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

Racoviceanu, Roxana; Trandafirescu, Cristina; Voicu, Mirela; Ghiulai, Roxana; Borcan, Florin; Dehelean, Cristina; Watz, Claudia; Aigner, Zoltán; Ambrus, Rita; Coricovac, Dorina; Circioban, Denisa; Mioc, Alexandra; Szuhanek, Camelia; Şoica, Codruţa

doi:10.3390/molecules25215130

Cited by 16 publications

(12 citation statements)

References 73 publications

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“…Thus, cellular extension disruption not only inhibits tumor growth but is also vital for tumor cell dissemination and metastasis (Ross and Hunger, 2017). Similar morphological changes in MCF7 and MDA-MB-231 cells as a result of albendazole treatment is reported (Racoviceanu et al, 2020).…”

Section: Morphological Changes and Cell Migration Inhibitionmentioning

confidence: 58%

Encapsulating Anti-Parasite Benzimidazole Drugs into Lipid-Coated Calcium Phosphate Nanoparticles to Efficiently Induce Skin Cancer Cell Apoptosis

Movahedi

Soares

et al. 2021

Front. Nanotechnol.

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Benzimidazole (BMZ) family of anti-worm drugs has been now repurposed as anti-cancer drugs. However, offering a general reformulation method for these drugs is essential due to their hydrophobicity and low aqueous solubility. In this work, we developed a general approach to load typical BMZ drugs as tiny nanocrystals within lipid-coated calcium phosphate (LCP) nanoparticles. BMZ drug-loaded LCP nanoparticles increased their solubility in PBS by 100–200% and significantly enhanced the anti-cancer efficacy in the treatment of B16F0 melanoma cells. These drug-LCP nanoparticles induced much more cancer cell apoptosis, generated much more reactive oxygen species (ROS) and inhibited Bcl-2 expression of cancer cells. Moreover, BMZ drug-loaded LCP nanoparticles caused morphological change and extension disruption of cancer cells, and significantly reduced migration activity, representing high possibility for inhibition of tumor dissemination and metastasis. Very advantageously, BMZ drug-loaded LCP nanoparticles did not show any obvious toxicity, Bcl-2 inhibition and morphological changes in HEK293T healthy cells. In conclusion, BMZ drug-incorporated LCP nanoformulations may be a valuable nanomedicine that is able to inhibit primary tumors and prevent tumor dissemination with minimum side effects on healthy cells and tissues.

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Section: Morphological Changes and Cell Migration Inhibitionmentioning

confidence: 58%

Encapsulating Anti-Parasite Benzimidazole Drugs into Lipid-Coated Calcium Phosphate Nanoparticles to Efficiently Induce Skin Cancer Cell Apoptosis

Movahedi

Soares

et al. 2021

Front. Nanotechnol.

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“…5 mL samples were collected in each case at ¼, ½, 1, 2, 4, 6, 8, 10, 18 and 24 h to evaluate the release profile of acyclovir. Briefly, the concentration of acyclovir was assessed spectrophotometrically by means of an UVi Line 9400 Spectrophotometer SI Analytics (Mainz, Germany) using calibration curves for acyclovir for each dissolution medium; the compositions of simulated gastric/intestinal medium were already described in one of our previous papers [ 25 ]. All the measurements were conducted in triplicate in order to gain statistical value.…”

Section: Methodsmentioning

confidence: 99%

Design and Assessment of a Polyurethane Carrier Used for the Transmembrane Transfer of Acyclovir

et al. 2020

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The Herpes simplex viruses (HSV-1, HSV-2) are responsible for a wide variety of conditions, from cutaneous-mucosal to central nervous system (CNS) infections and occasional infections of the visceral organs, some of them with a lethal end. Acyclovir is often used intravenously, orally, or locally to treat herpetic infections but it must be administered with caution to patients with kidney disease and to children of early age. The main objectives of this study were to synthesize and evaluate new polyurethane nanoparticles that might be used as proper transmembrane carriers for acyclovir. Polyurethane particles were obtained by a polyaddition process: a mixture of two aliphatic diisocyanates used as organic phase was added to a mixture of butanediol and polyethylene glycol used as aqueous phase. Two different samples (with and without acyclovir, respectively) were synthesized and characterized by UV-Vis spectra in order to assess the encapsulation efficacy and the release profile, FT-IR, DSC, SEM, and SANS for structural characterization, as well as skin irritation tests. Nearly homogeneous samples with particle sizes between 78 and 91 nm have been prepared and characterized revealing a medium tendency to form clusters and a high resistance to heat up to 300 °C. The release profile of these nanoparticles is characteristic to a drug delivery system with a late discharge of the loaded active agents. Very slight increases in the level of transepidermal water loss and erythema were found in a 15-day evaluation on human skin. The results suggest the synthesis of a non-irritative carrier with a high encapsulation efficacy that can be successfully used for the transmembrane transfer of acyclovir.

