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1.
Acta Pharmaceutica Sinica ; (12): 494-505, 2023.
Article in Chinese | WPRIM | ID: wpr-965612

ABSTRACT

Malignant tumors are major diseases that endanger human health. Due to their complex and variable microenvironment, most anti-tumor drugs cannot precisely reach the focal tissue and be released in a controlled manner. Intelligent responsive nano carriers have become a hot spot in the field of anti-tumor drug delivery systems. As an excellent nano material, mesoporous silica has the advantages of non-toxic, stable, adjustable pore volume and pore diameter, and easy functional modification on the surface. By virtue of its perceptive response to the tumor microenvironment or physiological changes, it can achieve the targeted drug release or controlled drug release of the drug delivery system in the tissue, making it an ideal carrier for intelligent response drug delivery system. In this paper, we review the design strategies and current research status of smart responsive anti-tumor drug delivery systems based on mesoporous silica, in order to provide a reference for the development of anti-tumor drug nanoformulations.

2.
China Journal of Chinese Materia Medica ; (24): 390-398, 2023.
Article in Chinese | WPRIM | ID: wpr-970476

ABSTRACT

This study aimed to investigate the effects of nanoparticles PLGA-NPs and mesoporous silicon nanoparticles(MSNs) of different stiffness before and after combination with menthol or curcumol on the mechanical properties of bEnd.3 cells. The particle size distributions of PLGA-NPs and MSNs were measured by Malvern particle size analyzer, and the stiffness of the two nanoparticles was quantified by atomic force microscopy(AFM). The bEnd.3 cells were cultured in vitro, and the cell surface morphology, roughness, and Young's modulus were examined to characterize the roughness and stiffness of the cell surface. The changes in the mechanical properties of the cells were observed by AFM, and the structure and expression of cytoskeletal F-actin were observed by a laser-scanning confocal microscope. The results showed that both nanoparticles had good dispersion. The particle size of PLGA-NPs was(98.77±2.04) nm, the PDI was(0.140±0.030), and Young's modulus value was(104.717±8.475) MPa. The particle size of MSNs was(97.47±3.92) nm, the PDI was(0.380±0.016), and Young's modulus value was(306.019±8.822) MPa. The stiffness of PLGA-NPs was significantly lower than that of MSNs. After bEnd.3 cells were treated by PLGA-NPs and MSNs separately, the cells showed fine pores on the cell surface, increased roughness, decreased Young's modulus, blurred and broken F-actin bands, and reduced mean gray value. Compared with PLGA-NPs alone, PLGA-NPs combined with menthol or curcumol could allow deepened and densely distributed surface pores of bEnd.3 cells, increase roughness, reduce Young's modulus, aggravate F-actin band breakage, and diminish mean gray value. Compared with MSNs alone, MSNs combined with menthol could allow deepened and densely distributed surface pores of bEnd.3 cells, increase roughness, reduce Young's modulus, aggravate F-actin band breakage, and diminish mean gray value, while no significant difference was observed in combination with curcumol. Therefore, it is inferred that the aromatic components can increase the intracellular uptake and transport of nanoparticles by altering the biomechanical properties of bEnd.3 cells.


Subject(s)
Animals , Mice , Menthol/pharmacology , Actins/metabolism , Endothelial Cells/metabolism , Nanoparticles/chemistry
3.
Acta Pharmaceutica Sinica ; (12): 2512-2521, 2023.
Article in Chinese | WPRIM | ID: wpr-999114

ABSTRACT

To investigate the crucial role of particle size in the biological effects of nanoparticles, a series of mesoporous silica nanoparticles (MSNs) were prepared with particle size gradients (50, 100, 150, 200 nm) with the traditional Stober method and adjusting the type and ratio of the silica source. The correlation between toxicity and size-caused biological effects were then further examined both in vitro and in vivo. The results indicated that the prepared MSNs had a uniform size, good dispersal, and ordered mesoporous structure. Hemolytic toxicity was found to be independent of particle size. At the cellular level, MSNs with smaller particle sizes were more readily internalized by cells, which initiated to more intense oxidative stress, therefor inducing higher cytotoxicity, and apoptosis rate. In vivo studies demonstrated that MSNs primarily accumulated in the liver and kidneys of mice. Pharmacokinetic analysis revealed that larger MSNs were eliminated more efficiently by the urinary system than smaller MSNs. The mice's body weight monitoring, blood tests, and pathological sections of major organs indicated good biocompatibility for MSNs of different sizes. Animal welfare and the animal experimental protocols were strictly consistent with related ethics regulations of Zhejiang Chinese Medical University. Overall, this study prepared MSNs with a particle size gradient to investigate the correlation between toxicity and particle size using macrophages and endothelial cells. The study also examined the biosafety of MSNs with different particle sizes in vivo and in vitro, which could help to improve the safety design strategy of MSNs for drug delivery systems.

