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A series of five guest–host inclusion complexes containing the antimalarial and anticancer agent artesunate (ATS) were obtained and characterized in the present study. Different cyclodextrins (CDNs) were used as hosts [α-cyclodextrin (CDN1), β-cyclodextrin (CDN2), γ-cyclodextrin (CDN3), (2-hydroxypropyl)-β-cyclodextrin (CDN4) and (2-hydroxypropyl)-γ-cyclodextrin (CDN5)], and the formation of the adducts was simulated using molecular modelling. The results indicating the hypothetical formation of all complexes were confirmed on the prepared samples by FTIR spectroscopy and thermal analysis (TG—thermogravimetric/DTG—derivative thermogravimetric/HF—heat flow). Our results showed that the partially entrapment of ATS inside the cavity of each cyclodextrin is a consequence of H-bonds formation, electrostatic interactions (dipole–dipole) and hydration water substitution. Also, all complexes formed in a 1:1 molecular ratio presented with higher thermal stability than pure ATS, making the analysed adducts possible alternatives in the drug design process of new and improved pharmaceutical formulations containing ATS.

Dihydroartemisinin (DHA), the hydrogenated derivative of the naturally originated sesquiterpene lactone artemisinin, is a well-known antimalarial agent that is currently researched because of its potential as an anticancer medication. Because DHA has been associated with a low oral bioavailability and a short half-life, new formulations meant to overcome these shortcomings are currently under development. As such, the present paper aims to present a comprehensive physico-chemical profile of DHA containing data of great importance for the preformulation stages of the drug design process. As instrumental techniques, attenuated total reflection Fourier transform infrared spectroscopy (ATR-FTIR) spectroscopy and thermal analysis (TG—thermogravimetric/DTG—derivative thermogravimetric/HF—heat flow) were performed, followed by a kinetic study realized using three isoconversional methods (Friedman—Fr, Flynn–Wall–Ozawa—FWO and Kissinger–Akahira–Sunose—KAS), as well as the nonparametric kinetic method (NPK). FTIR spectroscopy confirmed the identity and purity of DHA, and thermal analysis revealed a relatively low thermal stability and a multistep thermooxidation that was proved during the performed kinetic study. The latter unveiled a two-process decomposition determined by both chemical degradations and physical transformations.

Aripiprazole (ARP) is one of the newest antipsychotic drugs, exhibiting very low aqueous solubility and high lipophilicity. Considering the necessity of improvement of ARP physicochemical properties and its biopharmaceutical profile, cyclodextrin complexation of the drug substance was performed. As selected cyclodextrin, a functionalized β-cyclodextrin was used, namely heptakis(2,6-di-O-methyl)-β-cyclodextrin (DIMEB), and the supramolecular adduct ARP/DIMEB was prepared by kneading technique and characterized using thermoanalytical tools (TG—thermogravimetry/DTG—derivative thermogravimetry/HF—heat flow), powder X-ray diffractometry patterns (PXRD), universal-attenuated total reflectance Fourier transform infrared (UATR-FTIR) and UV (ultraviolet) spectroscopy and, as well, saturation solubility studies. Job’s method was used for the stoichiometry of APR/DIMEB inclusion complex determination, which was found to be 1:2. Molecular modeling studies were complementary realized as to get a view over the way that ARP is hosted inside the cyclodextrin. The compatibility between the inclusion complex and some common pharmaceutical excipients, namely starch, magnesium stearate, lactose monohydrate, microcrystalline cellulose and methylcellulose, has been evaluated by means of thermal methods of analysis (TG/DTG/HF), UATR-FTIR spectroscopy and PXRD pattern. The preformulation data regarding the compatibility of ARP/DIMEB complex with selected excipients suggested that under ambient conditions, chemical interactions are observed solely between ARP/DIMEB inclusion complex and magnesium stearate, as indicated by the UATR-FTIR spectroscopy. The incompatibility in the system ARP/DIMEB + MgS is also confirmed by the PXRD study, this second investigational technique revealing also the advanced amorphization of components during mixing of complex with starch, microcrystalline cellulose and methylcellulose, but without indicating interactions. Later on, under thermal stress, thermally induced interactions occur between the components in the systems containing magnesium stearate and methylcellulose, while starch, microcrystalline cellulose and lactose can be safely used as excipients in developing solid formulations containing ARP/DIMEB inclusion complex as active pharmaceutical ingredient.

