Poorly-water-soluble compounds are difficult to develop as drug products using conventional formulation techniques and are frequently abandoned early in discovery. The use of media milling technology to formulate poorly-water-soluble drugs as nanocrystalline particles offers the opportunity to address many of the deficiencies associated with this class of molecules. NanoCrystal Technology is an attrition process wherein large micron size drug crystals are media milled in a water-based stabilizer solution. The process generates physically stable dispersions consisting of nanometer-sized drug crystals. Nanocrystalline particles are a suitable delivery system for all commonly used routes of administration, i.e. oral, injectable (IV, SC, and IM) and topical applications. In addition, aqueous dispersions of nanoparticles can be post-processed into tablets, capsules, fast-melts and lyophilized for sterile product applications. The technology has been successfully incorporated into all phases of the drug development cycle from identification of new chemical entities to refurbishing marketed products for improving their performance and value.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/s0928-0987(02)00251-8 | DOI Listing |
Int J Pharm
January 2025
Institut Galien Paris-Saclay, CNRS UMR8612, 17 avenue des Sciences, 91400 Orsay, France. Electronic address:
Multiparticulate drug delivery systems offer advantages in controlled release, dose flexibility, and personalized medicine. Fusion prilling, a process that produces spherical lipid-based microparticles through vibrating nozzles, is gaining interest in the field. This study aims to explore the use of fusion prilling to encapsulate crystallizable water-in-oil emulsions, enabling the incorporation of hydrophilic active pharmaceutical ingredients (APIs) within lipid matrices.
View Article and Find Full Text PDFPharmaceutics
December 2024
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia.
One of the major challenges in dermal drug delivery is the adequate penetration of the active compound into the skin without causing any skin irritation and inflammation. Nanocrystals (NCs) are nanoscale particles, and their sizes are below 1000 nm. NCs are made up of drug particles only, which are used to improve the aqueous solubility and bioavailability of poorly water-soluble drugs.
View Article and Find Full Text PDFYakugaku Zasshi
January 2025
Graduate School of Pharmaceutical Sciences, Osaka University.
In recent years, functional foods have attracted increasing attention due to growing health consciousness. When functional food ingredients are poorly water-soluble, they largely fail to be absorbed due to their low solubility in the digestive tract, limiting their ability to exert their functions. To develop poorly water-soluble compounds into viable functional food ingredients, it is important to increase their gastrointestinal absorption so that they can fully exert their functions, and to ensure their safety and efficacy through ADMET research.
View Article and Find Full Text PDFCarbohydr Res
December 2024
Department of Physics, Rayat Shikshan Sanstha's Dada Patil Mahavidyalaya, Karjat, Dist - Ahemadnagar, M.S. 414 402, India.
The discovery of branched molecules like dextrin by Schardinger in 1903 marked the inception of cyclodextrin (CD) utilization, catalyzing its journey from laboratory experimentation to widespread commercialization within the pharmaceutical industry. CD, a cyclic oligosaccharide containing glucopyranose units, acts as a versatile guest molecule, forming inclusion complexes (ICs) with various host molecules. Computational studies have become instrumental in elucidating the intricate interactions between β-CD and guest molecules, enabling the prediction of binding energy, forces, affinity, and complex stability.
View Article and Find Full Text PDFEur J Pharm Sci
January 2025
Soft Matter Chemistry, Department of Chemistry, and Helsinki Institute of Sustainability Science, Faculty of Science, University of Helsinki, Helsinki 00014, Finland. Electronic address:
Improving the solubility of poorly water-soluble drugs is essential for enhancing bioavailability, formulation flexibility and reducing patient-to-patient variability. The preparation of amorphous solid dispersions (ASDs) is an attractive strategy to formulate such drugs, leading to higher apparent water solubility and therefore higher bioavailability. For such ASDs, water-soluble polymer excipients, such as poly(vinyl pyrrolidone) (PVP) or poly(vinyl pyrrolidone-co-vinyl acetate) (P(VP-co-VA)), are employed to solubilize and stabilize the drug against crystallization.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!