Exploring the Preparation of Albendazole-Loaded Chitosan-Tripolyphosphate Nanoparticles

Abstract

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.

Enhancing the in vitro anticancer activity of albendazole incorporated into chitosan-coated PLGA nanoparticles

“…An excess amount of ABZ was dissolved in various organic solvents including acetone, ethanol, dichloromethane, and chloroform according to our previous study (Kang, Lee, Ng, Kim, & Park, 2015). To prevent vaporization of organic solvents, the vials were capped after loading the ABZ.…”

“…Degradation of CS is maximal at pH 4.6 and 55ºC; the material is stable below pH 3.0 and at body temperature (Tao, Wei, Mao, Zhang, & Xia, 2005). Furthermore, ABZ is solubilized at harshly acidic pHs (Kang, Lee, Ng, Kim, & Park, 2015). Therefore, we selected CS-coated PLGA NPs to deliver ABZ; we sought to inhibit enzymatic degradation of solubilized ABZ under gastric conditions, to increase particle mucoadhesiveness to the gastric mucosal surface, and to improve drug absorption.…”

Increased Loading, Efficacy and Sustained Release of Silibinin, a Poorly Soluble Drug Using Hydrophobically-Modified Chitosan Nanoparticles for Enhanced Delivery of Anticancer Drug Delivery Systems

“…CS is known for its superior features such as biocompatibility, biodegradable and non-toxicity, which makes it an excellent candidate to be utilized in agriculture, biomedicine, food industries and many other fields. A previous study by Kang et al [ 25 ] has successfully synthesized chitosan nanoparticles (CNP) loaded with albendazole, a poorly water-soluble but extremely permeable anthelmintic drug, where a stable nanoparticle system was established. Besides this, Chai et al [ 26 ] also demonstrated that CNP can function as a drug delivery system for Doxorubicin, an anticancer drug.…”

The Chemistry of Chitin and Chitosan Justifying their Nanomedical Utilities

“…The application of chitin and chitosan in nanomedicine had been widely reported for the targeted delivery of drugs in nanoparticle formulations and also for gene therapy [8][9][10][11][12].…”