scholarly journals Assessment of a mathematical model considering the effect of flow rate on in-vitro drug-release from PLGA films

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.

Author(s):  
Pravin S Patil ◽  
Shashikant C Dhawale

 Objective: The purpose of the present investigation was to develop a nanosuspension to improve dissolution rate and oral bioavailability of ritonavir.Methods: Extended-release ritonavir loaded nanoparticles were prepared using the polymeric system by nanoprecipitation technique. Further, the effect of Eudragit RL100 (polymeric matrix) and polyvinyl alcohol (surfactant) was investigated on particle size and distribution, drug content, entrapment efficiency, and in vitro drug release from nanosuspension where a strong influence of polymeric contents was observed. Drug-excipient compatibility and amorphous nature of drug in prepared nanoparticles were confirmed by Fourier transform infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffraction studies, respectively.Results: Hydrophobic portions of Eudragit RL100 could result in enhanced encapsulation efficiency. However, increase in polymer and surfactant contents lead to enlarged particle size proportionately as confirmed by transmission electron microscopy. Nanosuspension showed a significant rise in dissolution rate with complete in vitro drug release as well as higher bioavailability in rats compared to the pure drug.Conclusion: The nanoprecipitation technique used in present research could be further explored for the development of different antiretroviral drug carrier therapeutics.


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.


2014 ◽  
Vol 136 (11) ◽  
Author(s):  
Xiaoxiang Zhu ◽  
Richard D. Braatz

Increasing interests have been raised toward the potential applications of biodegradable poly(lactic-co-glycolic acid) (PLGA) coatings for drug-eluting stents in order to improve the drug delivery and reduce adverse outcomes in stented arteries in patients. This article presents a mathematical model to describe the integrated processes of drug release in a stent with PLGA coating and subsequent drug delivery, distribution, and drug pharmacokinetics in the arterial wall. The integrated model takes into account the PLGA degradation and erosion, anisotropic drug diffusion in the arterial wall, and reversible drug binding. The model simulations first compare the drug delivery from a biodegradable PLGA coating with that from a biodurable coating, including the drug release profiles in the coating, average arterial drug levels, and arterial drug distribution. Using the model for the PLGA stent coating, the simulations further investigate drug internalization, interstitial fluid flow in the arterial wall, and stent embedment for their impact on drug delivery. Simulation results show that these three factors, while imposing little change in the drug release profiles, can greatly change the average drug concentrations in the arterial wall. In particular, each of the factors leads to significant and yet distinguished alterations in the arterial drug distribution that can potentially influence the treatment outcomes. The detailed integrated model provides insights into the design and evaluation of biodegradable PLGA-coated drug-eluting stents for improved intravascular drug delivery.


2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Tulsi Sagar Sheth ◽  
Falguni Acharya

AbstractThe objective of this article is to optimize the similarity factor within immediate release (IR) and modified release (MR) of in vitro drug release profiles. The least square method is used to minimize the difference between empirical and regression curve fitting data of in vitro IR/MR drug release profiles. An estimation of percentage drug release at intermediate timepoints has been done to improve the similarity factor $f_{2}$ f 2 using linear curve fit method. In this study linear regression model is used to analyze the similarity factor $f_{2}$ f 2 for Nitrofurantoin MR Capsules, Venlafaxine HCl MR Tablets and Lurasidone IR Tablets in order to exhibit the significance as well as similarity owing to the consideration of extra intervening timepoints. This linear regression model may help pharmaceutical industries to examine the inside comparison of IR/MR in vitro drug release profile with few modifications in timepoint selection to improve similarity factor $f_{2}$ f 2 .


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