In Vitro Drug Release and Hemocompatibility of Biodegradable Plga/Peg Coated Paclitaxel-Eluting Stents

2013 ◽  
Vol 651 ◽  
pp. 49-53
Author(s):  
Sergey Pavlinich ◽  
Xi Wei Liu ◽  
Li Da Hou ◽  
Hong Zhao ◽  
Zhen Li ◽  
...  
Keyword(s):  
316L Stainless Steel ◽  
Drug Carrier ◽  
Weight Ratio ◽  
High Dose ◽  
Clotting Time ◽  
Copolymer Coating ◽  
Poly Ethylene ◽  
Surface Morphologies ◽  
Spraying Method

The Paclitaxel-eluting stents (PTX) with biodegradable copolymer coating were studied in investigations. The polymer blend composition of PLGA (polylactic acid-co-glycolic acid) and PEG (poly ethylene glycol) have been applied as drug carrier and fabricated on the surface of 316L stainless steel stents by ultrasonic atomization spraying method. Were explored three doses: low-dose (~80μg per stent, 10 wt%), moderate-dose (~150μg per stent , 20 wt%), and high-dose (~220μg per stent , 30 wt%). The weight ratio of Paclitaxel to PLGA/PEG blends was 10:90, 20:80, and 30:70. Pre- and post-expansion surface morphologies of the Paclitaxel-eluting copolymer coating stents were examined by scanning electron microscopy (SEM). The quantitative analysis of Paclitaxel release in vitro and hemocompatibility by hemolysis ratio and dynamic clotting time measurement also were investigated.

Study on Kinetics and Biocompatibility Evaluation of Multiple Polymer Layer with Biochemical Material Properties in Drug-Eluting Stent

2013 ◽  
Vol 644 ◽  
pp. 183-188
Author(s):  
Sergey Pavlinich ◽  
Xi Wei Liu ◽  
Hong Zhao ◽  
Zhen Li ◽  
Li Li
Keyword(s):  
Release Kinetics ◽  
Drug Carrier ◽  
Comparative Method ◽  
Single Layer ◽  
Drug Eluting Stent ◽  
Multiple Layer ◽  
Drug Eluting ◽  
Poly Ethylene ◽  
Surface Morphologies ◽  
Spraying Method

The Paclitaxel-eluting stents (PTX) with three-layered polymer coating were studied in this work. The PLGA (polylactic acid-co-glycolic acid) with 15 percent PEG (poly ethylene glycol) concentration in blend have been applied for preparing multiple layer drug carrier and fabricated on the surface of 316L stainless steel stents by ultrasonic atomization spraying method. The Paclitaxel was explored in doses: (~255μg) for single layer coated PTX (30 wt%), and (~275μg) for multiple layer coated PTX in accordance. Pre- and post-expansion surface morphologies of multiple layer stent were examined by scanning electron microscopy (SEM). The Paclitaxel release kinetics was studied by comparative method of release profiles of single layer PTX with 3-layered polymer coated PTX. The biocompatibility by hemolysis ratio and dynamic clotting time with platelet adhesion measurements also was investigated.

scholarly journals Poly(δ-valerolactone)/Poly(ethylene-co-vinylalcohol)/β-Tricalcium Phosphate Composite as Scaffolds: Preparation, Properties, and In Vitro Amoxicillin Release

Polymers ◽  
2020 ◽  
Vol 13 (1) ◽  
pp. 46
Author(s):  
Mohammed Badwelan ◽  
Mohammed Alkindi ◽  
Osama Alghamdi ◽  
Waseem Sharaf Saeed ◽  
Abdel-Basit Al-Odayni ◽  
...  
Keyword(s):  
Hybrid Materials ◽  
Tricalcium Phosphate ◽  
Drug Carrier ◽  
Human Mesenchymal Stem Cells ◽  
In Vitro Study ◽  
Micro Computed Tomography ◽  
Scanning Calorimetry ◽  
Sem Images ◽  
Poly Ethylene

