Friday , 3 February 2023

DissoCubes: A Novel Formulation to Enhance Solubility

About author
S.S Siddheshwar*, S.B. Somwanshi, R.T. Dolas, A.N. Merekar, R.K. Godge, S. R. Pattan
Department of Pharmaceutics, P.R.E.S.’s, Pravara Rural College of Pharmacy, Loni.
Department of Pharmaceutical Chemistry, P.R.E.S.’s, Pravara Rural College of Pharmacy, Loni.
E-mail: ssiddheshwar@gmail.com

Abstract
Most of drugs are poorly soluble and have bioavailability problems. Therefore, there is an urgent need to find solutions for the formulation of these poorly soluble drugs. To achieve a broadly applicable technology, increasing interest has been focused on drug nanoparticles in the last few years. Going beyond micronization leads to a further increase in the dissolution velocity due to an even larger surfacearea. An additional effect can be achieved by a controlled structural change in drug nanoparticles, which means reducing the crystallinity and increasing the amorphous fraction eg Dissocubes. DissoCubes are crystalline nanoparticles of active substance obtained by a liquid state high energy process using a high pressure piston gap homogenizer to reduce the drug particle size in the presence of surface modifiers that associate at the freshly generated drug interface. A particle size reduction from approximately 50µm to about 0.5µm is achieved resulting in a very homogenous and stable formulation. The nanosuspensions could be formulated into various dosages forms. DissoCubes™ technology is a technology of choice for molecules with oral bioavailability issues and/or requiring rapid onset of absorption. However, there are two more interesting features of drug nanoparticles (i.e.,DissoCubes): (a) an increase in saturation solubility and (b) structural changes inside the particles.
Key words: DissoCubes, nanoparticles, nanosuspensions.
Introduction
Most of drugs are poorly soluble and have bioavailability problems. Therefore, there is an urgent need to find solutions for the formulation of these poorly soluble drugs. Preferably, such a new formulation principle should be applicable to almost any poorly soluble drug, independent of its chemical structure and spatial molecular dimensions. A simple approach to improve the bioavailability of orally administered drugs is micronization. However, especially for drugs with a low saturation solubility, the achieved increase in dissolution velocity might not lead to sufficiently high blood levels. Therefore, alternative formulation techniques to existing approaches need to be developed. To achieve a broadly applicable technology, increasing interest has been focused on drug nanoparticles in the last few years. Going beyond micronization leads to a further increase in the dissolution velocity due to an even larger surfacearea. An additional effect can be achieved by a controlled structural change in drug nanoparticles, which means reducing the crystallinity and increasing the amorphous fraction. Examples of drug nanoparticles with structural changes are the products NanoMorphTM marketed by Knoll/BASF Pharma (company brochure) and the drug nanosuspensions marketed under the name DissoCubes . DissoCubes combine the advantages of using a size reduction technique (i.e., NonoCrystals) with the advantages of a precipitation technique(i.e., HydrosolsTM, NanoMorphTM) opening the opportunity to induce structural changes, which means increasing the amorphous fraction.

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