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EN
The fananserin derivative, such as 1-{6-[4-(2-fluorophenyl)piperazin-1-yl]hexyl}-benzo[cd]indol-2(1H)-one (compound FL-4), represents an interesting biologically active substance that can be incorporated into polymeric carriers. Due to its highly hydrophobic nature and poor solubility in conventional solvents, FL-4 was incorporated into a delivery system to improve its solubility, stability, and bioavailability. Based on preliminary studies and DLS analysis, an optimal concentration of FL-4 (10 mg) was selected, ensuring system stability. This system was incorporated into polymer matrices, resulting in two hydrogel delivery systems: M10-J, containing FL-4, and M10-T-J, which combines a thermosensitive nanocarrier with FL-4, both ionically cross-linked. The systems were evaluated for their physicochemical properties, including swelling abilities, degradation, chemical structure (based on FTIR spectra analysis), morphology (based on SEM images), and substance release profiles. The M10-T-J samples showed a swelling ratio of 0.27 g/g in PBS and 0.35 g/g in water, while M10-J exhibited 0.16 g/g in PBS and 0.2 g/g in water. The pH and conductivity analysis suggested a faster degradation process for M10-T-J hydrogel compared to M10-J. FT-IR analysis confirmed the chemical structure of the materials, revealing significant changes in M10-T-J samples, indicating interactions between FL-4 and CaCl₂ used during cross-linking. SEM and EDS analysis showed a uniform distribution of FL-4 on the matrix surface in both hydrogel variants, with the addition of the thermosensitive nanocarrier not significantly affecting the morphology. The M10-J hydrogel exhibited rapid release of FL-4 within the first 4 h, while M10-T-J showed limited release.
EN
Despite the diversity of available formulations for relieving topical symptoms of chronic skin diseases, inflammation, and hypergranulation tissue resulting from burn wounds, their efficacy is limited by side effects, application inconveniences, including the oiliness of the formulations, and the need for frequent application, which can affect patient compliance. Therefore, research has been carried out on freeze-dried hydrogel delivery systems of hydrocortisone, to evaluate their physicochemical (gel fraction, swelling ratio, pH and conductivity measurements), structural (FTIR), and morphological (SEM) properties, as well as their cytotoxicity (MTT tests). The gel fraction of freeze-dried hydrogel biomaterials (M-TH25 and M-TH50) reached 64% ± 0.3 and 63% ± 1.7, respectively, slightly higher than for the reference matrix (M) (61 ± 0.8). The swelling ratio (pH = 7.4) was in the range of 212–253% and 184–222%, respectively, comparable to the reference sample (208–277%). The incorporation of a thermosensitive polymeric nanocarriers (poly-N-isopropylacrylamide copolymers) containing hydrocortisone in the quantitative range 25–50 mg did not significantly change the overall morphology of the biomaterials. Both M and M-TH25 samples exhibit non-cytotoxicity towards mouse fibroblast cells BALB/3T3 (93% ± 10; 100% ± 8) and L929 (114% ± 8; 72% ± 10) cells with an observable variation in response for the M-TH25 sample, likely due to differences in cell behaviour and surface area. Importantly, M-TH50 sample shows cytotoxic effects (40% ± 5; 59% ± 4) mainly resulting from an excessively high concentration of the incorporated active substance. Further studies are planned (including on the release profile and kinetics of hydrocortisone and the assessment of the therapeutic effect), which may help to select an appropriate concentration of drug in the quantitative range 25-40 mg
EN
Curcumin is a natural polyphenol with anti-inflammatory and anticancer potential, but its poor aqueous solubility and limited incorporation into polymeric carriers hinder clinical translation. Covalent or ion-paired conjugation with a polymeric matrix may enhance drug retention and loading, thereby improving delivery efficiency. This study investigated whether introducing acidic conditions to oil-in-water emulsification would promote curcumin–polyanhydride conjugation and improve encapsulation efficiency (EE) and drug loading (DL) in poly(sebacic anhydride) (PSA) microparticles (MPs). The results obtained by fluorimetry show that encapsulation outcomes strongly depended on the acid used. Trifluoroacetic acid (TFA) yielded negligible curcumin incorporation, with EE ranging from 1.7 ± 0.1% to 19.7 ± 0.6% and DL between 0.28 ± 0.01% and 3.3 ± 0.1%. In contrast, hydrochloric acid (HCl) and sulfuric acid (H2SO4) produced results comparable to non-acidified controls, with EE around 30–35% and DL around 5–6%. A markedly different outcome was observed with 2% aqueous trichloroacetic acid (TCA). Condition X21 exhibited the best performance with 53.6 ± 0.5% (EE) and 8.9 ± 0.1% (DL), while another TCA-based formulation (X20) also showed high encapsulation values (EE = 45.5 ± 1.1%, DL = 7.6 ± 0.2%). However, despite this significant improvement in curcumin incorporation, TCA-derived MPs compromised L929 fibroblasts viability, whereas HCl- and H2SO4- treated formulations were cytocompatible. These findings demonstrate that low-concentration aqueous TCA enhances curcumin incorporation into PSA MPs, likely via conjugate formation, but compromises cytocompatibility due to residual TCA. Further optimization of TCA concentration and purification steps will be necessary to balance drug loading with safety for biomedical applications.
