In situ formation of nanoparticles upon dispersion of melt extrudate formulations in aqueous medium assessed by asymmetrical flow field-flow fractionation

Challenges and Strategies in Thermal Processing of Amorphous Solid Dispersions: A Review

“…The addition of surfactants can also be leveraged in ASDs to facilitate stability of nano/microdispersions formed in situ from the melt-extruded drug product once dispersed in aqueous media, as in the case of ritonavir and lopinavir extrudate produced by Meltrex® technology (78,79). In situ formation of nanoparticles released from the drug product has been shown to enhance dissolution rates and the use of surfactants can aid in the prevention of coalescence of these aggregates, with charge repulsion identified as a likely mechanism (80).…”

Impact of Solubilizing Additives on Supersaturation and Membrane Transport of Drugs

“…In addition, at very high supersaturations, a non-crystalline drug-rich may be formed (17)(18)(19). Formation of a disordered drug-rich phase has been widely observed during dissolution of amorphous solid dispersions (20)(21)(22)(23)(24)(25)(26). Certain polymers are believed to facilitate formation of this disordered phase by inhibiting crystallization and can stabilize the resultant drugrich phase in the nano-sized regime (23,24).…”

Using Environment-Sensitive Fluorescent Probes to Characterize Liquid-Liquid Phase Separation in Supersaturated Solutions of Poorly Water Soluble Compounds

“…Aisha et al (2) reported colloid formation in solid dispersions of mangostin and PVP whereas Friesen et al (3) and Alonzo et al (4) made similar observations with amorphous solid dispersions of poorly water soluble drugs prepared with hydroxypropylmethyl cellulose acetate succinate (HPMCAS) and hydroxypropylmethyl cellulose (HPMC) respectively. More recently, aggregates have also been observed during the dissolution of ritonavir solid dispersions (5). Supersaturated solutions generated by methods other than dissolution of amorphous solid dispersions can also exhibit nano-aggregate formation.…”