4.
Acta Pharmaceutica Sinica ; (12): 200-210, 2022.
Article in Chinese | WPRIM | ID: wpr-913169

ABSTRACT

Chemoimmunotherapy has attracted much attention as an emerging therapy pattern for the treatment of cancers. Exploring effective drug combination schemes and reasonable delivery methods remained the key issue in current research. Herein, we designed sorafenib (SF) and anti-Tim-3 monoclonal antibody (Tim-3 mAb) co-loaded MMP2-responsive mesoporous silica nanoparticles (ST-MSNs) for combined chemoimmunotherapy of hepatocellular carcinoma (HCC). The shell of ST-MSNs was fabricated by Tim-3 mAb through matrix metalloproteinase 2 (MMP2) sensitive peptides as "gatekeepers" to prevent drug release during the blood circulation. In tumor microenvironment, the high levels of MMP2 caused the responsive shedding of Tim-3 mAb, leading to the triggerred release of SF and Tim-3 mAb. Then, SF could be delivered to tumor cells and Tim-3 mAb could be delivered to T cells, respectively. In vivo tumor inhibition study results demonstrated that ST-MSNs can significantly enhance synergistic antitumor activity compared with sequential administration of free SF solution and Tim-3 mAb solution. Meanwhile, the expression of antitumor cytokines IFN-γ, IL-12 and the percentage of CD3+CD4+ cells, CD3+CD8+ cells in tumors were upregulated after the administration of ST-MSNs, demonstrating good immunomodulatory ability. In addition, within the dosage range, the ST-MSNs had low cytotoxicity and hemolysis, and no obvious tissue toxicity was observed. All animal experiments were performed in line with national regulations and approved by the Animal Experiments Ethical Committee of Shandong University. In conclusion, this study provided a promising drug combination of chemoimmunotherapy with good application prospects for clinical HCC treatment, and exhibited a potential drug carrier for clinical chemoimmunotherapy.

5.
Journal of Prevention and Treatment for Stomatological Diseases ; (12): 178-184, 2022.
Article in Chinese | WPRIM | ID: wpr-907001

ABSTRACT

Objective@#The antibacterial properties and bonding strength of 3M orthodontic adhesive resin modified by chlorhexidine acetate (CHA) composite mesoporous silica were investigated.@*Methods@# CHA with different mass fractions was encapsulated in mesoporous silica nanoparticles (MSNs) (denoted CHA@MSNs). Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM) were used to characterize the samples. The 3M Z350XT flow resin was divided into 4 groups: group A: 3M+CHA@MSNs (0%); group B: 3M+CHA@MSNs (3%); group C: 3M+CHA@MSNs (5%); and group D: 3M+CHA@MSNs (6.4%), with mass scores of 0%, 3%, 5%, and 6.4%, respectively. The shear strength of the modified adhesive was tested by a universal electronic material testing machine, the adhesive residue was observed by a 10 × magnifying glass, and the adhesive Remnant index (ARI) was calculated. The four groups of modified adhesives were cultured with Streptococcus mutans. The OD540 value of the bacterial solution was measured by a spectrophotometer, and the amount of plaque attachment was observed by scanning electron microscopy to evaluate the antibacterial performance of the adhesives.@*Results@#Infrared spectroscopic analysis of CHA@MSNs showed that CHA was successfully loaded onto MSNs. Under scanning electron microscopy, it could be seen that, after Cha was combined with MSNs, the structure of MSNs changed, as the boundary was fuzzy and aggregated into a layered structure. A comparison of shear strength revealed a statistically significant difference between the groups containing CHA@MSNs and the groups without CHA@MSNs (P<0.05). The value of the shear strength in group D decreased the most, while there was no statistically significant difference between group B and group C (P > 0.05). There was no statistical significance across all groups (P > 0.05), suggesting that the addition of CHA@MSNs had little effect on the bracket shedding. The OD540 value of bacterial fluid indicated that the difference among groups A, B and C was statistically significant (P < 0.05), and the antibacterial effect of group C was the best; there was no statistically significant difference between group C and group D (P > 0.05).@*Conclusions@#Therefore, adding 5% CHA@MSN antibacterial agent significantly improved the antibacterial effect and did not affect the bond strength.

