Daflon Gremiao, Maria PalmiraChorilli, MarlusTurco, Bruna OrtolaniBoni, Fernanda Isadora...
11页
查看更多>>摘要：Nanostructured polyelectrolyte complexes (nano PECs) were obtained by polyelectrolyte complexation technique from chitosan (CS) and sodium alginate (SA)。 Different polymer proportions were tested， as well as the addition order and homogenization type， to assess the influence on the nano PECs characteristics。 The spherical shape and nanometric scale of the systems were observed by scanning electron microscopy (SEM)。 Nano PECs size， PDI， and zeta potential (ZP) ranged from 252 to 616 nm， from 0。22 to 0。73 and -50 to 30 mV， respectively。 The increase of polymer proportion and the ultra-turrax homogenization led to the enlargement of particles size and PDI。 However， no influence was observed on the ZP。 The NP1s-Rb and NP4s-Rb， obtained through the sonicator with rifampicin (RIF) added before the CS and SA complexation， were selected due to the most promising characteristics of diameter (301 and 402 nm)， PDI (0。27 and 0。26)， and RIF incorporation (78 and 69%)。 The release profiles of RIF incorporated in both nano PECs were similar， with a sustained release of the drug for 180 min in phosphate buffer pH 7。2。 The Weibull and the Korsmeyer-Peppas models better describe the RIF release from NP1s-Rb and NP4s-Rb， respectively， demonstrating that the release process was driven by different mechanism according to the particle composition。 The nano PECs were lyophilized to prolong it stability and for possible nebulization。 The addition of dextrose to the system allowed for resuspension after lyophilization。 Therefore， with the results obtained， the incorporation of RIF in nano PECs based on CS and SA presents a promising system for the treatment of tuberculosis。
查看更多>>摘要：Solid supports like the extracellular matrix network are necessary for bone cell attachment and start healing in the damaged bone。 Scaffolds which are made of different materials are widely used as a supportive structure in bone tissue engineering。 In the current study， a 3D polycaprolactone/gelatin bone scaffold was developed by blending electrospinning and freeze-drying techniques for bone tissue engineering。 To improve the efficiency of the scaffold， different concentrations of epinephrine (EP) due to its effect on bone healing were loaded。 Fabricated scaffolds were characterized by different tests such as surface morphology， FTIR， porosity， compressive strength， water contact angle， and degradation rate。 The interaction between prepared scaffolds and blood and cells was evaluated by hemolysis， and MTT test， respectively， and bone healing was evaluated by a rat calvaria defect model。 Based on the results， the porosity of scaffolds was about 75% and by adding EP， mechanical strength decreased while due to the hydrophilic properties of it， degradation rate increased。 In vivo and in vitro studies showed the best cell proliferation and bone healing were in PCL/gelatin/EP1% treated group。 These results showed the positive effect of fabricated scaffold on osteogenesis and bone healing and the possibility of using it in clinical trials。
查看更多>>摘要：Objective The airway epithelium is a potential source of pathophysiology through activation of transient potential receptor vallinoid type 1 (TRPV1) channel。 A positive feedback cycle caused by TRPV1 activity is hypothesized to induce upregulation and production of inflammatory cytokines， leading to exacerbations of chronic airway diseases。 These cytokine and protein regulation effects were investigated in this study。 Methods Healthy (BEAS-2B) and cancer-derived (Calu-3) airway epithelial cell lines were assessed for changes to TRPV1 protein expression and mRNA expression following exposure to capsaicin (5-50 mu M)， and TRPV1 modulators including heat (43 degrees C)， and hydrochloric acid (pH 3。4 to pH 6。4)。 Cytotoxicity was measured to determine the working concentration ranges of treatment。 Subsequent bronchoconstriction by TRPV1 activation with capsaicin was measured on guinea pig airway tissue to confirm locally mediated activity without the action of known neuronal inputs。 Results TRPV1 protein expression was not different for all capsaicin， acidity， and heat exposures (p > 0。05)， and was replicated in mRNA protein expression (p > 0。05)。 IL-6 and IL-8 expression were lower in BEAS-2B and Calu-3 cell lines exposed with acidity and heat (p < 0。05)， but not consistently with capsaicin exposure， with potential cytotoxic effects possible。 Conclusions TRPV1 expression was present in airway epithelial cells but its expression was not changed after activation by TRPV1 activators。 Thus， it was not apparent the reason for reported TRPV1 upregulation in patients with airway disease states。 More complex mechanisms are likely involved and will require further investigation。
Aleanizy, Fadilah SfouqTaha, Ehab, ISalem-Bekhit, Mounir M.Felimban, Alaa M. J....
