Microcrystals for dissolution rate enhancement of poorly water-soluble drugs

Solubility Enhancement of Lornoxicam by Crystal Engineering

“…The most common causes of low oral bioavailability are poor solubility and low permeability of active pharmaceutical ingredient (API) [1] . Multiple approaches have been adopted to improve the solubility of poorly water soluble APIs including micronization [2] , complexation with cyclodextrins [3] , cosolvency [4,5] , solid dispersions [6] , salt forms [7] , nanoparticles [8] and surfactants [9] , etc. Cocrystals are a class of multicomponent molecular crystals demonstrated to enhance the solubility, bioavailability and/or stability of API, which has been proposed as a unique crystal engineering approach to alter the physicochemical properties of compounds [10][11][12] .…”

AC and DC electrospinning of hydroxypropylmethylcellulose with polyethylene oxides as secondary polymer for improved drug dissolution

“…Among other physical approaches such as nanosuspensions (Müller et al, 2001), crystallization techniques (Fages et al, 2004;Rasenack and Müller, 2002) and the use of solubilizers (e.g., surfactants (Lawrence and Rees, 2000;Pouton, 1997) and cyclodextrins (Brewster and Loftsson, 2007)), polymerbased solid dispersions has received a great deal of attention to overcome the hurdle of limited solubility (Vasconcelos et al, 2007). Amorphous solid dispersion of a drug in an inert water-soluble matrix (most often a polymer) ensure improved dissolution owing to three reasons: on the one hand higher solubility of the amorphous drug, on the other hand the wellsoluble hydrophilic carrier used, thirdly an increased surface area can be obtained depending on the preparation method (Nagy et al, 2012).…”

Natural halloysite nanotubes as mesoporous carriers for the loading of ibuprofen

“…A potential advantage of nanocrystal or amorphous IBU is that it could improve its bioavailability. Rasenack et al [60] demonstrated that the microcrystal forms of poorly water-soluble drugs could enhance their dissolution rates. Shen et al also found that nanocrystal [59] or amorphous [61] IBU had a higher bioavailability than crystalline IBU in bulk, because of a faster dissolution rate.…”