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“…Among various trials to overcome this problem, the most successful approach is to formulate or conjugate it into nanostructures or nanoformulations, in practice of improving aqueous solubility [ 358 ]. Albendazole-cyclodextrin complex, M1·albendazole, albumin nanoparticles, chitosan nanoparticles, solid lipid nanoparticles, PLGA nanoparticles, albendazole-copper oxide nanoparticles, and solid polymeric nanoparticles are examples of so far designed nanoformulations of albendazole [ 358 , 359 ].…”

Section: Anti-cancer Effectsmentioning

confidence: 99%

Albendazole and Mebendazole as Anti-Parasitic and Anti-Cancer Agents: an Update

2021

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The use of albendazole and mebendazole, i.e., benzimidazole broad-spectrum anthelmintics, in treatment of parasitic infections, as well as cancers, is briefly reviewed. These drugs are known to block the microtubule systems of parasites and mammalian cells leading to inhibition of glucose uptake and transport and finally cell death. Eventually they exhibit ovicidal, larvicidal, and vermicidal effects on parasites, and tumoricidal effects on hosts. Albendazole and mebendazole are most frequently prescribed for treatment of intestinal nematode infections (ascariasis, hookworm infections, trichuriasis, strongyloidiasis, and enterobiasis) and can also be used for intestinal tapeworm infections (taeniases and hymenolepiasis). However, these drugs also exhibit considerable therapeutic effects against tissue nematode/cestode infections (visceral, ocular, neural, and cutaneous larva migrans, anisakiasis, trichinosis, hepatic and intestinal capillariasis, angiostrongyliasis, gnathostomiasis, gongylonemiasis, thelaziasis, dracunculiasis, cerebral and subcutaneous cysticercosis, and echinococcosis). Albendazole is also used for treatment of filarial infections (lymphatic filariasis, onchocerciasis, loiasis, mansonellosis, and dirofilariasis) alone or in combination with other drugs, such as ivermectin or diethylcarbamazine. Albendazole was tried even for treatment of trematode (fascioliasis, clonorchiasis, opisthorchiasis, and intestinal fluke infections) and protozoan infections (giardiasis, vaginal trichomoniasis, cryptosporidiosis, and microsporidiosis). These drugs are generally safe with few side effects; however, when they are used for prolonged time (>14-28 days) or even only 1 time, liver toxicity and other side reactions may occur. In hookworms, Trichuris trichiura, possibly Ascaris lumbricoides, Wuchereria bancrofti, and Giardia sp., there are emerging issues of drug resistance. It is of particular note that albendazole and mebendazole have been repositioned as promising anti-cancer drugs. These drugs have been shown to be active in vitro and in vivo (animals) against liver, lung, ovary, prostate, colorectal, breast, head and neck cancers, and melanoma. Two clinical reports for albendazole and 2 case reports for mebendazole have revealed promising effects of these drugs in human patients having variable types of cancers. However, because of the toxicity of albendazole, for example, neutropenia due to myelosuppression, if high doses are used for a prolonged time, mebendazole is currently more popularly used than albendazole in anti-cancer clinical trials.

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

Cited by 16 publications

References 73 publications

Encapsulating Anti-Parasite Benzimidazole Drugs into Lipid-Coated Calcium Phosphate Nanoparticles to Efficiently Induce Skin Cancer Cell Apoptosis

Encapsulating Anti-Parasite Benzimidazole Drugs into Lipid-Coated Calcium Phosphate Nanoparticles to Efficiently Induce Skin Cancer Cell Apoptosis

Design and Assessment of a Polyurethane Carrier Used for the Transmembrane Transfer of Acyclovir

Albendazole and Mebendazole as Anti-Parasitic and Anti-Cancer Agents: an Update

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