8页
查看更多>>摘要：Surfactant-stabilized mucoadhesive nanogels (NGs) for vaginal delivery of fluconazole (FLZ) were studied and evaluated in this work。 FLZ-NG formulations were prepared using two different types of mucoadhesive polymers， Carbopol 934 (Ca934) and Pluronic F-127 (PF127)。 A rheology study revealed a non-Newtonian pseudoplastic flow behavior (shear thinning) in the prepared NGs。 The viscosity of Ca934 NG (0。47 Pa s) was much lower compared to the PF127 NG (6。10 Pa s)。 The rheology study results correlated well with the in vitro FLZ release profile from the NG formulations。 A pH study (pH = 3。90-4。90) revealed that the formulations were physiologically suitable for vaginal application， to avoid the irritation of the vaginal mucosa。 Finally， in vitro and in vivo antimicrobial tests were performed。 FLZ incorporated into the Ca934 gel had the strongest antimicrobial effect， with a mean inhibition zone of 24 +/- 1。6 mm。 Based on these results， it was concluded that the mucoadhesive NG incorporating FLZ resulted in a sustained release and enhanced antimicrobial effect， which would enhance and prolong the therapeutic effects of vaginally delivered FLZ。
查看更多>>摘要：Nanotechnology can be applied to design antibacterial agents to combat antibiotic resistance。 The aim of the present study was to assess the antimicrobial effects and cytotoxicity of GdYVO4:Eu3+ nanoparticles (NPs)。 Biofilm inhibition activity， antimicrobial activity， bacterial viability inhibition and DNA cleavage activity of GdYVO4:Eu3+ NPs were studied。 In addition， the impact of GdYVO4:Eu3+ NPs on the mitochondrial membrane potential (Delta psi(M)) of host immune cells and， hence， their apoptosis was analyzed by JC-1 staining using flow cytometry。 GdYVO4:Eu3+ NPs demonstrated good antimicrobial， cell viability inhibition and DNA cleavage activities。 In addition， GdYVO4:Eu3+ NPs showed good biofilm inhibition activity against S。 aureus and P。 aeruginosa and inhibition percentages were 89。15% and 79。54%， respectively。 However， GdYVO4:Eu3+ NPs promoted mitochondrial depolarization and apoptosis of leukocytes at high concentrations。 GdYVO4:Eu3+ nanoparticles are promising antibacterial agents。 However， more efforts should be exerted to ensure their safety。
查看更多>>摘要：Objective The purpose of this study was to develop pluronic F127/d-a-tocopheryl polyethylene glycol 1000 succinate mixed micelles-based hydrogel (MMs-gel) for topical delivery of glycyrrhizic acid (GL) to improve its skin permeability and atopic dermatitis (AD) treatment。 Significance GL loaded MMs-gel (GL-MMs-gel) could be potentially used as a promising nanocarrier for the treatment of AD。 Methods GL-MMs were prepared by thin film hydration method and then loaded into carbopol gel。 The formulation of GL-MMs-gel was optimized by full factorial design and systematically characterized for drug content， pH， spreadability， in vitro drug release and percutaneous permeation， etc。 The therapeutic effect of GL-MMs-gel was also investigated in AD-like skin lesion model in BALB/c mice and compared with GL solution-based gel (GL-sol-gel)。 Results Spherical GL-MMs with particle size of similar to 30 nm were successfully incorporated into carbopol gel to form GL-MMs-gel with drug content of (98。80 +/- 1。30) %， pH of 6。0 +/- 0。08， and spreadability of (7。1 +/- 0。2) cm。 In vitro drug release profile of GL-MMs-gel exhibited a sustained-release behavior。 The permeation flux for GL-MMs-gel (5。15 +/- 0。33 mu g/cm(2)/h) was significantly higher than that of GL-sol-gel (3。08 +/- 0。34 mu g/cm(2)/h) and GL-MMs-gel increased the accumulative amounts of GL in rats' skin 8。41 times than GL-sol-gel。 The GL-MMs-gel was more effective than GL-sol-gel in suppressions of various AD symptoms including skin lesions， edema， high IgE levels， epidermal hyperplasia， and mast cell infiltration。 Conclusion All results revealed that MMs-gel could be a promising carrier for topical delivery of GL for the treatment of AD。
