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Our research aims to expand the knowledge on relationships between the structure of cationic dicephalic surfactants—N,N-bis[3,3_-(dimethylamine)propyl]alkylamide dihydrochlorides and N,N-bis[3,3_-(trimethylammonio)propyl]alkylamide dibromides (alkyl: n-C9H19, n-C11H23, n-C13H27, n-C15H31)—and their antifungal mechanism of action on Candida albicans. The mentioned groups of amphiphilic substances are characterized by the presence of a weak, hydrochloride cationic center readily undergoing deprotonation, as well as a stable, strong quaternary ammonium group and alkyl chains capable of strong interactions with fungal cells. Strong fungicidal properties and the role in creation and eradication of biofilm of those compounds were discussed in our earlier works, yet their mechanism of action remained unclear. It was shown that investigated surfactants induce strong oxidative stress and cause increase in cell membrane permeability without compromising its continuity, as indicated by increased potassium ion (K+) leakage. Thus experiments carried out on the investigated opportunistic pathogen indicate that the mechanism of action of the researched surfactants is different than in the case of the majority of known surfactants. Results presented in this paper significantly broaden the understanding on multifunctional cationic surfactants and their mechanism of action, as well as suggest their possible future applications as surface coating antiadhesives, fungicides and antibiofilm agents in medicine or industry.

Our research aimed to expand the knowledge of relationships between the structure of multifunctional cationic dicephalic surfactants with a labile linker-N,N-bis[3,3-(dimethylamine)propyl]alkylamide dihydrochlorides and N,N-bis[3,3-(trimethylammonio)propyl]alkylamide dibromides (alkyl: n-C9H19, n-C11H23, n-C13H27, n-C15H31)-and their possible mechanism of action on fungal cells using the model organism Saccharomyces cerevisiae. General studies performed on surfactants suggest that in most cases, their main mechanism of action is based on perforation of the cell membranes and cell disruption. Experiments carried out in this work with cationic dicephalic surfactants seem to modify our understanding of this issue. It was found that the investigated compounds did not cause perforation of the cell membrane and could only interact with it, increasing its permeability. The surfactants tested can probably penetrate inside the cells, causing numerous morphological changes, and contribute to disorders in the lipid metabolism of the cell resulting in the formation of lipid droplet aggregates. This research also showed that the compounds cause severe oxidative stress within the cells studied, including increased production of superoxide anion radicals and mitochondrial oxidative stress. Dicephalic cationic surfactants due to their biodegradability do not accumulate in the environment and in the future may be used as effective antifungal compounds in industry as well as medicine, which will be environmentally friendly. KEY POINTS: • Dicephalic cationic surfactants do not induce disruption of the cell membrane. • Surfactants could infiltrate into the cells and cause accumulation of lipids. • Surfactants could cause acute oxidative stress in yeast cells. • Compounds present multimodal mechanism of action. Graphical abstract.

Much attention has been recently paid to the design of sustainable processes for the production of functional food additives based on renewable resources. Thus, methods for incorporation of green techniques in treatment of undeveloped biomass, resulting in value-added bioproducts, are in great demand. We focus here on the biological activity and chemical properties of Erigeron canadensis (horseweed) functional food fiber, which can be strongly affected by the extraction procedure employed. In the present contribution, we report on an attempt to introduce a sustainable and energy-efficient ultrasound-assisted extraction process, followed by a multistep purification procedure, resulting in a macromolecular plant-derived anticoagulant agent. The most efficient ultrasound-assisted process was determined by optimization through the response surface methodology I-optimal design (24). A comparison with the conventional procedure for retrieval of horseweed biomacromolecules revealed that the optimized ultrasound-assisted extraction was more sustainable, with the cumulative energy demand being 38% lower (12.2 MJ), 6.6 times reduced water consumption (3.5 L), and 1.2 times shorter (41 h) total processing time. Moreover, the optimal ultrasound-assisted extraction process-purified food fiber turned out to be a better anticoagulant agent by 57%, compared to a conventional product, and was a more selective indirect inhibitor of the human Xa coagulation factor.

