Search Results (19)

Polyelectrolyte complexes (PECs) are recognized as promising materials for the development of sustainable food packaging. In this study, eco-friendly PECs based on pectin (P) and chitosan (C) were prepared by solvent casting at different pH values and volume ratios (C, P, 1C:1P, 1C:2.5P, and 1C:5P) (v/v). The resulting films were characterized for numerous features, including thickness, opacity, moisture content, swelling degree, and water solubility, while mechanical performance (elongation at break and tensile strength), water vapor transmission rate (WVTR), surface energy, and anti-adhesive activity were evaluated for the most promising formulation. The results revealed that blending chitosan with pectin significantly improved the films’ physicochemical properties, notably by increasing thickness (up to 100 µm) and opacity (slightly above 2) while reducing the swelling degree (from over 1800% for pure chitosan to below 600% for 1C:2.5P film at pH 3.2) and the water solubility (from 100% for pectin films to around 45–50% for the blended films). The film 1C:2.5P at pH 3.2 showed improved barrier performance, with a lower WVTR (approximately 20 g/h·m²) compared to the single polymer films (more than 30 g/h·m²), and exhibited significant anti-adhesive activity by reducing bacterial adhesion to below 5% compared to 65% for the conventional packaging film. However, these improvements were accompanied by reduced tensile strength (From ~4.2 MPa to ~1.3 MPa) and in elongation at break (from ~50% to ~20%). Overall, PEC films demonstrate strong potential as sustainable packaging materials by combining improved barrier properties and anti-adhesive activity, despite some limitations in mechanical resistance. Full article

The low effectiveness of various brain cancer treatment methods is due to a number of significant challenges. Most of them are unable to penetrate the blood–brain barrier (BBB) when drugs are administered systemically through the bloodstream. Nanoscale particles play a special role among materials capable of binding drug molecules and successfully crossing the BBB. Biopolymeric nanoparticles (NPs) demonstrate excellent biocompatibility and have the remarkable ability to modify the environment surrounding tumor cells, thereby potentially improving cellular uptake of delivery agents. In our research, nanoscale polyelectrolyte complexes (PECs) ranging in size from 56 to 209 nm were synthesized by ionic interaction of the oppositely charged polysaccharides pectin and chitosan. The structural characteristics of these complexes were carefully characterized by infrared (FTIR) and Raman spectroscopy. The immobilization efficiency of antitumor drugs was comprehensively evaluated using UV spectrophotometry. The cytotoxicity of the NPs was evaluated in the U87-MG cell line. The preliminary data indicate a significant decrease in the metabolic activity of these tumor cells. Important details on the interaction of the NPs with an endothelial layer structurally similar to the BBB were obtained by simulating the BBB using a model based on human blood vessels. Our studies allowed us to establish a significant correlation between the kinetic parameters of drug immobilization and the ratio of biopolymer concentrations in the initial compositions, which provides valuable information for future optimization of drug delivery system design. Full article

Atorvastatin calcium, an antifungal agent, has the potential to be repositioned/repurposed to combat the increasing antimicrobial resistance. However, one of the most crucial issues in developing atorvastatin calcium-loaded products with a topical antifungal effect is achieving the optimal release and dissolution rates of this statin to produce the desired therapeutic effect. In this paper, we report on the development and pharmaceutical assessment of hydrogels composed of low-molecular-weight chitosan, tragacanth, and xanthan gum/pectin/κ-carrageenan as potential drug carriers for atorvastatin calcium for buccal delivery. Multidirectional analysis of the carriers with regard to their drug-release profiles and mucoadhesive, antimicrobial, and cytotoxic properties was accompanied by an evaluation of the freeze-drying process used to improve the hydrogels’ applicability. Using differential scanning calorimetry, Fourier transform infrared spectroscopy, and scanning electron microscopy techniques, the role of lyophilization in enhancing atorvastatin calcium delivery from polyelectrolyte complex-based matrices via drug amorphization was demonstrated. The freeze-dried hydrogels had significantly improved release and dissolution rates for the amorphic statin. Therefore, there is great potential for the use of lyophilization in the design of polyelectrolyte complex-based semi-solids in usable dosage forms for numerous crystalline and poorly water-soluble active substances. Full article