查看更多>>摘要：Xanthine oxidase (XO) is accountable for the uric acid synthesis in the body and is considered as a prominent therapeutic target in urate lowering treatment。 Eugenol is a natural compound commonly found in clove， cinnamon， etc。 and has various biological activities。 This study was designed to examine the anti-hyperuricemic effect of eugenol by in vitro and in vivo studies。 Potassium oxonate (PO) was used to induce hyperuricemia in Wistar rats。 Different doses of eugenol (1。25， 2。5， and 5 mg/kg bwt orally) were used for the treatment and various biological function markers (renal， hepatic， and hematological) were analyzed。 The IC50 value obtained for eugenol was 3。51 +/- 0。002 mu M。 The kinetic studies revealed that the eugenol exhibited a mixed type of inhibition。 Abnormality in the levels of various biological function markers was observed in the PO treated rats。 Upon the eugenol treatment， those biological function markers were retained near to its normal values。 The study proved the anti-hyperuricemic potential of eugenol against the PO induced hyperuricemia model。
查看更多>>摘要：Objective Rosuvastatin (ROS) is a class of antihyperlipidemic agents belonging to the class of statins with poor permeability， which results in low oral bioavailability， i。e。 20%。 The objective of the present study was to improve the permeability and bioavailability of ROS by developing nanocochelates using naturally biocompatible phosphatidylcholine， a type of lipid which is used as Ca2+ cations for the calcification process。 Significance For the loaded ROS， the trapping method was used to build nanocochelates to boost the intestinal permeability of phosphatidylcholine and divalent choline is a calcium chloride cationic solution。 Methods Nine different formulations have been produced and with varying lipid and cationic solution concentrations。 The formulation of nanocochelates characterized by scanning electron microscopy， particle size， and zeta potential。 Permeability studies have been conducted to determine the permeability improvement property of nanocochelates。 The pharmacokinetic study was performed in Wistar albino rats to determine the bioavailability enhancement potential of nanocochlelates。 Results The concentration of optimum lipid， calcium chloride was found to be 80 mg， 200 uL respectively which improve permeability by 3。44 times as compared to the marketed formulation。 The in-vitro drug release over a prolonged period i。e。12 h。 Which was substantially better than the traditional formulation of tablets。 Nearly five fold enhancement in bioavailability was observed in case of optimized formulation as compared to the marketed formulation (p < 0。05)。 Conclusion The findings suggest that the use of natural lipid carrier by nanocochelates of Rosuvastatin was promising drug delivery approach。
查看更多>>摘要：Context In the present study， hyaluronic acid (HA)-coated raloxifene-loaded poly(l-lactic-co-glycolic acid) (PLGA) nanoparticles have been developed to improve the anticancer potential and reduce side effects associated with the drug。 Aim and objectives The investigation was aimed to formulate and optimize raloxifene hydrochloride (RALH)-loaded PLGA nanoparticles with surface modification using HA as a targeting moiety。 To perform physicochemical characterization， in vitro cytotoxicity study (using MCF-7)， in vitro drug release study and in vivo pharmacodynamic study of optimized formulation。 Methodology Raloxifene hydrochloride-loaded PLGA nanoparticles were prepared by nanoprecipitation technique， followed by surface modification with HA。 Formulation was optimized by using 23 factorial design and characterized by physicochemical， in vitro drug release， in vitro cytotoxicity studies， and in vivo pharmacokinetics。 Results and discussion The particle size， PDI， zeta potential， entrapment efficiency， and loading capacity of spherically shaped RALH-loaded nanoparticles were 207。3 +/- 4。2 d。nm， 0。218 +/- 0。127， -。127 mV， 43。75 +/- 1。2%， and 7。55 +/- 1。14%， respectively。 The in vitro drug release showed sustained release and followed Korsmeyer-Peppas model with non-Fickian release pattern。 The in vitro cytotoxicity study of drug-loaded NPs by MTT assay on MCF-7 breast carcinoma cell showed anti-cancer activity after 48 h of treatment。 Conclusion The results of the present investigation suggested that RALH-loaded HA-modified PLGA nanoparticles showed sustained drug release with anticancer activity and can be a promising approach for treatment of breast cancer。
NSTL
Taylor & Francis