The use of cyclodextrins as carrier molecules is currently highly researched since they can improve not only the apparent water solubility and bioavailability of lipophilic drugs, but can also enhance stability or mask unpleasant tastes and smells. Artesunate is a naturally originated sesquiterpene derivative with great potential as an anticancer agent but poor water solubility. The aim of the present paper was the preparation, physicochemical characterization and biological activity assessment of three supramolecular adducts, namely guest–host inclusion complexes containing ATS as a guest molecule and randomly methylated-β-cyclodextrin (CD1), heptakis (2,6-di-O-methyl)-β-cyclodextrin (CD2) and heptakis (2,3,6-tri-O-methyl)-β-cyclodextrin (CD3), each of them used separately as hosts. The pure precursors and prepared complexes were analyzed using FTIR spectroscopy and thermal analysis, the formation of the adducts was simulated using molecular modeling and the MTT in vitro proliferation method was employed in order to evaluate their cytotoxicity on healthy (HaCaT) and pathologic (A375) skin cell lines. The instrumental techniques proved the results obtained from the molecular simulation and confirmed the formation of all three inclusion complexes. The biological activity evaluation revealed a dose-dependent cytotoxicity of ATS on the cancer cell line, effect that was diminished after complexation, but also a significantly reduced toxic effect on the healthy cells for the complexes when compared to that determined by pure ATS.

In the class of steroid hormones, glucocorticoids are belonging to the subclass of corticosteroids, consisting of numerous synthetic or naturally occurring compounds, widely used in medical practice either as replacement therapy in glucocorticoid deficiency or to suppress the immune system. Glucocorticoids are active pharmaceutical ingredients used in solid, semisolid or liquid formulations involved mainly in the treatment of different types of cancers, inflammatory and autoimmune disorders, but as well as allergies. Both thermal stability and heterogeneous degradation kinetics of prednisolone, prednisone and cortisone were investigated in dynamic inert atmosphere (dinitrogen), at five heating rates β = 7, 10, 12, 15 and 20 °C min−1 using isoconversional methods of Friedman, Kissinger–Akahira–Sunose and Flynn–Wall–Ozawa, and later the modified non-parametric kinetic (NPK) method. The variation of apparent activation energies versus conversion degree as revealed by isoconversional methods suggested multistep degradation, which was later confirmed by the NPK method. The NPK method disclosed that all three glucocorticoids are degraded by two parallel processes, with apparent activation energies of 171.7 kJ mol−1 for prednisolone, 78.8 kJ mol−1 for prednisone and 61.8 kJ mol−1 for cortisone, respectively. The results are in good agreement with the ones suggested by isoconversional methods, and a discussion regarding the relation between the structure and apparent activation energy is presented.

The purpose of this study was to analyze the chemical composition and antimicrobial activity of some thymus populations collected from five different locations in Western Romania. The chemical compositions of the essential oils (EOs) were studied through GC–MS, and the biological activities were evaluated using the microdilution method. The EO yield ranged between 0.44% and 0.81%. Overall, 60 chemical compounds were identified belonging to three chemotypes: thymol (three populations), geraniol (one population) and carvacrol (one population). Thymus vulgaris L. is distinguished by a high content of thymol, while species of spontaneous flora (Th. odoratissimus and Th. pulegioides) contain, in addition to thymol, appreciable amounts of carvacrol and geraniol. The antimicrobial activity of each the five oils was tested on Staphylococcus aureus (ATCC 25923), Streptococcus pyogenes (ATCC 19615), Esherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853), Shigella flexneri (ATCC 12022), Salmonella typhimurium (ATCC 14028), Haemophilus influenzae type B (ATCC 10211), Candida albicans (ATCC 10231) and Candida parapsilopsis (ATCC 22019). The EOs showed biological activity on Gram-positive/Gram-negative/fungal pathogens, the most sensitive strains proving to be S. pyogenes, S. flexneri, S. typhimurium and C. parapsilopsis with an MIC starting at 2 µL EO/100 µL. The species sensitive to the action of Thymus sp. from culture or spontaneous flora are generally the same, but it should be noted that T. odoratissimus has a positive inhibition rate higher than other investigated EOs, regardless of the administered oil concentration. To date, there is no research work presenting the chemical and antimicrobial profiling of T. odoratissimus and the correlations between the antimicrobial potential and chemical composition of wild and cultivated populations of thyme (Thymus sp.) growing in Western Romania.