Two poly(δ-valerolactone)/poly(ethylene-co-vinylalcohol)/β-tricalcium phosphate (PEVAL/PDVAL/β-TCP) composites containing an equal ratio of polymer and filled with 50 and 70 wt% of β-TCP microparticles were prepared by the solvent casting method. Interconnected pores were realized using the salt leached technique, and the porosity of the resulted composites was evaluated by the scanning electron microscopy (SEM) method. The homogeneity of the hybrid materials was investigated by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. The prepared materials’ SEM images showed interconnected micropores that respond to the conditions required to allow their uses as scaffolds. The porosity of each scaffold was determined from micro computed tomography (micro-CT) data, and the analysis of the mechanical properties of the prepared materials was studied through the stress-strain compressive test. The proliferation test results used human mesenchymal stem cells (MSCs) to grow and proliferate on the different types of prepared materials, reflecting that the hybrid materials were non-toxic and could be biologically acceptable scaffolds. The antibacterial activity test revealed that incorporation of amoxicillin in the specimens could inhibit the bacterial growth of S. aureus. The in vitro study of the release of amoxicillin from the PEVAL/PDVAL/amoxicillin and PEVAL/PDVAL/β-TCP/amoxicillin drug carrier systems in pH media 7.4, during eight days, gave promising results, and the antibiotic diffusion in these scaffolds obeys the Fickian model.

scholarly journals DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

2019 ◽  
Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

scholarly journals Poly(ethylene-co-vinylalcohol)/ Poly(δ-valerolactone)/Aspirin Composite: Model for a New Drug-Carrier System

Polymers ◽  
2019 ◽  
Vol 11 (3) ◽  
pp. 439 ◽  
Author(s):  
Abdulaziz Ali Alghamdi ◽  
Waseem Sharaf Saeed ◽  
Abdel-Basit Al-Odayni ◽  
Fahad A. Alharthi ◽  
Abdelhabib Semlali ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Cell Adhesion ◽  
Drug Carrier ◽  
Gastrointestinal Transit ◽  
Carrier System ◽  
Dynamic Mechanical ◽  
Degree Of Swelling ◽  
Poly Ethylene ◽  
Drug Carrier System

The release dynamics of aspirin(ASP), used as a drug model, from the poly(ethylene-co-vinyl alcohol)/poly(δ-valerolactone) (PE-co-VAL/Pδ-VL) hydrogel blend was controlled by varying the blend’s degree of swelling through a gradual loading of Pδ-VL (hydrophobic polymer) in this copolymer matrix. To achieve this goal, a series of PE-co-VAL/Pδ-VL blends with different ratios was prepared through the solvent casting method, and the miscibility of this polymer blend was evaluated by using Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and scanning electronic microscopy methods. The tests of cell adhesion and growth on the PE-co-VAL/Pδ-VL specimens were performed using the 3-(4,5-demethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method and the results obtained were the best performance in terms of cell viability, cell adhesion, and growth of the PE-co-VAL/Pδ-VL50 material. The dynamic mechanical properties of the prepared material were also examined by dynamic mechanical analysis; the results obtained showed a material having intermediary mechanical properties between those of the two components. On the basis of these characterizations, the blend showing the best performance, such as the PE-co-VAL/Pδ-VL50 system, was chosen as a carrier to study the in vitro control of the release dynamics of ASP from the ASP/PE-co-VAL/Pδ-VL drug-carrier system when administered orally, in which the influences of the ASP content and the degree of swelling of the PE-co-VAL/Pδ-VL blend were investigated. Based on the data obtained and the gastrointestinal transit time reported by Beltzer et al., it was possible to estimate the distribution of the in vitro cumulative ASP released in different digestive system organs regardless of the actions of any enzymes and microorganisms and select the best-performing drug-carrier system.

scholarly journals Polypeptides Micelles Composed of Methoxy-Poly(Ethylene Glycol)-Poly(l-Glutamic Acid)-Poly(l-Phenylalanine) Triblock Polymer for Sustained Drug Delivery

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 230 ◽  
Author(s):  
Xingzheng Liu ◽  
Rongrong Fan ◽  
Boting Lu ◽  
Yuan Le
Keyword(s):  
Drug Release ◽  
Ethylene Glycol ◽  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Poly Ethylene Glycol ◽  
Sustained Drug Release ◽  
Poly Ethylene ◽  
Triblock Polymers