6.
Acta Pharmaceutica Sinica B ; (6): 1432-1446, 2022.
Article in English | WPRIM | ID: wpr-929374

ABSTRACT

In the microscale, bacteria with helical body shapes have been reported to yield advantages in many bio-processes. In the human society, there are also wisdoms in knowing how to recognize and make use of helical shapes with multi-functionality. Herein, we designed atypical chiral mesoporous silica nano-screws (CMSWs) with ideal topological structures (e.g., small section area, relative rough surface, screw-like body with three-dimension chirality) and demonstrated that CMSWs displayed enhanced bio-adhesion, mucus-penetration and cellular uptake (contributed by the macropinocytosis and caveolae-mediated endocytosis pathways) abilities compared to the chiral mesoporous silica nanospheres (CMSSs) and chiral mesoporous silica nanorods (CMSRs), achieving extended retention duration in the gastrointestinal (GI) tract and superior adsorption in the blood circulation (up to 2.61- and 5.65-times in AUC). After doxorubicin (DOX) loading into CMSs, DOX@CMSWs exhibited controlled drug release manners with pH responsiveness in vitro. Orally administered DOX@CMSWs could efficiently overcome the intestinal epithelium barrier (IEB), and resulted in satisfactory oral bioavailability of DOX (up to 348%). CMSWs were also proved to exhibit good biocompatibility and unique biodegradability. These findings displayed superior ability of CMSWs in crossing IEB through multiple topological mechanisms and would provide useful information on the rational design of nano-drug delivery systems.

7.
Acta Pharmaceutica Sinica B ; (6): 520-533, 2021.
Article in English | WPRIM | ID: wpr-881151

ABSTRACT

Chemotherapy has been a major option in clinic treatment of malignant tumors. However, single chemotherapy faces some drawbacks, such as multidrug resistance, severe side effects, which hinder its clinic application in tumor treatment. Multifunctional nanoparticles loading with chemotherapeutic agent and photosensitizer could be a promising way to efficiently conduct tumor combination therapy. In the current study, a novel pH-sensitive and bubble-generating mesoporous silica-based drug delivery system (denoted as M(a)D@PI-PEG-RGD) was constructed. Ammonium bicarbonate (NH

8.
Journal of Prevention and Treatment for Stomatological Diseases ; (12): 306-313, 2021.
Article in Chinese | WPRIM | ID: wpr-873652

ABSTRACT

Objective @#To fabricate a co-delivery system of curcumin (CUR) and siRNA based on mesoporous silica nanoparticles (MSN) and investigate its potential application in inducing macrophage M2 polarization.@*Methods@# MSNs were synthesized using the conventional sol-gel method. The interior mesochannels were occupied by small-molecule CUR, while the exterior surface was adsorbed by cationic polymeric polyethyleneimine (PEI) to link the negatively charged siRNA molecules to formulate the (CUR@MSN)PEI/siRNA co-delivery system. The formulation process was monitored by transmission electron microscopy(TEM). The MTT assay was used to evaluate the cytotoxicity in RAW264.7 cells under various concentrations of nanoparticles. Confocal laser scanning microscopy and TEM were used to observe cell internalization using FAM-labeled siRNA. GAPDH-targeting siRNA was used to prepare nanoparticles and then was transfected into RAW264.7 cells to observe the silencing efficiency of target genes. The knockdown efficiency was examined by real-time quantitative PCR. The related control groups were untreated cells, CUR delivery only and the co-delivery of CUR and siRNA negative control. By loading miRNA-130a-3p antisense oligonucleotide (ASO) to transfect RAW264.7 cells, the effects on the polarization of macrophages were observed. The M2 polarization marker arginase 1 (Arg-1) was measured by western blotting. The related control groups were untreated cells, CUR delivery only and co-delivery of CUR and miRNA negative control. @* Results @# The (CUR@MSN)PEI/siRNA co-delivery system was successfully formulated. The nanoparticles exhibited dose-dependent cytotoxicity, and the cell viability was maintained over 90% when the nanoparticle concentration was less than 10 μg/mL. A high cell uptake efficiency was observed, and the target gene knockdown efficiency was greater than 80% (P < 0.05 vs. all the other groups). The CUR delivery-only group and co-delivery of the CUR-and miRNA-negative control group improved Arg-1 expression ~ 3-fold (P < 0.05 vs. untreated cells). Using the co-delivery of CUR and ASO, synergistic effects were obtained, and Arg-1 expression was increased ~ 8-fold (P < 0.05 vs. all the other groups).@*Conclusion @#The CUR-siRNA co-delivery system can effectively transfect macrophages and synergistically induce M2 polarization.

