Establishment of a solvent map for formation of crystalline and amorphous paclitaxel by solvent evaporation process

Abstract

This study intended to establish a solvent map for formation of crystalline and amorphous paclitaxel by a solvent evaporation process. Crystalline paclitaxel was produced by evaporation with polar solvents (acetone, acetonitrile, ethanol, isobutyl alcohol, methanol, methyl ethyl ketone, and n-butyl alcohol) having a polarity index above 4.00. On the other hand, amorphous paclitaxel was produced by evaporation with non-polar solvents (methylene chloride, n-butyl chloride, and toluene) having a polarity index of about 4.00 or lower. The formation of paclitaxel was very closely associated with the polarity index of the organic solvent used in the solvent evaporation process. In the case of crystalline paclitaxel, the higher the polarity index and the lower the viscosity of the organic solvent (n-butyl alcohol, methyl ethyl ketone, and acetonitrile), the higher the degree of crystallinity. In the case of amorphous paclitaxel, the shape and size of particles varied according to the solvent (methylene chloride, n-butyl chloride, and toluene) used in the solvent evaporation process.

μMESH-Enabled Sustained Delivery of Molecular and Nanoformulated Drugs for Glioblastoma Treatment

“…Therefore, especially at the higher concentrations in acetonitrile (i.e., 50 mg/mL), DTXL is expected to appear in the form of drug crystals, whereas PTXL would still be in its molecular form (Supporting Figure 3). 26 Importantly, regardless of the input amounts, the DTXL solutions were easily and uniformly spread within the ridges of the PVA microlayer, thus resulting in higher loaded amounts than those for PTXL.…”

<p>Formulation and evaluation of simvastatin polymeric nanoparticles loaded in hydrogel for optimum wound healing purpose</p>

“…The technique of SIM PoNP preparation mainly depended on dissolving the SIM in an organic solvent (acetone or methylene chloride); then, the organic solvent was mixed with an aqueous phase containing a water-soluble polymer 35. In general, SIM is poorly soluble in water26 and freely soluble in both acetone and methylene chloride,13 but acetone has a higher polarity index (5.1) and high water solubility (100% w/w) compared with methylene chloride, which has a lower polarity index (3.1) and low water solubility (1.6% w/w) 36,37. The low drug content values of formulae prepared with methylene chloride as an organic solvent were mainly due to its low water solubility as it prevented the SIM from diffusing freely into the water-soluble polymer, while using acetone as an organic solvent allowed a higher drug entrapment due to its more hydrophilic nature, which helped the drug to be retained in the water-soluble polymer 7.…”