Methoxy-poly(ethylene glycol)-poly(l-glutamic acid)-poly(l-phenylalanine) triblock polymers with different architecture were synthesized as drug carrier to obtain sustained and controlled release by tuning the composition. These triblock polymers were prepared by ring opening polymerization and poly(ethylene glycol) was used as an initiator. Polymerization was confirmed by 1H NMR, FT-IR and gel penetration chromatography. The polymers can self-assemble to form micelles in aqueous medium and their critical micelle concentrations values were examined. The micelles were spherical shape with size of 50–100 nm and especially can arranged in a regular manner. Sorafenib was selected as the model drug and the drug loading performance was dependent on the composition of the block copolymer. In vitro drug release indicated that the polymers can realize controlled and sustained drug release. Furthermore, in vitro cytotoxicity assay showed that the polymers were biocompatible and the drug-loaded micelles can increase toxicity towards tumor cells. Confocal fluorescence microscopy assays illustrated that the micelles can be uptaken quickly and release drug persistently to inhibit tumor cell growth.

scholarly journals Temperature-Responsive Molecular Assemblies Using Oligo(Ethylene Glycol)-Attached Polyamidoamine Dendron Lipids and their Functions as Drug Carriers

2020 ◽  
Vol 11 (1) ◽  
pp. 16
Author(s):  
Takuya Hashimoto ◽  
Yuji Hirai ◽  
Eiji Yuba ◽  
Atsushi Harada ◽  
Kenji Kono
Keyword(s):  
Ethylene Glycol ◽  
Drug Carrier ◽  
Drug Carriers ◽  
Head Group ◽  
Stimuli Responsive ◽  
Alkyl Chains ◽  
Temperature Responsive ◽  
Poly Ethylene ◽  
External Stimuli

Temperature-responsive nanocarrier systems using external stimuli are one of the most widely investigated stimuli-responsive strategies because heat is easy and safe to use for hyperthermia and controlled drug delivery. Polyamidoamine dendron lipids (PAMAM-DLs) composed of PAMAM dendron as head group and two alkyl chains can exhibit temperature-responsive morphological change through the attachment of suitable moieties to terminal of PAMAM dendron. In this study, oligo(ethylene glycol)s including ethoxy- or methoxy-diethylene glycols were attached to the terminals of PAMAM-DL, and temperature-responsive properties of their self-assemblies were evaluated by calorimetric and turbidity measurements. In the evaluation of temperature-responsive properties, ethoxy diethylene glycol (EDEG)-attached PAMAM-DL composed of two saturated alkyl chains and PAMAM dendron with 1st generation had lipid bilayer structure and suitable cloud point for the application as drug carrier. In vitro performances of the assemblies combining EDEG-attached PAMAM-DLs with cholesteryl-oxy-poly(ethylene glycol) (PEG-Chol) was evaluated using doxorubicin (DOX) as an anticancer drug. Cellular uptake of DOX-loaded EDEG-attached PAMAM-DL/PEG-Chol assemblies was promoted at 42 °C rather than 37 °C, resulting in an effective decrease in cell viability.

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 Fabrication of Quaternized Chitosan Nanoparticles Using Tripolyphosphate/Genipin Dual Cross-Linkers as a Protein Delivery System

Polymers ◽  
2018 ◽  
Vol 10 (11) ◽  
pp. 1226 ◽  
Author(s):  
Kuo-Yu Chen ◽  
Si-Ying Zeng
Keyword(s):  
Protein Delivery ◽  
Drug Carrier ◽  
Chitosan Nanoparticles ◽  
Weight Ratio ◽  
Water Soluble ◽  
Trimethylammonium Chloride ◽  
Sustained Delivery ◽  
Release Studies ◽  
Predicted Values

Various amounts of 2-((acryloyloxy)ethyl)trimethylammonium chloride were grafted onto chitosan (CS) via redox polymerization method to obtain water-soluble quaternized CS (QCS). The QCS nanoparticles loaded with bovine serum albumin (BSA) were then produced by ionic gelation with tripolyphosphate (TPP) and further covalently cross-linked with genipin. The formation of QCS nanoparticles was optimized as a function of monomer grafting yield, QCS/TPP weight ratio, and QCS/genipin weight ratio by Box-Behnken design and response surface methodology. The results showed that QCS nanoparticles prepared with a grafting yield of 50%, QCS/TPP weight ratio of 7.67, and QCS/genipin weight ratio of 60 had a particle size of 193.68 ± 44.92 nm, polydispersity of 0.232, zeta potential of +23.97 mV and BSA encapsulation efficiency of 46.37 ± 2.89%, which were close to the predicted values from mathematical models. In vitro drug release studies at pH 1.2 and pH 7.4 exhibited that the release rate of BSA was significantly decreased and the release period was significantly prolonged after QCS nanoparticles cross-linking with genipin. Therefore, QCS nanoparticles cross-linked with TPP/genipin dual cross-linkers may be a promising protein drug carrier for a prolonged and sustained delivery.