4
Content available remote Zastosowanie mezoporowatych nośników niesteroidowych leków przeciwzapalnych
PL
Dokonano przeglądu literaturowego zastosowań mezoporowatych krzemionek jako nośników niesteroidowych leków przeciwzapalnych (NLPZ), takich jak ibuprofen, indometacyna, naproksen i nimesulid. Stosowane nośniki przyczyniły się do poprawy dostępności biologicznej leków na skutek zwiększenia szybkości ich rozpuszczania z powodu dobrze rozwiniętej powierzchni adsorbentu.
EN
A review, with 35 refs., of mesoporous silicas used as carriers for non steroidal anti-inflammatory drugs such as ibuprofen, indomethacin, naproxen and nimesulide. Silicas significantly improved the bioavail ability of the drug as a result of increased dissoln. kinetics due to their well-developed adsorbent surface area.
PL
Przegląd literaturowy dotyczący zastosowania mezoporowatych krzemionek modyfikowanych aptamerami jako nośników leków oraz elementów czujników chemicznych. Przedstawiono rolę aptamerów jako czynników umożliwiających celowane dostarczanie substancji leczniczych do miejsca ich działania. Aptamery stosowane były również jako czynniki wiążące różne ligandy, co umożliwiło otrzymanie testów analitycznych służących do selektywnego wykrywania i oznaczania różnych analitów (środki ochrony roślin, markery nowotworowe).
EN
A review, with 20 refs., of the use of aptamer-modified mesoporous silicas as drug carriers and chem. probes elements. The role of aptamers as the elements enabling targeted drug delivery was described. The aptamers were also shown to be the factors linking different ligands. The usage of as-prepared aptamers enabled to obtain anal. tests to be used for selective detection and detn. of various analytes (pesticides, biological agents).
EN
Biological functionalization is a critical area of research aimed at enhancing the functionality and application of biomaterials in various biomedical fields. One of the key aspects of biofunctionalization involves the addition of growth factors, which can significantly improve the biocompatibility of materials. Enhanced biocompatibility allows these materials to integrate more effectively with surrounding tissues, promoting their acceptance by the body and minimizing the risk of rejection or inflammation. This study is focused on investigations of the surface properties of polyelectrolyte layers, micelles, and complex systems utilizing red blood cells (RBCs) as carriers for growth factors. Through electrostatic interactions between negatively charged RBCs and positively charged polyelectrolytes, it becomes possible to modify red blood cells for use as effective delivery systems. Additionally, polyelectrolyte micelles can be employed for delivery purposes through grafting with suitable polymers. All of the tested surfaces exhibited hydrophilic characteristics, as indicated by measurements of the contact angle. Furthermore, the study determined the zeta potential of modified red blood cells and presented methods for the docking of vascular endothelial growth factor (VEGF) onto both RBCs and micelles. The obtained results highlight the potential of these biofunctionalized systems for improving therapeutic outcomes in regenerative medicine and drug delivery.
EN
MOF materials (metal-organic frameworks) are a relatively organic-inorganic (hybrid) materials. Due to very good adsorption properties, large specific surfaces and large pore volumes, these compounds are quite intensively studied, and the number of organic-inorganic hybrids obtained is growing year by year. Most MOF compounds are crystalline two- or three-dimensional organometallic structures. They are an example of hybrid materials that are made of both inorganic and organic component. The inorganic part is represented by metal ions/clusters, while the organic skeleton contains neutral or charged organic linkers [1-3]. The most common metal cations included in organometallic lattices are: Zn2+, Cu2+, Cr3+, Al3+ and Mg 2+. Organic ligands can be neutral, positively or negatively charged, but they must be primarily electron pair donors, which means that they have nitrogen or oxygen-containing functional groups in their structure. Ligands’ role is to stitch these building units together to create extended framework structures, while metal ions provide structural integrity and durability. These materials have a well-developed specific surface and a large pore volume (570-3800 m2/g). Thanks to the presence of coordination bonds in the structure, the skeletons of organometallic networks are flexible. Based on literature data, several methods of cancer treatment using MOFs are distinguished, e.g.: using passive targeting, active targeting, physicochemical targeting, and in a particular case using all three strategies (Fig. 2, Table 1) [12,13]. The ongoing work on the modification of the synthesized MOF structures based on zinc ions allows the preparing various types of cancer drugs based on their durability and high porosity. The ability to synthesize multifunctional Zn-MOFs is a new chapter in the design of chemotherapeutic agents. A particular example is ZIF-8. The combination of different strategies for the influence of the pH value of the environment or photochemical elements gives the opportunity to use the compounds in imaging and cancer diagnosis.
