Solid Lipid Nanoparticles of Albendazole for Enhancing Cellular Uptake and Cytotoxicity against U-87 MG Glioma Cell Lines

Abstract

Albendazole (ABZ) is an antihelminthic drug used for the treatment of several parasitic infestations. In addition to this, there are reports on the anticancer activity of ABZ against a wide range of cancer types. However, its effect on glioma has not yet been reported. In the present study, cytotoxicity of ABZ and ABZ loaded solid lipid nanoparticles (ASLNs) was tested in human glioma/astrocytoma cell line (U-87 MG). Using glyceryl trimyristate as lipid carrier and tween 80 as surfactant spherical ASLNs with an average size of 218.4 ± 5.1 nm were prepared by a combination of high shear homogenization and probe sonication methods. A biphasic in vitro release pattern of ABZ from ASLNs was observed, where 82% of ABZ was released in 24 h. In vitro cell line studies have shown that ABZ in the form of ASLNs was more cytotoxic (IC50 = 4.90 µg/mL) to U-87 MG cells compared to ABZ in the free form (IC50 = 13.30 µg/mL) due to the efficient uptake of the former by these cells.

Solid Polymeric Nanoparticles of Albendazole: Synthesis, Physico-Chemical Characterization and Biological Activity

“…Many approaches have been conducted in order to improve the water solubility and consequently the bioavailability of albendazole, such as complexion with cyclodextrins, preparation of solid dispersions with polyvinylpyrrolidone, the use of surfactants [2,27], or the synthesis of ABZ-chitosan microparticles [35]. Also, anticancer ABZ-based formulations were obtained such as thiolated carboxymethyl chitosan-graft-β-cyclodextrin NP which showed good entrapment efficiency of ABZ and mucoadhesive properties [36], a nanosystem based on folate-conjugated bovine serum albumin with potent anti-tumor activity both in vitro and in vivo [32], ABZ-loaded albumin NP with antiproliferative properties on ovarian cancer cells [4], solid lipid NP with antitumor activity against glioma cell lines [15], inclusion complex with hydroxypropyl-beta-CD with cytotoxicity on ovarian cancer cells [5], and chitosan-tripolyphosphate NP with anticancer effect on cancer hepatic cells [16]. In addition, encapsulation in a nanocarrier may provide efficient and/or targeted delivery of the chemotherapeutic agent into the cancer cells [14,16] via endocytosis [37].…”

“…For the simulated intestinal medium, the cumulated drug release was less than the stipulated percentages for all the mentioned time intervals presumably due to the poor solubility of ABZ at higher pH values. Marslin et al reported in 2017 the preparation of ABZ-loaded solid lipid nanoparticles (SLN) which induced the slow release of the drug over a 24 h time period in phosphate buffer (pH = 7.4) reaching an 82% cumulative drug release [15]. Another study was published by Liu et al in 2013 regarding the synthesis of ABZ-loaded chitosan nanoparticles which were tested in acidic, slightly acid and neutral environments, respectively; the chitosan-nanoparticles revealed a similar behavior to our nanoformulations with the drug's highest dissolution in acid medium and a sustained release of the drug following encapsulation [69].…”

“…In recent years, 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.…”

New Directions in the Creation of Innovative Antiparasitic Drugs

“…Так, твердые липидные наночастицы (ТЛНЧ) являются альтернативой полимерным наночастицам, эмульсиям и липосомам, и представляют собой коллоидные носители.Xie et al, 2011, Marslin et al, 2017 сообщали о повышении растворимости, Международная научная конференция Выпуск 21…”

Development of dry powder inhalation systems using ciprofloxacin hydrochloride

“…The cytotoxicity test is one of the biological assessments and screening tests that apply for living cells in vivo to detect the cell growth, reproduction and morphological effects by pharmaceutical products (Suresh et al, 2012;Marslin et al, 2017). Cytotoxicity assays are extensively used by the pharmaceutical research to screen for cytotoxicity in studying of compounds.…”