Modulation of particle size and molecular interactions by sonoprecipitation method for enhancing dissolution rate of poorly water-soluble drug

Abstract

Aim of present work was to originally elucidate the roles of ultrasonication method for modulating the size and molecular interactions in controlling release of poorly water-soluble drug. Curcumin was chosen as a model drug. Three types of polymers were investigated as carriers for preparation of polymeric nanoparticles under various ultrasonication conditions and polymer-drug ratios. Changes in drug crystallinity, particle size, and molecular interactions which would be factors enhancing drug dissolution rate were evaluated. Amorphous form of curcumin, size reduction of nanoparticles and interaction between drug and polymer in formulations were attributed to improved drug dissolution rate. Particle size was strongly affected by polymer type, polymer-drug ratio and ultrasonication conditions. Interestingly, control of those factors caused differences in molecular interactions of the hydroxyl groups and then, highly affected particle size of the nanoparticles. It was obvious that there was a reciprocal influence between the drug-polymer interactions and particle size of the nanoparticles. This relation could be modulated by polymers and ultrasonication processes for enhancing drug dissolution rate.

Effect of Particle Size and Polymer Loading on Dissolution Behavior of Amorphous Griseofulvin Powder

“…Effective delivery of Biopharmaceutics Classification System class II active pharmaceutical ingredients (APIs), defined as having high permeability and low solubility, 1 is challenging due to their low bioavailability. 2 To enhance their bioavailability, several technologies have been examined, such as particle size reduction, [3][4][5] cyclodextrin complexes, 6 polymeric micelles, 7 freeze-dried liposomes, 8 solid lipid nanoparticles, 9 and amorphous solid dispersions (ASDs). 10,11 Among them, amorphous solids dispersions technology has been proved to be one of the promising solutions.…”

“…26 Fine APIs are widely used for enhancement of available surface areas and hence dissolution rates. 4,[27][28][29][30] In addition, faster dissolution rates result in shorter residence time of API powders in the dissolution media, which is expected to reduce the time available for recrystallization of ASDs. This may in turn lower the amounts of polymeric crystallization inhibitor needed.…”

Development of a modified – solid dispersion in an uncommon approach of melting method facilitating properties of a swellable polymer to enhance drug dissolution

“…Specifically, solubility of CUR at pH 1.2 and pH 6.8 were 7.230 AE 0.35 and 12.6 23 AE 3.54, respectively. For this reason, most dissolution release rate of CUR from SDs in the current studies in intestinal fluid (pH 6.8) was faster than that in gastric fluid (pH 1.2) and the percentage of pure CUR released in these media was under 5% in previous studies (Tran et al, 2015). Therefore, the improvement of dissolution rate in these conditions was discovered.…”

Enhancement of Curcumin Solubility by Phase Change from Crystalline to Amorphous in Cur‐TPGS Nanosuspension

“…It has been also reported that sonication process was very effective to decrease particle size and produce homogeneous colloidal system by reducing agglomeration through management of nucleus growth condition and population (Luque de Castro and Priego‐Capote ; Vasconcelos and others ; Abbas and others ). Reduced particle size may improve water solubility and dissolution rate of the water insoluble compounds which can correlate with substantial enhancement of oral bioavailability (Tran and others ). PDI values were also significantly decreased after UH and maintained less than 0.3 which means that Cur‐TPGS NSs were maintained in high homogeneity after UH.…”