Hypothesis The excellent performance of zwitterionic alkylamide-type surfactants may be tuned by slight modifications of their structures, especially concerning linking groups between hydrophilic and hydrophobic moieties and the moderation of strong NH hydrogen bonds via the introduction of a methyl group attached to the nitrogen. Experiments The influence of the structure of alkylamidehydroxysulfobetaine-type surfactants on their adsorption and micellization, lime soap dispersing ability, wettability, as well as antimicrobial and hemolytic activities was studied in this work. We synthesized a series of novel surfactants with labile CO N(Me)CH2 or CH2N(Me) CO spacers that were adjacent to the hydrophobic tail CnH2n+1 and separated from the zwitterionic hydroxysulfobetaine headgroup by C3H6 or C2H4 linkers, i.e., [(3-alkanoyilomethyoamine)propyl] dimethylammonium 2-hydroxypropanesulfonates (CnTMDAS) and [3-(alkylmetyloamino)-3-oxopropyl] dimethylammonium 2-hydroxypropanesulfonates (CnDMPAS), respectively. Findings The CnTMDAS surfactants showed slightly higher surface activity and lower CMC than the respective CnDMPAS with the same number of carbon atoms. Moreover, the CnTMDAS series exhibited significantly higher lime soap dispersing abilities and softer interactions with biological systems than CnDMPAS. The molecular modeling computations revealed that the difference in surface activity originated from lower dipole moment of CnTMDAS, hence, lower polarity, whereas higher free energy of dimerization of those surfactants with oleic acid may account for the favorable formation of mixed micelles.

This up-to-date review describes the design, fabrication approaches, properties and applications that have been employed in the field of hydrophobically decorated polyelectrolytes (HD-PEs), used as functionalized building blocks for speciality materials with tuneable features. These include, in particular, synthetic strategies for modification/hydrophobization of polyelectrolytes, self-organization of HD-PEs in aqueous systems, adsorption phenomena and applications in the field of surface chemistry. Rationally engineered HD-PEs can be achieved via either step-growth copolymerization of different reactive end groups of monomers, followed by appropriate post-synthesis treatment or as a result of decoration of a given polymer backbone with hydrophobic side groups. The influence of HD-PEs' chemical structure on their self-assembling and interfacial properties is dependent on the overall hydrophobicity, i.e. length, number and type of side chains stretched out to charged segment, number, type and strength of ionizable groups. We also conclude that the linking entity structure (ester, secondary amide, etc.) between the hydrophobic side chain and the charged polyelectrolyte backbone in the tailor-made HD-PEs plays a crucial role in self-aggregation behaviour in water and at interfaces. The examples of the unique ability of HD-PEs to adsorb at hydrophilic and hydrophobic interfaces is discussed considering the effect of the self-aggregation on the interfacial properties.

The removal of graffiti or over-painting requires special attention in order to not induce the surface destruction but to also address all of the important eco-compatibility concerns. Because of the necessity to avoid the use of volatile and toxic petroleum-based solvents that are common in cleaning formulations, much attention has recently been paid to the design of a variety of sustainable formulations that are based on biodegradable raw materials. In the present contribution we propose a new approach to graffiti cleaning formulations that are composed of newly synthesized green solvents such as esterified plant oils, i.e., rapeseed oil (RO), sunflower oil (SO), or used cooking oil (UCO), ethyl lactate (EL), and alkylpolyglucosides (APGs) as surfactants. Oil PEG-8 ester solvents were synthesized through the direct esterification/transesterification of these oils using monobutyltin(IV) tris(2-ethylhexanoate) and titanium(IV) butoxide catalysts under mild process conditions. The most efficient formulations, determined by optimization through the response surface methodology (RSM) was more effective in comparison to the reference solvents such as the so-called Nitro solvent (denoting a mixture of toluene and acetone) and petroleum ether. Additionally, the optimal product was found to be effective in removing graffiti from glass, metal, or sandstone surfaces under open-field conditions in the city of Wrocław. The performed studies could be an invaluable tool for developing future green formulations for graffiti removal.

