scholarly journals Development of a Model Based on Physical Mechanisms for the Explanation of Drug Release: Application to Diclofenac Release from Polyurethane Films

Polymers ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1230
Author(s):  
Navideh Abbasnezhad ◽  
Mohamed Kebdani ◽  
Mohammadali Shirinbayan ◽  
Stéphane Champmartin ◽  
Abbas Tcharkhtchi ◽  
...  

In this study, we present a method for prediction of the drug-release profile based on the physical mechanisms that can intervene in drug release from a drug-carrier. The application presented here incorporates the effects of drug concentration and Reynolds number defining the circulating flow in the testing vein. The experimental data used relate to the release of diclofenac from samples of non-degradable polyurethane subjected to static and continuous flow. This case includes simultaneously three mechanisms: burst-release, diffusion and osmotic pressure, identified beforehand here as being able to contribute to the drug liberation. For this purpose, authors coded the Sequential Quadratic Programming Algorithm to solve the problem of non-linear optimization. The experimental data used to develop the mathematical model obtained from release studies carried out in water solution at 37 °C, for three concentrations of diclofenac and two water flow rates. We discuss the contribution of mechanisms and kinetics by considering two aforementioned parameters and, following that, we obtain the specific-model and compare the calculated results with the experimental results for the reserved cases. The results showed that drug percentage mostly affect the burst release, however flow rate has affected the osmotic release. In addition, release kinetics of all the mechanisms have increased by increasing the values of two considered parameters.

2006 ◽  
Vol 6 (9) ◽  
pp. 2929-2935 ◽  
Author(s):  
Tse-Ying Liu ◽  
Ting-Yu Liu ◽  
San-Yuan Chen ◽  
Shian-Chuan Chen ◽  
Dean-Mo Liu

In order to explore the effect of nanofiller on the regulation of the drug release behavior from microsphere-embedded hydrogel prepared by carboxymethyl-hexanoyl chitosan (HNOCC) and O-hexanoyl chitosan (OHC), the release kinetics was investigated in terms of various amounts of calcium-deficient hydroxyapatite (CDHA) nanoparticles incorporated. HNOCC is a novel chitosan-based hydrophilic matrix with a burst release profile in a highly swollen state. The drug release kinetics of the HNOCC hydrogel can be regulated by incorporation of well-dispersed CDHA nanoparticles. It was found that the release duration of ibuprofen (IBU) from HNOCC was prolonged with increasing amounts of CDHA which acts as a crosslink agent and diffusion barrier. On the contrary, the release duration of the IBU from OHC (hydrophobic phase) was shortened through increasing the CDHA amount over 5%, which is due to the hydrophilic nature of the CDHA nanoparticles destroying the intermolecular hydrophobic interaction and accelerating OHC degradation. Thus, water accessibility and molecular relaxation were enhanced, resulting in a higher release rate. In addition, sustained and sequential release behavior was achieved by embedding the OHC microspheres (hydrophobic phase) into the HNOCC (hydrophilic phase) matrix, which could significantly prolong the release duration of the HNOCC drug-loaded implant.


Author(s):  
J. I. Ordu ◽  
I. E. Udenze

Micro crystalline cellulose (MCC) is a major derivative from the bio composite of natural materials such as D. arborea plant stem. It could be useful as a secondary binder and disintegrant in tablet formulation especially following direct compression technique anticipating it to provide high level of disintegration at low use level and utilizing dual mechanisms of wicking and swelling. Tablets of aceclofenac a BCS class II and non steroidal anti inflammatory drug (NSAID) which potently inhibits the cyclo oxygenase enzyme (COX-2) involved in prostaglandin synthesis was formulated by direct compression using MCC from D. arborea stem. Qualitative assessment of the plant extract was carried out and the presence of cellulose confirmed by the appearance of violet – blue coloration while the physicochemical and physicotechnical properties were comparatively evaluated with reference to avicel and corn starch. Three batches of aceclofenac tablets involving Batch A (D. arborea MCC), Batch B (Corn starch) and Batch C (Corn starch and D. arborea MCC in a 1:1 ratio), were implcated in the formulation. Physicochemical study of the MCC reveals a pH of 7.8, mean swelling index 1.14±0.05 ml and hydration capacity of 3.60±0.15 g while the pH of corn starch is 3.90 with swelling and hydration capacity at 5.09±0.03 ml and 8.26±0.01 g respectively. Quality control evaluation of resulting tablet was investigated and the wetting time of batch A tablets was 1.50, batch B 2.30 and batch C 1.80 with percentage moisture content (%) of 60.5, 56.56 and 57.8 and disintegration time (minutes) of 0.22±0.07, 0.35±0.051 and 1.60±0.286 respectively. The drug release profile of batch A, reveals an initial burst release within 10 minutes followed by gradual release while batch C had consistent drug release which was maintained although faster than that of batch A after 10 minutes but batch B had the least drug release rate.


