Drug release profile and reduction in the in vitro burst release from pectin/HEMA hydrogel nanocomposites crosslinked with titania

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 ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Profile ◽  
Burst Release ◽  
Drug Release Profile ◽  
Initial Release ◽  
Hydrogel Nanocomposites

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.

DEVELOPMENT AND CHARACTERIZATION OF MUCOADHESIVE PATCHES OF NICERGOLINE FOR BUCCAL DRUG DELIVERY BY USING FACTORIAL DESIGN OF EXPERIMENT (DOE)

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (07) ◽  
pp. 52-57
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Design Of Experiment ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Drug Content ◽  
Release Study

The aim of this research was to develop mucoadhesive buccal patches of nicergoline by using Factorial Design of Experiment, in order to provide a sustained release of drug into the systemic circulation. A 33 factorial experimental design was employed for optimization and to study the effect of formulation variables on responses R1 (% swelling index), R2 (% drug content), R3 (mucoadhesion time) and R4 (mucoadhesion strength). In vitro drug release study was performed on the optimized formulations. All the prepared formulations had good mechanical strength, mucoadhesion strength, neutral surface pH and drug content up to 98.17%. In vitro drug release study revealed that F-5 formulation showed promising sustained drug release profile (98.21%) for over 8 h and could be a potential substitute for marketed conventional formulations. The developed formulation (F5) was found to be optimized with considerably good stability and extended drug release profile.

scholarly journals Preparation of Biodegradable Silk Fibroin/Alginate Blend Films for Controlled Release of Antimicrobial Drugs

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Yaowalak Srisuwan ◽  
Yodthong Baimark
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Silk Fibroin ◽  
Water Soluble ◽  
Drug Release Profile ◽  
Sem Images ◽  
Blend Ratio ◽  
Blend Films ◽  
Vis Spectroscopy

Silk fibroin (SF)/alginate blend films have been prepared for controlled release of tetracycline hydrochloride, an antimicrobial model drug. The blend films were analysed by Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and UV-vis spectroscopy. The functional groups of the SF/alginate blends were monitored from their FTIR spectra. The homogeneity of the blend films was observed from SEM images. The dissolution and film transparency of the blend films depended on the SF/alginate blend ratio. Thein vitrodrug release profile of the blend films was determined by plotting the cumulative drug release versus time. It was found that the drug release significantly decreased as the SF/alginate blend ratio increased. The results demonstrated that the SF/alginate blend films should be a useful controlled-release delivery system for water-soluble drugs.

A Novel Biodegradable Multichamber Microstructure for Implantable Drug Controlled Release

2010 ◽  
Vol 654-656 ◽  
pp. 2269-2272
Author(s):  
Rui Xia Yu ◽  
Xiang Yang Zhou ◽  
Zeng Zhao
Keyword(s):  
Topology Optimization ◽  
Controlled Release ◽  
Drug Release ◽  
Research Work ◽  
Release Profile ◽  
Drug Release Profile ◽  
Drug Controlled Release ◽  
Simulation Results ◽  
Micro Molding

The research work reported in this paper design a novel biodegradable multichamber microstructure for implantable drug controlled release by introducing the approach of topology optimization. It is therefore highly desirable to overcome these restrictions that pre-defined topology of the device result in difficulty to obtain a linear or pulsed drug release profile. The designed biodegradable multichamber microstructure is fabricated using UV-LIGA microfabrication and Micro-molding technique. The simulation results show that the multichamber microstructure exhibits a preferable linear drug release profile.

scholarly journals Application of Mathematical Models in Drug Release Kinetics of Cyanocobalamine Fast Dissolving Sublingual Film

2021 ◽  
pp. 72-81
Author(s):  
Adil Patel ◽  
Ami Kalsariya ◽  
Srushti Patel ◽  
Chandni Patel ◽  
Shreya Patel
Keyword(s):  
Drug Release ◽  
Mathematical Models ◽  
Release Kinetics ◽  
Release Profile ◽  
Suitable Model ◽  
Order Model ◽  
Drug Release Profile ◽  
Casting Technique ◽  
Kinetics Of

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.

scholarly journals Formulation and Evaluation of Colchicine Sustained release tablet by using factorial designs

2021 ◽  
Vol 11 (5-S) ◽  
pp. 100-107
Author(s):  
M. Pradeep Kumar ◽  
Goparaju Suryanarayana Murthy ◽  
Annamdasu Lakshmi Poojitha ◽  
P. Sindhuri ◽  
A Sreekanth ◽  
...  
Keyword(s):  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Release Profile ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Similarity Factor ◽  
Time Required ◽  
Full Factorial

