Nanoparticle Formulation for Eye-Drop

Lanolin based DDS for poorly-soluble compounds to deep inside of eyes

Advantage and Core Benefit

  •  Utilizes clinically available additives, does not contain toxic compounds.
  •  Simple manufacturing steps, easy to store and automatically preservative-free.
  •  Lanosterol, main component of lanolin has possibly disease-modifying effect for cataract.

Background and Technology

Many of pharmaceutical active ingredients (APIs) in ophthalmology are poorly soluble, and often used as suspensions. However corneal permeation rates are very low and most are excreted with tear. It is still more difficult to deliver drug through the eye to uvea, crystalline lens or retina.
We have established nanoparticle drug delivery system (DDS) utilizing medically used compounds and demonstrated the efficient delivery to the deep inside of the eyeball and therapeutic effects.
There are several other nanoparticle options, but they are often toxic, like liposomes, or high-cost production are required. Our nanoparticles are prepared by simple steps;

STEP1: Preparation of mixture of API and several additives including lanolin, alcohol,biocompatible polymer, and water.
STEP2: Rapid freezing with liquid nitrogen followed by freeze-drying to obtain drug nanoparticle powder in which alcohol has been removed.
STEP3: Resolving the powder in water by ultrasonic stirring and filtration by 0.22um sterilizing membrane.

Lanolin nanoparticle formulation may have disease modifying effect for cataract. It has been reported in journal Nature that lanosterol, one of a main components of lanolin reverses protein aggregation in cataracts (doi:10.1038/nature14650).  The problem is that lanosterol is hydrophobic and hard to dissolve in water thus eye-drop administration of lanosterol per se is extremely difficult.

Data Described in Patent

  • In Experimental autoimmune uveoretinitis (EAU) mouse model, nano-formulation had significant effects compared to commercially available fluorometholone eye drops.
  • Confirmed higher API concentration by nearly an order of magnitude at anterior chamber of rabbits.
  • In retinitis pigmentosa mouse model, calpain inhibitor nanoparticle reduced apoptosis at retina.

Patent

Patent No. JP.5900938.B2, EP.2842545.B1

Researcher

Koichi Baba (Department of Ophthalmology, Osaka University)

Expectations

We are seeking a company who will develop and commercialize this technology.
We can provide you with samples under CDA and MTA.
We recommend starting with dry-eye indication by fluorometholone.

Product No. KJ-03431

Medicine

Published

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