2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Takashi Sasaki ◽  
Hiroaki Matsuura ◽  
Kazuki Tanaka

Porous polymer spheres are promising materials as carriers for controlled drug release. As a new drug-carrier material, blend particles composed of poly(L-lactic acid) (PLLA) and rifampicin were developed using the freeze-drying technique. The blend particles exhibit high porosity with a specific surface area of 10–40 m2 g−1. Both the size and porosity of the particles depend on the concentration of the original solution and on the method of freezing. With respect to the latter, we used the drop method (pouring the original solution dropwise into liquid nitrogen) and the spray method (freezing a mist of the original solution). The release kinetics of rifampicin from the blend particles into water depends significantly on the morphology of the blend particles. The results show that the release rate can be controlled to a great extent by tuning the size and porosity of the blend particles, both of which are varied by parameters such as the solution concentration and the method of freezing.


2014 ◽  
Vol 894 ◽  
pp. 364-368 ◽  
Author(s):  
Ahmed Hassanin ◽  
Ahmed A. El-Moneim ◽  
Mohamed Ghaniem ◽  
Hassan Nageh

Building on the success of the many earlier studies on electrospun nanofibers technique which provide a non woven web to the order of nanometers introducing superior properties such as large surface area, superior mechanical properties and ease of implementation in many fields of applications, elctrospun nanofibers became an important issue for many researchers in various fields. Using elctrospun fibers as a drug carrier, is showing a huge promising potential for the future of biomedical application. Our work in this research is focusing on engineering a system to control the drug release profile rate especially for wound dressing. Nanocomposite multilayer fibrous membranes, using electrospinning method, have been developed for drug release in form of sandwich structure of three layers. Inner layer which is kept Polycaprolactane (PCL) loaded with drug. The two outer layers have been changed with different blend ratios between Chitosan (Cs) and PCL as follow [0%:100% Cs:PCL, 30%:70% Cs:PCL, 50%:50% Cs:PCL, 70%:30% Cs:PCL]. The results showed that the release rate has been affected dramatically by the outer layer composition. SEM images showed changing in the morphology due to the different in the composition of outer layer.


RSC Advances ◽  
2016 ◽  
Vol 6 (23) ◽  
pp. 19060-19068 ◽  
Author(s):  
Elisangela P. da Silva ◽  
Marcos R. Guilherme ◽  
Francielle P. Garcia ◽  
Celso V. Nakamura ◽  
Lucio Cardozo-Filho ◽  
...  

Hydrogel nanocomposites of pectin, HEMA and titania for Vit-B12 controlled release with reduced initial release burst were prepared. A reduction of up to ca. 60% was observed.


2019 ◽  
Vol 9 (1) ◽  
pp. 38-45 ◽  
Author(s):  
Santoshi Naik ◽  
Prasiddhi Raikar ◽  
Mohammed Gulzar Ahmed

In the present study an attempt has been made to formulate and evaluate a sustained release periodontal film of Sparfloxacin with biodegradable, cost effective polymer Chitosan. The objective of the study was to formulate intra-pocket periodontal films, which could be easily placed into the periodontal pocket, and thus be capable of delivering therapeutic concentrations of drug. Sparfloxacin is an antibiotic, showing wide spectrum antibacterial activity against a number of periodontal pathogens. Hence Sparfloxacin is selected as model for site specific delivery, i.e., into periodontal pocket for the treatment of periodontitis. In the present investigation Chitosan films containing Sparfloxacin were prepared by solution casting method using acetic acid. The copolymers HPMC K4M, Sodium CMC and Eudragit RL 100 in the concentrations of 10%, 20% and 30% w/w of Chitosan were added into the polymeric solution. Propylene glycol was used as plasticizer. FT-IR and UV spectroscopic methods revealed no interaction between Sparfloxacin and polymers. The drug loaded films were evaluated for their thickness, weight variation, content uniformity, tensile strength, percent elongation, percentage moisture loss, surface pH, folding endurance, in- vitro drug release studies, in - vitro antibacterial activity and stability studies. Periodontal films showed initial burst release of drug on 1st day and then the release was sustained for a period of 8 days. In – vitro antibacterial activity was carried out on staphylococcus aureus and the antibacterial activity was retained for 96 hours. In - vitro release from periodontal films was fit to kinetic models to reveal drug release kinetics. Keywords: Periodontitis, Sparfloxacin, Bio-adhesive polymers.