The study on the effect of polymer concentration on in vitro drug release profile revealed that there is a change in vitro drug release parameters (t50, t80, and MDT) with a change in polymer concentration. Fraction of HPMC K4M, HPMC K 100 M, and Ethyl Cellulose were required to be 15, 10, and 7 mg respectively for designing optimized batch F7. The release rate of Colchicine decreased proportionally with an increase in the concentration of ethyl Cellulose and HPMC K100 M. Also the high amount of HPMC K4M leads to the less initial release and sustain effect. A theoretical drug release profile was generated using pharmacokinetic parameters of Colchicine. The value of t50 and t80 of theoretical drug release profile was found to be 242 min and 529 min respectively. The similarity factor f2 was applied between the in vitro drug release profile of optimizing batches and theoretical profile, which indicate a decent similarity between all in vitro drug release profiles (f2 = 68.28 for F7). All the batches except F1shows the value of f2 value within a range. Batch F7 showed the highest f2 (f2 = 68.28) among all the batches and this similarity was also reflected in t50 (≈ 256 min) and t80 (≈ 554 min) values. A 23 full factorial design was applied to systemically optimize in vitro drug release profile. The HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) were selected as independent variables. The time required for 50% drug released (t50), the time required for 80% drug release (t80), similarity factor f2, and mean dissolution time (MDT) were selected as dependent variables. The results of full factorial design indicate that the HPMC K4M (X1), Concentration of HPMC K100 M (X2), and concentration of EC (X3) have a significant effect on in vitro drug release profile. To find out the release mechanism the in vitro release data were fitted in the Korsmeyer-Peppas equation. All Batches except F1 and F3 show Anomalous diffusion-controlled release (combined mechanism of diffusion and case II transport).  

scholarly journals Preparation and characterization of azathioprine microspheres for colon specific delivery

2019 ◽  
Vol 9 (2) ◽  
pp. 97-101
Author(s):  
Rinku Gonekar ◽  
Mohan Lal Kori
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Study Drug ◽  
Entrapment Efficiency ◽  
Release Profile ◽  
Intestinal Fluid ◽  
Drug Release Profile ◽  
Fecal Matter

The objective of the present study is to develop colon targeted drug delivery system using dextrin (polysaccharide) as a carrier for Azathioprine.  Microspheres containing azathioprine, dextrin and various excipients were prepared by solvent evaporation technique. The prepared microsphere were evaluated by different methods parameters like particle size,  drug entrapment efficiency, percentage yield, shape and surface morphology  and in vitro drug release study. Drug release profile was evaluated in simulated gastric, intestinal fluid and simulated colonic fluid. Best formulation was decided on the basis drug release profile in simulated gastric, intestinal fluid and simulated colonic fluid. In dextrin based microspheres, dextrin as a carrier was found to be suitable for targeting of Azathioprine for local action in the site of colon. Dextrin microspheres released 95-99% of azathioprine in simulated colonic fluid with 4% human fecal matter solution. The results of in-vitro studies of the azathioprine microspheres indicate that for colon targeting dextrin are suitable carriers to deliver the drug specifically in the colonic region. Dextrin based azathoprine microspheres showed no significance change in particle size and % residual upon storage at 5 ± 3ºC, 25 ± 2ºC/60 ± 5% RH (room temperature) and 40 ± 2ºC/75 ±5%RH humidity for three months. Keywords: azathioprine, microsphere, dextrin, colon specific drug delivery.

The Measurement and Mathematical Analysis of 5-Fu Release from Magnetic Polymeric Nanocapsules, following the Application of Ultrasound

2018 ◽  
Vol 18 (3) ◽  
pp. 438-449 ◽  
Author(s):  
Ziaeddin Abed ◽  
Samideh Khoei ◽  
Behafarid Ghalandari ◽  
Jaber Beik ◽  
Ali Shakeri-Zadeh ◽  
...  
Keyword(s):  
Drug Release ◽  
Mathematical Analysis ◽  
Ultrasound Irradiation ◽  
Controlled Drug Release ◽  
Release Profile ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Ultrasound Intensity ◽  
Dialysis Bag

