Objective:To enhance the effective diagnosis of tumor by magnetic resonance imaging(MRI),aptamer-targeted liposomes combined with gadolinium(Gd)were designed and constructed as a novel MRI contrast *** aptamer use...
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Objective:To enhance the effective diagnosis of tumor by magnetic resonance imaging(MRI),aptamer-targeted liposomes combined with gadolinium(Gd)were designed and constructed as a novel MRI contrast *** aptamer used in this study was a modified GBI-10,which has high affinity to tenascin C(TN-C)overexpressed in various ***:Non-targeted liposomes(NLs) were first prepared by lipid film hydration and extrusion *** aptamer-targeted liposomes(TLs) were obtained by incubating GBI-10-Chol with ***-6 was loaded into NLs and TLs respectively to compare their interaction with tumor cells by confocal laser scanning microscopy and flow *** particle size and zeta potential of NLs and TLs were *** clinical 3.0 Tesla MR scanner was used to assess the imaging efficiency(indicated as Ti) of NLs and TLs,which were compared to that of commercially available contrast agents,Gd-DTPA(magnevist).The relaxation rate(r) was obtained by the linear fitting curve of concentration gradient and 1/T).Results:The particle size ofNLs and TLs were 126.4±2.4 nm and 157.2±1.9nm,while zeta potential were-3.94±0.53 mV and-12.85±0.35 mV,*** images of confocal laser scanning microscopy(Figure 1 A) for NLs and TLs shows the amount of NLs entered in cytoplasm was much less compared to TLs at 37℃.The fluorescence intensity of TLs increased to about 3 times than that of NLs(Figure 1B).The MR images for NLs,TLs and Gd-DTPA were shown in Figure *** values of r calculated for NLs,TLs and Gd-DTPA were 4.7±0.3 mMs,4.4±0.2mMs and3.9±0.1 mMs,respectively(n=3).Conclusion:The results suggested that GBI-10-targeted paramagnetic liposomes prepared in this study were potential contrast agent for MRI diagnosis of tumor with the high expression of TN-C.
Objective:The aim of this study was to investigate the in vitro permeation of ropinirole,an anti-Parkinson drug,across bovine nasal ***:The permeation of ropinirole across bovine nasal mucosa was determined using Vert...
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Objective:The aim of this study was to investigate the in vitro permeation of ropinirole,an anti-Parkinson drug,across bovine nasal ***:The permeation of ropinirole across bovine nasal mucosa was determined using Vertical Diffusion *** vitro experiments were conducted to assess the effect of directionality,donor concentration and various absorption enhancers including p-cycbdextrin(β-CD),Hydroxypropyl-p-cyclodextrin(HP-P-CD),dimethyl-P-cyclodextrin(DM-β-CD) and chitosan(CS) on the permeation of ropinirole across excised bovine nasal ***(200 u,L) were withdrawn from the receiver chamber at predetermined time intervals up to 120 min and analyzed using a validated HPLC-UV *** analysis was also performed to observe the potential irritation or toxicity of ropinirole to nasal mucosa by in vitro toad palate mucosa ***:As shown in Fig.1,the Jm-s(mucosal-submucosal flux) and Js-m(submucosal-mucosal flux) of ropinirole across the olfactory mucosa at pH 6.5 were linearly dependent upon the donor concentration range from 2 to 200 mM without any evidence of saturable ***,no significant difference was found between the Jm-s and Js-m at donor concentrations tested except 20 and 50 mM(Fig.2).Efflux transports such as P-gp might play a role in the submucosal-mucosal flux of ropinirole across the olfactory ***,no significant increase of drug permeation through the mucosa using 0.5%P-CD,1.5%HP-p-CD,1.5%DM-p-CD and 1.5%CS as absorption promoters was observed(Fig.3;Table 1).Interestingly,the permeation coefficient was found to be higher in olfactory mucosa than respiratory mucosa *** sections of the mucosa after 2 h exposure in ropinirole and saline(negative control) were similar in tissue architecture without any structure alteration,while the histological structure significantly changed after the treatment with sodium deoxycholate(positive control),indicating that ropinirole did no
This paper reports a drug-loaded three-phase microbubble fabrication method using a silicon capillary inserted three-phase microfluidic chips(Figure la),which can precise control fluid,to improve the size uniformity,t...
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This paper reports a drug-loaded three-phase microbubble fabrication method using a silicon capillary inserted three-phase microfluidic chips(Figure la),which can precise control fluid,to improve the size uniformity,the drug entrapment efficiency and the
Polymeric micelles represent a promising drug carrier system that has gained considerable attention due to its simplicity,small sizes(10-100 nm),and the ability to solubilize water-insoluble drugs and accumulate speci...
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Polymeric micelles represent a promising drug carrier system that has gained considerable attention due to its simplicity,small sizes(10-100 nm),and the ability to solubilize water-insoluble drugs and accumulate specifically at the *** of the carrier materials in polymeric drug delivery systems(including lipid-core micellar
A tumor cell-targeted prodrug was developed for quercetin,using hyaluronic acid as polymeric *** acid-quercetin(HA-QT)bioconjugates were synthesized by linking the hydroxy of quercetin via a succinate ester to adipic
A tumor cell-targeted prodrug was developed for quercetin,using hyaluronic acid as polymeric *** acid-quercetin(HA-QT)bioconjugates were synthesized by linking the hydroxy of quercetin via a succinate ester to adipic
The lack of safe and efficient gene delivery systems is a major obstacle to achieve successful human gene *** synthetic gene delivery systems,although safer and more versatile than natural viruses,generally do not pos...
