(Drug Dev Ind Pharm[TA])
- Formulation and evaluation of injectable in situ forming microparticles for sustained delivery of lornoxicam. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Oct 21; :1-10
- The objective of this study is to formulate biodegradable in situ microparticles (ISM) containing lornoxicam for post-operative and arthritic pain management. ISM emulsions were prepared according to...
The objective of this study is to formulate biodegradable in situ microparticles (ISM) containing lornoxicam for post-operative and arthritic pain management. ISM emulsions were prepared according to 2(5) full factorial experimental design to investigate the influence of formulation variables on the release profile of the drug. The independent variables studied are the polymer type, polymer inherent viscosity, polymer concentration, oil type and polymer:oil ratio. In vitro drug release, microscopical examination, particle size determination and syringeability measurement were selected as dependent variables. The effect of γ-sterilization on the prepared formulae was also examined. The prepared formulae showed extended drug release over two weeks, and flow time below 5 s/ml. Scanning electron microscope revealed that the prepared microparticles were spherical in shape, with diameter ranging from 3.45 to 22.78 µm. In vivo pharmacokinetic evaluation of two selected optimum formulations in rabbits showed prolonged drug absorption indicated by delayed Tmax and the extended mean residence time. In conclusion, the prepared injectable ISM could be a promising approach for providing extended delivery of lornoxicam with low initial burst effect.
- Optimization of the Ussing Chamber Setup with Excised Rat Intestinal Segments for Dissolution/Permeation Experiments of Poorly Soluble Drugs. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Oct 20; :1-31
- CONCLUSIONS: The compatibility of Fa/FeSSIFmod depends on the excised intestinal region. The chosen conditions enable dissolution/permeation experiments with excised rat duodenal segments. The experiments correctly predicted the superior permeation of nanosized over unmilled aprepitant that is observed in vivo.The optimized setup uses FaSSIFmod as donor medium, excised rat duodenal sheets as permeation membrane and a receiver medium containing bovine serum albumin and Antifoam B.
- Hot melt extrusion versus spray drying: hot melt extrusion degrades albendazole. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Oct 20; :1-15
- The purpose of this study was to enhance the dissolution properties of albendazole (ABZ) by the use of amorphous solid dispersions. Phase diagrams of ABZ-polymer binary mixtures generated from Flory-...
The purpose of this study was to enhance the dissolution properties of albendazole (ABZ) by the use of amorphous solid dispersions. Phase diagrams of ABZ-polymer binary mixtures generated from Flory-Huggins theory were used to assess miscibility and processability. Forced degradation studies showed that ABZ degraded upon exposure to hydrogen peroxide and 1 N NaOH at 80 °C for 5 min, and the degradants were albendazole sulfoxide (ABZSX), and ABZ impurity A, respectively. ABZ was chemically stable following exposure to 1 N HCl at 80 °C for one hour. Thermal degradation profiles show that ABZ, with and without Kollidon(®) VA 64, degraded at 180 °C and 140 °C, respectively, which indicated that ABZ could likely be processed by thermal processing. Following hot melt extrusion, ABZ degraded up to 97.4%, while the amorphous ABZ solid dispersion was successfully prepared by spray drying. Spray-dried ABZ formulations using various types of acids (methanesulfonic acid, sulfuric acid and hydrochloric acid) and polymers (Kollidon(®) VA 64, Soluplus(®) and Eudragit(®) E PO) were studied. The spray-dried ABZ with methanesulfonic acid and Kollidon(®) VA 64 substantially improved non-sink dissolution in acidic media as compared to bulk ABZ (8-fold), physical mixture of ABZ:Kollidon(®) VA 64 (5.6-fold) and ABZ mesylate salt (1.6-fold). No degradation was observed in the spray-dried product for up to six months and less than 5% after one-year storage. In conclusion, amorphous ABZ solid dispersions in combination with an acid and polymer can be prepared by spray drying to enhance dissolution and shelf-stability, whereas those made by melt extrusion are degraded.
- The performance of HPMC matrix tablets using various agglomeration manufacturing processes. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Oct 14; :1-32
- CONCLUSIONS: Compression mixtures made using the wet-granulation method exhibit better flow and compression properties than compression mixtures made using the dry-granulation method. The direct compression method proved to be the least appropriate manufacturing method because the compression mixture has very poor flow and the lowest compressibility/compactibility index. The choice of granulation technique significantly influences the swelling behavior and drug-dissolution profile of the final matrix tablets, also resulting in dissimilar release profiles. The choice of granulation method has the greatest influence on the drug-release profile. The direct compression method provides tablets with the fastest drug-release profile, followed by the dry-granulation and wet-granulation methods. The particle size of granules and porosity of tablets play an important role, contributing to differences in drug-release profiles.