The purpose of this study was to compare the application of several extraction methods, including cold extraction (CAE), hot extraction (HAE), ultrasonic-assisted extraction (UAE), and microwave-assisted extraction (MAE), all carried out in 0.1 M NaOH, under their respective best parameters, for obtaining products from leaf of Fragaria vesca L. The extracts with the highest anticoagulant activity were purified by multi-step extraction procedure and separated by gel permeation chromatography, giving rise to the macromolecular complexes. They were subsequently structurally characterized using colorimetric methods, FT-IR, GC–MS, and NMR (1H and 1H/13C HSQC), as polyphenolic-polysaccharide conjugates with the anticoagulant activity. The polysaccharide parts of the conjugates obtained by different extraction procedures were found to vary significantly. The most selective in their activity were the glycoconjugates extracted in UAE and MAE processes, i.e. arabinogalactan and pectin-like conjugates, respectively. In terms of their anticoagulant activity all of them were non-direct factor Xa inhibitors mediated by antithrombin.

The oil core nanocapsules platform holds great potential to enhance the efficiency and accuracy of anticancer therapies. In this work, we describe the preparation of well-defined multilayer oil core nanocapsules built of oppositely charged polyelectrolytes via a layer-by-layer (LbL) assembly strategy and their use as advanced drug delivery systems for photodynamic therapy (PDT). The prepared nanocapsules show great stability in a physiological environment with uniform morphology and diameters of around 120 nm as disclosed by stability investigation, TEM and DLS analysis. By in vitro cellular experiments based on MTT assays, CLSM, FACS analysis and ROS detection, we confirmed that tetraphenylporphyrin TPP-loaded multilayer nanocapsules were selectively PDT-active against A549 cancer cells (human lung adenocarcinoma). Cellular uptake results showed that TPP NCs were readily taken up by A549 cells and enhanced TPP uptake was detectable in the NCs-treated cells in comparison to carrier free drug. TPP NCs also elicited intracellular ROS generation, which leads to enhanced toxicity in A549 cells. Toxicological impact of developed nanocapsules was further investigated using newly designed microfluidic Lab-on-a-chip system enabling photodynamic activity studies on three types of cell culture. Our results demonstrate a major potential of TPP-loaded multilayer oil core nanocapsules for PDT therapeutic treatment of a lung cancer.

In cancer research, it is important to develop culture models which will reproduce natural environment of tumor, e.g. three-dimensional (3D) cell arrangement, cell-cell interactions, the presence of various cell types. To meet the demands, it is proposed a new microfluidic culture model based on spheroids composed of a co-culture of cancer and non-malignant mammary cells. This culture model is utilized for evaluation of photodynamic therapy (PDT) effectiveness with a nanoencapsulated photosensitizer (meso-tetraphenylporphyrin, nano-TPP). Thanks to such a model the mechanisms of breast cell response in spheroid co-culture and mono-culture could be investigated under microfluidic conditions. It is observed that the breast spheroid co-culture exhibits resistance to PDT procedures more than the spheroid mono-cultures. This effect could result from a different accumulation of nano-TPP and different ROS generation in both spheroid models: mono- and co-cultures. Summarizing, in this paper an innovative approach for the development of a 3D in vitro breast tumor model and its usage for the evaluation of PDT procedure effectiveness is presented.