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The lack of safe and efficient gene delivery systems is a major obstacle to achieve successful human gene *** synthetic gene delivery systems,although safer and more versatile than natural viruses,generally do not possess the required delivery *** recent years,with the growing understanding the mechanisms of non-viral gene delivery,and inspired by the viral structures and functions,much effort has been directed to the development of intelligent polymers based bio-inspired and biomimetic multifunctional gene delivery *** polymers show promise in gene delivery due to their branched and layered architectures,globular shape and multivalent groups on their surface[1].Arginine functionalized L-lysine-based peptide dendrimers demonstrated efficient gene delivery[2,3].Furthermore,supramolecular self-assembly of peptide dendrimers based capsid-like nanostructure,they could also serve as pH-responsive nanovehicles and use to develop towards artificial virus for gene delivery[4,5].Low aggregated magnetic gene complexes have realized serum resistance and tumor accumulation effect for PEI-mediated gene transfection in vitro and in vivo,and the mechanism under this serum-tolerant transfection was defined[6].These structures contain elements that mimic the delivery functions and structures of viral particles and surface domains that shield against undesired biological interactions and enable tumor accumulatioa Recently,the dynamic ternary polyplexes based on disulfide bond modified hyaluronic acid and diselenMe conjugated ohgoethylenimine were designed for virus-mimicking gene delivery systems[7-9].With virus-like entry functions,the dynamic nanovehicles recognize the cues provided by cells and sense their biologic micro-environment,respond in a more dynamic manner to alterations in enzyme or redox environment both at tumor site and in the cell,undergo programmed molecular structural changes compatible with the different gene delivery steps to mod
Objective:The aim of the study was to observe the characteristic of permeation of capsaicin across jejunum,ileum and colon in the rat,and to investigate the role of transient receptor potential cation channel(TRPV1).T...
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Objective:The aim of the study was to observe the characteristic of permeation of capsaicin across jejunum,ileum and colon in the rat,and to investigate the role of transient receptor potential cation channel(TRPV1).The interaction of capsaicin with P-glycoprotein(P-gp),multidrug resistance-associated protein 2(MRP2) and breast cancer resistance protein(BCRP) was also ***:The transport of capsaicin across three intestinal segments in rats was investigated using Ussing-chamber ***:The permeabihty of capsaicin across the colonic,ileac or jejunal membrane was significantly different in M-S direction(11.679±2.001,5.336±1.248,1.395±0.673,×10-6 cnVs).TRPV1 non-competitive antagonist ruthenium red significantly decreased the permeabihty of capsaicin in M-S direction across colonic *** permeabihty of capsaicin could also be inhibited unconventionally by the BCRP inhibitor novobiocin in M-S direction across ***,either the P-gp inhibitor verapamil or the MRP2 inhibitor probenecid did not affect the transport of capsaicin in all three ***:In this primary study,we excitedly realized that it was the first time to find the permeability of capsaicin across the colonic mucosa in M-S direction is remarkably higher than that across jejunal or ileac ***1 might participate in the intestinal permeation of ***,the different distribution of TRPV1 abng the intestine caused the site-specific transport of *** is no influence of P-gp or MRP2 on the transport of ***,the permeability of capsaicin is decreased by novobiocin,which reveals that there is another interaction between capsaicin and ***,the mechanisms are not clear so far,and more investigations are necessary to reveal ***,we believe that these data could be useful for further study of the transport mechanisms of capsaicin across *** addition,further investigations are still need
A variety of pharmaceutical agents have been developed for cancer ***,because the hydrophobic cell membrane hampers cellular uptake in the absence of active transport,it is not trivial for anti-tumor agents to reach t...
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A variety of pharmaceutical agents have been developed for cancer ***,because the hydrophobic cell membrane hampers cellular uptake in the absence of active transport,it is not trivial for anti-tumor agents to reach their designated intracellular *** internalization of c he mo therapeutic
Typically,sustained drug release is expected to reach high tumor accumulation and reduce drug leakage during the systemic circulation of ***,only drugs that exist as free molecules are able to interact with target mol...
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Typically,sustained drug release is expected to reach high tumor accumulation and reduce drug leakage during the systemic circulation of ***,only drugs that exist as free molecules are able to interact with target molecules and act their pharmacological *** TDDS have been shown to substantially increase
Mesoporous silica nanoparticbs(MSNs)refer to porous silica which exhibit pores diameters between 2 and 50 nm Due to their large surface area and pore volume,adjustable pore diameter,easily modified surface and excelle...
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Mesoporous silica nanoparticbs(MSNs)refer to porous silica which exhibit pores diameters between 2 and 50 nm Due to their large surface area and pore volume,adjustable pore diameter,easily modified surface and excellent biocompatibility,MSNs have attracted considerable attention for their application in drug delivery
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