scholarly journals Folate-Functionalized Mesoporous Hollow SnO2 Nanofibers as a Targeting Drug Carrier to Improve the Antitumor Effect of Paclitaxel for Liver Cancer Therapy

2018 ◽  
Vol 2018 ◽  
pp. 1-11
Author(s):  
Huiling Lv ◽  
Chao Wu ◽  
Xuan Liu ◽  
Andi Bai ◽  
Yue Cao ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Liver Cancer ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Hollow Structure ◽  
Amorphous State ◽  
Outer Diameter ◽  
Drug Delivery Carrier

In this study, we prepared PTX-loaded mesoporous hollow SnO2 nanofibers conjugated with folic acid (SFNFP) for liver cancer therapy. According to SEM and TEM characterization, SFNF showed a mesoporous hollow structure. The average outer diameter was 200 nm, and the wall thickness was 50 nm. The DSC and XRD study showed that PTX in the channels of nanofibers was present in an amorphous state. The in vitro release experiments demonstrated that SFNF could efficiently improve the dissolution rate of PTX. Both in vitro cell experiments and in vivo antitumor experiments showed that SFNFP could efficiently inhibit the growth of liver cancer cells. Therefore, SFNF is a promising targeting antitumor drug delivery carrier.

Uniform hollow mesoporous silica nanocages for drug delivery in vitro and in vivo for liver cancer therapy

2011 ◽  
Vol 21 (14) ◽  
pp. 5299 ◽  
Author(s):  
Tingting Wang ◽  
Fang Chai ◽  
Qin Fu ◽  
Lingyu Zhang ◽  
Haiyan Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Therapy ◽  
Liver Cancer ◽  
Mesoporous Silica ◽  
Hollow Mesoporous Silica

scholarly journals The Good, the Bad, the Question–H19 in Hepatocellular Carcinoma

Cancers ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 1261 ◽  
Author(s):  
Lysann Tietze ◽  
Sonja M. Kessler
Keyword(s):  
Hepatocellular Carcinoma ◽  
Cancer Therapy ◽  
Liver Cancer ◽  
Primary Liver Cancer ◽  
Human Patient ◽  
In Vivo Models ◽  
Study Results ◽  
Novel Target

Hepatocellular carcinoma (HCC), the most common primary liver cancer, is challenging to treat due to its typical late diagnosis, mostly at an advanced stage. Therefore, there is a particular need for research in diagnostic and prognostic biomarkers and therapeutic targets for HCC. The use of long noncoding (lnc) RNAs can widen the list of novel molecular targets improving cancer therapy. In hepatocarcinogenesis, the role of the lncRNA H19, which has been known for more than 30 years now, is still controversially discussed. H19 was described to work either as a tumor suppressor in vitro and in vivo, or to have oncogenic features. This review attempts to survey the conflicting study results and tries to elucidate the potential reasons for the contrary findings, i.e., different methods, models, or readout parameters. This review encompasses in vitro and in vivo models as well as studies on human patient samples. Although the function of H19 in HCC remains elusive, a short outlook summarizes some ideas of using the H19 locus as a novel target for liver cancer therapy.

scholarly journals Improved In vivo Effect of Chrysin as an Absorption Enhancer Via the Preparation of Ternary Solid Dispersion with Brij®L4 and Aminoclay

2018 ◽  
Vol 16 (1) ◽  
pp. 86-92 ◽  
Author(s):  
Sang Hoon Lee ◽  
Yeo-song Lee ◽  
Jae Geun Song ◽  
Hyo-Kyung Han
Keyword(s):  
Drug Release ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Absorption Enhancer ◽  
Cancer Resistance ◽  
Surface Acting ◽  
Strong Inhibitor