The aim of the performed studies was to thoroughly examine the internal structure of self-assembled nanocarriers (i.e., polymeric micelles-PMs) by means of a hydrophobic phthalocyanine probe in order to identify the crucial features that are required to enhance the photoactive probe stability and reactivity. PMs of hydrophilic poly(ethylene glycol) and hydrophobic poly(e-caprolactone) (PCL) or poly(d,l-lactide) (PDLLA) were fabricated and loaded with tetra tert-butyl zinc(II) phthalocyanine (ZnPc-t-but4), a multifunctional spectroscopic probe with a profound ability to generate singlet oxygen upon irradiation. The presence of subdomains, comprising "rigid" and "flexible" regions, in the studied block copolymers' micelles as well as their interactions with the probe molecules, were assessed by various high-resolution NMR measurements [e.g., through-space magnetic interactions by the 1D NOE effect, pulsed field gradient spin-echo, and spin-lattice relaxation time (T1) techniques]. The studies of the impact of the core-type microenvironment on the ZnPc-t-but4 photochemical performance also included photobleaching and reactive oxygen species measurements. ZnPc-t-but4 molecules were found to exhibit spatial proximity effects with both (PCL and PDLLA) hydrophobic polymer chains and interact with both subdomains, which are characterized by different rigidities. It was deduced that the interfaces between particular subdomains constitute an optimal host space for probe molecules, especially in the context of photochemical stability, photoactivity (i.e., for significant enhancement of singlet oxygen generation rates), and aggregation prevention. The present contribution proves that the combination of an appropriate probe, high-resolution NMR techniques, and UV-vis spectroscopy enables one to gain complex information about the subtle structure of PMs essential for their application as nanocarriers for photoactive compounds, for example, in photodynamic therapy, nanotheranostics, combination therapy, or photocatalysis, where the micelles constitute the optimal microenvironment for the desired photoreactions.

An antimicrobial peptide, nisin Z, was embedded within polyelectrolyte multilayers (PEMs) composed of natural polysaccharides in order to explore the potential of forming a multilayer with antimicrobial properties. Using attenuated total reflection Fourier transform infrared spectroscopy (ATR FTIR), the formation of carrageenan/chitosan multilayers and the inclusion of nisin Z in two different configurations was investigated. Approximately 0.89 µg cm−2 nisin Z was contained within a 4.5 bilayer film. The antimicrobial properties of these films were also investigated. The peptide containing films were able to kill over 90% and 99% of planktonic and biofilm cells, respectively, against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus (MRSA) strains compared to control films. Additionally, surface topography and wettability studies using atomic force microscopy (AFM) and the captive bubble technique revealed that surface roughness and hydrophobicity was similar for both nisin containing multilayers. This suggests that the antimicrobial efficacy of the peptide is unaffected by its location within the multilayer. Overall, these results demonstrate the potential to embed and protect natural antimicrobials within a multilayer to create functionalised coatings that may be desired by industry, such as in the food, biomaterials, and pharmaceutical industry sectors.

Moderate and prolonged payload release in response to a particular factor is highly demanded for efficient carriers of low-molecular-weight, chemically unstable phytopharmaceuticals. Thus, the objective of our contribution was to establish the effect of pH-responsive polyelectrolyte coatings on the release properties of carboxymethyl cellulose-based microparticles designed to deliver phytopharmaceuticals through the gastrointestinal tract. Microparticles were fabricated via extrusion coupled with external gelation and further coated with polyelectrolytes (PEs) (chitosan, gelatin, or PAH and PSS) involving electrostatic interactions. Successful deposition of PEs was confirmed by FTIR, and their thickness and viscosity were characterized in terms of QCM-D and ellipsometric techniques. The encapsulation efficiency of esculin, used as a model phytopharmaceutical, as proven by UV-Vis studies, was over 57%. SEM and fluorescence microscopy revealed a micrometric size, a mostly spherical shape and an altered topography of the investigated microcapsules. The physical stability of the microcapsules in media of various pH values was confirmed with CLSM and gravimetric studies. Studies on human gingival fibroblasts in vitro revealed that the obtained microparticles did not induce any cytotoxic effects. Payload release was monitored in situ by means of CLSM and ex situ under gastrointestinal conditions in vitro. Mathematical evaluation of the microparticle release profiles using classical models led to the establishment of a new hybrid model that revealed the mechanism behind esculin release. We demonstrated that the application of a polyelectrolyte shell onto CMC-based microspheres may provide controlled delivery of the payload, with its release triggered by the pH and ionic strength of the medium. These observations suggest that the release manner of small-molecule glycosides under gastrointestinal conditions can be tailored by careful selection of suitable materials to obtain biocompatible and functional hydrogel microparticles.

