Abstract: An estimated 40% of approved drugs in the market and nearly 90% of molecules in the developmental pipeline are poorly water-soluble. The challenge to formulate insoluble drugs has met with advent of various insoluble drug formulation technologies. This review discusses the different insoluble drug formulation technologies, the clinical benefits and business potentials are elaborated. PubDate: 04/14/2014 05:15:02 pm
Abstract: This review provides an overview of the use of microscopy as a tool to characterize shape and dimension of micro and nanoparticulate systems. In pharmaceutical field the use of microscopy has been exerted an important role since the advent of micro and nanotechnology. Indeed the morphology of particles and their inner structure does influence the modalities of administration and release of encapsulated drugs. Scanning electron microscopy (SEM) can be employed to study the morphology of dry powders, in particular microparticles made of polymers can be well visualized and their diameters can be measured. By cutting the powder during sample preparation, it is possible to obtain important information about the inner morphology of the microstructures, discriminating either the capsule or the sphere microstructure. Cryo transmission electron microscopy (cryo-TEM) is a precious tool for characterizing colloidal systems. In particular external as well as internal shape of nanoparticulate systems such as solid lipid nanoparticles or lyotropic mesophases can be well identified. Moreover size of disperse phase and the overall structure of the dispersion can be monitored. We provide an overview about the use of electron microscopy as technique for characterizing microparticles and nanosystems recently developed by our research group. In particular polyesters or acrylic polymer microparticles for fenretinide administration are here presented. Moreover, with regard to nanosystems, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) for prednisone and clotrimazole administration and monooleine aqueous dispersion (MAD) are discussed. PubDate: 04/14/2014 05:15:02 pm
Abstract: Drug discovery and development is an intense, lengthy and an inter-disciplinary venture. Recently, a trend towards the use of in-silico chemistry and molecular modeling for computer-aided drug design has gained significant momentum. In-silicodrug design skills are used in nanotechnology, molecular biology, biochemistry etc. The main benefit of thein-silico drug design is cost effective in research and development of drugs. There are wide ranges of software are used in in-silico drug design, Grid computing, window based general PBPK/PD modeling software, PKUDDS for structure based drug design, APIS, JAVA, Perl and Python,in-silico drug design as well as software including software libraries. There are different techniques used in in-silico drug design visualization, homology, molecular dynamic, energy minimization molecular docking and QSAR etc.In-silico drug design can take part considerably in all stages of drug development from the preclinical discovery stage to late stage clinical development. Its exploitation in drug development helps in the selection of only a potent lead molecule and may thus thwart the late stage clinical failures; thereby a major diminution in cost can be achieved. This article gives an insight to all the aspects of in-silico drug design; its potential, drivers, current development and the future prospects. PubDate: 04/14/2014 05:15:02 pm
Abstract: Introduction:Quality by design is a risk management and science based approach promoted by the United States Food and Drug Administration to enhance pharmaceutical development throughout a product’s life cycle. Risk-assessment approaches, Process Analytical Technology tools, mathematical, statistical and continuous improvement tools are important elements of quality by design continuum which mainly focuses on identification of critical parameters and defining a design space statistically. Discussion: In this paper, quality by design principles were discussed on the basis of several published case studies including development of bulk powder, granules, capsules, orally dispersible tablets, botanical drug products, nanoparticles, and biopharmaceutical drugs. The use of quality by design approach in development of different methods, formulations, and systems such as chromatographic and dissolution methods, physiologically absorption models, in situ implant formulations and single-use bioreactors was also considered. Conclusion: Full adoption of quality by design has great long-term benefits including enhanced understanding, well-defined system and regulatory flexibility. Quality by design has a great application potential for almost every step of pharmaceutical development. Industry, academia and regulatory bodies should cooperate to increase the level of quality by design implementation in the future. PubDate: 04/14/2014 05:15:02 pm
Abstract: Introduction:Over the last couple of decades, area of drug delivery has become important for its possible gainings in pharmaceutical industry. Studies shows drug delivery systems which developed by nanotechnology offer the opportunity to achieve more efficient drugs and to minimize side effects. Discussion:The aim of this present article is to overview nanocarrier systems and point to their contributions to drug delivery systems. Pharmaceutical nanocarrier systems offer us plenty of possible solutions for drug delivery difficulties and overcome to important barriers such as ocular, intestinal barriers and blood brain barrier. Conclusion:Novel drug delivery systems can enhance important characteristics of drugs such as bioavailability, drug solubility. Pharmacokinetic and pharmacodynamic properties of drug molecules can be improved by nanotechnology. In spite of all possible advantages of nanosystems they have some practical problems to overcome. Nanosystems have potential to become one of the main human health care products in the future therefore pharmaceutical nanotechnology area needs more studies to completely understand their characteristics. PubDate: 04/14/2014 05:15:02 pm
Abstract: The present paper deals with modeling of the acute toxicity of 56 phenylsulfonyl carboxylates to Vibrio fischeri. Multiple regression analysis (MLR) has been used as the data-processing step for the selection of independent variables. The statistical quality of the best model (without deleting outliers) using topological & indicator parameters is as follows: N=56, R=0.8802, AR2=0.7570, MSE=0.0516, F=43.834 & Q=17.0576 and statistical quality of the best model (after deleting outliers) is as follows: N=53, R=0.9397, AR2=0.8733, MSE=0.0254, F=90.577 & Q=36.9953. Use of the topological and indicator parameters has suggested that negative contributions of steric bulk, branching, functionality of C10, functionality of chloro substituent at X1 position and presence of unsaturation at the substituent(s) on C10, and positive contributions of functionality of O13 and presence of substituent’s with electronegative atoms at R2 and R3 positions. Cross-validation analysis of obtained models has been checked by employing the leave one out (LOO) method. PubDate: 04/14/2014 05:15:02 pm
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