Author(s):  
Adil Patel ◽  
Ami Kalsariya ◽  
Srushti Patel ◽  
Chandni Patel ◽  
Shreya Patel

The aim of present work is to determine and analyse the kinetics of drug release from the fast dissolving sublingual by employing various mathematical models. A study was done with Cyanocobalamine fast dissolving sublingual films, 1.5 mg/film by employing solvent casting technique using dehydrated banana starch and Gelatin. The in-vitro drug release profile was carried out in pH 6.8 phosphate buffer (900 mL) using USP dissolution apparatus I (Basket) at 50 rpm for 20 mins. The drug release data was obtained, quantitatively correlated and interpreted with various mathematical models viz. Zero order model, first order model, Higuchi model, Hixson-Crowell model and Korsmeyer-Peppas model and evaluated to understand the kinetics of drug release. The criterion for the most suitable model was based on the high degree of coefficient of correlation of drug release profile of Cyanocobalamine fast dissolving sublingual films.


Materials ◽  
2021 ◽  
Vol 14 (20) ◽  
pp. 6142
Author(s):  
Bożena Łosiewicz ◽  
Agnieszka Stróż ◽  
Patrycja Osak ◽  
Joanna Maszybrocka ◽  
Anna Gerle ◽  
...  

This work concerns the development of a method of functionalization of the surface of the biomedical Ti–6Al–7Nb alloy by producing oxide nanotubes (ONTs) with drug-eluting properties. Shaping of the morphology, microstructure, and thickness of the oxide layer was carried out by anodization in an aqueous solution of 1 M ethylene glycol with the addition of 0.2 M NH4F in the voltage range 5–100 V for 15–60 min at room temperature. The characterization of the physicochemical properties of the obtained ONTs was performed using SEM, XPS, and EDAX methods. ONTs have been shown to be composed mainly of TiO2, Al2O3, and Nb2O5. Single-walled ONTs with the largest specific surface area of 600 cm2 cm−2 can be obtained by anodization at 50 V for 60 min. The mechanism of ONT formation on the Ti–6Al–7Nb alloy was studied in detail. Gentamicin sulfate loaded into ONTs was studied using FTIR, TG, DTA, and DTG methods. Drug release kinetics was determined by UV–Vis spectrophotometry. The obtained ONTs can be proposed for use in modern implantology as carriers for drugs delivered locally in inflammatory conditions.


Author(s):  
Maher Amer ◽  
Roland K. Chen

Abstract Microneedles (MNs) provide a minimally invasive alternative to intravitreal injections and a promising means to sustainable ocular drug delivery. To optimize the sustained drug release profile and to ease the administration of the MN array to the eye, the number of MNs in an MN array and their layout need to be carefully selected. In this study, the drug release kinetics of MN arrays with varying numbers of MNs (8, 12, and 16) is studied over a four-week period. The MN arrays show a much more uniform drug release profile than the single injections. Only the 16-needle MN array fully released all the amount of loaded drug at the end of the 4-week period. Both 8- and 12-needle arrays showed a steady release rate over the 4-week period, which is the longest sustained release duration that has been reported. Zero-order models are created to predict drug release profiles for the three MN arrays. It is estimated that the MN array with 8 needles can deliver the drug for up to 6 weeks. The models can be used to design MN arrays with a given targeted therapeutic index for sustained drug delivery.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 719
Author(s):  
Sara Bom ◽  
Catarina Santos ◽  
Rita Barros ◽  
Ana M. Martins ◽  
Patrizia Paradiso ◽  
...  

The development of printable hydrogel inks for extrusion-based 3D printing is opening new possibilities to the production of new and/or improved pharmaceutical forms, specifically for topical application. Alginate and starch are natural polysaccharides that have been extensively exploited due to their biocompatibility, biodegradability, viscosity properties, low toxicity, and relatively low cost. This research work aimed to study the physicochemical and release kinetic effects of starch incorporation in alginate-based 3D hydrogel patches for topical delivery using a quality by design approach. The incorporation of a pregelatinized starch is also proposed as a way to improve the properties of the drug delivery system while maintaining the desired quality characteristics. Critical material attributes and process parameters were identified, and the sensitivity and adequacy of each parameter were statistically analyzed. The impact of alginate, starch, and CaCl2·2H2O amounts on relevant quality attributes was estimated crosswise. The amount of starch revealed a synergetic impact on porosity (p = 0.0021). An evident increase in the size and quantity of open pores were detected in the as printed patches as well as after crosslinking (15.6 ± 5.2 µm). In vitro drug release studies from the optimized alginate-starch 3D hydrogel patch, using the probe Rhodamine B, showed an initial high burst release, followed by a controlled release mechanism. The results obtained also showed that the viscoelastic properties, printing accuracy, gelation time, microstructure, and release rates can be modulated by varying the amount of starch added to the system. Furthermore, these results can be considered an excellent baseline for future drug release modulation strategies.


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