Artemisinin is a sesquiterpene lactone with vastly proved anti-cancer effects and a low toxicity profile. However, the compound has poor water solubility, bioavailability and a short half-life. As such, the present paper aims to evaluate the cytotoxic effect on breast cells of three guest-host inclusion complexes containing artemisinin as the active compound and different cyclodextrins as hosts. These were tested using two different concentrations (i.e. 12.5 mM and 25 mM) and three cell lines, namely two human breast adenocarcinoma cell lines (MCF7 and MDA-MB-231) and one human non-tumorigenic breast epithelial cell line (MCF10A) employing the colorimetric microculture tetrazolium assay. After a 72h stimulation period, the most promising results were obtained for the complex containing artemisinin and Heptakis(2,3,6-tri-O-methyl)-b-cyclodextrin, the cell viability decrease being significant for the estrogen positive MCF7 cell line (80.0 � 2.3 %), making the complex a potential candidate for further in vivo testing.

Risperidone (RSP) is an atypical antipsychotic drug used in treating schizophrenia, behavioral, and psychological symptoms of dementia and irritability associated with autism. The drug substance is practically insoluble in water and exhibits high lipophilicity. It also presents incompatibilities with pharmaceutical excipients such as magnesium stearate, lactose, and cellulose microcrystalline. RSP encapsulation by randomly methylated β-cyclodextrin (RM-β-CD) was performed in order to enhance drug solubility and stability and improve its biopharmaceutical profile. The inclusion complex formation was evaluated using thermal methods, powder X-ray diffractometry (PXRD), universal-attenuated total reflectance Fourier transform infrared (UATR-FTIR), UV spectroscopy, and saturation solubility studies. The 1:1 stoichiometry ratio and the apparent stability constant of the inclusion complex were determined by means of the phase solubility method. The compatibility between the supramolecular adduct and pharmaceutical excipients starch, anhydrous lactose, magnesium stearate, and cellulose microcrystalline was studied employing thermoanalytical tools (TG-thermogravimetry/DTG-derivative thermogravimetry/HF-heat flow) and spectroscopic techniques (UATR-FTIR, PXRD). The compatibility study reveals that there are no interactions between the supramolecular adduct with starch, magnesium stearate, and cellulose microcrystalline, while incompatibility with anhydrous lactose is observed even under ambient conditions. The supramolecular adduct of RSP with RM-β-CD represents a valuable candidate for further research in developing new formulations with enhanced bioavailability and stability, and the results of this study allow a pertinent selection of three excipients that can be incorporated in solid dosage forms.

Risperidone (RSP) is an atypical antipsychotic drug which acts as a potent antagonist of serotonin-2 (5TH2) and dopamine-2 (D2) receptors in the brain, it is used to treat schizophrenia, behavioral and psychological symptoms of dementia and irritability associated with autism. It is a poorly water soluble benzoxazole derivative with high lipophilicity. Supramolecular adducts between drug substance and two methylated &beta, cyclodextrins, namely heptakis(2,6-di-O-methyl)-&beta, cyclodextrin (DM-&beta, CD) and heptakis(2,3,6-tri-O-methyl)-&beta, cyclodextrin (TM-&beta, CD) were obtained in order to enhance RSP solubility and improve its biopharmaceutical profile. The inclusion complexes were evaluated by means of thermoanalytical methods (TG&mdash, thermogravimetry/DTG&mdash, derivative thermogravimetry/HF&mdash, heat flow), powder X-ray diffractometry (PXRD), universal-attenuated total reflectance Fourier transform infrared (UATR-FTIR), UV spectroscopy and saturation solubility studies. Job&rsquo, s method was employed for the determination of the stoichiometry of the inclusion complexes, which was found to be 2:1 for both guest&ndash, host systems. Molecular modeling studies were carried out for an in-depth characterization of the interaction between drug substance and cyclodextrins (CDs). The physicochemical properties of the supramolecular systems differ from those of RSP, demonstrating the inclusion complex formation between drug and CDs. The RSP solubility was enhanced as a result of drug encapsulation in the CDs cavity, the higher increase being obtained with DM-&beta, CD as host, the guest&ndash, host system RSP/DM-&beta, CD can thus be a starting point for further research in developing new formulations containing RSP, with enhanced bioavailability.