PL
Przegląd literaturowy dotyczący zastosowania mezoporowatych sit molekularnych jako nośników przeciwzapalnych leków steroidowych. Przedstawiono wykorzystanie mezoporowatych krzemionek jako składników systemów dostarczania leków w przypadku takich substancji leczniczych, jak deksametazon, propionian flutikazonu, furoinian mometazonu oraz fosforan sodu betametazonu. Korzyści terapeutyczne wynikające z zastosowania nośników wynikały głównie z poprawy dostępności biologicznej leku na skutek zwiększenia szybkości jego rozpuszczania z dobrze rozwiniętej powierzchni mezoporowatego adsorbentu.
EN
A review, with 40 refs., of use of mesoporous silicas as the carriers for anti-inflammatory steroid drugs such as dexamethasone, fluticasone propionate, mometasone furoate, and betamethasone sodium phosphate. The advantages resulting from the use of mesoporous silicas as the drug carriers were mainly ascribed to the drug biological availability improvement. The latter was the result of the acceleration of dissolution kinetics of drug adsorbed onto the large surface area of mesoporous adsorbent.
EN
As a natural mineral, calcium carbonate (CaCO3) is widely investigated for various medical applications. It is a biocompatible material characterized by high degradation rate and great osteoconductivity. Many researchers evaluate CaCO3 in the form of particles as a candidate for use in drug delivery systems. In this study we present an optimization of the process of producing CaCO3 particles by the precipitation method with the use of combinations of different time of ultrasound treatment and surfactant concentrations used. Depending on the synthesis conditions, various sizes of particles were fabricated. The particles were loaded with sodium alendronate (Aln, 5% or 10% by weight) with a relatively high encapsulation efficiency between 40 and 50%, depending on the amount of Aln added and the drug loading of approximately 9% for both cases. MG-63 osteoblast-like cells were contacted with 10% wt./vol extracts of fabricated particles to assess their cytotoxicity. None of the extracts investigated was found to be cytotoxic. Furthermore, an in vitro study in direct contact of MG-63 cells with particles suspended in culture medium was performed. The results showed that the fabricated particles are cytocompatible with osteoblast-like MG-63 cells. However, the higher the concentration of the particle suspension and the greater the amount of alendronate present in the solution, the lower the metabolic activity of the cells was measured. The presented method of CaCO3 particles manufacturing is simple, cost-effective, and allows one to fabricate particles of the required size and shape that are cytocompatible with MG-63 cells in defined concentrations of particle suspensions.
PL
Porównano właściwości adsorpcyjne krzemionki SBA-15 oraz Aerosil wobec terfenadyny jako modelowej substancji leczniczej. Dowiedziono, że krzemionka mezoporowata odznacza się prawie dwukrotnie większą pojemnością adsorpcyjną (160,4 mg/g) wobec leku aniżeli krzemionka koloidalna (85,7 mg/g) przy jednocześnie dwukrotnie mniejszej wartości ilości adsorbatu przypadającej na jednostkę powierzchni adsorbentu. Przeprowadzono matematyczną interpretację procesu adsorpcji, stosując modelowe izotermy: Freundlicha, Langmuira, Jovanovicia, Dubinina i Astachowa oraz Redlicha i Petersona. Wykazano, że dominującą siłą oddziaływania leku z powierzchnią krzemionek jest adsorpcja fizyczna.
EN
Terfenadine was adsorbed from its solns. in MeCN on a SBA-15 and Aerosil SiO2. Nonlinear fitting anal. was used to estimate the parameters of the Freundlich, Langmuir, Jovanovic, Dubinin-Astakhov and Redlich-Peterson isotherms. The max. adsorption capacity was 160.4 mg/g and 85.7 mg/g (Dubinin-Astakhov model) for SBA-15 and Aerosil silicas resp. It was shown that phys. adsorption was the main force of drug-SiO2 surface interactions.
