Development of Diclofenac Sodium Releasing Bio-Erodible Polymeric Nanomats

2006 ◽  
Vol 6 (9) ◽  
pp. 3310-3320 ◽  
Author(s):  
A. M. Piras ◽  
L. Nikkola ◽  
F. Chiellini ◽  
N. Ashammakhi ◽  
E. Chiellini
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Release Kinetics ◽  
Diclofenac Sodium ◽  
High Surface ◽  
Active Agent ◽  
Volume Ratio ◽  
Homogeneous Distribution ◽  
Scanning Calorimetry ◽  
Nano Structure

Application of nanofiber-based nanomats in medicine is attractive and thanks to the 3D nano-structure and the high surface to volume ratio they are excellent for local controlled drug delivery. The use of bioactive bioerodible polymers for developing drug delivery nanomats may allow for drug release and targeting control. Objective of the current study was to evaluate the suitability of bioerodible polymeric material based on n-butyl hemiester of [poly(maleic anhydride-alt-2-methoxyethyl vinyl ether)] (PAM14) for the preparation of nanomats for controlled administration of anti-inflammatory, diclofenac sodium (DS) drug. Samples were prepared using different polymer concentrations (5–10%) in either ethanol or acetic acid as solvent. Morphology was investigated by using scanning electron microscopy (SEM). Thermal analysis such as differential scanning calorimetry (DSC) was performed to detect effect on polymer arrangement. DS localization in electrospun nanomats was evaluated by using electron back scattering microanalysis, based on the detection of chlorine, and drug release kinetics was assessed using UV-Vis. Average fiber diameter resulted in the range of 100 nm to 1.0 μm and a homogeneous distribution of the loaded drug into the fibers was observed. The DS release was immediate and despite the preliminary nature of the performed electrospinning experiments, the achieved results appear promising for the future development of a novel system for the controlled and targeted administration of drug and active agent.

scholarly journals Role of Mathematical Modeling in Controlled Drug Delivery

2009 ◽  
Vol 1 (3) ◽  
pp. 539-550 ◽  
Author(s):  
Moharram A. Khan ◽  
Shafeeq. T
Keyword(s):  
Mathematical Modeling ◽  
Drug Delivery ◽  
Drug Release ◽  
Drug Transport ◽  
Release Kinetics ◽  
Active Agent ◽  
Controlled Drug Delivery ◽  
Design Parameters ◽  
Mass Transport Mechanisms

Controlled drug delivery occurs when a polymer or lipid (natural or synthetic) is judiciously combined with a drug or other active agent in such a way that the active agent is released from the material in a pre-designed manner. The aim of controlling the drug delivery is to achieve more effective therapies while eliminating potential for both under- and overdosing. Controlled delivery systems includes the maintenance of drug levels within a desired range, the need for fewer administrations, optimal use of the drug in question, and increased patient compliance. Mathematical modeling of controlled drug delivery can help to provide a scientific knowledge base concerning the mass transport mechanisms that are involved in the control of drug release. Mathematically, it is identified for designing a particular pharmaceutical system and it can be used to simulate the effect of the device design parameters (viz., geometry and composition) on the resulting drug release kinetics. The objective of this review outlines the application of mathematical modeling to the controlled drug delivery mechanisms, focusing particular attention on drug transport in human breast cancer, treated with the drug Doxorubicin. Keywords: Controlled drug delivery; Diffusion; Doxorubicin; Mathematical Modeling; Release Kinetics.© 2009 JSR Publications. ISSN: 2070-0237 (Print); 2070-0245 (Online). All rights reserved.DOI: 10.3329/jsr.v1i3.2581              J. Sci. Res. 1 (3), 539-550 (2009) 

scholarly journals Hydrogels Based on Imino-Chitosan Amphiphiles as a Matrix for Drug Delivery Systems

Polymers ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 2687
Author(s):  
Daniela Ailincai ◽  
William Porzio ◽  
Luminita Marin
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery Systems ◽  
Release Kinetics ◽  
Diclofenac Sodium ◽  
Intermolecular Forces ◽  
Delivery Systems ◽  
Molar Ratio ◽  
Hydrogel Matrix ◽  
Vis Spectroscopy

This paper reports new formulations based on chitosan, citral, and diclofenac sodium salt (DCF). The central idea was to encapsulate an anionic drug into a polycationic hydrogel matrix in order to increase the intermolecular forces between them and thus to ensure slower drug release, while citral was used as a penetration enhancer to assure efficient delivery of the drug. Hydrogels without drug were also synthesized and used as a reference. The structure, morphology, and supramolecular architecture of the drug delivery systems were evaluated by FTIR spectroscopy, scanning electron microscopy, polarized optical microscopy, and wide-angle X-ray diffraction. The drug release kinetics was monitored in vitro by UV-VIS spectroscopy, in physiological conditions, while the enzymatic and hydrolytic degradability of the hydrogels were evaluated in the presence of lysozyme and phosphate buffer saline (PBS), at 37 °C. All of the data revealed that the anionic DCF was strongly anchored into the polycationic matrix and the drug was slowly released over 7 days. Moreover, the release rate can be controlled by simple variation of the molar ratio between the polycationic chitosan and lipophilic citral.

