(Drug Dev Ind Pharm[TA]) articles in PubMed
- Design and evaluation of acrylate polymeric carriers for fabrication of pH-sensitive microparticles. [Journal Article]
- Drug Dev Ind Pharm 2016 Sep 21; :1-47DD
- Colon targeted microparticles loaded with a model anti-inflammatory drug were fabricated using especially designed acrylic acid-butylmethacrylate copolymers. Microparticles were prepared by oil-in-oi...
Colon targeted microparticles loaded with a model anti-inflammatory drug were fabricated using especially designed acrylic acid-butylmethacrylate 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 FTIR. However, XRD and 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 < 0.05) in the disease activity score (disease symptoms), the colon-to-body weight ratio (tissue edema) and the myeloperoxidase, TNF-α and IL-1β activities.
- Pilosebaceous Targeting by Isotretenoin Loaded Invasomal Gel for the Treatment of Eosinophilic Pustular Folliculitis: Optimization, efficacy and cellular analysis. [Journal Article]
- Drug Dev Ind Pharm 2016 Sep 21; :1-39DD
- 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]
- Drug Dev Ind Pharm 2016 Sep 20; :1-34DD
- 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 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]
- Drug Dev Ind Pharm 2016 Sep 20; :1-49DD
- CONCLUSIONS: The developed formulation can be a potential and safe carrier for the oral delivery of curcumin.
- Solid-state amorphization of rebamipide and investigation on solubility and stability of the amorphous form. [Journal Article]
- Drug Dev Ind Pharm 2016 Sep 20; :1-31DD
- 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).
- Modified Release Itraconazole Amorphous Solid Dispersion to Treat Aspergillus fumigatus: Importance of the Animal Model Selection. [Journal Article]
- Drug Dev Ind Pharm 2016 Sep 19; :1-35DD
- Previously, modified release itraconazole in the form of a melt-extruded amorphous solid dispersion based on a pH dependent enteric polymer combined with hydrophilic additives (HME-ITZ), exhibited im...
Previously, modified release itraconazole in the form of a melt-extruded amorphous solid dispersion based on a pH dependent enteric polymer combined with hydrophilic additives (HME-ITZ), exhibited improved in vitro dissolution properties. These properties agreed with pharmacokinetic results in rats showing high and sustained itraconazole (ITZ) systemic levels. The objective of the present study was to better understand the best choice of rodent model for evaluating the pharmacokinetic and efficacy of this orally administered modified release ITZ dosage form against invasive Aspergillus fumigatus. A mouse and guinea pig model were investigated and compared to results previously published. In the mouse model, despite similar levels as previously reported values, plasma and lung levels were variable and fungal burden was not statistically different for placebo controls, HME-ITZ and Sporanox ® (ITZ oral solution). This study demonstrated that the mouse model is a poor choice for studying modified release ITZ dosage forms based on pH dependent enteric polymers due to low fluid volume available for dissolution and low intestinal pH. To the contrary, guinea pig was a suitable model to evaluate modified release ITZ dosage forms. Indeed, a significant decrease in lung fungal burden as a result of high and sustained ITZ tissue levels was measured. Sufficiently high intestinal pH and fluids available for dissolution likely facilitated the dissolution process. Despite high ITZ tissue level, the primary therapeutic agent voriconazole exhibited an even more pronounced decrease in fungal burden due to its reported higher clinical efficacy specifically against Aspergillus fumigatus.
- Tear fluid-eye drops compatibility assessment using surface tension. [Journal Article]
- Drug Dev Ind Pharm 2016 Sep 19; :1-21DD
- CONCLUSIONS: There are a number of quality requirements for the eye drops (e.g., tonicity, pH, viscosity, refractive index) that needs to comply with the physiological parameters of the eye surface. However, the adjustment of surface tension properties of the eye drops to the normal range of surface tension at the air/tear fluid interface (40-46 mN/m) has received rather less attention thus far. Yet, the surface tension at the air/tear fluid interface is of vital importance for the normal function of the eye surface.Our results provide a rationale for clinical studies aiming to assess the correlation between the eye drops surface tension and the tear film (in)stability.
- Development of Separation Technology for the Removal of Radium-223 from Targeted Thorium Conjugate Formulations Part I: Purification of Decayed Thorium-227 on Cation Exchange Columns. [Journal Article]
- Drug Dev Ind Pharm 2016 Sep 15; :1-31DD
- Targeted Thorium Conjugates (TTCs) are being explored as a potential future platform for specific tumour targeting pharmaceuticals. In TTCs the alpha emitting radionuclide thorium-227 ((227)Th) with ...
