scholarly journals Synthesis and Appraisal of Natural Drug-Polymer-Based Matrices Relevant to the Application of Drug-Eluting Coronary Stent Coatings

2020 ◽  
Vol 2020 ◽  
pp. 1-11
Author(s):  
Bakhtawar Ghafoor ◽  
Murtaza Najabat Ali ◽  
Zainab Riaz

Cardiovascular diseases are becoming a leading cause of death in the world, and attention is being paid to develop natural drug-based treatment to cure heart diseases. Curcumin, ginger, and magnolol are pharmaceutically active in many ways, having properties including anticoagulation, antiproliferation, anti-inflammatory, and antioxidant, and may be used to synthesis coatings for drug-eluting stents to treat cardiovascular diseases. In the present investigation, a degradable polymer with varying molecular weights was used as a drug carrier to control the degradation of polymer; three different natural drugs such as curcumin, magnolol, and ginger were used owing to their reported pharmacological properties. The results of in vitro measurements of all three natural drugs released from drug-loaded polymeric films showed an initial burst release followed by a sustained release for up to 38 days of measurement. On the other hand, different levels of hemocompatibility were observed by varying concentrations of natural drugs in human erythrocytes. As per the ASTM F756 standard, ginger having low concentration showed optimum hemocompatibility with regard to the drug-eluting stent application as compared with magnolol and curcumin concentrations, which showed suboptimal hemocompatibility and fall in the range of mild-to-severe blood toxicity category. The structure of the coating films was characterized by Fourier transform infrared (FTIR) spectroscopy and scanning electron microscopy (SEM) with results suggesting that there was no chemical bonding between the polymer and drug. Thus, according to this study, it can be concluded that after more detailed in vitro testing such as hemocompatibility tests and platelet adhesion testing, ginger can be a better candidate as a drug-coating material for drug-eluting stent applications.

Author(s):  
Анна Игоревна Простякова ◽  
Дмитрий Игоревич Зыбин ◽  
Дмитрий Валерьевич Капустин

Изучение профиля выделения лекарственного средства in vitro — необходимый этап при оптимизации полимерно-лекарственной композиции в процессе разработки стентов, выделяющих лекарственное вещество (ЛВ). В статье представлены результаты ВЭЖХ-анализа содержания ЛВ и кинетики его выделения из различных типов полимерно-лекарственного покрытия выделяющих ЛВ коронарных стентов (drug eluting stent — DES): биодеградируемого покрытия с сиролимусом и стабильного покрытия с зотаролимусом. Содержание ЛВ оценивали для кримпированных стентов на системе доставки, а также после раскрытия. Продемонстрирована связь морфологии лекарственного покрытия с кинетикой выделения ЛВ и показано, что крупные морфологические дефекты покрытия приводят к отклонению параметров выделения ЛВ.


2021 ◽  
Vol 321 ◽  
pp. 04011
Author(s):  
Navideh Abbasnezhad ◽  
Farid Bakir ◽  
Stéphane Champmartin ◽  
Mohammadali Shirinbayan

Drug-eluting stents implanted in blood vessels are subject to various dynamics of blood flow. In this study, we present the evaluation of a mathematical model considering the effect of flow rate, to simulate the kinetic profiles of drug release (Diclofenac Sodium (DS)) from in-vitro from PLGA films. This model solves a set of non-linear equation for modeling simultaneously the burst, diffusion, swelling and erosion involved in the mechanisms of liberation. The release parameters depending on the flow rate are determined using the corresponding mathematical equations. For the evaluation of the proposed model, test data obtained in our laboratory are used. To quantify DS release from drug-carrier PLGA films, we used the flow-through cell apparatus in a closed-loop. Four flow rate values are applied. For each value, the model-substance liberation kinetics showed an increase in drug released with the flow rate. The simulated release profiles show good agreement with the experimental results. Therefore, the use of this model could provide a practical tool to assess in-vitro drug release profiles from polymer matrices under continuous flow rate constraint, and could help improve the design of drug eluting stents.


