ARTIFICIAL NEURAL NETWORKS: FUNCTIONINGANDAPPLICATIONS IN PHARMACEUTICAL INDUSTRY

Artificial Neural Network (ANN) technology is a group of computer designed algorithms for simulating neurological processing to process information and produce outcomes like the thinking process of humans in learning, decision making and solving problems. The uniqueness of ANN is its ability to deliver desirable results even with the help of incomplete or historical data results without a need for structured experimental design by modeling and pattern recognition. It imbibes data through repetition with suitable learning models, similarly to humans, without actual programming. It leverages its ability by processing elements connected with the user given inputs which transfers as a function and provides as output. Moreover, the present output by ANN is a combinational effect of data collected from previous inputs and the current responsiveness of the system. Technically, ANN is associated with highly monitored network along with a back propagation learning standard. Due to its exceptional predictability, the current uses of ANN can be applied to many more disciplines in the area of science which requires multivariate data analysis. In the pharmaceutical process, this flexible tool is used to simulate various non-linear relationships. It also finds its application in the enhancement of pre-formulation parameters for predicting physicochemical properties of drug substances. It also finds its applications in pharmaceutical research, medicinal chemistry, QSAR study, pharmaceutical instrumental engineering. Its multi-objective concurrent optimization is adopted in the drug discovery process, protein structure, rational data analysis also

RECENT UPDATE ON ORAL FILMS: A BENCH TO MARKET POTENTIAL

Oral films are gaining a lot of attention as a substitute approach to the conventional dosage form. Over the past few years, many of the pharmaceutical scientists throughout the world are focusing their research on oral films, trying to see the sights of oral films as a novel drug delivery system. The oral films are convenient to swallow for geriatric and pediatric patients, are self-administrable, used for systemic and local action and rapid release of a drug, which makes it an excellent system of drug delivery. This review article mainly discusses the manufacturing aspects of films and their characterization, applications and the constraints in the development of oral films along with highlights of market potential

SCREENING AND OPTIMIZATION OF VALACYCLOVIR NIOSOMES BY DESIGN OF EXPERIMENTS

Objective: The objective of the study was to perform a screening, optimization of valacyclovir niosomal formulation to achieve a sustained release of drug using the design of experiments by 32 full factorial design.Methods: Valacyclovir loaded niosomes were prepared using thin film hydration method by varying the ratio of Span 60 and Cholesterol. The prepared niosomes were evaluated for vesicle size, entrapment efficiency, cumulative drug release, fourier transformed infrared spectroscopy (FTIR), zeta potential and surface morphology by field emission scanning electron microscopy (FESEM).Results: The valacyclovir was successfully encapsulated and its entrapment efficiency ranged from 36.70 % to 50.62 %. The average vesicle size of the niosomes was found to be 431 to 623 nm. At 8th hour the drug release varied from 77.50% to 96.31 %. The optimized niosomes were multilamellar with a surface charge potential of about-43.2 mV. The studies revealed that the interaction of cholesterol and surfactant had a substantial effect on vesicle size, entrapment efficiency and drug release from the niosomes. The release kinetics of the optimized niosomes followed zero order kinetics with fickian diffusion controlled mechanism. The stability studies were performed for the optimized formulation and found that the formulation is stable at 4°C ± 2°C.Conclusion: Model equations were developed for the responses. No significant difference was observed between the predicted and observed value, showing that the developed model is reliable

23 Full Factorial Model for Particle Size Optimization of Methotrexate Loaded Chitosan Nanocarriers: A Design of Experiments (DoE) Approach

Purpose. To build and inquire a statistically significant mathematical model for manufacturing methotrexate loaded chitosan nanoparticles (CsNP) of desired particle size. The study was also performed to evaluate the effect of formulation variables in the explored design space. Method. Ionotropic gelation technique was followed for chitosan nanocarriers by changing formulation variables suggested as per Design Expert software. Altering the levels of Chitosan, tripolyphosphate, methotrexate by 23 factorial design served the purpose. The CsNP were characterized for nanocarrier formation, particle size, and statistical analysis. Then mathematical model was statistically analyzed for fabricating desired formulation having particle size less than 200nm. Results. FT-IR, XRD reports confirmed the structural change in chitosan which lead to the formation of CsNP. For particle size, linear model was found to be best fit to explain effect of variables. Besides, high R2 (0.9958) defends the constancy of constructed model. Chitosan exhibited higher t-value in Pareto chart and a p-value <0.0001. Based on maximum desirability, optimization was performed and amount of variables for preparing CsNP of 180nm was predicted. The experiment was carried out with software suggested combination and particle size was found to be 176±4nm. Conclusion. Low p-value endorsed the greater dominance of chitosan on particle size. Good model adequacy and small percentage error between predicted and experimented value established the reliability of constructed model for robust preparation of CsNP

Conformational effects of C-alpha,C-alpha-dipropargylglycine as a constrained residue

A useful synthon to approach artificial phenylalanyl peptides in a [2 + 2 + 2] cycloaddition reaction, C-alpha,C-alpha-dipropargylglycine (Dprg) is examined for its conformational preferences as a constrained residue. Crystal structure analysis and preliminary NMR results establish possible preference of the residue for folded (alpha) rather than extended (beta) region of the phi,psi conformational space. Boc-Dprg-L-Leu-OMe (1) displays two molecular conformations within the same crystallographic asymmetric unit, with Dprg in the alpha (R) or alpha (L) conformation, participating in a type I beta -turn or an alpha (L)-alpha (R)-type fold, in which Leu(2) assumes the alpha (R) conformation stereochemically favored for an L-chiral residue. Boc-Dprg-D-Val-L-Leu-OMe (2) displays a type I ' beta -turn conformation in crystal, with both Dprg(1) and D-Val(2) assuming the alpha (L) conformation stereochemically favored for a D-chiral residue, with 4 --> 1 type hydrogen bond linking L-Leu(3) NH is with Boc CO. NMR analysis using temperature variation, solvent titration, and a spin probe study suggests a fully soh,ent-exposed nature of Dprg NH, ruling out a fully extended C-5-type conformation for this residue, and soli,ent sequestered nature of L-Leu(3) NH, suggesting possibility of a beta -turn due to Dprg assuming a folded conformation. (C) 2001 , Inc

Ethyl 2-formamido-2-(4-iodobenzyl)-3-(4-iodophenyl)propionate and ethyl 2-(3-bromobenzyl)-3-(3-bromophenyl)-2-formamidopropionate

The title compounds, C19H19I2NO3 and C19H19Br2NO3, are derivatives of alpha-aminoisobutyric acid with halogen substituents at the para and meta positions, respectively. The ethoxycarbonyl and formamide side chains attached to the C-alpha atom of the molecule adopt extended and folded conformations, respectively. The crystal structures are stabilized by N-H...O, C-H...O, C-Br...O and C-I...O interactions