Controlled and targeted delivery of diclofenac sodium to the intestine from pH-Responsive chitosan/poly(vinyl alcohol) interpenetrating polymeric network hydrogels (original) (raw)
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Preparation and evaluation of chitosan/carrageenan beads for controlled release of sodium diclofenac
AAPS PharmSciTech, 2007
The polyelectrolyte complex (PEC) hydrogel beads based on chitosan (CS) and carrageenan (CR) have been studied as a controlled release device to deliver sodium diclofenac (DFNa) in the simulated gastrointestinal condition. Various factors potentially influencing the drug release (ie, CS/CR proportion, DFNa content, types and amount of cross-linking agents) were also investigated. The optimal formulation was obtained with CS/CR proportion of 2/1 and 5% (wt/vol) DFNa. The controlled release of the drug from this formulation was superior to other formulations and was able to maintain the release for~8 hours. Upon cross-linking with glutaric acid and glutaraldehyde, the resulting beads were found to be more efficient for prolonged drug release than their non-cross-linking counterparts. The bead cross-linked with glutaraldehyde was able to control the release of the drug over 24 hours. The difference in the drug release behavior can be attributed to the differences in ionic interaction between the oppositely charged ions and to the concentrations of the drug within the beads, which depends on the compositions of the formulation and the pH of the dissolution medium. The release of drug was controlled by the mechanism of the dissolution of DFNa in the dissolution medium and the diffusion of DFNa through the hydrogel beads.
Hydrogels from xylan/chitosan complexes for the controlled release of diclofenac sodium
Cellulose, 2019
Hydrogels were prepared from colloidal suspensions of polyelectrolyte complexes of xylan (Xyl) and chitosan (Ch) (mass ratio: 70 wt% Xyl/30 wt% Ch). They were formed at pH 5.0, at which both polyelectrolytes were highly charged according to their corresponding potentiometric titrations. They were treated with a polycarboxylic acid, sodium citrate, at different concentrations (0%, 3% and 7% w/v), and characterized by means of FTIR, scanning electron microscopy, wet-mechanical properties, swelling and solubility. FTIR spectra confirmed the presence of sodium citrate in the treated hydrogels. Wet-stress and wet-strain at break were increased by 150% and 57% respectively, when hydrogels were treated with 7% w/v of sodium citrate. The swelling capacity was clearly modified due to the presence of this compound and to the ionic strength of the liquid medium. The ability of these hydrogels for drug loading and controlled release was studied in vitro using diclofenac sodium (DS) as model drug. It was found that at pH 7.4, the hydrogel treated with sodium citrate absorbed significantly higher amounts of diclofenac sodium (up to 255 mg DS/g hydrogel) and its release was better controlled compared to that of the non-treated hydrogel. Particularly, the presence of sodium citrate in the liquid medium after the diclofenac sodium loading process and the influence of the ionic strength on the drug release rate indicated that an ion exchange process occurred, first between sodium citrate and diclofenac sodium and then between this drug and the ions present in the solution.
The objective of this study is to fabricate and Evaluate Chitosan Matrix tablets of Diclofenac.The effect of various polymers like ethyl cellulose, cellulose acetate phthalate on the release of Diclofenac have been evaluated. Tablets were evaluated for physical and chemical parameters such as Hardness, Friability, Thickness, Weight variation, Drug Content uniformity and invitro release. All batches are complied physical and chemical parameters with in the U.S.P limit.Invitro release profile of Diclofenac with 3%HPMC polymer (FH2) Showed that 97% of the drug was released at the end of 12 th hr which is considered as optimized formulation. The tablets showed no significant change either in physical appearance or in dissolution pattern after storing at 40 0 c / 75% RH and 60 0 C / 80% RH for three months. The drug release data fit well to Higuchi equation, Peppas and Korsemeyer equation. The drug release was found to have swelling and diffusion.
Future Journal of Pharmaceutical Sciences, 2021
Background An enteric coating is a multistep technique that involves deposition of a polymeric barrier over uncoated orally administered tablets to prevent them from dissolving or disintegrating in the stomach. However, as soon as the coating dissolves in the alkaline environment of intestine, the whole of the drug come in direct contact with gastric mucosa leading to irritation to distal parts of the gastrointestinal tract (GIT). Considering the above facts, there is clear need to develop a simple and effective enteric release formulation for gastric irritant drugs like Diclofenac sodium (DS). The goal of this study was to create enteric release polymeric polyelectrolyte complex (PEC) beads made up of cationic Chitosan (CH) and anionic Gellan Gum (GG) for sustained DS delivery to the intestine. The beads were prepared by extruding a solution of GG and Gum Ghatti (GT) or GG and Gum Karaya (GK) bearing DS into CH solution in 1% w/v acetic acid, with the help of a syringe fitted with ...
Materials
The hydrogels responding to pH synthesized by graft copolymerization only and then concurrent grafting and crosslinking of monomer N-isopropyl acrylamide (NIPAAM) and binary comonomers acrylamide, acrylic acid and acrylonitrile (AAm, AA and AN) onto chitosan support were explored for the percent upload and release study for anti-inflammatory diclofenac sodium drug (DS), w.r.t. time and pH. Diclofenac sodium DS was seized in polymeric matrices by the equilibration process. The crosslinked-graft copolymers showed the highest percent uptake than graft copolymers (without crosslinker) and chitosan itself. The sustainable release of the loaded drug was studied with respect to time at pH 2.2, 7.0, 7.4 and 9.4. Among graft copolymers (without crosslinking), Chit-g-polymer (NIPAAM-co-AA) and Chit-g-polymer (NIPAAM-co-AN) exhibited worthy results for sustainable drug deliverance, whereas Crosslink-Chit-g-polymer (NIPAAM-co-AA) and Crosslink-Chit-g-polymer (NIPAAM-co-AAm) presented the best r...
