Albendazole, a vital medication endorsed by the World Health Organization for combating parasitic infections, encounters a challenge stemming from its low solubility, significantly impeding absorption and bioavailability. Albendazole has near-insolubility in most organic solvents, so the solid dispersions of albendazole were predominantly using the fusion method. However, the solvent method could offer the advantage of achieving molecular-level mixing homogeneity. In this investigation, we incorporated the pH adjustment to prepare albendazole solid dispersion using a solvent method, which utilizes trace amounts of HCl in methanol, yielding notably enhanced albendazole solubility. Subsequently, carriers such as PEG6000/Poloxamer 188 (PEG: polyethylene glycol) and PVP K30/Poloxamer 188 (PVP: polyvinylpyrrolidone) were employed to create albendazole solid dispersions. Comprehensive characterization through dissolution rate analysis, PXRD (Powder X-ray diffraction), SEM (Scanning electron microscopy), DSC (differential scanning calorimetry), and pharmacokinetic (PK) studies in mice and rats was conducted. The findings indicate that the solid dispersion effectively transforms the crystalline state of albendazole into an amorphous state, resulting in significantly enhanced in vivo absorption and a 5.9-fold increase in exposure. Besides, the exposure increased 1.64 times of commercial albendazole tablets. Notably, PEG6000/Poloxamer 188 and PVP K30/Poloxamer 188 solid dispersions exhibited superior dissolution rates and pharmacokinetic profiles compared to commercially available albendazole tablets.

Download : Download high-res image (76KB)Download : Download full-size image

Albendazole, a vital medication endorsed by the World Health Organization for combating parasitic infections, encounters a challenge stemming from its low solubility, significantly impeding the absorption and bioavailability. In this investigation, we engaged the pH adjustment to prepare albendazole solid dispersion using a solvent method, which utilizing trace amounts of HCl in methanol, yielding notably enhanced albendazole solubility. Subsequently, carriers such as PEG6000/Poloxamer 188 and PVP K30/Poloxamer 188 were employed to create albendazole solid dispersions. The solid dispersion effectively transforms the crystalline state of albendazole into an amorphous state, resulting in significantly enhanced in vivo absorption and a 5.9-fold increase in exposure. Besides, the exposure increased 1.64 times of commercial albendazole tablets. The albendazole solid dispersion using PEG6000/Poloxamer 188 and PVP K30/Poloxamer 188 as carrier through solvent method exhibited superior dissolution rates and pharmacokinetic profiles compared to commercially available albendazole tablets.

Image for graphical abstract

Albendazole

Solid dispersion

Dissolution rate

Bioavailability

Solvent method

The data that has been used is confidential.

© 2024 The Authors. Published by Elsevier B.V.