Every year many drug molecules discovered to be effective in treatment of many diseases, however not all of these drugs succeed in reaching the market. One of the main reasons for such failure is the lipophilicity or low water solubility of these chemicals which results in poor bioavailability. Nanoemulsion has the ability to deliver these drugs in an efficient way. Nanoemulsion, which is usually o/w emulsion can incorporate this lipophilic drug into nanolipoidal droplets. However, the difficulty in applying liquid dosage form can be overcome by using nanoemulgel system. Nanoemulgel considered as a suitable way to deliver lipophilic drugs through topical route. This review tries to highlight the importance of nanoemulgel as a drug delivery system. The components of the systems have been explored and the methods of preparations including high energy methods and low energy methods have been discussed. Different methods were used in characterization of such delivery system; all of these methods and techniques were reviewed briefly. Finally, the recent researches about different applications of emulgel in local delivery or systemic delivery has been discussed. To conclude, the nanoemulgel applications in drug delivery is very promising and many products will find their way to the markets soon.

• MeSH
• aplikace kožní MeSH
• emulze * aplikace a dávkování   farmakologie   MeSH
• nanočásticový lékový transportní systém * farmakologie   MeSH
• nanogely chemie   MeSH
• změna skupenství MeSH
• Publikační typ
• práce podpořená grantem MeSH
• přehledy MeSH

The molecular weight (Mw) of dextran derivatives, such as regioselectively oxidized dicarboxydextran (DXA), is greatly influencing their faith in an organism, which could be possibly used to improve anticancer drug delivery. Here we present a modified method of sulfonation-induced chain scission allowing direct and accurate control over the Mw of DXA without increasing its polydispersity. Prepared DXA derivatives (Mw = 10-185 kDa) have been conjugated to cisplatin and the Mw of the carrier found to have a significant impact on cisplatin release rates, in vitro cytotoxicity, and migrastatic potential. Conjugates with the high-Mw DXA showed particularly increased anticancer efficacy. The best conjugate was four times more effective against malignant prostatic cell lines than free cisplatin and significantly inhibited the ovarian cancer cell migration. This was traced to the characteristics of spontaneously formed cisplatin-crosslinked DXA nanogels influenced by Mw of DXA and amount of loaded cisplatin.

• MeSH
• adenokarcinom farmakoterapie   metabolismus   MeSH
• antitumorózní látky chemie   farmakologie   MeSH
• buňky A549 MeSH
• cisplatina chemie   farmakologie   MeSH
• dextrany chemie   MeSH
• lidé MeSH
• molekulová hmotnost MeSH
• nádory prostaty farmakoterapie   metabolismus   MeSH
• nádory vaječníků farmakoterapie   metabolismus   MeSH
• nádory farmakoterapie   metabolismus   MeSH
• nanogely chemie   MeSH
• nosiče léků chemie   MeSH
• oxidace-redukce MeSH
• pohyb buněk účinky léků   MeSH
• systémy cílené aplikace léků metody   MeSH
• Check Tag
• lidé MeSH
• mužské pohlaví MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH

Horseradish peroxidase (HRP)/H2O2-mediated crosslinking of polypeptides in inverse miniemulsion is a promising approach for the development of next-generation biocompatible and biodegradable nanogels. Herein, we present a fundamental investigation of the effects of three surfactants and their different concentrations on the (HRP)/H2O2-mediated nanogelation of poly[N5-(2-hydroxyethyl)-l-glutamine-ran-N5-propargyl-l-glutamine-ran-N5-(6-aminohexyl)-l-glutamine]-ran-N5-[2-(4-hydroxyphenyl)ethyl)-l-glutamine] (PHEG-Tyr) in inverse miniemulsion. The surfactants sorbitan monooleate (SPAN 80), polyoxyethylenesorbitan trioleate (TWEEN 85), and dioctyl sulfosuccinate sodium salt (AOT) were selected and their influence on the nanogel size, size distribution, and morphology was evaluated. The most effective nanogelation stabilization was achieved with 20 wt% nonionic surfactant SPAN 80. The diameter of the hydrogel nanoparticles was 230 nm (dynamic light scattering, DLS) and was confirmed also by nanoparticle tracking analysis (NTA) which showed the diameters ranging from 200 to 300 nm. Microscopy and image analyses showed that the nanogel in the dry state was spherical in shape and had number-average diameter Dn = 26 nm and dispersity Р= 1.91. In the frozen-hydrated state, the nanogel appeared porous and was larger in size with Dn = 182 nm and Р= 1.52. Our results indicated that the nanogelation of the polymer precursor required a higher concentration of surfactant than classical inverse miniemulsion polymerization to ensure effective stabilization. The developed polypeptide nanogel was radiolabeled with 125I, and in vivo biodistribution and blood clearance evaluations were performed. We found that the 125I-labeled nanogel was well-biodistributed in the bloodstream, cleared from mouse blood during 48 h by renal and hepatic pathways and did not provoke any sign of toxic effects.

