scholarly journals Physical Characterization and Biodistribution of Cisplatin Loaded in Surfactant Modified-Hybrid Nanoparticles Using Polyethylene Oxide-b-Polymethacrylic Acid

2020 ◽  
Author(s):  
Andang Miatmoko
Keyword(s):  
Polyethylene Oxide ◽  
Tween 80 ◽  
Sodium Deoxycholate ◽  
Sodium Cholate ◽  
Hybrid Nanoparticles ◽  
Molar Ratio ◽  
Particle Sizes ◽  
Polymethacrylic Acid ◽  
Tumor Accumulation

Purpose: Conjugating cisplatin into hybrid nanoparticles is intended to enhance tumor accumulation due to drug interaction with polymer and prevent premature drug release because of the presence of a lipid layer. Methods: Hybrid nanoparticles composed of polyethylene oxide-b-polymethacrylic acid, egg phosphatidylcholine, and surfactant, i.e. sodium cholate/sodium deoxycholate/Tween 80, were prepared by the injection method. Cisplatin was subsequently loaded by incubating the polymer-drug mixtures at the molar ratio of carboxylate ions of 2:1. Results: The results showed that the addition of surfactants produced particle sizes between 33 and 52 nm. The addition of cisplatin increased the ζ-potential to slightly positive charges with encapsulation efficiencies of 5-18%. An in vivo biodistribution study of mice identified a cisplatin plasma concentration of sodium cholate-modified hybrid nanoparticles ten times higher than cisplatin solution, thus producing high tumor accumulation. Conclusion: Conjugating cisplatin into sodium cholate-modified hybrid nanoparticles improves its accumulation in tumors.

Substitution of Lipids with Bile Salts in the Formation of Thrombin

1969 ◽  
Vol 22 (01) ◽  
pp. 013-027 ◽  
Author(s):  
Monika Barthels ◽  
W. H Seegers
Keyword(s):  
Calcium Ions ◽  
Bile Salts ◽  
Thrombin Generation ◽  
Sodium Deoxycholate ◽  
Sodium Cholate ◽  
Phosphatidyl Serine ◽  
Molar Ratio ◽  
Platelet Factor ◽  
Analytical Reagents ◽  
Autoprothrombin C

SummaryThe generation of thrombin was studied in an activating system consisting of purified thrombin zymogens, purified autoprothrombin C, purified Ac-globulin, lipid or bile salts, and calcium chloride. With the concentration of calcium ions and pH fixed, the effect of varying the other three procoagulants was studied. Bile salts were effective substitutes for lipids in a concentration where micelles form. The approximate effectiveness from highest to lowest was: conjugated sodium salt of taurocholic acid, sodium cholate, sodium deoxycholate. Sodium dehydrocholate was ineffective. Autoprothrombin C is the enzyme for thrombin formation. For accelerating its activity best results were obtained with the simultaneous presence of optimal concentrations of calcium ions, Ac-globulin and lipids or bile salts. Reducing any one of the three to zero concentration decreased the rate and yield of thrombin generation.The form in which the zymogen is used was found to be important. Prothrombin complex, DE AE-prothrombin and prethrombin were studied. Each substrate has its peculiar requirements for yielding thrombin. Prothrombin complex and DEAE-pro-thrombin activated far more rapidly and required 10 times less autoprothrombin C than prethrombin. The yield of thrombin from these substrates was also higher than from prethrombin. DE AE-prothrombin required the least amount of lipid. For the bile salts the required concentrations were nearly always the same from one substrate to another. To a certain extent Benadryl could also be substituted for lipids. In association with rapid thrombin generation from DE AE-prothrombin the Ac-globulin and autoprothrombin C Avere represented in approximately a 6:1 molar ratio. As compared with the weight of the enzyme large amounts of Ac-globulin and cholate were required.DE AE-prothrombin was readily made refractory to the two-stage analytical reagents with purified platelet factor 3 and calcium ions. Combinations of sodium cholate and phosphatidyl serine were also effective, but either one alone was ineffective.