Polyelectrolyte complexes (PECs) have gained increasing attention in recent decades due to their importance in various applications, such as water treatment and paper processing. These complexes are formed by mixtures of polycations (n+) and polyanions (n−), known as polyelectrolytes (PEs). In this study, a series of PECs were prepared with different molar charge ratios (n−/n+) using biopolymers such as chitosan (lch) and pectin (p) at pH 5, in addition to the synthetic polymer poly(ethylene alt maleic acid) (PEMA) at the same pH. Two types of chitosan—low molecular weight chitosan (lch) and high molecular weight chitosan (hch)—were used as polycations, and these were mixed with two types of pectin with either a high esterification degree (hp) or a low esterification degree (lp), as well as PEMA as polyanions. These components interacted via electrostatic forces to form the following PEC combinations: (lch&lp), (lch&hp), (hch&hp), and (lch&PEMA). The charge density, turbidity, and particle size of the formed PECs were examined to evaluate the influence of molecular weight and mixing speed on the formation process. Full article

Conventional chemotherapeutic approaches currently used for brain tumor treatment have low efficiency in targeted drug delivery and often have non-target toxicity. Development of stable and effective drug delivery vehicles for the most incurable diseases is one of the urgent biomedical challenges. We have developed polymer nanoparticles (NPs) with improved temozolomide (TMZ) delivery for promising brain tumor therapy, performing a rational design of polyelectrolyte complexes of oppositely charged polysaccharides of cationic chitosan and anionic pectin. The NPs’ diameter (30 to 330 nm) and zeta-potential (−29 to 73 mV) varied according to the initial mass ratios of the biopolymers. The evaluation of nanomechanical parameters of native NPs demonstrated changes in Young’s modulus from 58 to 234 kPa and adhesion from −0.3 to −3.57 pN. Possible mechanisms of NPs’ formation preliminary based on ionic interactions between ionogenic functional groups were proposed by IR spectroscopy and dynamic rheology. The study of the parameters and kinetics of TMZ sorption made it possible to identify compounds that most effectively immobilize and release the active substance in model liquids that simulate the internal environment of the body. A polyelectrolyte carrier based on an equal ratio of pectin–chitosan (0.1% by weight) was selected as the most effective for the delivery of TMZ among a series of obtained NPs, which indicates a promising approach to the treatment of brain tumors. Full article

Worldwide, 40 to 50% of women suffer from reproductive tract infections. Most of these infections are mixed infections, are recurrent and difficult to treat with antimicrobials or antifungals alone. For symptomatic relief of infections, oral antimicrobial therapy must be combined with topical therapy. The purpose of this work is to optimize and develop a polyelectrolyte complex (PEC) of chitosan/anion for the formulation of posaconazole- and probiotic-loaded vaginal hydrogel inserts with prolonged release and significant mucoadhesion. PECs were prepared using chitosan as cationic and carrageenan, pectin and polycarbophil as anionic polymers via a lyophilization technique. PEC formation was confirmed by scanning electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry, by observing changes in its surface, physical and thermal properties. The probiotic, Lactobacillus casei, was added to the PEC during the lyophilization process and the effect on the probiotic viability was studied. The PECs were further compressed along with posaconazole to form hydrogel inserts and optimized using a 3² full-factorial design. The hydrogel inserts were assessed for swelling behavior, drug release, in vitro mucoadhesion and in vitro antifungal activity. The chitosan–pectin hydrogel insert demonstrated excellent mucoadhesion (1.25 N), sustained drug release (88.2 ± 2.4% in 8 h) and a swelling index of 154.7%. The efficacy of hydrogel inserts was evaluated using in vitro study with a co-culture of Lactobacillus casei and Candida albicans. This study revealed an increase in Lactobacilli casei count and a significant drop in the viable count of Candida albicans (4-log reduction in 24 h), indicating the effectiveness of hydrogel inserts in alleviating the fungal infection. Overall, our study demonstrated the potential of the hydrogel insert for preventing vaginal infection and restoring normal vaginal microbiota. Full article

Preparation of stable hydrogels using physically (electrostatically) interacting charge-complementary polyelectrolyte chains seems to be more attractive from a practical point of view than the use of organic crosslinking agents. In this work natural polyelectrolytes—chitosan and pectin—were used, due to their biocompatibility and biodegradability. The biodegradability of hydrogels is confirmed by experiments with hyaluronidase as an enzyme. It has been shown that the use of pectins with different molecular weights makes it possible to prepare hydrogels with different rheological characteristics and swelling kinetics. These polyelectrolyte hydrogels loaded with cytostatic cisplatin as a model drug provide an opportunity for its prolonged release, which is important for therapy. The drug release is regulated to a certain extent by the choice of hydrogel composition. The developed systems can potentially improve the effects of cancer treatment due to the prolonged release of cytostatic cisplatin. Full article