Targeted Thorium Conjugates (TTCs) are being explored as a potential future platform for specific tumour targeting pharmaceuticals. In TTCs the alpha emitting radionuclide thorium-227 ((227)Th) with a half-life of 18.697 days is labelled to targeting moieties, such as monoclonal antibodies (mAbs). The amount of daughter nuclide radium-223 ((223)Ra, t1/2 = 11.435 days) will increase during manufacture and distribution, and so a technology for purification is required to assure an acceptable level of (223)Ra is administrated to the patient. Since (223)Ra is the only progeny of (227)Th with a long half-life (days), the progenies of (223)Ra will have a very limited stay in the formulation once (223)Ra is removed. The focus in this study has therefore been on the removal of (223)Ra. In this study, the sorption and separation of (223)Ra (radium(II)) and (227)Th (thorium(IV)) on cation exchange columns has been evaluated as a purification method of decayed (227)Th (i.e. prior to radiolabelling of a mAb and formation of TTC). The goal is to minimise the sorption of (227)Th and maximise the sorption of (223)Ra. Statistical experimental design with formulation and process parameters, including buffered formulations comprising citrate and acetate, at various concentrations and pH, presence of free radical scavenger and chelator, and resin amount have been evaluated for impact on the purification process. The studies have been interpreted by the aid of multivariate data analysis. The correlations between design of experimental variables and sorption are summarised by regression models. The predictive accuracy of radionuclide sorption was given by standard deviation and 95% confidence intervals originating from statistical cross validation. Experimental results and statistical models for citrate buffered formulations verified reproducible and acceptable sorption levels of (223)Ra and (227)Th under selected conditions. For acetate buffered formulations prediction of (227)Th sorption was influenced by complex variable relationships and hence a risk of obtaining irreproducibility. Fine-tuned variable levels showed, however, variable combinations predicting high sorption of (223)Ra (>90%) and low sorption of (227)Th (<3%) also for the acetate buffered formulations. The optimal separation conditions should be decided based on tuning the variables levels for (223)Ra in the citrate buffered formulations, while for acetate the optimal separation should be based on tuning variable levels for (227)Th sorption. The ionic strength of the formulation also seemed to affect the radionuclide sorption. Labelling of an antibody-chelator conjugate with purified (227)Th (i.e. preparation of TTC) was successful in the selected citrate buffered formulations tested.
- Quality by Design (QbD), Process Analytical Technology (PAT) and Design of Experiment Applied to the Development of Multifunctional Sunscreens. [Journal Article]
- Drug Dev Ind Pharm 2016 Sep 14; :1-30DD
- Multifunctional formulations are of great importance to ensure better skin protection from harm caused by ultraviolet radiation (UV). Despite of the advantages of Quality by Design and Process Analyt...
Multifunctional formulations are of great importance to ensure better skin protection from harm caused by ultraviolet radiation (UV). Despite of the advantages of Quality by Design and Process Analytical Technology approaches to the development and optimization of new products, we found in literature only a few studies concerning their applications in cosmetic product industry. Thus, in this research work, we applied the QbD and PAT approaches to the development of multifunctional sunscreens containing bemotrizinol, ethylhexyl triazone and ferulic acid. In addition, UV transmittance method was applied to assess qualitative and quantitative critical quality attributes of sunscreens using chemometrics analyses. Linear discriminant analysis allowed classifying unknown formulations, which is useful for investigation of counterfeit and adulteration. Simultaneous quantification of ethylhexyl triazone, bemotrizinol, and ferulic acid presented at the formulations was performed using PLS regression. This design allowed to verify the compounds in isolation and in combination and to prove that the antioxidant action of ferulic acid as well as the sunscreen actions, since the presence of this component increased 90% of antioxidant activity in vitro.
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- Crystallisation kinetics of orthorhombic paracetamol from supercooled melts studied by nonisothermal DSC. [Journal Article]
- Drug Dev Ind Pharm 2016 Sep 14; :1-29DD
- A simple and highly reproducible procedure was established for the study of orthorhombic paracetamol crystallization kinetics, comprising melting, quench-cooling of the melt and scanning the formed g...
A simple and highly reproducible procedure was established for the study of orthorhombic paracetamol crystallization kinetics, comprising melting, quench-cooling of the melt and scanning the formed glass by DSC at different heating rates. Results were analysed on the basis of the mean as well as local values of the Avrami exponent, n, the energy of activation, as well as the Šesták-Berggren two-parameter autocatalytic kinetic model. The mean value of the Avrami kinetic exponent, n, ranged between 3 to 5, indicating deviation from the nucleation and growth mechanism underlying the Johnson-Mehl, Avrami-Kolmogorov (JMAK) model. To verify the extent of the deviation, local values of the Avrami exponent as a function of the volume fraction transformed were calculated. Inspection of the local exponent values indicates that the crystallisation mechanism changes over time, possibly reflecting the uncertainty of crystallisation onset, instability of nucleation due to an autocatalytic effect of the crystalline phase, and growth anisotropy due to impingement of spherulites in the last stages of crystallisation. The apparent energy of activation, Ea, has a rather low mean value, close to 81 kJ/mol, which is in agreement with the observed instability of glassy-state paracetamol. Isoconversional methods revealed that Ea tends to decrease with the volume fraction transformed, possibly because of the different energy demands of nucleation and growth. The exponents of the Šesták-Berggren two-parameter model showed that the crystallised fraction influences the process, confirming the complexity of the crystallisation mechanism.