With an aim to preserve the life of existing antibiotics and to guide better clinical decisions, Venus Medicine Research Centre, the research wing of Venus Remedies Limited, has developed a unique platform called Stealth Targeted Nanoparticles (STN). STN is a novel concept of stealth-targeted nanomedicine. It employs a polymeric backbone with stealth properties to bypass macrophagic detection by body's immune system, along with a targeting moiety for delivering the drugs with "zero" or very low oral bioavailability of BCS Class 3/4 like Ceftazidime, Ceftriaxone, Meropenem, Vancomycin, many other BL + BLI combinations through the intestine and achieve serum concentrations sufficient to produce the desired pharmacodynamic effect. This biodegradable and biocompatible platform removes the inherent hurdles of permeability and solubility posed by these drugs.
The platform has been tested on multiple IV drugs like Ceftriaxone, Meropenem, and Vancomycin in the early proof-of-concept studies. These were developed as pH-sensitive, stealth-targeted nanoparticles with a size range around 20 to 200 nm. In vivo pharmacokinetic studies after oral administration in Albino Wistar rats revealed relative bioavailability of these drugs up to 70 percent compared to IV administration (unpublished data). Caco-2 cell uptake studies in VRP001 (a novel BL+BLI combined with a very poor bioavailability of the main beta-lactam drug) revealed higher uptake of targeting-ligand functionalized nanoparticles in comparison with their plain counterparts and pristine drug solutions. Further studies revealed a spherical shape of nanoparticles with a smooth surface, exhibiting excellent stability in simulated biological fluids, a high melting point, and no chemical molecular interaction. An amorphous molecular level dispersion of the drug in the matrix was observed, allowing increased absorption.
STN delivered antibiotics due to its size, bioavailability and targeting ligand is suspected to have the same blood/tissue concentrations as its IV counterpart, which will also lead to the same therapeutic response.
The resultant product from the STN platform is a drug-containing nanoparticle matrix that is easily dissoluble in water and other fluids. This was done to increase therapy compliance among the pediatric and geriatric set of patients that are most susceptible to URIs. STN delivered antibiotics due to its size, bioavailability and targeting ligand is suspected to have the same blood/tissue concentrations as its IV counterpart, which will also lead to the same therapeutic response. We strongly believe that this platform is a promising tool for oral delivery of poorly bioavailable drugs, especially those for which IV formulations are already available and are widely used.
The rational use of economic resources is as important as the consistent use of clinical resources, and this importance is especially significant for antibiotics, which represent a significant portion of health care expenses. STN has the potential to redefine the economics of antibacterial drug development, improving ROI and Incentivising innovators to re-explore anti-infective research. This may, in turn, help us avoid a post-ant.
Formulation development is the core (sanctum sanctorum) art and science of preparation.More
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