9.
China Journal of Orthopaedics and Traumatology ; (12): 784-787, 2020.
Article in Chinese | WPRIM | ID: wpr-828206

ABSTRACT

As a new potential bone graft material, tissue engineered bone effectively compensates for the defects of today's bone repair materials. Meanwhile, mesoporous silica nanomaterials(MSNs) have been widely recognized due to their large specific surface area, good biocompatibility, and capability of further processing and modification. They have promising application prospects in bone tissue engineering. For the basic scientific research results that have been carried out in the early stage, the basic characteristics of mesoporous silica nano biomaterials and their application advantages, research status and development prospects in bone tissue engineering are reviewed. As for the research status, there are two aspects--as a carrier or as a component of engineering scaffolds. For the first aspect, different kinds of loaded drugs and different loading methods are reviewed. For the second, microstructure and mechanical properties of various complex scaffolds containing MSNs and the molecular and cellular behavior of seeded cells on these scaffolds are reviewed. The research of MSNs in bone cements and metal ions doped MSNs in bone tissue engineering are also included. The future development of MSNs in bone tissue engineering is also discussed.


Subject(s)
Bone and Bones , Nanoparticles , Porosity , Silicon Dioxide , Tissue Engineering
10.
Chinese Pharmaceutical Journal ; (24): 367-374, 2020.
Article in Chinese | WPRIM | ID: wpr-857766

ABSTRACT

OBJECTIVE: To construct a biomimetic delivery system (U251/MSN-DOX), and assess its application of glioma targeted therapy. METHODS: U251 cell membrane was coated on the surface of mesoporous silica nanoparticles(MSN) by co-extrusion to prepare cell membrane biomimetic nanoparticles U251/MSN-DOX. The particle size, potential and morphology were characterized. The physical characteristics, loading content (LC) and encapsulation efficiency (EE) of these nanoparticles were determined. Their toxicity of normal cells was investigated. Their cellular uptake of different formulations in U251 was studied by flow cytometry and fluorescence confocal microscope. Additionally, we assessed the transmembrane transport efficiency of nanoparticles via in vitro BBB. RESULTS: The cell membrane-coated nanoparticles U251/MSN were spherical, and a distinct "core-shell" structure could be observed. The particle size was (135.70±3.85) nm, the LC was (18.57±2.17)%, and the EE was (64.99±2.52)%. The cell experiment showed that U251/MSN had low cytotoxicity and U251/MSN-DOX exhibited stronger cellular uptake ability and BBB transporting efficiency. CONCLUSION: The glioma cell membrane can be coated on the surface of MSN to construct biomimetic nanoparticles U251/MSN. The biomimetic nanoparticles not only are capable of targeting the homologous tumor cells, but also show the enhanced ability to penetrate BBB, which indicate potential applications in the field of tumor targeted drug delivery especially in brain tumor.

11.
J. appl. oral sci ; 28: e20200131, 2020. tab, graf
Article in English | LILACS, BBO | ID: biblio-1134780

ABSTRACT

Abstract Objective There is increasingly common the consumption more times a day of foods and acidic drinks in the diet of the population. The present study aimed to evaluate and compare the effects of a calcium mesoporous silica nanoparticle single application of other calcium and/or fluoride products in reducing the progression of dental erosion. Methodology Half of the eroded area was covered of 60 blocks of enamel, after which the block was submitted to the following treatments: (Ca2+-MSN), casein phosphopeptide-amorphous calcium phosphate (CPP-ACP); CPP-ACP/F-(900 ppm F−); titanium tetrafluoride (TiF4 1%) (positive control); sodium fluoride (NaF 1.36%) (positive control); and Milli-Q® water (negative control) before being submitted to a second erosive challenge. A surface analysis was performed via a three-dimensional (3D) noncontact optical profilometry to assess the volumetric roughness (Sa) and tooth structure loss (TSL) and and through scanning electron microscopy (MEV). An analysis of variance (ANOVA) and Tukey's test were performed. Results Regarding Sa, all experimental groups exhibited less roughness than the control (p<0.05). The TSL analysis revealed that the Ca2+-MSN and NaF groups were similar (p>0.05) and more effective in minimizing tooth loss compared with the other groups (p<0.05). Conclusions The Ca2+-MSN and NaF treatments were superior compared with the others and the negative control.