6-ethyl chenodeoxycholic acid (6ECDA) and deoxycholic acid (DCA) are two similar-structured cholanoic acids, the first being used in the treatment of primary biliary cholangitis, while the second is one of the natural secondary bile acids, currently being tested as a treatment component in the destruction of gallstones. This study was realised as no literature reference was found over thermal behaviour and the evaluation of the decomposition kinetics of the compounds from this class. Both acids were characterised by UATR-FTIR spectroscopy, thermal analysis and the kinetics of decomposition in dynamic oxidative atmosphere, by employing three isoconversional methods, namely Friedman, Kissinger–Akahira–Sunose and Flynn–Wall–Ozawa, respectively, the modified NPK method. Isoconversional methods suggested that no modification of the decomposition mechanism occurs with the modification of thermal treatment of the samples. Later, the modified NPK method was employed in order to estimate the kinetic triplet that describes the decomposition process of both compounds. All kinetic methods indicate a very good thermal stability of the bile acids, with apparent activation energies between 190.6 and 208.7 kJ mol−1 for the decomposition of 6ECDA and 205.5 and 221.7 kJ mol−1 for the decomposition of CDA, respectively. The modified NPK method suggested that both bile acids are degraded by the contribution of two distinctive chemical processes without any physical process associated.

The influence of excipients on the stability of sodium levothyroxine pentahydrate (LTSS) under ambient conditions and thermal stress was evaluated. Since LTSS is a synthetic hormone with a narrow therapeutic index, the interactions of LTSS with excipients can lead to a drastic diminution of therapeutic activity. Ten commonly used pharmaceutical excipients with different roles in solid formulations were chosen as components for binary mixtures containing LTSS, namely, starch, anhydrous lactose, D-mannitol, D-sorbitol, gelatin, calcium lactate pentahydrate, magnesium stearate, methyl 2-hydroxyethyl cellulose (Tylose), colloidal SiO2 (Aerosil) and talc. As investigational tools, universal attenuated total reflectance- Fourier transform infrared spectroscopy UATR-FTIR spectroscopy and thermal analysis were chosen and used as follows: UATR-FTIR spectra were drawn up for samples kept under ambient conditions, while thermoanalytical tools (TG/DTG/HF data) were chosen to evaluate the inducing of interactions during thermal stress. The corroboration of instrumental results led to the conclusion that LTSS is incompatible with lactose, mannitol and sorbitol, and these excipients should not be considered in the development of new generic solid formulations.

In this paper, the bioactive compound artemisinin (ART) was evaluated by instrumental techniques, regarding its thermal stability and mechanism of decomposition, but for the biological activity as well, using in vitro techniques, namely the cytotoxic activity evaluation on two cell types (HaCaT and A375) employing the MTT proliferation method, and the antioxidant activity (AOA) using the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging assay. The results of the isoconversional kinetic study first lead to an indication of complex decomposition mechanism, which was later confirmed by the modified nonparametric kinetics (NPK) method. According to the NPK method, it was shown that ART is mainly degraded by the involvement of two parallel processes, with different energetic contributions that are due to chemical and physical transformations. However, the estimated mean apparent activation energy yields similar results with all four kinetic methods, ranging between 61.3 and 68.7 kJ mol−1, confirming the low thermal stability of the compound, which can be explained by the presence of reactive functional groups, such as the peroxide one. Regarding the biological activity of ART, it was shown that it can be used to induce cell growth arrest on human melanoma cell line A375, but affecting in a smaller measure the viability of HaCaT cell line, while the AOA is negligible, in comparison with standard antioxidants.