The activation of cystacanths of Polymorphus minutus (Acanthocephala) in vitro

Parasitology ◽  
1974 ◽  
Vol 68 (2) ◽  
pp. 135-146 ◽  
Author(s):  
Ann M. Lackie
Keyword(s):  
Surrounding Medium ◽  
Sodium Taurocholate ◽  
Sodium Deoxycholate ◽  
Sodium Cholate ◽  
Apparent Effect ◽  
Activation Rate ◽  
Marked Enhancement ◽  
Rate Of Activation

The factors responsible for stimulating activation of cystacanths of Polymorphus minutus in vitro have been investigated. Under the conditions used, the optimum temperature for activation was found to be 42–44 °C, at a pH of 7·0. A marked enhancement of activation rate was observed after preincubation in a 1 mM solution of sodium taurocholate and in solutions of sodium cholate, sodium glycocholate or sodium deoxycholate. This apparent effect of bile salts has been compared with that of other detergents, and a significant enhancement of activation rate above control was observed with saponin and sodium fusidate. Trypsin did not affect the rate of activation, and some inhibition occurred with lipase. The osmotic pressure of the surrounding medium has an effect on activation, the rate of which varies inversely with osmolarity. The conditions for activation in vitro are compared with those of the physicochemical environment in vivo.

scholarly journals Ultra-strong bio-glue from genetically engineered polypeptides

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Chao Ma ◽  
Jing Sun ◽  
Bo Li ◽  
Yang Feng ◽  
Yao Sun ◽  
...  
Keyword(s):  
Soft Tissues ◽  
Covalent Bond ◽  
Genetically Engineered ◽  
Supramolecular Interactions ◽  
Molar Ratio ◽  
High Adhesion ◽  
Strong Adhesion ◽  
Order Of Magnitude

AbstractThe development of biomedical glues is an important, yet challenging task as seemingly mutually exclusive properties need to be combined in one material, i.e. strong adhesion and adaption to remodeling processes in healing tissue. Here, we report a biocompatible and biodegradable protein-based adhesive with high adhesion strengths. The maximum strength reaches 16.5 ± 2.2 MPa on hard substrates, which is comparable to that of commercial cyanoacrylate superglue and higher than other protein-based adhesives by at least one order of magnitude. Moreover, the strong adhesion on soft tissues qualifies the adhesive as biomedical glue outperforming some commercial products. Robust mechanical properties are realized without covalent bond formation during the adhesion process. A complex consisting of cationic supercharged polypeptides and anionic aromatic surfactants with lysine to surfactant molar ratio of 1:0.9 is driven by multiple supramolecular interactions enabling such strong adhesion. We demonstrate the glue’s robust performance in vitro and in vivo for cosmetic and hemostasis applications and accelerated wound healing by comparison to surgical wound closures.

scholarly journals MSCs-engineered biomimetic PMAA nanomedicines for multiple bioimaging-guided and photothermal-enhanced radiotherapy of NSCLC

2021 ◽  
Vol 19 (1) ◽  
Author(s):  
Yipengchen Yin ◽  
Yongjing Li ◽  
Sheng Wang ◽  
Ziliang Dong ◽  
Chao Liang ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Cell Membranes ◽  
Imaging System ◽  
Fluorescence Signal ◽  
Bimodal Imaging ◽  
Red Blood Cell Membranes ◽  
Magnetic Resonance Imaging Mri ◽  
Tumor Accumulation

Abstract Background The recently developed biomimetic strategy is one of the mostly effective strategies for improving the theranostic efficacy of diverse nanomedicines, because nanoparticles coated with cell membranes can disguise as “self”, evade the surveillance of the immune system, and accumulate to the tumor sites actively. Results Herein, we utilized mesenchymal stem cell memabranes (MSCs) to coat polymethacrylic acid (PMAA) nanoparticles loaded with Fe(III) and cypate—an derivative of indocyanine green to fabricate Cyp-PMAA-Fe@MSCs, which featured high stability, desirable tumor-accumulation and intriguing photothermal conversion efficiency both in vitro and in vivo for the treatment of lung cancer. After intravenous administration of Cyp-PMAA-Fe@MSCs and Cyp-PMAA-Fe@RBCs (RBCs, red blood cell membranes) separately into tumor-bearing mice, the fluorescence signal in the MSCs group was 21% stronger than that in the RBCs group at the tumor sites in an in vivo fluorescence imaging system. Correspondingly, the T1-weighted magnetic resonance imaging (MRI) signal at the tumor site decreased 30% after intravenous injection of Cyp-PMAA-Fe@MSCs. Importantly, the constructed Cyp-PMAA-Fe@MSCs exhibited strong photothermal hyperthermia effect both in vitro and in vivo when exposed to 808 nm laser irradiation, thus it could be used for photothermal therapy. Furthermore, tumors on mice treated with phototermal therapy and radiotherapy shrank 32% more than those treated with only radiotherapy. Conclusions These results proved that Cyp-PMAA-Fe@MSCs could realize fluorescence/MRI bimodal imaging, while be used in phototermal-therapy-enhanced radiotherapy, providing desirable nanoplatforms for tumor diagnosis and precise treatment of non-small cell lung cancer.

