Abstract
The objective of this study was to improve the solubility of albendazole and optimize the preparation of an oral nanoparticle formulation, using β-cyclodextrin (βCD) and chitosan-tripolyphosphate (TPP) nanoparticles. The solubility of albendazole in buffers, surfactants, and various concentrations of acetic acid solution was investigated. To determine drug loading, the cytotoxic effects of the albendazole concentration in human hepatocellular carcinoma cells (HepG2) were investigated. The formulations were prepared by mixing the drug solution in Tween 20 with the chitosan solution. TPP solution was added dropwise with sonication to produce a nanoparticle through ionic crosslinking. Then the particle size, polydispersity index, and zeta potential of the nanoparticles were investigated to obtain an optimal composition. The solubility of albendazole was greater in pH 2 buffer, Tween 20, and βCD depending on the concentration of acetic acid. Drug loading was determined as 100 µg/mL based on the results of cell viability. The optimized ratio of Tween 20, chitosan/hydroxypropyl βCD, and TPP was 2:5:1, which resulted in smaller particle size and proper zeta positive values of the zeta potential. The chitosan-TPP nanoparticles increased the drug solubility and had a small particle size with homogeneity in formulating albendazole as a potential anticancer agent.
Highlights
Albendazole is a poorly water-soluble but highly permeable anthelmintic drug [1], classified as a type II drug based on the Biopharmaceutical Classification System
Because this process depends on the solubility of the drug, the solubility of albendazole in various pH buffers and surfactants was evaluated as a first step for optimizing the nanoparticle formulation
A minimum solubility of albendazole was found at pH 8 and solubility remained low over the pH 4–10 range, which was considered in the preparation of albendazole-loaded chitosan-TPP nanoparticles because chitosan is generally solubilized in 1% acetic acid
Summary
Albendazole is a poorly water-soluble but highly permeable anthelmintic drug [1], classified as a type II drug based on the Biopharmaceutical Classification System. The anticancer effects of albendazole were investigated [2,3], its antitumor efficacy is limited by low solubility. An appropriate solubilization formulation of albendazole is necessary to increase drug efficacy. Β-cyclodextrin (βCD) is an efficient carrier for the delivery of albendazole [4,5]. Cyclodextrins (CDs) are cup-shaped molecules with hydrophobic cavities and hydrophilic exteriors that can interact with various hydrophobic guest molecules to form supramolecular inclusion complexes [6,7]. CDs have been exploited to enhance the bioavailability of insoluble drugs by increasing drug solubility and permeability. The safety of CDs in humans has been well established [6,8]
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