Background: Chrysin is a strong inhibitor of breast cancer resistance protein (BCRP) but it is practically insoluble in water. Effective solubilization of chrysin is critical for its pharmaceutical application as an absorption enhancer via inhibition of BCRP-mediated drug efflux. Objective: This study aimed to develop an effective oral formulation of chrysin to improve its in vivo effect as an absorption enhancer. Method: Solid dispersions (SDs) of chrysin were prepared with hydrophilic carriers having surface acting properties and a pH modulator. In vitro and in vivo characterizations were performed to select the optimal SDs of chrysin. Results: SDs with Brij&®L4 and aminoclay was most effective in increasing the solubility of chrysin by 13-53 fold at varying drug-carrier ratios. Furthermore, SDs significantly improved the dissolution rate and extent of drug release. SDs (chrysin: Brij&®L4: aminoclay=1:3:5) achieved approximately 60% and 83% drug release within 1 h and 8 h, respectively, in aqueous medium, while the dissolution of the untreated chrysin was less than 13%. XRD patterns indicated the amorphous state of chrysin in SDs. The SD formulation was effective in improving the bioavailability of topotecan, a BCRP substrate in rats. Following oral administration of topotecan with the SDs of chrysin, the Cmax and AUC of topotecan was enhanced by approximately 2.6- and 2-fold, respectively, while the untreated chrysin had no effect. Conclusion: The SD formulation of chrysin with Brij&®L4 and aminoclay appeared to be promising in improving the dissolution of chrysin and enhancing its in vivo effect as an absorption enhancer.

scholarly journals Injectable Vaginal Hydrogels as a Multi-Drug Carrier for Contraception

2019 ◽  
Vol 9 (8) ◽  
pp. 1638 ◽  
Author(s):  
Nie ◽  
Zou ◽  
Dong ◽  
Sun ◽  
Ding ◽  
...  
Keyword(s):  
Ethinyl Estradiol ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Temperature Sensitive ◽  
Dosage Group ◽  
Contraceptive Effect ◽  
Poly Ethylene ◽  
Release Profiles

Injectable intravaginal hydrogels could deliver drugs systemically without hepatic first pass effect. This paper focuses on the contraceptive function of an injectable temperature-sensitive four-arm star-shaped poly(D,L-lactic-co-glycolic acid)-b-methoxy poly(ethylene glycol) (4sPLGA-mPEG) block copolymer hydrogels as a carrier of three drugs. In vitro controlled release profiles were investigated via HPLC, and it showed that the cumulative release amounts of indomethacin (IMC), gestodene (GSD), and ethinyl estradiol (EE) from copolymer hydrogels could be regulated by adjusting the lactide/glycolide (LA/GA) mol ratio. In addition, in vitro release profiles of IMC, GSD, and EE well corresponded to Higuchi model. The acute toxicity of copolymer hydrogels loaded with different dosage contents multi-drug was evaluated in vivo. As to the high dosage group, the uterus was hydropic at day 1 and ulcerated at day 5, followed with intestinal adhesion. Regarding the middle dosage group, no festering of tissues was observed and, blood coagulum existed in the uterus at different days. For low dosage group, no significant tissue necrosis was found. Finally, the antifertility experiments confirmed that hydrogels loaded with the multi-drug had an excellent contraceptive effect. The above results indicated that injectable copolymer hydrogel as a multi-drug carrier was promising as a novel contraception method.

scholarly journals Delay Tumor Growth Properties of LA-PEG-G Molecule and Its' Application as Drug Carrier

2020 ◽  
Author(s):  
guangcheng wei ◽  
Meixiu Xin ◽  
Hao Wang ◽  
Yehong Huo ◽  
Wei Hu ◽  
...  
Keyword(s):  
Tumor Growth ◽  
Antitumor Effect ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Serum Biochemistry ◽  
Delay Tumor Growth ◽  
In Vivo Experiments ◽  
Low Cytotoxicity