• MeSH
• myši MeSH
• nanogely MeSH
• peptidy MeSH
• peroxid vodíku * MeSH
• polyethylenglykoly MeSH
• polyethylenimin MeSH
• povrchově aktivní látky * MeSH
• tkáňová distribuce MeSH
• zvířata MeSH
• Check Tag
• myši MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH

Nanogels represent a pivotal class of biomaterials in the therapeutic intracellular treatment of many diseases, especially those involving the central nervous system (CNS). Their biocompatibility and synergy with the biological environment encourage their cellular uptake, releasing the curative cargo in the desired area. As a main drawback, microglia are generally able to phagocytize any foreign element overcoming the blood brain barrier (BBB), including these materials, drastically limiting their bioavailability for the target cells. In this work, we investigated the opportunity to tune and therefore reduce nanogel internalization in microglia cultures, exploiting the orthogonal chemical functionalization with primary amine groups, as a surface coating strategy. Nanogels are designed by following two methods: the direct grafting of aliphatic primary amines and the linkage of -NH2 modified PEG on the nanogel surface. The latter synthesis was proposed to evaluate the combination of PEGylation with the basic nitrogen atom. The achieved results indicate the possibility of effectively modulating the uptake of nanogels, in particular limiting their internalization using the PEG-NH2 coating. This outcome could be considered a promising strategy for the development of carriers for drugs or gene delivery that could overcome microglia scavenging.

• MeSH
• aminy farmakologie   MeSH
• biokompatibilní potahované materiály farmakologie   MeSH
• dynamický rozptyl světla MeSH
• endocytóza účinky léků   MeSH
• fluorescence MeSH
• mikroglie cytologie   účinky léků   MeSH
• molekulární modely MeSH
• myši inbrední C57BL MeSH
• nanogely chemie   MeSH
• protonová magnetická rezonanční spektroskopie MeSH
• spektroskopie infračervená s Fourierovou transformací MeSH
• velikost částic MeSH
• viabilita buněk účinky léků   MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH

BACKGROUND: The development of encapsulation technologies has played an important role in improving cryopreservation outcomes for many cell and tissue types over the past 20 years. Alginate encapsulation cryopreservation (AECryo) has been incorporated into a range of applications in biotechnology, species conservation and clinical therapies, using cells from many different phyla, including higher plants, animal and human cells. This review describes the background to the origins of AECryo, the development of AECryo in higher plant tissues, broadening to current applications in algal conservation, the roles for AECryo in preserving phytodiversity, fungal species and in animal and human cells. OBJECTIVE: The main aims are to provide information resources on AECryo in different areas of biology and to stimulate new ideas for wider applications and future improvement. The translation of this useful biopreservation strategy into new opportunities for cell cryopreservation and storage at non-freezing temperatures are also discussed.

• MeSH
• algináty farmakologie   MeSH
• houby účinky léků   fyziologie   MeSH
• kryoprezervace metody   MeSH
• kyselina glukuronová farmakologie   MeSH
• kyseliny hexuronové farmakologie   MeSH
• lidé MeSH
• PEG-DMA hydrogel farmakologie   MeSH
• rostliny účinky léků   MeSH
• zmrazování * MeSH
• zvířata MeSH
• Check Tag
• lidé MeSH
• zvířata MeSH
• Publikační typ
• časopisecké články MeSH
• přehledy MeSH