Subject(s)
Humans , Tooth Erosion , Tooth Remineralization , Nanoparticles , Sodium Fluoride , Caseins , Calcium , Silicon Dioxide , Fluorides
12.
Braz. J. Pharm. Sci. (Online) ; 56: e17560, 2020. tab, graf
Article in English | LILACS | ID: biblio-1285514

ABSTRACT

Urea's thermal instability and burning on sensitive skin can cause problems for cosmetic formulations. To overcome these drawbacks, urea was incorporated into ordered mesoporous silica (SBA-15). SBA-15 was synthesized using tetraethyl orthosilicate and Pluronic® P123 in an acid medium. Urea (20 wt.%) was incorporated into calcined SBA-15 by the incipient wetness impregnation method. Several techniques were used to characterize the samples. Skin hydration and transepidermal water loss were measured using Corneometer® CM 825 PC and Tewameter® 300 TM. Results showed that the structural properties of SBA-15Urea were similar to pure SBA-15, indicating that SBA-15 remained structured even after urea incorporation. Nitrogen physisorption data showed the volume and surface area of the pores in SBA-15Urea were much lower than those in SBA-15, demonstrating that urea was deposited inside the mesopores. In vivo moisturization studies revealed that SBA-15Urea was not able to reduce transepidermal water loss compared to the other products and control, while forming a non-occlusive surface film on the skin. We conclude that incorporation of urea in the pores of the inorganic SBA-15 matrix is a promising approach to enhancing its stability and providing a prolonged moisturizing effect.


Subject(s)
Urea/analysis , Silicon Dioxide/administration & dosage , Skin/drug effects , Fluid Therapy/adverse effects
13.
International Journal of Biomedical Engineering ; (6): 66-70, 2019.
Article in Chinese | WPRIM | ID: wpr-743006

ABSTRACT

In recent years, mesoporous silica nanoparticles (MSNs) have been widely used in the construction of various intelligent drug delivery systems due to their unique and excellent properties. The stimuli-responsive drug delivery system based on mesoporous silica nanoparticles can effectively load anticancer drugs and target them to tumor cells, and then responsively release anticancer drugs under the action of specific stimulation signals. The method of specifically delivering anticancer drugs to target sites not only can greatly improvethe drug efficacy, but also effectively reduce the side effects of anticancer drugs on normal tissues and organs. Thereby the advantages of anticancer drugs in tumor therapy are improved. In this paper, the applications and developments of stimuliresponsive mesoporous silica nano drug delivery systems in tumor therapy were summarized.

14.
Chinese Journal of Cancer Biotherapy ; (6): 1083-1088, 2019.
Article in Chinese | WPRIM | ID: wpr-793229

ABSTRACT

@#Objective: To construct indocyanine green-loaded silica nanoparticles (ICG@MSNs) and evaluate their killing effect on cervical cancer HeLa cells. Methods: Mesoporous silica nanoparticles (MSNs) were synthesized by template method, and indocyanine green (ICG) containing photothermal agent was loaded to prepare ICG@MSNs with photothermal effect, which were applied in the research of HeLa cells in vitro. Results: The particle of ICG@MSNs was uniform and in regular spherical shape with the size about 200 nm. ICG@MSNs was similar photothermal effect with pure ICG. Cell endocytosis experiments showed that ICG encapsulated in silica nanoparticles is more likely to be endocytosed by tumor cells, and then played a photothermal role in killing cervical cancer HeLa cells. On the other hand, cytotoxicity experiments showed that under the irradiation of 808 nm laser, ICG@MSNs significantly increased cytotoxicity, which could significantly kill cervical cancer HeLa cells. Conclusion: ICG@MSNs has good stability and biocompatibility, as well as good thermogenesis. It’s photothermal treatment effect on tumor is obvious, which has a good prospect for the treatment of cervical cancer.