- Editorial Board. [Journal Article]
- DDDrug Dev Ind Pharm 2016; 42(12):ebi
- Design and evaluation of acrylate polymeric carriers for fabrication of pH-sensitive microparticles. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Oct 6; :1-14
- Colon-targeted microparticles loaded with a model anti-inflammatory drug were fabricated using especially designed acrylic acid-butyl methacrylate copolymers. Microparticles were prepared by oil-in-o...
Colon-targeted microparticles loaded with a model anti-inflammatory drug were fabricated using especially designed acrylic acid-butyl methacrylate copolymers. Microparticles were prepared by oil-in-oil solvent evaporation method using Span 80 as emulsifier. Microparticles were found to be spherical in shape, hemocompatible and anionic with zeta potential of -27.4 and -29.0 mV. Entrapment of drug in the microparticles was confirmed by Fourier transform infrared (FTIR) spectroscopy. However, X-ray diffraction (XRD) and differential scanning calorimetry (DSC) revealed amorphous nature of microparticles due to the dilution effect of amorphous polymer. The microparticles released less than 5% drug at pH 1.2, while more than 90% of the drug load was released at pH 7.4. This suggested the colon targeting nature of the formulations. In experimentally developed colitis in Wistar rats, the microparticle formulation showed significant reduction (p < .05) in the disease activity score (disease symptoms), the colon-to-body weight ratio (tissue edema) and the myeloperoxidase, tumor necrosis factor (TNF)-α and interleukin (IL)-1β activities.
- Pilosebaceous Targeting by Isotretenoin Loaded Invasomal Gel for the Treatment of Eosinophilic Pustular Folliculitis: Optimization, efficacy and cellular analysis. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Sep 21; :1-39
- CONCLUSIONS: Clinical phase I, II and III studies will be required before using on human patients.CLSM validate that IG successfully reaches the pilosebaceous follicular unit and further studied on cell line (SZ-95) exhibited IC50 of ≤ 8 (25µM of isotretenoin). Cell cycle analysis confirmed IG arrested the cell growth up to 82% with insignificant difference to pure isotretenion.
- New doxorubicin nanoparticles engineered from calcium-crosslinked carbomer and a microemulsion precursor. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Oct 6; :1-9
- The purpose of this study was to investigate a new polymeric system and production process in which self-assembled doxorubicin-loaded nanoparticles were synthetized by using a water-in-oil microemuls...
The purpose of this study was to investigate a new polymeric system and production process in which self-assembled doxorubicin-loaded nanoparticles were synthetized by using a water-in-oil microemulsion as a template and calcium ions as cross-linkers. The manufacturing process combined cross-linking of carbomer within a W/O microemulsion followed by a phase-separation technique to avoid using organic solvents for extraction. To assess the sustained release behavior of doxorubicin from the nanoparticles, we have developed a new simple method based on the permeability coefficient of a synthetic membrane mounted on Franz diffusion cell system. Franz cells were preferred over the commonly used dialysis tubing because they provide adequate measures of the diffusion area as well as the volumes of the media in both sides of the membrane. The lower permeability values obtained for nanoparticles have shown that the release is a limiting step of the diffusion process, while the calculated straight lines may imply that the apparent release rate of the nanoparticle ensembles is close to a zero-order kinetics. The new drug release method for the evaluation of nano-carriers, utilizing a simple linear model to determine the permeability coefficient, has been proposed for perfect sink and non-sink conditions.
- A combination of complexation and self-nanoemulsifying drug delivery system for enhancing oral bioavailability and anticancer efficacy of curcumin. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Oct 6; :1-15
- CONCLUSIONS: The developed formulation can be a potential and safe carrier for the oral delivery of curcumin.
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- Solid-state amorphization of rebamipide and investigation on solubility and stability of the amorphous form. [Journal Article]
- DDDrug Dev Ind Pharm 2016 Oct 6; :1-10
- Solid-state amorphization of crystalline rebamipide (RBM) was realized by ball milling and spray drying. The amorphous content of samples milled for various time was quantified using X-ray powder dif...
Solid-state amorphization of crystalline rebamipide (RBM) was realized by ball milling and spray drying. The amorphous content of samples milled for various time was quantified using X-ray powder diffraction. Crystalline RBM and three amorphous RBM obtained by milling and spray drying were characterized by morphological analysis, X-ray diffraction, thermal analysis and vibrational spectroscopy. The crystal structure of RBM was first determined by single-crystal X-ray diffraction. In addition, the solubility and dissolution rate of the RBM samples were investigated in different media. Results indicated that the solubility and the dissolution rates of spray-dried RBM-PVP in different media were highly improved compared with crystalline RBM. The physical stabilities of the three amorphous RBM were systematically investigated, and the stability orders under different storage temperatures and levels of relative humidity (RH) were both as follows: spray dried RBM < milled RBM < spray dried RBM-PVP. A direct glass-to-crystal transformation was induced under high RH, and the transformation rate rose with increasing RH. However, amorphous RBM could stay stable at RH levels lower than 57.6% (25 °C).