The purpose of this study was to compare the chemical composition and biological properties of Polish propolis. Ethanol, ethanol-hexane, hexane and hexane-ethanol extracts of propolis from three different regions of Poland were prepared. On the basis of the evaluation of their chemical composition as well as the extraction yield and free radical scavenging activity, the ethanol and hexane-ethanol extractions were proposed as the most effective methods. Subsequently, the biological properties of the extracts were evaluated to investigate the selectivity of an anticancer effect on tongue cancer cells in comparison to normal gingival fibroblasts. The obtained products demonstrated anticancer activity against tongue cancer cells. Additionally, when the lowest extract concentration (100 &micro, g/mL) was applied, they were not cytotoxic to gingival fibroblasts. Finally, a possible anti-inflammatory potential of the prepared products was revealed, as reduced mitochondrial activity and proliferation of macrophages exposed to the extracts were observed. The results obtained indicate a potential of Polish propolis as a natural product with cancer-selective toxicity and anti-inflammatory effect. However, further studies are still needed to thoroughly explain the molecular mechanisms of its action and to obtain the promising health benefits of this versatile natural product.

Malignant melanoma is an emerging problem worldwide due to the high degree of lethalness. Its aggressiveness and the ability to metastasize along with the heterogeneity at the molecular and cellular levels, limit the overall therapeutic efficacy. Despite significant advances in melanoma treatment over the last decade, there is still a need for improved therapeutic modalities. Thus, we demonstrate here a combinatorial approach that targets multiple independent therapeutic pathways, in which polymeric micelles (PMs) were used as efficacious colloidal nanocarriers loaded with both daunorubicin (DRB) as a cytotoxic drug and IR-768 as a photosensitizer. This afforded the dual drug loaded delivery system IR-768 + DRB in PMs. The fabricated mPEG-b-PLGA micelles (hydrodynamic diameters ≈ 25 nm) had a relatively narrow size distribution (PdI > ca. 0.3) with uniform spherical shapes. CLSM study showed that mPEG-b-PLGA micelles were uptaken by mitochondria, which further contributed to excellent singlet oxygen generation capacity for PDT in A375 melanoma cells. Furthermore, the PMs were efficiently internalized by tested cells through endocytosis, resulting in much higher cellular uptake comparing to the free drug. As a result of these properties, IR-768 + DRB in PMs exhibited very potent and synergistically enhanced anticancer activity against A375 cells. Additionally, this combination approach allowed to reduce drug doses and provided low side effects towards normal HaCaT. This study indicates excellent properties of mPEG-b-PLGA micelles resulting in great therapeutic potential possessed by the developed nanoscale drug delivery system for combined chemo-photodynamic therapy of melanoma.

The studies were aimed to contribute to the elucidation of the relationships between structure of the double-headed cationic surfactants – N,N-bis[3,3′-(dimethylamine)propyl]alkylamide dihydrochlorides and N,N-bis[3,3′-(trimethylammonio)propyl]alkylamide dibromides (alkyl: n-C9H19, n-C11H23, n-C13H27, n-C15H31), which are of particular interest, as they contain a labile amide group in the molecule and their antifungal activity. Therefore, the minimal inhibitory and fungicidal concentrations (MIC and MFC) of dicephalic surfactants against various fungi were tested using standardized methods. Most of the tested fungi were resistant to the Cn(TAPABr)2 compounds. The strongest growth inhibition was caused by Cn(DAPACl)2 series, which MICs ranged from 6.5 to 16 μM. The influence of dicephalic surfactants on Candida albicans biofilm and adhesion to the various surfaces was investigated with crystal violet staining or colony counting. The reduction of fungal adhesion was also observed, especially to the glass surface. One of the compounds (C14(DAPACl)2) caused DNA leakage from C. albicans cells. Further studies showed the impact of dicephalic surfactants on ROS production, accumulation of lipid droplets and filament formation. This study points to the possibility of application of dicephalic surfactants as the surface-coating agents to prevent biofilm formation or as disinfectants. The results give an insight into the possible mechanism of action of newly synthesized dicephalic surfactants in yeast cells.