15.
China Pharmacy ; (12): 2056-2061, 2019.
Article in Chinese | WPRIM | ID: wpr-817181

ABSTRACT

OBJECTIVE: To study release behavior in vitro of Risperidone sustained-release tablets and its pharmacokinetics in rabbits. METHODS: Risperidone sustained-release tablets were prepared by using mesoporous silica as matrix. Release rates in vitro within 12 h (Q12 h) of commercially available Risperidone tablets, Risperidone sustained-release tablets and its physical mixture in 0.1 mol/L HCl fluid were investigated with basket method. The release model of Risperidone sustained-release tablets were fitted. Using clozapine as an internal standard, HPLC method was used to determine blood concentration of risperidone and 9-hydroxyrisperidone in rabbits 48 h (n=6) after intragastric administration of commercially available Risperidone tablets and Risperidone sustained-release tablets 2 mg. Pharmacokinetic parameters were calculated by using non-compartmental model of Kinetica 4.4 software. RESULTS: Compared with commercially available Risperidone tablets (Q12 h=97%) and physical mixtures (Q12 h=95%), release rate of Risperidone sustained-release tablets (Q12 h=83.7%) slowed down significantly, and the release of Risperidone sustained-release tablets in 0.1 mol/L HCl fluid was closed to first-order release (R2=0.998 9), with diffusion as the main factor and dissolution as the supplement. By risperidone, the pharmacokinetic parameters of commercially available Risperidone tablets and Risperidone sustained-release tablets included that t1/2 were (4.64±0.93),(6.65±0.92) h; cmax were (34.46±7.75) and (8.57±6.91) ng/mL; MRT were (11.48±1.23), (17.46±2.10) h; AUC0-48 h were (314.39±10.33),(192.98±49.14) ng·h/mL, respectively. By 9-hydroxyrisperidone, the pharmacokinetic parameters of them included that t1/2 were(7.08±0.93),(10.45±0.78) h; cmax were (98.08±5.43),(54.55±4.88) ng/mL; MRT were (11.48±1.23), (17.46±2.10) h; AUC0-48 h were (894.71±131.15), (1 227.99±112.12) ng·h/mL (n=6), respectively. Compared with commercially available Risperidone tablets, t1/2 and MRT of Risperidone sustained-release tablets prolonged significantly, while cmax decreased significantly (P<0.05). CONCLUSIONS: Risperidone loaded in mesoporous silica has sustained release effect and prolong the time of drug efficacy.

16.
Journal of Shanghai Jiaotong University(Medical Science) ; (12): 1329-1334, 2019.
Article in Chinese | WPRIM | ID: wpr-843319

ABSTRACT

Until now, great progress has been made in anti-tumor therapy. A series of novel anti-tumor drugs, such as molecular targeted drugs and monoclonal antibodies, have been emerging one after another, which have benefited a great number of tumor patients in different degrees. However, there are still many dilemmas in clinical anti-tumor therapy at present, for instance, obvious side effects, tumor resistance and so on. In recent years, the nano drug delivery system with mesoporous silica as the carrier has overcome many flaws of traditional anti-tumor treatment to a certain extent, especially the mesoporous silica nanosystem for controlling reactive oxygen species generation which has excellent tumor targeting property and biocompatibility, and minimal injury effects on normal tissue cells. So it has been regarded as one of the most promising agents in clinical application by playing significant anti-tumor roles through multiple approaches. This paper reviews this kind of potent nanosystem and its application to anti-tumor therapy.

17.
Chinese Pharmaceutical Journal ; (24): 110-116, 2019.
Article in Chinese | WPRIM | ID: wpr-858095

ABSTRACT

OBJECTIVE: To establish a drug delivery system based on hyaluronic acid functionalized mesoporous silica nanoparticles MCM-41 loaded with paclitaxel (HA-MCM-41-PTX). The physical and chemical properties, in vitro drug release and the antitumor effect were investigated. METHODS: The morphological structure and particle size of MCM-41 were observed by TEM. The drug delivery system was characterized by PXRD and FTIR. The in vitro release experiments was carried out to investigate the dissolution rate of HA-MCM-41-PTX. The in vitro cells experiment was carried out to explore the mechanism of HA-MCM-41-PTX on cells. RESULTS: The drug loading capacity of HA-MCM-41-PTX was 28.75%. The in vitro drug release experiments showed that HA-MCM-41-PTX exhibited controlled release with a cumulative release of (86.19±5.11)% until 48 h. In vitro cell experiments showed that HA-MCM-41-PTX had excellent targeting effect due to the modification of hyaluronic acid, which was easier to be uptaken by cells and exhibited great antitumor effect. CONCLUSION: HA-MCM-41-PTX is an excellent drug delivery system with both controlled release and targeting antitumor effect.