Artemisinin is one of the most important naturally occurring compound found in Artemisia annua, being highly active against Plasmodium falciparum, the malaria causing parasite, and currently studied in the oncological field. The aim of this study was to obtain and characterize the host–guest inclusion complexes formed between artemisinin and three functionalized cyclodextrins, namely Randomly methylated-β-cyclodextrin (CD1), Heptakis(2,6-di-O-methyl)-β-cyclodextrin (CD2) and Heptakis(2,3,6-tri-O-methyl)-β-cyclodextrin (CD3). As instrumental tools, thermal analysis (TG/DTG/HF) and UATR-FTIR spectroscopy were used. Later on, the inclusion complexes were tested as to evaluate their antioxidant (AOA) and in vitro activity on both healthy keratinocytes and a human melanoma cell line, A375. Both instrumental techniques suggested the formation of inclusion complexes and the increase of thermal stability of artemisinin in complexes versus pure compound. Regarding the antioxidant activity evaluation of all samples, it was shown that this is significantly inferior in comparison to ascorbic acid, while the in vitro biological activity showed that inclusion complexes (CPX2 and CPX3) exerted an inhibitory effect on human melanoma cells growth, similar to the effect induced by artemisinin.

This paper presents the results obtained after the investigation of two artemisinin derived sesquiterpenes, namely artesunate and artemether, currently studied for their antitumor properties. The chosen methods of analysis included UATR–FTIR spectroscopy, characterization of the thermal behavior (TG/DTG/HF) in oxidative dynamic atmosphere, and a complete kinetic analysis. The latter was realized using two integral methods (Kissinger–Akahira–Sunose and Flynn–Wall–Ozawa), a differential one (Friedman), and was later completed with the modified NPK method. The study showed that both compounds show similar thermal stability in terms of apparent activation energies and the degradation processes occur in two parallel steps for each compound, this being solely due to chemical transformations.

In this paper, we present the spectroscopic description (by the means of UATR-FTIR spectroscopy) for four naturally occurring bile acids, namely lithocholic acid (LC), taurocholic acid sodium salt hydrate (TC), taurodeoxycholic acid sodium salt hydrate (TDC) and chenodeoxycholic acid (CDC), as well as their thermal behaviour in dynamic oxidative atmosphere, by TG/DTG/HF means. It was shown that all samples have a good thermal stability, favourized by the presence of cholan-24-oic structural moiety in all samples, as well as the solid-state structure (intermolecular H-bondings for the carboxylic acids CDC and LC and saline structures for TDC and TC, respectively). These data are simple, but of great interest in identifying the presence of these compounds by fast, reproducible and precise instrumental techniques in complex mixtures, such as biliary stones.

Entacapone, a selective and reversible inhibitor of catechol-O-methyltransferase, is used in the treatment of Parkinson’s disease in combination with levodopa/carbidopa to treat the symptoms of end-of-dose “wearing-off” effect. Considering that new formulations are researched constantly, proper knowledge of the active pharmaceutical ingredients is crucial in the preformulation stages. Kinetic analysis was performed using three methods: one integral—Flynn–Wall–Ozawa method, one differential—Friedman method, and modified nonparametric kinetics method (NPK). The thermoanalytical curves were registered at five different heating rates: β = 5, 7, 10, 12, and 15 °C min−1. Analysis was conducted in the dynamic air atmosphere to highlight potential thermooxidative processes. This paper deals with the investigation of solid-state stability and compatibility of binary mixture of entacapone with various pharmaceutical excipients by two instrumental techniques, such as universal attenuated total reflection Fourier transform infrared and thermal analysis (TG/DTG/HF). The excipients used in the mixture were: mannitol, silicon dioxide, talc, sorbitol, magnesium stearate, and povidone.

In this paper, we present the results obtained during the investigation of thermal stability of antiparkinsonian drug Levodopa in oxidative atmosphere and under non-isothermal conditions. As investigational tools, thermoanalytical methods were used along with ATR-FTIR spectroscopy and later completed with kinetic study for the main degradative process that occurs in the 260–330 °C temperature range, at four heating rates. Four kinetic methods were used as follows: ASTM E698 which leads to an activation energy of 209.72 kJ mol−1, while isoconversional methods suggested the values 177.6 ± 13.1 kJ mol−1 (Friedman) and 188.8 ± 4.5 kJ mol−1 (Kissinger–Akahira–Sunose), with a clear indication of multistep degradation. The last method used was NPK, which revealed that the degradation occurs in three steps, with different physical and chemical contributions with mean activation energy equal to 191.3 ± 9.5 kJ mol−1.