We present a series of multilayered alginate/chitosan microparticles fabricated via combining ionic gelation with the layer-by-layer (LbL) approach to improve oral administration of large cranberry fruit extract (CFE). Sodium alginate of low (ALGlv) or medium (ALGmv) viscosity was used as a core polymer, and chitosan (CHIT) and ALGmv layers were alternately assembled to form up to seven layers’ coating. Microparticles size ranged between 640 and 1120 μm, and their morphology, moisture content, and structural integrity were affected mainly by the outermost layer’s composition. Both the microgel core and shell composition of these microparticles influenced the mechanical properties determined by the parallel plates compression test. Microparticles exhibited good CFE entrapment efficiency (E.E. > 55%) and favorable release profiles in the simulated gastro-intestine environment, well described by the hybrid model of the release kinetics. Our results evidence that polysaccharide-inspired microparticles are good platforms for enhancing the oral bioavailability of poorly water-soluble therapeutic agents.

The aim of the study was to develop and characterize alginate microparticles coated with polyelectrolytes and containing hesperidin – a natural bioflavonoid of great nutritional potential. Hesperidin's solubility is moderate, thus it was essential to develop a stable carrier which enables its targeted delivery to the intestine. The cargo was entrapped in the alginate (ALG) hydrogel matrix by means of the extrusion/external gelation technique. To achieve customized functional properties of microbeads, biopolymers (chitosan, gelatin) and synthetic polymers (PAH/PSS pair) were deposited on the ALG cores. The fabricated microparticles successfully encapsulated hesperidin (>87%) and were compared in terms of moisture content, surface morphology and particle size (SEM). FTIR spectroscopy confirmed the formation of polyelectrolyte complexes and the microsystems were further characterized with DSC. The swelling and release behaviors were studied in detail, including in vitro release experiments. The results obtained indicate that the fabricated microcapsules revealed the desired pH-dependent release ability.

Exploration of novel lipid-based formulations has been an aim for researchers over the last decades. Lipid nanoparticles have been extensively studied as bioactive agent carriers in the pharmaceutical and biomedical fields. In our studies, we have provided properties of two different types of lipid nanocarriers, i.e. solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) prepared via high pressure homogenization. The choice of surfactants in the structural design is one of the most significant approaches to achieve nanocarriers with desirable parameters that acquire both good stability and requested physical state. The present work has been carried out to explore the potential for fabrication of stable and nearly monodisperse lipid nanoparticles stabilized by functionalized phosphatidylcholine, i.e., 1,2-di(conjugated)linoleoyl-sn-glycero-3-phosphocholine ((CLA)PC) which may comprise a potential lipid prodrug. Additionally, 1,2-distearoyl-sn-glycero-3-phosphocholine ((SA)PC) was taken into account as the surfactant to be compared. The sizes of the studied nanosystems (about 130–230 nm in diameter DH) along with the size distribution (polydiyspersity index PdI below 0.3) were determined by dynamic light scattering (DLS), while the morphology was imaged by atomic force microscopy (AFM). The studied nanoparticles physical state was characterized by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The NLCs have shown less ordered crystalline structure than the SLNs nanoproducts, this observation being conferred by the inclusion of a liquid lipid. The in vitro cytotoxicity studies were performed on human cancer epidermoid carcinoma (A431) and MeWo cells using trypan blue staining and MTT assays. Nanocarriers labeled by cyanine IR-780 were efficient in bioimaging (MeWo). Our results give new insights into the lipid nanoparticles containing the pharmaceutically promising (CLA)PC and may serve as guidelines for design and preparation of new effective delivery nanosystems, including anti-cancer applications.