Úvod: Materiály pro moderní wound-management dnes představují velmi širokou a heterogenní skupinu. Jedním z nejvýznamnějších představitelů této skupiny jsou přírodní materiály, nebo přesněji polysacharidy izolované z různých rostlin a živočichů. Při narůstající rezistenci patogenů k zavedeným antimikrobiálním látkám je zároveň snaha o objevování nových mechanismů účinku těchto materiálů. Gum karaya (GK) představuje velmi nadějného zástupce skupiny přírodních polysacharidů, a protože je získávána ze stromu Sterculia urens jako pryskyřice, dá se předpokládat také její určitá antimikrobiální aktivita. Materiál a metodika: Antimikrobiální potenciál GK jsme testovali na několika předem vybraných kmenech tak, aby korespondovaly s reálnou epidemiologickou situací původců infekčních komplikací v oblasti ošetřování popálenin. Mezi testovanými kmeny byli zástupci jak grampozivitního i gramnegativního spektra bakterií, tak kvasinky. Meticillin citlivý Staphylococcus aureus CCM 4223 (ATCC 29213), meticillin rezistentní Staphylococcus aureus CCM 4750 (ATCC 43300), Klebsiella pneumoniae CCM 4985 (ATCC 700603), Candida albicans CCM 8261 (ATCC 90028), Pseudomonas aeruginosa CCM 3955 (ATCC 27853) byly získány z České kolekce mikroorganismů. Pseudomonas aeruginosa FF 1, Pseudomonas aeruginosa FF 2 a Pseudomonas aeruginosa FF 3 (všechny multirezistentní kmeny) byly získány z kolekce mikroorganismů Fakultní nemocnice u svaté Anny. Antimikrobiální testování bylo provedeno pomocí diskového difuzního testu. Další sada antimikrobiálních testů byla provedena za pomocí měření růstových křivek. Výsledky: V rámci testování bakteriostatické aktivity se ukázala 1% koncentrace GK a také 1% a 0,5% koncentrace chitosanu (Ch) jako efektivní vůči všem testovaným patogenům. Podobnou efektivitu si dále uchovala i kombinace GK50/Ch50 v koncentraci 1% a 0,5%. Nižší koncentrace kombinovaného materiálu byly pouze velmi slabě efektivní vůči testovaným kmenům Candida albicans. Testování baktericidní aktivity ovšem nepřineslo pozitivní výsledky, mimo kandid, u kterých byl zaznamenán pouze částečný efekt GK50/Ch50 při 1% koncentraci. Testování pomocí růstových křivek se ukázalo, že efektivita jak samotné GK, tak také chitosanu byla výrazně vyšší u grampozitivních bakterií v porovnání s bakteriemi gramnegativními. V případě tohoto experimentu byla použita pouze desetinová koncentrace v porovnání s koncentrací u diskového difuzního testu. Tyto výsledky korespondují s daty získanými při testování bakteriostatické aktivity. Závěr: Jedná se o první publikaci, která se pokouší komplexně definovat potenciál v antimikrobiální aktivitě GK a také možné potenciace této aktivity pomocí chitosanu. V oblasti gramnegativního spektra je ovšem potřeba dalších experimentů zejména s vyšší koncentrací GK.

Introduction: Materials for modern wound-management are a very broad and heterogeneous group. One of the most important representatives is natural materials, or more precisely polysaccharides isolated from various plants and animals. With the increasing resistance of pathogens to established antimicrobial agents, there is also an attempt to discover new mechanisms of the effects of these materials. Gum karaya (GK) is a very promising representative of the natural polysaccharides group and, since it is obtained from Sterculia urens as resin, it is also possible to assume its certain antimicrobial activity. Material and methodology: The antimicrobial potential of GK and chitosan (Ch) has been tested on several preselected strains to match the real epidemiological situation of the agents of infectious complications in the field of burned wounds. Tested strains included representatives of gram-positive and gram-negative bacteria as well as selected yeasts. Methicillin susceptible Staphylococcus aureus CCM 4223 (ATCC 29213), methicillin resistant Staphylococcus aureus CCM 4750 (ATCC 43300), Klebsiella pneumoniae CCM 4985 (ATCC 700603), Candida albicans CCM 8261 (ATCC 90028), Pseudomonas aeruginosa CCM 3955 (ATCC 27853) were obtained from the Czech Collection of Microorganisms. Pseudomonas aeruginosa FF 1, Pseudomonas aeruginosa FF 2 and Pseudomonas aeruginosa FF 3 (all multi-resistant clinical strains), Staphylococcus epidermidis A 013, Staphylococcus epidermidis A 117, and Candida parapsilosis BC 11 were obtained from the Collection of Microorganisms at the St. Anne’s University Hospital, Brno. Antimicrobial tests were performed using the disk diffusion test methodology. Another set of antimicrobial tests was obtained by measuring the growth curves. Results: Bacteriostatic activity testing showed 1% GK concentration and both 1% and 0.5% chitosan concentration effective against all pathogens tested. The combination of GK50/Ch50 in concentrations of 1% and 0.5% had similar or better effect. Lower concentrations of the combined material are poorly effective against tested strains. Bactericidal activity testing has not produced positive results, except for Candida spp., where only a partial effect of GK50/Ch50 was observed at 1% concentration. In the growth curve test, the efficiency of both GK alone and chitosan was found to be significantly higher in gram-positive bacteria compared to gram-negative ones. In the case of this experiment, only a one-tenth concentration was used compared to the disk diffusion test concentration. This results correspond with the data from the bacteriostatic activity testing. Conclusion: This is the first publication that attempts to comprehensively define the potential for GK antimicrobial activity and also the possible potentiation of this activity with the use of chitosan. Further experiments are needed to extend the antimicrobial efficiency to gram-negative bacteria.

