Pro-Nano Lipospheres  vehicle 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. 

Our Innovation

  • The PNL formulation is composed of GRAS status[1] materials
  • Enables oral administration of drugs, which is a key component in patient compliance compared to other routes.
  • Overcomes absorption obstacles of lipophilic drugs: improved solubility in the GI tract and decreased intestinal first pass metabolism
  • The ratio between components can be adjusted so that an optimal nano emulsion is formed with a plethora of compounds. 

Technology

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.

  • The formulation self emulsifies in the GI milieu forming an O/W nano emulsion with particle size of 50nm and less (Figure 1)

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Figure 1: Clear o/w nano-emulsion formation upon PNL dilution with water

 

 

Opportunity

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 

 

[1] GRAS - Generally Recognized As Safe

Patent Status

Granted US 7,919,113

Contact for more information:

Ariela Markel
VP, Business Development, Healthcare
+972-2-6586608