Enhanced dissolution and systemic availability of albendazole formulated as solid dispersions

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Pharmacokinetics

Background:

• Albendazole (ABZ) is an anthelmintic drug with poor aqueous solubility.
• Solid dispersions (SDs) are a strategy to improve the bioavailability of poorly soluble drugs.
• Pluronic 188 (P 188) and polyethylene glycol 6000 (PEG 6000) are hydrophilic polymers used as carriers in SDs.

Purpose of the Study:

• To formulate and characterize solid dispersions of albendazole (ABZ) with Pluronic 188 (P 188) and polyethylene glycol 6000 (PEG 6000).
• To evaluate the effect of these SDs on ABZ dissolution rates and systemic availability.
• To assess the utility of pharmacokinetic assays in mice for preliminary drug formulation screening.

Main Methods:

• Formulation of albendazole solid dispersions using P 188 and PEG 6000.
• Solid-state characterization of drug-polymer interactions.
• In vitro dissolution studies.
• In vivo pharmacokinetic studies in mice, measuring AUC and Cmax.

Main Results:

• P 188 significantly enhanced ABZ dissolution rates compared to PEG 6000, particularly within the first 30 minutes.
• ABZ-P 188 SDs resulted in a statistically significant increase in systemic availability (50% enhancement in AUC, 130% increase in Cmax) compared to an ABZ suspension.
• ABZ-PEG 6000 SDs did not show a statistically significant improvement in systemic availability compared to the control.

Conclusions:

• Pluronic 188 is a more effective carrier than PEG 6000 for promoting albendazole dissolution and enhancing its systemic exposure.
• Solid dispersions formulated with P 188 offer a promising approach to improve the pharmacokinetic profile of albendazole.
• Pharmacokinetic studies in mice serve as a valuable model for early-stage drug formulation screening.