In the present contribution we focus on the fabrication and characterization of targeted delivery systems suitable for encapsulation of hesperidin (HESP) − a natural health-promoting flavonoid glycoside. We fabricated and extensively studied pH-responsive, biodegradable double-compartment hydrogel carriers composed of sodium carboxymethyl cellulose particles (ACP) filled with hesperidin-loaded sodium alginate microparticles (AMP). Additionally, hesperidin was encapsulated directly in sodium alginate or sodium carboxymethyl cellulose particles (AP or CP, respectively). The obtained carriers were characterized in respect to their morphology and size by using scanning electron microscopy (SEM). The cargo encapsulation was confirmed by spectroscopic analysis (FTIR), while the process efficacies were derived spectrophotometrically (UV–vis). The effect of different pH on the stability of the beads has been assessed. The in vitro release kinetics of the fabricated HESP-loaded particles was studied in simulated gastric and intestinal environments. The fabrication processes yielded stable particles of desired properties. Comparing the results obtained for both single- and double-compartment systems, makes it possible to conclude that the latter is superior in regard to prolonged delivery of hesperidin to the place of action under simulated intestinal conditions.

This study aimed to characterize the hydrogel micro- and macro-particles designed to deliver curcumin to human colon cancer cells (LoVo). Six series of vehicles based on sodium alginate (micro- and macro-particles, uncoated, coated with chitosan or gelatin) were synthesized. The uncoated microparticles were fabricated using an emulsion-based technique and the uncoated macroparticles with an extrusion technique, with both coupled with ionotropic gelation. The surface morphology of the particles was examined with scanning electron microscopy and the average size was measured. The encapsulation efficiency, moisture content, and swelling index were calculated. The release of curcumin from the particles was studied in an experiment simulating the conditions of the stomach, intestine, and colon. To evaluate the anticancer properties of such targeted drug delivery systems, the cytotoxicity of both curcumin-loaded and unloaded carriers to human colon cancer cells was assessed. The microparticles encapsulated much less of the payload than the macroparticles and released their content in a more prolonged manner. The unloaded carriers were not cytotoxic to LoVo cells, while the curcumin-loaded vehicles impaired their viability—more significantly after incubation with microparticles compared to macroparticles. Gelatin-coated or uncoated microparticles were the most promising carriers but their potential anticancer activity requires further thorough investigation.

Understanding the factors that control biopolymeric carriers' drug release profiles is essential to determine their applicability as drug delivery systems. We attempted to evaluate the relationships between the kinetics of the release of selected phytopharmaceuticals from a series of polysaccharide-based particles and the physicochemical properties of the resulting macro- and microcarriers, including alginate (ALG)- and carboxymethyl cellulose (CMC)-based particles with gelatine (GEL) or chitosan (CHIT) shells. Hydrogel beads (612–1080 μm) and microparticles (8.5–44 μm) were successfully loaded with esculin (ESC), hesperidin (HES), or thyme oil (TO), their morphology was elucidated by scanning electron microscopy (SEM), and the encapsulation efficiency was determined by spectrophotometry. The hydrogel carriers exhibited a prolonged payload release (~90–300 min) under simulated gastrointestinal conditions, dependent on the coating type and pH environment. The variations in the particle composition influenced the drug release profiles, which were directly related to the carrier composition and payload characteristics. The Korsmeyer-Peppas and Peppas-Sahlin models, as well as a newly proposed hybrid model, provided the most appropriate description of the payload release from our particles when considered separately under the simulated gastric and intestinal conditions. Additionally, the Gallagher-Corrigan model was selected as the adequate one for predicting the consecutive payload release under those conditions. Establishing the most desirable mathematical model to predict the release profiles facilitated our comprehensively study the mechanism and release kinetics from multiple types of polysaccharide-based delivery vehicles loaded with phytopharmaceuticals possessing different structural and chemical features (i.e., water solubility and log P).