2019 ◽  
Vol 303 ◽  
pp. 151-161 ◽  
Author(s):  
Craig M. McKittrick ◽  
Sean McKee ◽  
Simon Kennedy ◽  
Keith Oldroyd ◽  
Marcus Wheel ◽  
...  

2018 ◽  
Vol 33 (3) ◽  
pp. 352-362 ◽  
Author(s):  
Tarek M Bedair ◽  
Il Jae Min ◽  
Wooram Park ◽  
Yoon Ki Joung ◽  
Dong Keun Han

Polymer-based drug-eluting stents (DESs) represented attractive application for the treatment of cardiovascular diseases; however, polymer coating has caused serious adverse responses to tissues such as chronic inflammation due to acidic by-products. Therefore, polymer-free DESs have recently emerged as promising candidates for the treatment; however, burst release of drug(s) from the surface limited its applications. In this study, we focused on delivery of therapeutic drug from polymer-free (or -less) DESs through surface modification using cobalt oxide nanowires (Co3O4 NWs) to improve and control the drug release. The results demonstrated that Co3O4 NWs could be simply fabricated on cobalt–chromium substrate by ammonia-evaporation-induced method. The Co3O4 NWs were uniformly arrayed with diameters of 50–100 nm and lengths of 10 µm. It was found that Co3O4 NWs were comparatively stable without any delamination or change of the morphology under in vitro long-term stability using circulating system. Sirolimus was used as a model drug for studying in vitro release behavior under physiological conditions. The sirolimus release behavior from flat cobalt–chromium showed an initial burst (over 90%) after one day. On the other hand, Co3O4 NWs presented a sustained sirolimus release rate for up to seven days. Similarly, the polymer-less specimens on Co3O4 NWs substrates sustained sirolimus release for a longer-period of time when compared to flat Co–Cr substrates. In summary, the current approach of using Co3O4 NWs-based substrates might have a great potential to sustain drug release for drug-eluting implants and medical devices including stents.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (6) ◽  
pp. 500
Author(s):  
Agnieszka Lis-Cieplak ◽  
Filip Charuk ◽  
Marcin Sobczak ◽  
Anna Zgadzaj ◽  
Agata Drobniewska ◽  
...  

Polymer-drug conjugates are currently being more widely investigated for the treatment of hypertension. In view of the above, in the first stage of our work, we used nontoxic β-cyclodextrin (β-CD) as effective, simple, inexpensive, and safe for the human body initiator for the synthesis of biocompatible and biodegradable functionalized polymers suitable for the medical and pharmaceutical applications. The obtained polymeric products were synthesized through a ring-opening polymerization (ROP) of ε-caprolactone (CL), d,l-, and l,l-lactide (LA and LLA). The chemical structures of synthesized materials were elucidated based on 1H NMR and solid-state carbon-13 cross-polarization/magic angle spinning nuclear magnetic resonance (13C CP/MAS NMR) analysis, while the incorporation of β-CD molecule into the polymer chain was confirmed by matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS). Furthermore, molecular modeling has been applied to investigate the intrachain rigidities and chain architectures for several representative structures. The obtained and thoroughly characterized branched matrices were then used to generate the first β-cyclodextrin/biodegradable polymer/β-blocker conjugate through the successful conjugation of pindolol. The conjugates were fabricated by carbodiimide-mediated coupling reaction. The branched biodegradable materials released the drug in vitro in a sustained manner and without “burst release” and thus have the ability to treat different heart diseases.


2010 ◽  
Vol 21 (4) ◽  
pp. 529-552 ◽  
Author(s):  
Nathan A. Lockwood ◽  
Robert W. Hergenrother ◽  
Laura M. Patrick ◽  
Sean M. Stucke ◽  
Rob Steendam ◽  
...  

2012 ◽  
Vol 40 (12) ◽  
pp. 2697-2697
Author(s):  
Caroline C. O’Brien ◽  
Charles H. Finch ◽  
Tracie J. Barber ◽  
Penny Martens ◽  
Anne Simmons

2013 ◽  
Vol 644 ◽  
pp. 183-188
Author(s):  
Sergey Pavlinich ◽  
Xi Wei Liu ◽  
Hong Zhao ◽  
Zhen Li ◽  
Li Li

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.


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