Abstract LA–PEG–G molecule was prepared through the covalent conjugation of linoleic acid, polyethylene glycol and guanosine. LA–PEG–G molecule can self-assemble into spherical aggregate in aqueous solution. The size of the LA–PEG–G aggregate was approximately 132.1 ± 13.718 nm, and the Zeta potential was −36.3 ± 0.9644 mv. The loading rate of LA–PEG–G aggregates to Dox was 84.62 ± 1.810%. In vitro release experiments showed that Dox release from the LA–PEG–G–Dox nanomedicine was slow-release. Cell experiments showed that LA–PEG–G aggregates have low cytotoxicity, and the relative cancer cells survival rate decreased with the increasing of time and LA–PEG–G–Dox nanomedicine concentration. In vivo experiments showed that LA–PEG–G–Dox nanomedicine can inhibit tumor growth, and the LA–PEG–G aggregate could also delay the tumor growth which is very important to play the synergistic antitumor effect with the anticancer drug. Serum biochemistry showed that LA–PEG–G–Dox nanomedicine which reduced the Dox toxicity had very good antitumor effect. The tumor tissue sections indicated that LA–PEG–G–Dox nanomedicine can effectively induce tumor cell apoptosis, and finally cause tissue necrosis to achieve tumor treatment.

scholarly journals Sorafenib-Loaded Long-Circulating Nanoliposomes for Liver Cancer Therapy

2020 ◽  
Vol 2020 ◽  
pp. 1-12
Author(s):  
Haiwei Ye ◽  
Liping Zhou ◽  
Haili Jin ◽  
Yunhua Chen ◽  
Die Cheng ◽  
...  
Keyword(s):  
Cancer Therapy ◽  
Liver Cancer ◽  
Tumor Targeting ◽  
Entrapment Efficiency ◽  
Antitumor Effects ◽  
Therapeutic Efficiency ◽  
Loading Efficiency ◽  
Tumor Region

A type of sorafenib- (SOR-) loaded long-circulating nanoliposome was constructed, and the targeting performance and antitumor effects of the prepared liposome were evaluated in the present study. Polyethylene glycol- (PEG-) modified long-circulating nanoliposomes (LC-NPs) were designed and prepared using reverse evaporation, and the LC-NPs were used for delivering sorafenib (LC-PEG-SOR-NPs). Then, the anti-VEGFR antibody as a targeting moiety was chemically coupled with LC-PEG-SOR-NPs to form liver cancer-targeted nanoliposomes (anti-VEGFR-LC-PEG-SOR-NPs). The drug entrapment and loading efficiency were measured. And the cancer-targeting performance and therapeutic efficiency were evaluated both in vitro and in vivo. The anti-VEGFR-LC-PEG-SOR-NPs with an average of 119.8±4.2 nm showed a uniform spherical structure. The drug entrapment and loading efficiency were 92.5% and 18.5%, respectively. The killing efficiency of anti-VEGFR-LC-PEG-SOR-NPs was up to 18% after incubating with liver cancer cells for 72 h. Furthermore, the anti-VEGFR-LC-PEG-SOR-NPs could actively target at the tumor region and could efficiently inhibit tumor growth with negligible side effects. This newly designed nanoliposomes had desirable dispersibility, high drug entrapment efficiency, tumor targeting and therapeutic efficiency, and good safety. As a biocompatible nanocomposite, it was promising to become a novel and useful tumor-targeting nanodrug for liver cancer therapy.

scholarly journals Electrospinning Preparation of Timosaponin B-II-Loaded PLLA Nanofibers and Their Antitumor Recurrence Activities In Vivo

2015 ◽  
Vol 2015 ◽  
pp. 1-9 ◽  
Author(s):  
Zhonghua Huo ◽  
Yan Qiu ◽  
Zhuling Chu ◽  
Peng Yin ◽  
Wenquan Lu ◽  
...  
Keyword(s):  
Drug Carrier ◽  
Amorphous State ◽  
Water Soluble ◽  
Sustained Delivery ◽  
Water Soluble Drug ◽  
Release Studies ◽  
Long Time ◽  
Model Drug

Poly(L-lactic)-acid (PLLA) as a drug carrier and a water-soluble drug timosaponin B-II (TB-II) as a model drug were selected to prepare drug-loaded nanofibers by electrospinning. The average diameters of pure PLLA nanofibers and TB-II-loaded nanofibers were 212.5 ± 68.5, 219.7 ± 57.8, 232.8 ± 66.9, and 232.9 ± 97.7 nm, respectively. DSC and XRD results demonstrated that TB-II was well incorporated into the nanofibers in an amorphous state. FI-TR spectroscopy indicated that TB-II had good compatibility with PLLA. In vitro release studies showed that TB-II was rapidly released from the nanofibers within 6 h, followed by a gradual release for long time. In vivo biosafety test revealed no noticeable toxicity of these TB-II nanofibers. The TB-II released from the nanofibers had obvious inhibition effect against human hepatocellular carcinoma SMMC 7721 cells both in vivo and in vitro. It was confirmed that the TB-II-loaded nanofibers were a sustained delivery system which could effectively inhibit the tumor growth and recurrence after surgery.