• MeSH
• antiinfekční látky MeSH
• guma karaya * terapeutické užití   MeSH
• hojení ran * MeSH
• lidé MeSH
• mikrobiální testy citlivosti MeSH
• PEG-DMA hydrogel terapeutické užití   MeSH
• popálení terapie   MeSH
• rostlinné gumy MeSH
• techniky in vitro MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• práce podpořená grantem MeSH

A potential delivery system has to be fabricated for crossing the blood–brain barrier (BBB) to reach the brain fluid for effective delivery of drugs for any neurological disorders. The present study is aimed for the delivery of donepezil through functionalized PNIPAM nanogel by overcoming the BBB using zebrafish model. We had synthesized the poly N-isopropyl acrylamide nanogels with 20 nm size for sustained drug release. The entrapment of donepezil in the nanogel was quantified as 87.5% by HPLC and its sustained drug release pattern was achieved at 37 °C using Janus green dye release assay. Acetylcholineesterase inhibition assay for the donepezil conjugated nanogel (DCN) has confirmed thermoresponsive drug release by obtaining the donepezil peak at 9.3 min retention time in HPLC. Swim behavior and heart beat rates were found to be biocompatible for the functionalized nanogel DCN in zebrafish. Histological analysis revealed increased pial surface in anterior telenchepalon region of zebrafish brain for the DCN administered fishes. DCN treated embryos exhibited minor developmental deformities above 5 μg/ml and thus confirmed its minimal toxicity and its therapeutic efficiency. This study may shed light on the development of neurospecific nanogel for targeted and sustained drug release to brain by crossing the blood–brain barrier.

• Klíčová slova
• PNIPAM,
• MeSH
• acetylcholinesterasa MeSH
• akrylové pryskyřice MeSH
• chemie farmaceutická MeSH
• dánio pruhované MeSH
• donepezil MeSH
• hematoencefalická bariéra * metabolismus   MeSH
• indany farmakokinetika   farmakologie   MeSH
• kardiotoxicita etiologie   MeSH
• modely u zvířat MeSH
• nanočástice MeSH
• nanotechnologie * MeSH
• PEG-DMA hydrogel chemická syntéza   MeSH
• piperidiny farmakokinetika   farmakologie   MeSH
• polysorbáty MeSH
• systémy cílené aplikace léků * MeSH
• uvolňování léčiv MeSH
• velikost částic MeSH
• vysokoúčinná kapalinová chromatografie MeSH
• zvířata MeSH
• Check Tag
• zvířata MeSH
• Publikační typ
• práce podpořená grantem MeSH

• Klíčová slova
• Prontosan, Granuflex Extra Thin, Suprasorb, Nu-Gel,
• MeSH
• antibakteriální látky aplikace a dávkování   terapeutické užití   MeSH
• antiinfekční látky lokální terapeutické užití   MeSH
• hodnocení rizik metody   MeSH
• hojení ran MeSH
• intenzivní péče o novorozence MeSH
• kůže zranění   MeSH
• lékové roztoky terapeutické užití   MeSH
• lidé MeSH
• neonatologie MeSH
• novorozenec nedonošený MeSH
• novorozenec MeSH
• obvazy hydrokoloidní MeSH
• okluzivní ošetření rány MeSH
• PEG-DMA hydrogel terapeutické užití   MeSH
• rány a poranění * farmakoterapie   ošetřování   prevence a kontrola   MeSH
• výsledek terapie MeSH
• Check Tag
• lidé MeSH
• novorozenec MeSH
• Publikační typ
• kazuistiky MeSH