EN
Microparticles (MPs) made of fast biodegrading biomaterials, loaded with drugs, are considered a superior treatment method for pulmonary infections. One of the promising biomaterials for obtaining such a drug delivery system (DDS) is poly(sebacic anhydride) (PSA) due to its favourable degradation kinetics and mechanism. In this paper, we present a study of manufacturing MPs from PSA loaded with curcumin (CU) for pulmonary purposes. MPs were manufactured by oil-in-water emulsification; their morphology and size distribution were evaluated using optical microscopy, while the encapsulation efficiency and drug loading were obtained by the fluorometric assay. The cytotoxicity of the MPs, both the empty ones and loaded with CU, was analysed by in vitro tests with BEAS-2B human lung epithelial cells. To this end, metabolic activity by AlamarBlue assay and fluorescent staining (DAPI/ eosin) of the cells were performed. The MPs produced were round, regular in shape with diameters in the range of 1-5 µm and of yellow colour originating from CU. The CU encapsulation efficiency ranged from 42% to 55% and decreased with a higher CU ratio. The drug loading ranged from 4% to 11% and increased at a higher CU ratio. Both empty and CU-loaded MPs did not show a cytotoxic effect at concentrations up to 10 µg/ml.
EN
In recent decades, research has focused on the development of modern hydrogel dressings due to their open porous structure, moisture retention and good mechanical strength, which ensures an optimal environment for cell migration and proliferation. Active hydrogel dressings, currently available on the market, are not endowed with additional medicinal substances. In this work the authors attempted to introduce a carrier-drug system into the hydrogel matrix to improve the wound healing process and the tissue recovery. The main goal of the research was to obtain the bio-hybrid sodium alginate/poly(vinyl alcohol)/Aloe vera (SA/PVA/AV)-based hydrogel matrices modified with the thermosensitive polymeric carrier – the active substance (hydrocortisone) system. First, thermosensitive polymeric nanocarriers were obtained, then the encapsulation was conducted, using varied amounts of hydrocortisone (25 and 50 mg) to maintain the stability of the resulting emulsions. The last stage was preparing the bio-hybrid hydrogel matrices by the chemical cross-linking method. The non-invasive dynamic light scattering (DLS) technique was employed for the analysis of the average particle size of the polymeric carriers and the carrier-drug systems. Moreover, the studies also determined the swelling behaviour and the gel fraction of the obtained bio-hybrid hydrogel matrices modified with carrier-drug systems by the infrared spectroscopy (FT-IR). The presented research results constitute a good experimental basis for further modifications, the final effect of which is assumed to be a modern bio-hybrid 3rd generation dressing.
EN
This overview will discuss the smart polymers as drug nanocarries, their construction and shapes showing their using for controlled insulin release. The report will focus on diabetes mellitus as a disease unit, its etiology and treatment by injection and by using smart polymers. The ingredients described in this article are: poly- (methacrylic acid-g-ethylene glycol), hyaluronic acid, G-CSF-transferrin conjugate in cultured enterocyte-like Caco-2 monolayers, poly(hydroxybutyrate-co-hydroxyhexanoate) and chitosan. Such “intelligent” polymers and their use in a controlled insulin release in diabetic therapy are immensely promising.
EN
Reactive surfactants, due to their versatility, are being rapidly developed and they are finding more and more applications. The aim of this paper is to present recent advances in the chemistry and technology of functional surfactants: surfmers (polymerizable surfactants), inisurfs (surface-active initiators), and transurfs (surfaceactive transfer agents). Reactive surfactants, beside other advantages, are also environmentally friendly and their use can reduce costs of chemical processes. In this part of a brief review, basic information about reactive surfactants is presented and surfmers are described and discussed. Surfmers combine properties of surfactants (surface activity) and monomers (ability to polymerize). They are widely used for emulsion polymerization, but their other, more sophisticated applications include miniemulsion stabilization, nanomaterials synthesis, drug-delivery systems, and hydrogels.