18.
Chinese Traditional and Herbal Drugs ; (24): 2057-2062, 2018.
Article in Chinese | WPRIM | ID: wpr-851999

ABSTRACT

Objective To prepare a mesoporous silica-coated polypyrrole nanoparticles loaded with honokiol (PPy@MSN-HK) and evaluate their in vitro release behavior. Methods In this study, PPy@MSN-HK was obtained in three steps: First, prepared polypyrrole nanoparticles; Second, coated mesoporous silica shell on its surface; Third, absorbed honokiol. The TEM, particle size, zeta potential, drug loading, infrared spectroscopy, in vitro photothermal properties, and in vitro release characteristics were chosen as indexes to investigate its potential as antitumor nanocarries. The release profiles were analyzed by simulating factor (f2), and the dissolution profiles were fitted by a variety of commonly used mathematical models. Results The results showed that the prepared nanoparticles had uniform particle size and uniform size distribution. The average particle size was (220.4 ± 4.2) nm, polydispersity coefficient was 0.042 ± 0.010, zeta potential was (-21.1 ± 0.8) mV, drug loading was (2.58 ± 0.53)%, and entrapment efficiency was (75.04 ± 0.95)%, respectively. The results of in vitro photothermal experiments showed that with the constant laser power density, the temperature change value of nanoparticles suspension increased with the increase of nanoparticles concentration. This showed that PPy@MSN have a good photothermal effect. In vitro release test revealed that the two release curves were not similar, and fitting best with Ritger-Peppas eqution and Logistic eqution respectively. Conclusion The water solution method could be used to prepare PPy@MSN, which may provide a promising drug delivery strategy for tumor treatment.

19.
Acta Pharmaceutica Sinica ; (12): 716-726, 2018.
Article in Chinese | WPRIM | ID: wpr-779927

ABSTRACT

Mesoporous silica nanoparticles (MSNs) have been widely used as drug carriers in the diagnosis and treatment of diseases due to their specific characteristics, which include a large surface area, ordered mesoporous structures, easy surface modification and feasible sustained release action for encapsulated drugs. With the research development of MSNs, the biodegradability and removability of mesoporous silica nanomaterials have attracted considerable attention in the clinical application of the MSNs-based formulations. This paper was prepared to emphasize the preparation approaches of biodegradable mesoporous silica nanoparticles through the metal oxide doping method and the organic compound doping method. We discussed the biodegradable mechanism and process of such nanoparticles, and finally, provided an insightful and helpful review of the prospective application of the biodegradable mesoporous silica nanoparticles in medical field.

20.
Chinese Pharmaceutical Journal ; (24): 1381-1387, 2018.
Article in Chinese | WPRIM | ID: wpr-858241

ABSTRACT

OBJECTIVE: To prepare mesoporous silica nanoparticles (MSNs) modified by targeted ingredients to improve the tumor cell lethality of antitumor drugs. METHODS: MSNs were prepared by template-hot water method, and modified with amino group and polyethyleneimine. The nano-carriers were characterized by their morphology, particle size and infrared absorption. Meanwhile, the intracellular uptake and in vitro antitumor activity of MSNs were evaluated on human breast carcinoma cell line (MCF-7). RESUTLS Three kinds of nanoparticles, MSNs, MSNs-NH2 and MSNs-PEI were all spherical, with mean diameters of (65±19), (77±17) and (117±21) nm, respectively. Infrared spectrum and differential thermal analysis RESULTS: indicated that the functional groups were linked onto the surface of MSNs, and slower drug release was observed for MSNs-NH2 and MSNs-PEI. Moreover, the cellular uptake of three nanoparticles were 2.05, 2.89, and 2.63 times higher than free doxorubicin, and the cytotoxicity activity against MCF-7 cells were 1.77, 2.21, and 2.19 times, respectively. CONCLUSION: The preparation method can be used to prepare MSNs nano-carriers. MSNs-NH2 and MSNs-PEI have improved carrier property and antitumor activity.

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