Abstract
Cyclodextrins (CDs) and their derivatives significantly increase drug solubility by forming drug/CD complexes known as solid dispersions (SDs), which consist of an inclusion complex (IC), where the drug is entrapped within the CD cavity, and a non-IC. Here, the SDs of curcumin (CUR) and hydroxypropyl-β-cyclodextrin (HPβCD) were prepared using the grinding, freeze-drying (FD), and common solvent evaporation (CSE) methods and were physicochemically characterized using solubility, powder X-ray diffraction, Fourier transform infrared, differential scanning calorimetry, and dissolution studies. The second or higher order complex of CUR-HPβCD indicated the co-existence of ICs and non-ICs known as the SD system. When comparing the soluble drug amount with CUR crystals, the solubility of SDs was enhanced by up to 299-, 180-, and 489-fold, corresponding to the ground mixtures (GMs), freeze-drying mixtures (FDs), and common solvent evaporation mixtures (CSEs), respectively. The total transformation into the amorphous phase of CUR was observed in GMs and in CSE12, CSE14, and CSE18. The drug was well dispersed within HPβCD in GMs and CSEs, suggesting the formation of hydrogen bonds between CUR and HPβCD, whereas the dispersed behavior of FDs was similar to that of physical mixtures. In SDs, the melting temperature of CUR was in an increased order of CUR in 1:2 ICs, CUR in 1:1 ICs, and CUR crystals. The dissolution rate of CUR was positively improved as the amount of HPβCD in SDs increased. The SD system consisting of CUR and HPβCD significantly increased the drug solubility compared to ICs.
Highlights
Based on the solubility and permeability of active pharmaceutical ingredients (APIs) that regulate drug absorption, Amidon et al divided drugs into the following four categories [1]: class I, class II, class III, and class IV
The solid dispersions (SDs) system consisting of CUR and HPβCD significantly increased the drug solubility compared to inclusion complex (IC)
The second or higher order complex of CUR-HPβCD indicated the co-existence of ICs and non-ICs, known as the SD system
Summary
Based on the solubility and permeability of active pharmaceutical ingredients (APIs) that regulate drug absorption, Amidon et al divided drugs into the following four categories [1]: class I (high solubility–high permeability), class II (low solubility–high permeability), class III (high solubility–low permeability), and class IV (low solubility–low permeability). One of the basic goals of drug formulations is to improve the solubility of these two drug classes Numerous strategies such as spray-drying [3], co-solvency [4,5], solid dispersion [6,7,8], complexation [9,10], and hydrotrophy [5] are used to increase drug absorption, resulting in higher bioavailability. Pharmacy 2020, 8, 203 solvency [4,5], solid dispersion [6,7,8], complexation [9,10], and hydrotrophy [5] are used to increase drug absorption, resulting in higher bioavailability.
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