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

scholarly journals Fabrication and In Vitro Evaluation of pH-Sensitive Polymeric Hydrogels as Controlled Release Carriers

Gels ◽  
2021 ◽  
Vol 7 (3) ◽  
pp. 110
Author(s):  
Muhammad Suhail ◽  
Chih-Wun Fang ◽  
Arshad Khan ◽  
Muhammad Usman Minhas ◽  
Pao-Chu Wu
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Acrylic Acid ◽  
Chondroitin Sulfate ◽  
Diclofenac Sodium ◽  
Research Work ◽  
Controlled Delivery ◽  
Scanning Calorimetry ◽  
Release Studies

The purpose of the current investigation was to develop chondroitin sulfate/carbopol-co-poly(acrylic acid) (CS/CBP-co-PAA) hydrogels for controlled delivery of diclofenac sodium (DS). Different concentrations of polymers chondroitin sulfate (CS), carbopol 934 (CBP), and monomer acrylic acid (AA) were cross-linked by ethylene glycol dimethylacrylate (EGDMA) in the presence of ammonium peroxodisulfate (APS) (initiator). The fabricated hydrogels were characterized for further experiments. Characterizations such as Scanning electron microscopy (SEM), Thermogravimetric analysis (TGA), Differential scanning calorimetry (DSC), Powder X-ray diffractometry (PXRD), and Fourier transform infrared spectroscopy (FTIR) were conducted to understand the surface morphology, thermodynamic stability, crystallinity of the drug, ingredients, and developed hydrogels. The swelling and drug release studies were conducted at two different pH mediums (pH 1.2 and 7.4), and pH-dependent swelling and drug release was shown due to the presence of functional groups of both polymers and monomers; hence, greater swelling and drug release was observed at the higher pH (pH 7.4). The percent drug release of the developed system and commercially available product cataflam was compared and high controlled release of the drug from the developed system was observed at both low and high pH. The mechanism of drug release from the hydrogels followed Korsmeyer–Peppas model. Conclusively, the current research work demonstrated that the prepared hydrogel could be considered as a suitable candidate for controlled delivery of diclofenac sodium.

scholarly journals COMPARATIVE EVALUATION OF SELECTED POLYMERS AND PLASTICIZER ON TRANSDERMAL DRUG DELIVERY SYSTEM

2018 ◽  
Vol 10 (1) ◽  
pp. 67
Author(s):  
Bhawana Sethi ◽  
Rupa Mazumder
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Propylene Glycol ◽  
Drug Delivery System ◽  
Transdermal Drug Delivery ◽  
Release Kinetics ◽  
Content Uniformity ◽  
Transdermal Drug Delivery System ◽  
Transdermal Patches

Objective: The present work was aimed at preparation of transdermal patches by a solvent casting method using a varying concentration of polymers i.e. methocel (K15 and K100), ethocel (4 and 10), gelatin, chitosan, eudragit (RL and RS) grade using plasticizer (glycerin and propylene glycol).Methods: The ratio of drug to polymers and plasticizer was varied and the effect of formulation variables was studied. Prepared transdermal patches were evaluated for physicochemical properties, in-vitro permeation studies, content uniformity, primary skin irritation studies and FT-IR studies.Results: The formulated transdermal patch by using Methocel K 100 M showed good physical properties. The average weight of patches prepared using glycerin as a plasticizer were ranged from 42.33-67.00 mg and propylene glycol as a plasticizer were ranged from 40.67-67.67 mg. The percentage moisture absorption varies from 1.76 to 10.73 for patches formulated using glycerin and 2.28 to 7.97 for propylene glycol patches. The percentage moisture loss from patches prepared using glycerin was ranged from 2.75 to 11.54 and 2.87 to 12.02 from propylene glycol. The water vapour transmission rate from patches prepared using glycerin was ranged from 0.25 to 0.92 and 0.41 to 1.76. The formulated patch showed the acceptable quantity of medicament ranged from (100.20-101.05%). This result met the test content uniformity as per BP (85% to 115%). According to that, the drug was consistent throughout the patches. The formulation PGD is considered as the best formulation, since it shows a maximum in vitro drug release as 43.75 % at 24 h. The drug release kinetics studied showed that the majority of formulations was following zero order.Conclusion: In conclusion, controlled release transdermal drug delivery system patches of aliskiren can be prepared using polymer combinations, with a different plasticizer. The release rate of drug depends upon the polymer. However, release kinetics followed zero order.