The eco-friendly polyelectrolyte bilayer films were prepared by layer-by-layer (LBL) casting method using chitosan (CS) and four types of edible citrus pectin as film substrates. The results showed that the polyelectrolyte bilayer films exhibited excellent comprehensive properties. Furthermore, the interaction between CS and pectin was closely related to the degree of methyl-esterification (DM), molecular weight (M_w), and zeta potential of pectin. The low DM, M_w, and high zeta potential of the low methyl-esterified pectin (LM) resulted in a denser internal structure of the bilayer film, stronger UV shielding performance, and stronger gas barrier ability. The high DM and M_w of the high methyl-esterified pectin (HM) endow the bilayer film with stronger mechanical properties, thermal stability, and antifogging property. The microstructural and spectroscopic analysis showed that there are hydrogen bonds and electrostatic interactions between the layers. Overall, the developed CS-pectin polyelectrolyte bilayer films provided potential applications for food bioactive packaging. Full article

Polyelectrolyte multilayers (PEMs) based on polyelectrolyte complex (PEC) structures are recognized as interesting materials for manufacturing functionalized coatings or drug delivery platforms. Difficulties in homogeneous PEC system development generated the idea of chitosan (CS)/low-methoxy amidated pectin (LM PC) multilayer film optimization with regard to the selected variables: the polymer ratio, PC type, and order of polymer mixing. Films were formulated by solvent casting method and then tested to characterize CS/LM PC PECs, using thermal analysis, Fourier transform infrared spectroscopy (FTIR), turbidity, and zeta potential measurements. The internal structure of the films was visualized by using scanning electron microscopy. Analysis of the mechanical and swelling properties enabled us to select the most promising formulations with high uniformity and mechanical strength. Films with confirmed multilayer architecture were indicated as a promising material for the multifunctional systems development for buccal drug delivery. They were also characterized by improved thermal stability as compared to the single polymers and their physical mixtures, most probably as a result of the CS–LM PC interactions. This also might indicate the potential protective effect on the active substances being incorporated in the PEC-based films. Full article

Considering the significance of its demand around the world, the accurate determination of fish freshness with a simple and rapid procedure has become an interesting issue for the fishing industry. Hence, we aimed to fabricate a new optical pH sensor based on a polyelectrolyte (PEC) membrane of pectin–chitosan and the active material chromoionophore ETH 5294. A trial-and-error investigation of the polymer compositions revealed that the optimum ratio of pectin to chitosan was 3:7. With an optimum wavelength region (λ) at 610 nm, the constructed sensor was capable of stable responses after 5 min exposure to phosphate-buffered solution. Furthermore, the obtained sensor achieved optimum sensitivity when the PBS concentration was 0.1 M, while the relative standard deviation values ranged from 2.07 to 2.34%, suggesting good reproducibility. Further investigation revealed that the sensor experienced decreased absorbance of 16.67–18.68% after 25 days of storage. Employing the optimum conditions stated previously, the sensor was tested to monitor fish freshness in samples that were stored at 4 °C and ambient temperature. The results suggested that the newly fabricated optical sensor could measure pH changes on fish skin after 25 h storage at room temperature (pH 6.37, 8.91 and 11.02, respectively) and 4 °C (pH 6.8, 7.31 and 7.92, respectively). Full article

Buccal films are recognized as easily applicable, microbiologically stable drug dosage forms with good retentivity at the mucosa intended for the therapy of oromucosal conditions, especially infectious diseases. Multilayer films composed of layers of oppositely charged polymers separated by ionically interacting polymeric chains creating polyelectrolyte complexes represent very interesting and relatively poorly explored area. We aimed to develop the antifungal multilayer systems composed of cationic chitosan and anionic pectin as potential platforms for controlled delivery of clotrimazole. The systems were pharmaceutically characterized with regard to inter alia their release kinetics under different pH conditions, physicomechanical, or mucoadhesion properties with using an animal model of the buccal mucosa. The antifungal activity against selected Candida sp. and potential cytotoxicity with regard to human gingival fibroblasts were also evaluated. Interactions between polyions were characterized with Fourier transform infrared spectroscopy. Different clotrimazole distribution in the films layers highly affected their in vitro dissolution profile. The designed films were recognized as intelligent pH-responsive systems with strong antifungal effect and satisfactory safety profile. As addition of chitosan resulted in the improved antifungal behavior of the drug, the potential utilization of the films in resistant cases of oral candidiasis might be worth of further exploration. Full article