Inflammation targeted chitosan-based hydrogel for controlled release of diclofenac sodium
International Journal of Biological Macromolecules, 2020
Inflammation is a key challenge in the treatment of chronic diseases. Spurred by topical advancement in polymer chemistry and drug delivery, hydrogels that release a drug in temporal, spatial and dosage controlled fashion have been trendy. This research focused on the fabrication of hydrogels with controlled drug release properties to control inflammation. Chitosan and polyvinyl pyrrolidone were used as base polymers and crosslinked with epichlorohydrin to form hydrogel films by solution casting technique. Prepared hydrogels were analyzed by swelling analysis in deionized water, buffer and electrolyte solutions and gel fraction. Functional groups confirmation and development of new covalent and hydrogen bonds, thermal stability (28.49%) and crystallinity were evaluated by FTIR, TGA and WAXRD, respectively. Rheological properties including gel strength and yield stress, elasticity (2309 MPa), porosity (75%) and hydrophilicity (73°) of prepared hydrogels were also evaluated. In vitro studies confirmed that prepared hydrogels have good biodegradability, excellent antimicrobial property and admirable cytotoxicity. Drug release profile (87.56% in 130 min) along with the drug encapsulation efficiency (84%) of prepared hydrogels was also studied. These results paved the path towards the development of hydrogels that can release the drugs with desired temporal patterns.
2020
Two formulations embedding diclofenac sodium salt into a chitosan hydrogel matrix with different crosslinking degree were prepared by in situ hydrogelation. The formulations were investigated by polarized light microscopy and scanning electron microscopy, and the in vitro drug release was tested in a medium mimicking the physiological environment. The mechanism of the drug release has been assessed by a theoretical model which was developed and it was based on the multifractal theory of motion. The drug release mechanism are described through continuous and nondifferentiable curves – multifractal curves.
International Research Journal of Pharmacy, 2015
Diclofenac sodium is a non-steroid anti-inflammatory drug for inflammation, analgesic and antipyretic. To obtain optimal therapeutic effects, diclofenac sodium has several drawbacks, e.g. high adverse effects, undergoes gastrointestinal degradation and first pass metabolism. The aims of this research were to investigate the characterization and the stability of chitosan-loaded sodium diclofenac in dissolution medium. Preparation of diclofenac sodium nanoparticle was to improve the delivery in the nanoparticles form in which medium chain chitosan as polymer and sodium tripolyphosphate as a cross-linker. The characterization of nanoparticle chitosan-loaded sodium diclofenac included morphology, distribution and particle size, zeta potential, entrapment efficiency and yield percentage respectively. The stability test was conducted in simulated gastric fluid (SGF) pH 1.2 ± 0.1 and artificial intestinal fluid (AIF) pH 7.0. The result of the research showed that preparation of chitosan-loaded sodium diclofenac nanoparticles can be made by an ionotropic gelation method using medium chain chitosan and sodium tripolyphosphate as a cross-linker. The obtained nanoparticles size were in the range of 200-500 nm with spherical shape, zeta potential was + 4.66 mV, entrapment efficiency ranged from 95.616 to 97.056 % and the yield percentage ranged from 55.61 to 184.26 %. In vitro release tests showed that nanoparticles stability depends on pH and ionic strength of the medium used. Nanoparticle chitosan-loaded diclofenac sodium was stable in simulated gastric fluid (SGF) pH 1.2 ± 0.1 and artificial intestinal fluid (AIF) pH 7.0 respectively.
The preparation and characterization of novel materials for drug delivery has rapidly gained importance in development of innovative medicine. The paper concerns the uses of chitosan as an excipient in oral formulations and as a drug delivery vehicle for burnt painful injuries. The use of chitosan (CTS) as base in polyelectrolyte complex systems, to prepare liquid release systems as hydrogels and solid release systems as sponges is presented. In this paper the preparation of CTS hydrogels and sponges carrying diclofenac (DCF), as antiinflammatory drug is reported. The immobilization of DCF in CTS is done by mixing the CTS hydrogel with the anti-inflammatory drug solutions. The concentration of anti-inflammatory drug in the CTS hydrogel generating the sponges was of 57 mg/l, 72 mg/l and 114 mg/l. The CTS sponges with anti-inflammatory drugs were prepared by freeze-drying at -610°C and 0,09 atm. The characterization of the hydrogels and sponges was done by infrared spectra (FTIR) and ultraviolet-visible spectroscopy (UV-VIS). The results indicated the formation of CTS-DCF intermediates. The DCF molecules are forming temporary chelates in CTS hydrogels and sponges and they are compatible with skin or some of biological fluids with satisfactory results.
2020
Objective: The objective of this investigation is to develop a sustained release matrix tablet by taking a mixture of chitosan (CS) and Eudragit L100 polymers and then to study the drug release pattern for a low solubility drug of diclofenac sodium (DS). Materials and Methods: The short biological half-life and frequent dosing make DS an ideal candidate for sustained release dosage forms. The tablets were prepared by direct compression method. All the batches were evaluated for thickness, weight variation, hardness, and drug content uniformity and in vitro drug release. Results: Fourier-transform infrared spectroscopy study was conducted to study any interaction between dug and ingredients. Hydrophilic matrix of CS alone could not control the diclofenac release effectively for 12 h whereas when combined with Eudragit L100 could slow down the release of drug and can be successfully employed for: formulating sustained-release matrix tablets. Conclusion: Fitting the data to Korsmeyer e...