Controlled Release Of Diclofenac Sodium Research Articles

Thermo-responsive release of diclofenac sodium from poly (ε-caprolactone)/glyceryl trilaurate co-continuous composite prepared by heat treatment

Nowadays, it is still a tough challenge to prepare thermo-responsive drug delivery system without the use of poly(N-isopropylacrylamide) (PNIAPAM) and its derivatives. Herein, we attempted to fabricate a novel co-continuous composite with thermo-responsive drug release behavior induced by the phase transition of dispersed phase. Poly (ϵ-caprolactone) (PCL) scaffold with connected porous structure was prepared first, followed by the introduce and impregnating of diclofenac sodium/glyceryl trilaurate (DS/C12) hot melt mixture. After solidification at 25 °C, PCL/C12 composites with co-continuous structure were obtained. The connected porous structure of PCL scaffold and morphology of PCL/C12 composites were confirmed by scanning electron microscope. The thermo-responsive drug release mechanism of PCL/C12 composites was investigated by differential scanning calorimeter and two-dimensional infrared correlation spectroscopy. The results indicated that the temperature of onset melting and melting point of C12 was about 41.5 °C and 47.5 °C, respectively. When the temperature was switched from 37 °C to 45 °C, C12 underwent a melt transition, and the regular aggregation of C12 molecular chain was disrupted, accelerating the release of DS. The in vitro release results presented that PCL/C12 composites could achieve on-off controlled release of DS under alternative temperature of 45 °C and 37 °C. According to the comprehensive test results, this PCL/C12 composites should have promising application in bone tissue engineering. Schematic diagram illustrating of the preparation of poly (ϵ-caprolactone)/glyceryl trilaurate (PCL/C12) co-continuous composite (a) and its on-off controlled release behavior of diclofenac sodium (DS) under alternative temperature of 45 °C and 37 °C (b and c). • Poly (ϵ-caprolactone)/glyceryl trilaurate (PCL/C12) co-continuous composite was fabricated. • PCL/C12 composite achieved on-off controlled release of diclofenac sodium under alternative temperature of 45 °C and 37 °C. • The controlled drug release behavior of PCL/C12 composite was induced by the phase transition of C12. • This thermo-responsive composite was prepared without the use of poly(N-isopropylacrylamide) and its derivatives. • This work provided a promising strategy and method for the preparation of thermo-responsive drug delivery systems.

Development and Evaluation of Diclofenac sodium Controlled Release Dosage Forms Using Natural, Hydrophilic and Hydrophobic Polymers and its Comparative Studies

Abstract: The aim of the present study is to develop the controlled release dosage form of diclofenac using hydrophilic polymers (xanthan gum from natural origin, hydroxy propyl methyl cellulose K 100M from semisynthetic origin) and hydrophobic polymer (compritol 888 ATO from synthetic origin). Diclofenac sodium matrix tablets were prepared by xanthan gum and hydroxy propyl methyl cellulose by wet granulation method. Hot melt granulation method was used for compritol as it was insoluble polymer. Fourier transform infrared spectroscopy (FTIR) analysis, differential scanning calorimetry (DSC) and X-Ray diffraction (XRD) studies indicated that there was no interaction between drug and polymers. Matrix tablets were formulated according to formulae and evaluated the suitability for controlled release systems for 24 h. Tablets prepared with xanthan gum, hydroxy propyl methyl cellulose and compritol matrix tablets showed zero order drug release. The hardness for all the formulations found to be in the range of 4-5 kg/cm2. The friability values of all formulations were found to be less than 1 %. The drug content of each individual preparation was found to be within the specified limits of the stated amount of diclofenac sodium. XGD4, HPD4 and CD2 formulations were considered as optimum formulations for oral controlled release of diclofenac sodium. Key words: Diclofenac sodium, Hydroxy propyl methyl cellulose K 100M, Xanthan gum, controlled release dosage forms, Compritol 888 ATO.

PH sensitive mesoporous materials for immediate or controlled release of NSAID

The aim of this research was to investigate novel mesoporous materials, polysaccharide aerogels, as drug delivery carries in order to achieve controlled release of a model drug, diclofenac sodium. Pectin, alginate and composite pectin–alginate aerogels were prepared by cross-linking with three different ions, zinc, strontium and calcium. Calcium ions are not the best cross-linkers when controlled release is desired, since the release of a model drug was achieved in initial 1 h. Oppositely, zinc cross-linking provided more controlled release of diclofenac sodium. Therefore, zinc cross-linked pectin aerogels were used as the final drug delivery carriers in order to compare the release profile with two commercially available drugs. Pectin–zinc aerogel capsule degraded completely within the 24 h, oppositely both commercial drugs did not degrade even after 72 h. Moreover, the release profiles of all three tested drugs were dissimilar. Pectin–zinc aerogel capsule released 80% of the model drugs in 7 h, first commercial drug around 60% and second commercial drug nearly 100%.

Controlled-release of diclofenac sodium from wax matrix granule

A twin-screw compounding extruder was used to prepare wax matrix granules (WMG) consisting of carnauba wax, diclofenac sodium (DS) as a model drug, and rate-controlling agents such as hydroxypropylcellulose (HPC-SL), methacylic acid copolymer L (Eudragit L-100), and sodium chloride (NaCl). In this preparation, a wax matrix with high mechanical strength was obtained even at temperatures lower than the wax melting point. Dissolution behaviors of DS from WMG were strongly influenced by granule formulation, in which an increase in the content of HPC-SL or Eudragit L-100 brought a significant increase in the dissolution rate. The extent of this enhancing effect in HPC-SL was identical in two different dissolution mediums (pH 6.8 buffer solution and water), but in Eudragit L-100 was more significant in pH 6.8 buffer solution than in water. Only a small increase in the dissolution rate was observed in NaCl-containing WMG. These different behaviors were attributed to the physicochemical properties (i.e. swelling and solubility) of the rate-controlling agent in the dissolution medium. Further, mechanical strengths of the wetted WMG after dissolution studies were > 70 g/mm 2 suggesting that burst release of DS in the gastrointestinal tract would be avoided.