Biopolymers have several advantages for the development of drug delivery systems, since they are biocompatible, biodegradable and easy to obtain from renewable resources. However, their most notable advantage may be their ability to adhere to biological tissues. Many of these biopolymers have ionized forms, known as polyelectrolytes. When combined, polyelectrolytes with opposite charges spontaneously form polyelectrolyte complexes or multilayers, which have great functional versatility. Although only one natural polycation—chitosan has been widely explored until now, it has been combined with many natural polyanions such as pectin, alginate and xanthan gum, among others. These polyelectrolyte complexes have been used to develop multiple mucoadhesive dosage forms such as hydrogels, tablets, microparticles, and films, which have demonstrated extraordinary potential to administer drugs by the ocular, nasal, buccal, oral, and vaginal routes, improving both local and systemic treatments. The advantages observed for these formulations include the increased bioavailability or residence time of the formulation in the administration zone, and the avoidance of invasive administration routes, leading to greater therapeutic compliance. Full article

A simple optical pH sensor based on immobilization, Dioscorea alata L. anthocyanin methanol extract, onto a pectin–chitosan polyelectrolyte complex (pectin–chitosan PEC), has been successfully fabricated. The optical pH sensor was manufactured as a membrane made of pectin–chitosan PEC and the extracted anthocyanin. This sensor has the highest sensitivity of anthocyanin content at 0.025 mg/L in phosphate buffer and 0.0375 mg/L in citrate buffer. It also has good reproducibility with a relative standard deviation (%RSD) of 7.7%, and gives a stable response at time values greater than 5 min from exposure in a buffer solution, and the sensor can be utilized within five days from its synthesis. This optical pH sensor has been employed to determine saliva pH of people of different ages and showed no significant difference when compared to a potentiometric method. Full article

This work proposes a novel complex multi-layered material consisting of porous titanium as a substrate and a complex coating consisting of a chitosan film engulfing microsphere loaded with growth factors such as BMP2 (bone morphogenic protein 2) and IGF1 (insulin-like growth factor-1). The microspheres were obtained through deposition of dual layers of calcium cross linked pectin–chitosan/pectin polyelectrolyte onto a BSA (bovine serum albumin) gel core. The multilayer was conceived to behave like a 3rd generation biomaterial, by slow delivery of viable growth factors around implants, and to assist the healing of implantation wound and the development of new vital bone. The biologic effect of the delivery of growth factors was studied in vitro, on MSC-CD1 mesenchymal stem cells, and in vivo, on CD1 mice. Proliferation and differentiation of cells were accelerated by growth factors, especially IGF1 for proliferation and BMP2 for differentiation. In vivo tests analyzed histologically and by MicroCT show a more structured tissue around BMP2 samples. The present concept will give the best clinical results if both growth factors are delivered together by a coating film that contains a double population of microcarriers. Full article

In recent years, liposomes have gained increasing attention for their potential applications as drug delivery systems in the pharmaceutic, cosmetic and food industries. However, they have a tendency to aggregate and are sensitive to degradation caused by several factors, which may limit their effectiveness. A promising approach to improve liposomal stability is to modify liposomal surfaces by forming polymeric layers. Among natural polymers, chitosan has received great interest due to its biocompatibility and biodegradability. This review discussed the characteristics of this combined system, called chitosomes, in comparison to those of conventional liposomes. The coating of liposomes with chitosan or its derivatives improved liposome stability, provided sustained drug release and increased drug penetration across mucus layers. The mechanisms behind these results are highlighted in this paper. Alternative assembly of polyelectrolytes using alginate, sodium hyaluronate, or pectin with chitosan could further improve the liposomal characteristics. Chitosomal encapsulation could also ensure targeted delivery and boost the antimicrobial efficacy of essential oils (EOs). Moreover, chitosomes could be an efficient tool to overcome the major drawbacks related to the chemical properties of EOs (low water solubility, sensitivity to oxygen, light, heat, and humidity) and their poor bioavailability. Overall, chitosomes could be considered as a promising strategy to enlarge the use of liposomes. Full article