scholarly journals In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

2021 ◽  
Author(s):  
Mohsen Hedaya ◽  
Farzana Bandarkar ◽  
Aly Nada
Keyword(s):  
Particle Size ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
In Vivo Evaluation ◽  
Poorly Soluble ◽  
Extent Of Absorption ◽  
Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

scholarly journals Optimized 5-Fluorouridine Prodrug for Co-Loading with Doxorubicin in Clinically Relevant Liposomes

Pharmaceutics ◽  
2021 ◽  
Vol 13 (1) ◽  
pp. 107
Author(s):  
Debra Wu ◽  
Douglas Vogus ◽  
Vinu Krishnan ◽  
Marta Broto ◽  
Anusha Pusuluri ◽  
...  
Keyword(s):  
Single Agent ◽  
Molar Ratio ◽  
Control Group ◽  
Drug Tolerability ◽  
Breast Cancer Model ◽  
In Vivo Testing ◽  
Chemical Profiles ◽  
Hydrolysis Of ◽  
Doxorubicin Liposomes

Liposome-based drug delivery systems have allowed for better drug tolerability and longer circulation times but are often optimized for a single agent due to the inherent difficulty of co-encapsulating two drugs with differing chemical profiles. Here, we design and test a prodrug based on a ribosylated nucleoside form of 5-fluorouracil, 5-fluorouridine (5FUR), with the final purpose of co-encapsulation with doxorubicin (DOX) in liposomes. To improve the loading of 5FUR, we developed two 5FUR prodrugs that involved the conjugation of either one or three moieties of tryptophan (W) known respectively as, 5FUR−W and 5FUR−W3. 5FUR−W demonstrated greater chemical stability than 5FUR−W3 and allowed for improved loading with fewer possible byproducts from tryptophan hydrolysis. Varied drug ratios of 5FUR−W: DOX were encapsulated for in vivo testing in the highly aggressive 4T1 murine breast cancer model. A liposomal molar ratio of 2.5 5FUR−W: DOX achieved a 62.6% reduction in tumor size compared to the untreated control group and a 33% reduction compared to clinical doxorubicin liposomes in a proof-of-concept study to demonstrate the viability of the co-encapsulated liposomes. We believe that the new prodrug 5FUR−W demonstrates a prodrug design with clinical translatability by reducing the number of byproducts produced by the hydrolysis of tryptophan, while also allowing for loading flexibility.

scholarly journals Selective Targeting of Breast Cancer by Tafuramycin a Using SMA-Nanoassemblies

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3532
Author(s):  
Ibrahim M. El-Deeb ◽  
Valeria Pittala ◽  
Diab Eltayeb ◽  
Khaled Greish
Keyword(s):  
Breast Cancer ◽  
Progesterone Receptors ◽  
In Vivo Studies ◽  
Chemotherapy Agent ◽  
Anticancer Effects ◽  
Tumor Tissues ◽  
Potential Strategy ◽  
Tumor Accumulation

Triple-negative breast cancer (TNBC) is a heterogeneous subtype of tumors that tests negative for estrogen receptors, progesterone receptors, and excess HER2 protein. The mainstay of treatment remains chemotherapy, but the therapeutic outcome remains inadequate. This paper investigates the potential of a duocarmycin derivative, tafuramycin A (TFA), as a new and more effective chemotherapy agent in TNBC treatment. To this extent, we optimized the chemical synthesis of TFA, and we encapsulated TFA in a micellar system to reduce side effects and increase tumor accumulation. In vitro and in vivo studies suggest that both TFA and SMA–TFA possess high anticancer effects in TNBC models. Finally, the encapsulation of TFA offered a preferential avenue to tumor accumulation by increasing its concentration at the tumor tissues by around four times in comparison with the free drug. Overall, the results provide a new potential strategy useful for TNBC treatment.

scholarly journals Carbothermal Synthesis of Ni/Fe Bimetallic Nanoparticles Embedded into Graphitized Carbon for Efficient Removal of Chlorophenol

Nanomaterials ◽  
2021 ◽  
Vol 11 (6) ◽  
pp. 1417
Author(s):  
Min Zhuang ◽  
Wen Shi ◽  
Hui Wang ◽  
Liqiang Cui ◽  
Guixiang Quan ◽  
...  
Keyword(s):  
Removal Efficiency ◽  
Surface Passivation ◽  
Bimetallic Nanoparticles ◽  
Zero Valent Iron ◽  
Molar Ratio ◽  
Particle Sizes ◽  
Iron Corrosion ◽  
Graphitized Carbon ◽  
Nanoscale Zero Valent Iron ◽  
Iron Nickel