SYNTHESIS AND CHARACTERIZATION OF POLYSIALIC ACID-N-TRIMETHYL CHITOSAN NANOPARTICLES FOR DRUG DELIVERY

Nano LIFE ◽  
2012 ◽  
Vol 02 (03) ◽  
pp. 1241003 ◽  
Author(s):  
NAN ZHANG ◽  
REBECCA A. BADER
Keyword(s):  
Drug Delivery ◽  
Sodium Tripolyphosphate ◽  
Drug Carrier ◽  
Polysialic Acid ◽  
Chitosan Nanoparticles ◽  
Weight Ratio ◽  
Reticuloendothelial System ◽  
Optimal Size ◽  
Passive Targeting ◽  
Poly Ethylene

In drug delivery, the nanoparticles must be of proper size and charge to achieve high efficacy and low toxicity of associated therapeutics. In this study, nanoparticles were developed via ionic gelation of two polysaccharide-based molecules, negatively charged polysialic acid (PSA) and positively charged N,N,N-trimethylchitosan (TMC). PSA is unique in that the highly hydrated backbone may be used in a manner similar to that of poly(ethylene glycol) to extend circulation times. Although not necessary for nanoparticle formation, sodium tripolyphosphate (TPP) was added to enhance stability, as indicated by a reduced polydispersity. We investigated three different ratios by weight of PSA:TMC (0.5:1, 1:1, 1:2 and five different TPP concentrations ranging from 0.1 mg/ml to 0.8 mg/ml. As controls, nanoparticles were also formed without PSA from chitosan and TMC with TPP. Optimal size and surface charge were achieved with a PSA:TMC weight ratio of 0.5:1 and a TPP concentration 0.2 mg/ml. For the nanoparticles prepared in the latter fashion, a more in depth characterization was conducted. The nanoparticles were distinct solid, spherical nanogels with a size of 106 ± 25 nm, an ideal size to reduce uptake by the reticuloendothelial system while facilitating passive targeting of diseased tissue. The zeta potential of the nanoparticles was +33.9 ± 1.2 mV, suggesting that the nanoparticles will be stable under physiological conditions. Encapsulation and controlled release by the nanoparticles was demonstrated using methotrexate, a therapeutic indicated in both cancer and rheumatoid arthritis. The results obtained thus far strongly indicate that PSA–TMC nanoparticles are suitable drug carrier systems for systemic administration.

scholarly journals Improved Dissolution Rate and Intestinal Absorption of Fexofenadine Hydrochloride by the Preparation of Solid Dispersions: In Vitro and In Situ Evaluation

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 310
Author(s):  
Basanth Babu Eedara ◽  
Dinesh Nyavanandi ◽  
Sagar Narala ◽  
Prabhakar Reddy Veerareddy ◽  
Suresh Bandari
Keyword(s):  
Intestinal Absorption ◽  
Carrier Concentration ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Linear Increase ◽  
Phase Solubility ◽  
Poloxamer 188 ◽  
Time Required

The objective of this study was to enhance dissolution and permeation of a low soluble, absorbable fexofenadine hydrochloride (FFH) by preparing solid dispersions using polyethylene glycol 20,000 (PEG 20,000) and poloxamer 188 as carriers. The phase solubility measurement for the supplied FFH revealed a linear increase in the solubility of fexofenadine with increasing carrier concentration in water (1.45 mg/mL to 11.78 mg/mL with 0% w/v to 30% w/v PEG 20,000; 1.45 mg/mL to 12.27 mg/mL with 0% w/v to 30% w/v poloxamer 188). To select the appropriate drug carrier concentration, a series of solid dispersions were prepared in the drug carrier weight ratios of 1:1, 1:2 and 1:4 by fusion method. The solid dispersions composed of drug carrier at 1:4 weight ratio showed highest dissolution with the time required for the release of 50% of the drug <15 min compared to the supplied FFH (>120 min). The intestinal absorption study presented a significant improvement in the absorption of drug from the solid dispersions composed of poloxamer 188 than PEG 20,000. In summary, the solid dispersions of FFH prepared using PEG 20,000 and poloxamer 188 demonstrated improved dissolution and absorption than supplied FFH and could be used to improve the oral bioavailability of fexofenadine.

Sign in / Sign up

Export Citation Format

Share Document