PL
Ze względu na wszechstronność zastosowań reaktywnych surfaktantów następuje szybki rozwój metod syntezy tej grupy związków. W artykule zaprezentowano najnowsze osiągnięcia chemii i technologii reak­tywnych surfaktantów: surfmerów (surfaktantów zdolnych do polimeryzacji), inisurfów (powierzchniowo czynnych inicjatorów) oraz transurfów (powierzchniowo czynnych środków przeniesienia łańcucha). Zastosowanie reaktywnych surfaktantów może uczynić proces chemiczny bardziej przyjaznym środowisku i obniżyć koszty jego prowadzenia. W tej części artykułu przedstawiono najważniejsze informacje dotyczące reaktywnych surfaktantów oraz opisano szerzej surfmery, które łączą w sobie właściwości charakterystyczne dla surfaktantów (aktywność powierzchniowa) oraz monomerów (zdolność do polimeryzacji). Surfmery są szeroko stosowane w polimeryzacji emulsyjnej, ale mają również inne, bardziej wyrafinowane zastosowania, takie jak: stabilizacja miniemulsji, synteza nanomateriałów, systemy dostarczania leków i hydrożele.
PL
Przedstawiono sposób otrzymywania układów terapeutycznych opartych na połączeniu mezoporowatej krzemionki SBA-15 i polimerów w celu osiągnięcia spowolnionego uwalniania winianu metoprololu. Wykazano, że wzrastająca zawartość polimeru sprzyjała wolniejszemu uwalnianiu substancji leczniczej z matrycy SBA-15. Najwolniejszą kinetykę uwalniania winianu metoprololu obserwowano dla krzemionki zawierającej 4% mas. alginianu sodu lub 16% mas. poli(alkoholu winylowego). Dokonano charakterystyki nośników leków z użyciem skaningowej mikroskopii elektronowej, sorptometrii azotu oraz analizy dyfraktometrycznej (XRD).
EN
Mesoporous SiO2 was impregnated with aq. solns. of poly(vinyl pyrrolidone), poly(vinyl alc.) and Na alginate and used as a support for metoprolol tartrate in a drug-delivery system. The addn. of polymers resulted in a decrease in the drug release (increase in residence time from 5 h up to 10–15 h).
PL
Celem pracy było doświadczalne wykazanie na przykładzie substancji modelowej - witaminy B12 (cyjanokobalaminy) możliwości wykorzystania membran do kontrolowanego spowolnienia transportu masy. Sam alginian sodu w niewystarczający sposób reguluje tempo uwalniania substancji organicznych. Przez zastosowanie porowatych membran polimerowych z octanu celulozy czy też z polieterosulfonu transport masy spowolniono kilkaset razy, przybliżając wartość strumienia masy do wartości oczekiwanych przy transporcie leków.
EN
The aim of this paper was to prove experimentally, based on model organ compound - vitamin B12 (cyanocobalamin), the possibility of membrane application in the controlled slowdown of mass transport. A sodium alginate alone does not control sufficiently the rate of organic compound release The mass transport was slowed down several hundred times using porous, polymer membranes made of cellulose acetate or polyethersulfone, achieving mass stream values expected in drug delivery.
PL
W pracy przedstawiono wyniki badań uwalniania radiouczulacza metronidazolu z jednowarstwowych oraz trójwarstwowych matryc kopolimeru glkolidu z laktydem do sztucznego płynu mózgowo rdzeniowego ACFs. Przeprowadzono analizę mikrostruktury łańcuchów polimerowych w oparciu o spektroskopię magnetycznego rezonansu jądrowego. Badanie uwalniania leku prowadzono w systemie dynamicznym z regularną wymianą buforu we fiolkach poddanych wytrząsaniu. Ekstrakty analizowano metodą spektrometrii UV-VIS. Równolegle prowadzono badania degradacji matryc z lekiem pod kątem oceny zmian w mikrostrukturze łańcucha polimerowego. Badania wykazały znacznie szybszą degradację matryc wykonanych z kopolimeru glikolidu z D,L-laktydem w porównaniu z matrycami z kopolimeru glikolidu z L-laktydem. Ponadto wykazano że opłaszczenie matrycy zawierającej lek polimerem bez leku (matryce trójwarstwowe) zapobiega nagłemu wyrzutowi leku z powierzchni w pierwszych dniach uwalniania.
EN
In this paper the results of radiosensitizer metronidazole release investigation from mono- and triple-layered copolymeric matrices in artificial cerebro- spinal fluid solution (ACFs) are presented. The analysis of polymeric chain microstructure by the NMR has been conducted. Drug release study was performed in the dynamic system with regular buffer exchange in constantly stirred glass ampoules. The extracts were analyzed by the UV-VIS spectrometry. Drug carrying matrices degradation research were conducted to evaluate possible changes in polymeric chain microstructure. The results showed that matrices containing poly(glycolide-co-D,L-lactide) demonstrate higher degradation rate than matrices containing poly(glycolide-co-L-lactide). It has been proved that drug carriers coated with drug-free polymer (triplelayered matrices) prevents from burst effect.
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