Fabrication of Hybrid Cell-Microbead Constructs Using Laser Direct-Write of Alginate Microbeads and Adherent Breast Cancer Cells

2013 ◽  
Author(s):  
Andrew D. Dias ◽  
David M. Kingsley ◽  
Douglas B. Chrisey ◽  
David T. Corr
Keyword(s):  
Drug Delivery ◽  
Mammalian Cells ◽  
Hybrid Cell ◽  
High Surface ◽  
High Surface Area ◽  
Volume Ratio ◽  
Direct Write ◽  
Cellular Interactions ◽  
Paracrine Signaling ◽  
Laser Direct Write

Microbeads are becoming popular tools in tissue engineering as 3D microstructure hydrogels. The gel nature of microbeads enables them to sequester soluble factors and mammalian cells, and their high surface area-to-volume ratio allows diffusion between the bead and the environment [1,2]. Microbeads are thus good systems for drug delivery and can serve as 3D microenvironments for cells. To fully maximize their potential as delivery systems and microenvironments, it is highly desirable to create spatially-precise hybrid cultures of microbeads and mammalian cells. Precise placement of microbeads in proximity to patterned cells will allow the study of spatial cellular interactions, paracrine signaling, and drug delivery.

scholarly journals Spray-Formed Layered Polymer Microneedles for Controlled Biphasic Drug Delivery

Polymers ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 369 ◽  
Author(s):  
Seok Park ◽  
Min Kim ◽  
Seung-Ki Baek ◽  
Jung-Hwan Park ◽  
Seong-O Choi
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Diffusion Barrier ◽  
Structural Changes ◽  
Tertiary Structure ◽  
Ex Vivo ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Drug Delivery System ◽  
Initial Burst

In this study we present polymeric microneedles composed of multiple layers to control drug release kinetics. Layered microneedles were fabricated by spraying poly(lactic-co-glycolic acid) (PLGA) and polyvinylpyrrolidone (PVP) in sequence, and were characterized by mechanical testing and ex vivo skin insertion tests. The compression test demonstrated that no noticeable layer separation occurred, indicating good adhesion between PLGA and PVP layers. Histological examination confirmed that the microneedles were successfully inserted into the skin and indicated biphasic release of dyes incorporated within microneedle matrices. Structural changes of a model protein drug, bovine serum albumin (BSA), in PLGA and PVP matrices were examined by circular dichroism (CD) and fluorescence spectroscopy. The results showed that the tertiary structure of BSA was well maintained in both PLGA and PVP layers while the secondary structures were slightly changed during microneedle fabrication. In vitro release studies showed that over 60% of BSA in the PLGA layer was released within 1 h, followed by continuous slow release over the course of the experiments (7 days), while BSA in the PVP layer was completely released within 0.5 h. The initial burst of BSA from PLGA was further controlled by depositing a blank PLGA layer prior to forming the PLGA layer containing BSA. The blank PLGA layer acted as a diffusion barrier, resulting in a reduced initial burst. The formation of the PLGA diffusion barrier was visualized using confocal microscopy. Our results suggest that the spray-formed multilayer microneedles could be an attractive transdermal drug delivery system that is capable of modulating a drug release profile.

scholarly journals In vitro study of sirolimus release from nonwoven PLLA matrices

2018 ◽  
Vol 4 (1) ◽  
pp. 591-594
Author(s):  
Sabine Illner ◽  
Stefanie Kohse ◽  
Claudia Michaelis ◽  
Thomas Reske ◽  
Niels Grabow ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Volume Ratio ◽  
In Vitro Study ◽  
Complete Wetting ◽  
In Vitro Drug Release ◽  
Spray Coatings ◽  
Plasma Pretreatment ◽  
Predetermined Time

AbstractSirolimus incorporated nonwoven polymer matrices were fabricated via electrospinning. Release kinetics considering different fiber diameters and layer thicknesses were investigated. In vitro drug release profiles were evaluated by measuring the drug concentration in an established drug release medium (0.9% saline solution with additives, not buffered) at predetermined time points. Furthermore, an NH3-plasma pretreatment was examined to ensure complete wetting from the beginning of the study. In comparison to thin drug-loaded PLLA spray coatings it was shown that the release of sirolimus is diffusion- and degradation-controlled regardless of the surface-to-volume ratio, though fiber diameters or a hydrophilization can affect its release kinetics.

Fabrication and characterization of smart karaya gum/sodium alginate semi-IPN microbeads for controlled release of D-penicillamine drug

2020 ◽  
pp. 096739112090447
Author(s):  
O Sreekanth Reddy ◽  
MCS Subha ◽  
T Jithendra ◽  
C Madhavi ◽  
K Chowdoji Rao
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Polymerization Reaction ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Drug Release Kinetics ◽  
Swelling Capacity ◽  
Release Data ◽  
Karaya Gum

This article reports the fabrication of pH-sensitive microbeads from sodium alginate (SA) and modified karaya gum (KG). KG was modified by graft copolymerization using 2-hydroxyethyl methacrylate (2-HEMA) through in situ free radical polymerization reaction. The graft copolymer was blended with SA to develop microbeads by a simple ionotropic gelation technique. The microbeads were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, and scanning electron microscopy. The effect of %HEMA and polymer blend ratio on the swelling capacity was investigated. Drug release kinetics of the microbeads was investigated under both pH 7.4 and pH 1.2 at 37°C. The drug release kinetics was analyzed by evaluating the release data using different kinetic models.

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