Reliability of a Single β-Thromboglobulin Measurement in a Diabetic Population : Importance of PGE1 in Anticoagulant Mixture

1987 ◽  
Vol 57 (02) ◽  
pp. 201-204 ◽  
Author(s):  
P Y Scarabin ◽  
L Strain ◽  
C A Ludlam ◽  
J Jones ◽  
E M Kohner
Keyword(s):  
In Vitro Release ◽  
Mean Value ◽  
Reliable Estimate ◽  
Diabetic Patients ◽  
Single Measurement ◽  
Diabetic Population ◽  
The Difference ◽  
Vitro Release

SummaryDuring the collection of samples for plasma β-thromboglobulin (β-TG) determination, it is well established that artificially high values can be observed due to in-vitro release. To estimate the reliability of a single β-TG measurement, blood samples were collected simultaneously from both arms on two separate occasions in 56 diabetic patients selected for a clinical trial. From each arm, blood was taken into two tubes containing an anticoagulant mixture with (tube A) and without (tube B) PGE!. The overall mean value of B-TG in tube B was 1.14 times higher than in tube A (p <0.01). The markedly large between-arms variation accounted for the most part of within-subject variation in both tubes and was significantly greater in tube B than in tube A. Based on the difference between B-TG values from both arms, the number of subjects with artifically high B-TG values was significantly higher in tube B than in tube A on each occasion (overall rate: 28% and 14% respectively). Estimate of between-occasions variation showed that B-TG levels were relatively stable for each subject between two occasions in each tube. It is concluded that the use of PGEi decreases falsely high B-TG levels, but a single measurement of B-TG does not provide a reliable estimate of the true B-TG value in vivo.

Fenofibrate Solid Dispersion for Improving Oral Bioavailability: Preparation, and Characterization and in vivo Evaluation

2020 ◽  
Vol 13 (5) ◽  
pp. 5102-5109
Author(s):  
Venu Madhav K ◽  
Somnath De ◽  
Chandra Shekar Bonagiri ◽  
Sridhar Babu Gummadi
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Fenofibrate (FN) is used in the treatment of hypercholesterolemia. It shows poor dissolution and poor oral bioavailability after oral administration due to high liphophilicity and low aqueous solubility. Hence, solid dispersions (SDs) of FN (FN-SDs) were develop that might enhance the dissolution and subsequently oral bioavailability. FN-SDs were prepared by solvent casting method using different carriers (PEG 4000, PEG 6000, β cyclodextrin and HP β cyclodextrin) in different proportions (0.25%, 0.5%, 0.75% and 1% w/v). FN-SDs were evaluated solubility, assay and in vitro release studies for the optimization of SD formulation. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and scanning electron microscopy (SEM) analysis was performed for crystalline and morphology analysis, respectively. Further, optimized FN-SD formulation evaluated for pharmacokinetic performance in Wistar rats, in vivo in comparison with FN suspension.  From the results, FN-SD3 and FN-SD6 have showed 102.9 ±1.3% and 105.5±3.1% drug release, respectively in 2 h. DSC and PXRD studies revealed that conversion of crystalline to amorphous nature of FN from FT-SD formulation. SEM studies revealed the change in the orientation of FN when incorporated in SDs. The oral bioavailability FN-SD3 and FN-SD6 formulations exhibited 2.5-folds and 3.1-folds improvement when compared to FN suspension as control. Overall, SD of FN could be considered as an alternative dosage form for the enhancement of oral delivery of poorly water-soluble FN.

Sign in / Sign up

Export Citation Format

Share Document