The use of albumin solid dispersion to enhance the solubility of unionizable drugs

Abstract

In this study, solid dispersions of prednisolone (PRD) and bovine serum albumin (BSA) were prepared by spray drying and freeze drying methods using a PRD:BSA solution [20:1 molar ratio (MR)]. PRD-BSA dispersed mixtures were characterized by scanning electron microscopy (SEM), and powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). PRD-BSA physical and dispersed mixtures showed significantly higher solubility in water than that of unprocessed drug. Enhancement factor of six was obtained in both physical mixture and solid dispersion solubility studies. In-vitro dissolution and release studies under physiological conditions showed an immediate release of PRD from the solid dispersions, with almost 90% of the drug dissolved in the first 10 min. PRD was immediately released from BSA binding complex. This study demonstrates the potential for the use of BSA to enhance the solubility and dissolution rate, hence bioavailability, of the unionizable drugs.

Thermostable small-molecule inhibitor of angiogenesis and vascular permeability that suppresses a pERK-FosB/ΔFosB–VCAM-1 axis

“…Adding serum to the diluent increased BT2 solubility (fig. S9B), consistent with reports that serum albumin can increase the dissolution of unionizable drugs ( 39 ). Neither BT2-MeOA nor any other BT2 analog had the ability to inhibit serum-inducible proliferation ( Fig.…”

Formulation of Nifedipine–Polyvinyl Pyrrolidone (PVP) Solid Dispersion System and Intrinsic Dissolution Rate Evaluation

“…Maximum wavelength scanning results in nifedipine readings having to be performed at a wavelength of 339 nm. The wavelengths of 208 nm and 239 nm were not chosen because readings of levels at these wavelengths could be disturbed due to the influence of the cut-off wavelength of the methanol solvent, which also has a UV cut-off wavelength of 205 nm (Khoder et al, 2018).…”

Potential Use of the Maillard Reaction for Pharmaceutical Applications: Gastric and Intestinal Controlled Release Alginate-Albumin Beads

“…Figure 1C shows the sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS-PAGE) pattern of BSA and BSA-ALG conjugates. Untreated BSA revealed a single band in the range of 60 kDa, reflecting the molecular weight of this molecule [24]. It is worth mentioning that the intensity of BSA bands decreased steadily as the Maillard progressed (lanes 3–7) [4,5].…”