Objective: To study the effects of ultrasound irradiation on the release profile of 5-fluorouracil (5-Fu) loaded magnetic poly lactic co-glycolic acid (PLGA) nanocapsules. Also, the controlled drug-release behaviour of the nanocapsules was mathematically investigated. Methods: The nanocapsules were synthesized, dispersed in phosphate buffered saline (PBS), transferred to a dialysis bag, and finally, irradiated by various ultrasound parameters (1 or 3MHz; 0.3-1W/cm2; 5-10 minutes). The release profile of the irradiated nanocapsules was recorded for 14 days. To find the in vitro drug release mechanism in the absence and presence of various intensities of ultrasound, the obtained data were fitted in various kinetic models for drug release. Results: The results demonstrated that the ultrasound speeded up the rate of drug release from the nanocapsules. The mathematical analysis illustrated that when the ultrasound intensity is increased, the probability of controlled release behaviour of the nanocapsules is raised. We found that drug release from the irradiated nanocapsules follows an erosion-controlled mechanism with the decrease in the velocity of diffusion. Conclusion: In conclusion, to attain a controlled drug-delivery strategy in the area of cancer therapy, the drug release profile of the nano-carriers may be well-controlled by ultrasound.

Metronidazole Loaded Polycaprolactone-Carbopol blends Based Biodegradable Intrapocket Dental Film for Local Treatment of Periodontitis

2020 ◽  
Vol 10 ◽  
Author(s):  
Nitin Dhedage ◽  
Gayasuddin Khan ◽  
Gufran Ajmal ◽  
Manish Kumar ◽  
Abhishek Jha ◽  
...  
Keyword(s):  
Drug Release ◽  
Gingival Crevicular Fluid ◽  
Local Treatment ◽  
Local Drug Delivery ◽  
Release Kinetic ◽  
Burst Release ◽  
Drug Release Profile ◽  
Initial Zone

: The goal of this research was to produce intrapocket dental film, composed of polycaprolactone and carbopol blends by a modified solvent casting method. Prepared films were consistent in thickness (2.10±0.56 to 2.50±0.39 mm) and weight (35.23±0.37 to 39.45±0.45 mg) with drug entrapment of up to 87.63±1.98 percent. The concentration of carbopol is observed to have a direct relationship with thickness, film weight, and swelling factor of the prepared dental film. The film has a surface pH close to gingival crevicular fluid pH and is therefore appropriate for the application. The developed film exhibited a biphasic drug release profile with an initial burst release followed by a continuous release for more than 11 days. Drug release kinetic study supports the release of the drug by a diffusion-based process, as best explained by the Korsmeyer Peppas kinetics (R2 = 0.9635). In-vitro antimicrobial activity was also in accordance with drug release, with a high initial zone of inhibition (ZOI) (49.32±0.156mm), followed by 14.28±0.080 mm ZOI on 11th day. The in-vivo study showed that the prepared film was able to prevent periodontal ligament degeneration as observed in the periodontitis experiment animal model. In conclusion, prepared intrapocket dental film based on caprolactone and carbopol can be used as a novel local drug delivery system for the management of periodontitis.

Formulation Development of Metoprolol Succinate Controlled Release Tablets using Ethyl-cellulose-polyvinyl-pyrrolidone Coating

2015 ◽  
Vol 8 (2) ◽  
pp. 2851-2857
Author(s):  
Kiran Kumar Vangara ◽  
Kishore K. Konda ◽  
Shiva K. Ravula ◽  
Pradeep K Vuppala ◽  
Vijay K. Sripuram ◽  
...  
Keyword(s):  
Weight Gain ◽  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Film Coating ◽  
Release Profile ◽  
Water Soluble ◽  
Metoprolol Succinate ◽  
Water Soluble Drug

It is challenging to develop a controlled release (CR) formulation for a freely water soluble drug molecule without using rate controlling polymers in the core matrix. This study is aimed to develop and evaluate cost-effective ethyl cellulose (EC)-polyvinyl pyrrolidone (PVP) film coating that can effectively control the release of freely water soluble drug, metoprolol succinate (MS) and to match that of release profile with its marketed tablet. Simple core tables of MS were compressed and coated with a solution composed of hydrophobic rate controlling polymer, EC and water soluble pore forming polymer, PVP. The effect of formulation parameters such as the ratio of EC to PVP and tablet coating weight gain on the in-vitro drug release were evaluated. Release profile of the optimized formulation at different pH conditions was determined and the similarity factor (f2) with marketed release profile was calculated.It was observed that drug release rate increased with a decrease in the ratio of ethyl cellulose to PVP and decreased with increased weight gain of the coating membrane. Among all the formulations, the formulation with EC and PVP at a ratio of 60:40 %w/w and 9% weight gain showed matching release profile to marketed tablet with f2 value of 72.25. The optimized formulation showed pH independent in-vitro release. This study successfully demonstrated that EC-PVP film coating can effectively control the release rate of freely soluble drugs. Once a day CR formulation of metoprolol succinate pharmaceutically equivalent to marketed tablet was developed.  

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