Researchers have created nanoparticles to increase the solubility of probucol, a nearly insoluble drug used to reduce cholesterol, with a technique that could be used for other drugs.
By using the formulation technique the researchers believe they could improve the solubility, bioavailability and efficiency of other hydrophobic drugs and organic compounds that are limited by insolubility.
The research was published online on March 12 in Molecular Pharmaceutics and details a process of cogrinding probucol with sodium dodecylsulfate and methacrylic copolymer.
By doing this the researchers, who are from Nihon University, Japan and the University of Michigan, US, created 72nm nanoparticles that were stable in an acidic buffer.
Stability in acidic environments means that the formulation will pass through the stomach before undergoing rapid release in the intestine. The nanoparticles were then spray-coated on to larger carrier particles to make them easier to handle and make oral administration possible.
Investigations into the bioavailability of the nanoparticles in the intestine were then performed using Caco-2 cells, which are commonly used in adsorption tests, and showed that the formulation permeates the cell membrane.
Cogrinding brings cost and environmental benefits
The researchers believe that their technique, which is subject to “ongoing investigations” into its broader pharmaceutical applications, offers cost and environmental benefits when compared to other methods of reducing particles to nanoscale.
These benefits are realised because cogrinding is a simple procedure that can be performed without solvents, which differentiates it from other techniques such as supercritical fluid processing or high pressure homogenisation.
The complete research paper can be found here .