The Effect of the Particle Size Reduction on the Biorelevant Solubility and Dissolution of Poorly Soluble Drugs with Different Acid-Base Character

Abstract

Particle size reduction is a commonly used process to improve the solubility and the dissolution of drug formulations. The solubility of a drug in the gastrointestinal tract is a crucial parameter, because it can greatly influence the bioavailability. This work provides a comprehensive investigation of the effect of the particle size, pH, biorelevant media and polymers (PVA and PVPK-25) on the solubility and dissolution of drug formulations using three model compounds with different acid-base characteristics (papaverine hydrochloride, furosemide and niflumic acid). It was demonstrated that micronization does not change the equilibrium solubility of a drug, but it results in a faster dissolution. In contrast, nanonization can improve the equilibrium solubility of a drug, but the selection of the appropriate excipient used for nanonization is essential, because out of the two used polymers, only the PVPK-25 had an increasing effect on the solubility. This phenomenon can be explained by the molecular structure of the excipients. Based on laser diffraction measurements, PVPK-25 could also inhibit the aggregation of the particles more effectively than PVA, but none of the polymers could hold the nanonized samples in the submicron range until the end of the measurements.

Modified Curcuminoid-Rich Extract Liposomal CRE-SDInhibits Osteoclastogenesis via the Canonical NF-κB Signaling Pathway

“…Wahyudiono et al reported that the injection of a greater concentration of phospholipids, comprising POPC, into a medium brings about an enhancement in liposome size and PDI [ 53 ]. Previous studies by Csicsák et al and Lee mentioned that the reduction in the size of drug particles can increase their surface area, resulting in an improvement in their dissolution and bioavailability, along with a narrow size distribution for drug particles [ 54 , 55 ]. In other words, decreasing the concentration of POPC utilized to produce liposomal CRE-SD may lead to reduced liposome size and PDI, as well as enhanced bioavailability.…”

Effects of Cuminum cyminum L. essential oil and its nanoemulsion on oxidative stability and microbial growth in mayonnaise during storage

“…Droplet size and microstructure of CEONIn general, reducing the particle size leads to an increase in the surface area of particles(Csicsák et al, 2023), especially at the nanoscale. Reducing the average size of essential oil droplets in the nanoemulsion system increases the availability of bioactive compounds and as a result, the antioxidant and antimicrobial properties of the nanoemulsion compared with pure essential oil(Sharifi & Sharifi, 2023).…”