Encapsulation is a well-established method of biomaterial protection, controlled release, and efficient delivery. Here we evaluated encapsulation of monoclonal antibody M75 directed to tumor biomarker carbonic anhydrase IX (CA IX) into alginate microbeads (SA-beads) or microcapsules made of sodium alginate, cellulose sulfate, and poly(methylene-co-guanidine) (PMCG). M75 antibody release was quantified using ELISA and its binding properties were assessed by immunodetection methods. SA-beads showed rapid M75 antibody release in the first hour, followed by steady release during the whole experiment of 7 days. In contrast, the M75 release from PMCG capsules was gradual, reaching the maximum concentration on the 7th day. The release was more efficient at pH 6.8 compared to pH 7.4. The released antibody could recognize CA IX, and target the CA IX-positive cells in 3D spheroids. In conclusion, SA-beads and PMCG microcapsules can be considered as promising antibody reservoirs for targeting of cancer cells.

• MeSH
• antigeny nádorové imunologie   metabolismus   MeSH
• antitumorózní látky aplikace a dávkování   MeSH
• buněčné sféroidy metabolismus   MeSH
• karboanhydrasa IX imunologie   metabolismus   MeSH
• koncentrace vodíkových iontů MeSH
• lidé MeSH
• mikrosféry * MeSH
• monoklonální protilátky aplikace a dávkování   imunologie   farmakokinetika   MeSH
• nádorové biomarkery imunologie   metabolismus   MeSH
• nádorové buňky kultivované MeSH
• nádory metabolismus   patologie   MeSH
• PEG-DMA hydrogel * MeSH
• systémy cílené aplikace léků metody   MeSH
• uvolňování léčiv MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• časopisecké články MeSH

OBJECTIVE: It was hypothesized that increasing the time for which onabotulinum toxin A (OnabotA) is exposed to the urothelium following intravesical instillation will augment its effect. TC-3 is an inert heat-sensitive hydrogel, which creates an intravesical bulk providing a slow release of the embedded drug after instillation. The aim of this study was to evaluate the effect of OnabotA, embedded in inert TC-3 hydrogel, in patients with idiopathic overactive bladder (OAB). METHODS: In total, 39 female patients (age 30-65, average 53.8 years) with OAB symptoms were randomized for the study into four groups, each receiving 50 ml of the following intravesical instillations: Group A, 0.9% NaCl (placebo, n = 11); Group B, TC-3 gel + 200 U OnabotA (n = 9); Group C, TC-3 gel + 200 U OnabotA + dimethyl sulfoxide (DMSO) (n = 10); and Group D, DMSO (n = 9). The parameters were compared before and 1 month after treatment. RESULTS: When comparing parameters using conventional statistical methods (Kruskal-Wallis test), no statistically significant changes were observed within the groups. Comparison of the medians using an analysis based on the mathematical gnostics showed the superiority of the method used in Group B over the other groups in the following parameters: number of urgency grade 3 + 4 episodes/72 h, number of leakage episodes/72 h, Overactive Bladder Questionnaire total score and Patient Perception of Bladder Condition total score. Group D showed its superiority over the other groups in respect to the number of nocturia episodes/72 h. CONCLUSIONS: The results indicate that intravesical instillation of OnabotA, embedded in TC-3 gel, could become an alternative to intramural injection for a well-selected subgroup of patients.

• MeSH
• aplikace intravezikální MeSH
• botulotoxiny typ A aplikace a dávkování   MeSH
• dospělí MeSH
• dvojitá slepá metoda MeSH
• hyperaktivní močový měchýř farmakoterapie   MeSH
• inhibitory uvolňování acetylcholinu aplikace a dávkování   MeSH
• lidé středního věku MeSH
• lidé MeSH
• nosiče léků MeSH
• PEG-DMA hydrogel MeSH
• pilotní projekty MeSH
• prospektivní studie MeSH
• senioři MeSH
• Check Tag
• dospělí MeSH
• lidé středního věku MeSH
• lidé MeSH
• senioři MeSH
• ženské pohlaví MeSH
• Publikační typ
• časopisecké články MeSH
• randomizované kontrolované studie MeSH
• srovnávací studie MeSH