Abstract
Albendazole is a benzimidazole derivative with documented antitumor activity and low toxicity to healthy cells. The major disadvantage in terms of clinical use is its low aqueous solubility which limits its bioavailability. Albendazole was incorporated into stable and homogeneous polyurethane structures with the aim of obtaining an improved drug delivery system model. Spectral and thermal analysis was used to investigate the encapsulation process and confirmed the presence of albendazole inside the nanoparticles. The in vitro anticancer properties of albendazole encapsulated in polyurethane structures versus the un-encapsulated compound were tested on two breast cancer cell lines, MCF-7 and MDA-MB-231, in terms of cellular viability and apoptosis induction. The study showed that the encapsulation process enhanced the antitumor activity of albendazole on the MCF-7 and MDA-MB-23 breast cancer lines. The cytotoxic activity manifested in a concentration-dependent manner and was accompanied by changes in cell morphology and nuclear fragmentation.
Highlights
Albendazole (ABZ), methyl[5-(propylthio)-1-H-benzimidazol-2-yl]carbamate, is one of the most effective broad-spectrum anti-helminthic agents used in human and veterinary chemotherapy of various intestinal and systemic parasitosis [1]
The mathematical interpretation of this entrapment percentage allowed us to calculate the concrete amount of ABZwhich was embedded in each mg of the PU matrix
The results provided by the differential scanning calorimetry (DSC), TG and derivative thermogravimetry (DTG) analysis confirms a reduction of the particle size and ABZ amorphization as a result of the encapsulation process
Summary
Albendazole (ABZ), methyl[5-(propylthio)-1-H-benzimidazol-2-yl]carbamate, is one of the most effective broad-spectrum anti-helminthic agents used in human and veterinary chemotherapy of various intestinal and systemic parasitosis [1]. Numerous reports in the field of biomedical nanoparticles (NP) have been documented for their usefulness in improving bioavailability, and subsequently, in the treatment and prevention of many diseases [11,12,13]; encapsulation of anticancer drugs in nanocarriers may provide efficient targeted delivery of the chemotherapeutic agent into the cancer cells [14]. The literature reports several studies focused on the development of novel nanoformulations containing ABZ, such as albumin nanoparticles [4], solid-lipid nanoparticles [15], chitosan-tripolyphosphate nanoparticles [16] and chitosan-PLGA nanoparticles [17] which were designed and tested as anticancer agents with promising results on various tumor cell lines. The anti-proliferative effect of ABZ alone and embedded in PU nanoformulations was assessed by in vitro analysis
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