The reactivity of nanoscale zero-valent iron is limited by surface passivation and particle agglomeration. Here, Ni/Fe bimetallic nanoparticles embedded into graphitized carbon (NiFe@GC) were prepared from Ni/Fe bimetallic complex through a carbothermal reduction treatment. The Ni/Fe nanoparticles were uniformly distributed in the GC matrix with controllable particle sizes, and NiFe@GC exhibited a larger specific surface area than unsupported nanoscale zero-valent iron/nickel (FeNi NPs). The XRD results revealed that Ni/Fe bimetallic nanoparticles embedded into graphitized carbon were protected from oxidization. The NiFe@GC performed excellently in 2,4,6-trichlorophenol (TCP) removal from an aqueous solution. The removal efficiency of TCP for NiFe@GC-50 was more than twice that of FeNi nanoparticles, and the removal efficiency of TCP increased from 78.5% to 94.1% when the Ni/Fe molar ratio increased from 0 to 50%. The removal efficiency of TCP by NiFe@GC-50 can maintain 76.8% after 10 days of aging, much higher than that of FeNi NPs (29.6%). The higher performance of NiFe@GC should be ascribed to the significant synergistic effect of the combination of NiFe bimetallic nanoparticles and GC. In the presence of Ni, atomic H* generated by zero-valent iron corrosion can accelerate TCP removal. The GC coated on the surface of Ni/Fe bimetallic nanoparticles can protect them from oxidation and deactivation.

scholarly journals Nanocrystal-Loaded Micelles for the Enhanced In Vivo Circulation of Docetaxel

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4481
Author(s):  
Meng Cheng ◽  
Qiaoming Liu ◽  
Tiantian Gan ◽  
Yuanying Fang ◽  
Pengfei Yue ◽  
...  
Keyword(s):  
Thin Film ◽  
Retention Time ◽  
Blood Circulation ◽  
Crystalline State ◽  
Circulation System ◽  
Particle Sizes ◽  
High Pressure Homogenization ◽  
Rapid Dissolution ◽  
Efficient Route

Prolonging in vivo circulation has proved to be an efficient route for enhancing the therapeutic effect of rapidly metabolized drugs. In this study, we aimed to construct a nanocrystal-loaded micelles delivery system to enhance the blood circulation of docetaxel (DOC). We employed high-pressure homogenization to prepare docetaxel nanocrystals (DOC(Nc)), and then produced docetaxel nanocrystal-loaded micelles (DOC(Nc)@mPEG-PLA) by a thin-film hydration method. The particle sizes of optimized DOC(Nc), docetaxel micelles (DOC@mPEG-PLA), and DOC(Nc)@mPEG-PLA were 168.4, 36.3, and 72.5 nm, respectively. The crystallinity of docetaxel was decreased after transforming it into nanocrystals, and the crystalline state of docetaxel in micelles was amorphous. The constructed DOC(Nc)@mPEG-PLA showed good stability as its particle size showed no significant change in 7 days. Despite their rapid dissolution, docetaxel nanocrystals exhibited higher bioavailability. The micelles prolonged the retention time of docetaxel in the circulation system of rats, and DOC(Nc)@mPEG-PLA exhibited the highest retention time and bioavailability. These results reveal that constructing nanocrystal-loaded micelles may be a promising way to enhance the in vivo circulation and bioavailability of rapidly metabolized drugs such as docetaxel.

UCNP@BSA@Ru nanoparticles with tumor-specific and NIR-triggered efficient PACT activity in vivo

2021 ◽  
Author(s):  
Chao Zhang ◽  
Xusheng Guo ◽  
Xuwen Da ◽  
Yishan Yao ◽  
Haihua Xiao ◽  
...  
Keyword(s):  
Bovine Serum Albumin ◽  
Serum Albumin ◽  
Bovine Serum ◽  
Short Wavelength ◽  
Ru Nanoparticles ◽  
Wavelength Absorption ◽  
Tumor Accumulation ◽  
Accumulation Ability

Ru(II)-based photoactivated chemotherapy (PACT) agents are promising, however, the short wavelength absorption (generally < 550 nm) and poor tumor accumulation ability limit their in vivo applications. Herein bovine serum albumin...

Sign in / Sign up

Export Citation Format

Share Document