Levodopa (L-Dopa or LD) is nowadays considered one of the essential medicines in the World Health Organization list, being a main treatment component for Parkinson’s disease. This paper deals with the investigation of solid-state stability and compatibility of binary mixtures of Levodopa with various pharmaceutical excipients, by employment of several instrumental techniques, such as attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy, powder X-ray diffraction (PXRD) data and thermal analysis (TG/DTG/HF). Along L-Dopa, eleven pharmaceutical excipients were investigated, namely calcium lactate (CaL), mannitol (Man), magnesium stearate (MgSt), anhydrous lactose (LAnh), talc (T), magnesium citrate (MgC), sorbitol (Sb), silica (SiO2), polyvinylpyrrolidone K30 (PVP), sodium carboxymethylcellulose (NaCMC) and starch (St). FTIR analysis suggested possible interactions with calcium lactate, mannitol, magnesium stearate, anhydrous lactose, talc and SiO2, which were confirmed by PXRD patterns, except for talc. When the samples were subjected to thermal stress, solely magnesium citrate did not present interactions in binary mixture, while all other excipients were incompatible with L-Dopa.

Nortriptyline (NRT), usually conditioned as hydrochloride, is a second-generation tricyclic antidepressant that is primarily used as a treatment option for major depression and chronic pain. In this study, a compatibility evaluation between an active pharmaceutical ingredient (API) and various excipients that form binary mixtures is presented. As investigational methods, ATR-FTIR analysis and PXRD data were recorded for the binary mixtures under ambient conditions, and were later investigated by thermal analysis (TG—thermogravimetry/DTG—derivative thermogravimetry/HF—heat flow) in dynamic air atmosphere. Nortriptyline hydrochloride (NRT) was used as an active pharmaceutical ingredient, and binary mixtures with 13 excipients from different categories were formed (mass ratio 1:1), namely: microcrystalline cellulose (MC), calcium lactate (CaLact), stearic acid (StA), lactose monohydrate (Lact), polyvinylpyrrolidone K30 (PVP), magnesium stearate (MgSt), sodium carboxymethylcellulose (CMCNa), sorbitol (Sorb), mannitol (Man), gelatine (Gel), silica (SiO2), starch (Starch), and talc (T). The PXDR patterns determined for the binary mixtures showed no incompatibility between the components since the diffraction profile consists in the superposing of the components’ patterns, while the ATR-FTIR study indicated interactions in the discussed binary mixtures, suggesting that NRT is incompatible with PVP, Sorb, Man, StA, and Lact even under ambient conditions. Under thermal stress, interactions between NRT and excipients were observed at temperatures below the melting point of the API in the binary mixtures with PVP, Sorb, Man, StA, and Lact, while at high temperatures, all binary mixtures are thermally degraded due to thermolysis.

Donepezil (Don) is one of the main compounds used in the therapy of Alzheimer’s disease. In this study, donepezil hydrochloride was investigated for solid-state compatibility with several pharmaceutical excipients like calcium lactate (CaL), mannitol (Man), magnesium stearate (MgSt), anhydrous lactose (LAnh), talc (T), magnesium citrate (MgC), sorbitol (Sb), silica (SiO2), polyvinylpyrrolidone K30 (PVP), sodium carboxymethylcellulose (NaCMC) and starch (St) under ambient conditions, by ATR–FTIR spectroscopy and PXRD data, and later by thermoanalytical techniques (TG/DTG/HF), in order to evaluate the thermal-induced interactions. The instrumental investigations carried at ambiental temperature revealed no interaction between Don and selected excipients, while thermal treatment induced interactions between components in eight binary mixtures, except the ones containing magnesium citrate, talc and polyvinylpyrrolidone.

This paper presents the results obtained in a screening study for binary adduct formation of desipramine with three dicarboxylic acids—namely succinic, malonic and glutaric acids. Adduct formation is important because most tricyclic antidepressants show limited water solubility as free bases. Three binary adducts were prepared using a wet kneading method in non-homogenous media in presence of ethanol. Investigations of the solid state (ATR-FTIR, PXRD) and thermal analysis (TG/DTG/HF) were used for characterization of the prepared samples. The corroboration of data from employed instrumental techniques suggests that binary adducts in molar ratio 1:1 were obtained under the used experimental conditions.

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.