Physicochemical analysis in the evaluation of reconstituted dry emulsion tablets

The aim of this study was to characterize the formation of emulsions by droplet size analysis and turbidimetry during reconstitution from a solid dosage form, namely from dry emulsion systems, which carry an oil phase for poorly soluble active ingredients. For the dry emulsion systems tablets were prepared either from oil-in-water systems using a freeze-drying process or through direct compression containing the same oil and excipients. The ratios of oil to emulgents and oil to xanthan gum were equal in both methods. In the preparation methods applied, mannitol, erythritol and lactose were used as excipients and mannitol was found to be the most effective excipient based on droplet size reconstitution, turbidimetry and physical properties. Quality control involved testing the physical properties of tablets and characterizing the reconstituted emulsions. © 2016 Elsevier B.V

Review on Starter Pellets: Inert and Functional Cores

A significant proportion of pharmaceuticals are now considered multiparticulate systems. Modified-release drug delivery formulations can be designed with engineering precision, and patient-centric dosing can be accomplished relatively easily using multi-unit systems. In many cases, Multiple-Unit Pellet Systems (MUPS) are formulated on the basis of a neutral excipient core which may carry the layered drug surrounded also by functional coating. In the present summary, commonly used starter pellets are presented. The manuscript describes the main properties of the various nuclei related to their micro- and macrostructure. In the case of layered pellets formed based on different inert pellet cores, the drug release mechanism can be expected in detail. Finally, the authors would like to prove the industrial significance of inert cores by presenting some of the commercially available formulations

Study on process parameters and optimization of microencapsulation based on phase separation

As surfactants are capable of influencing the droplet formation, our study primarily aims the investigation of the effect of a nonionic surfactant e.g. Polysorbate 80 on the formation of microspheres on the course of vibrating nozzle method with coacervation. The experiments also concern the impact of the different process parameters (e.g. vibration frequency, feed rate and voltage) on the shape and size distribution of microspheres characterized by laser diffraction size determination completed with particle image analysis. The calcium-alginate microspheres were processed using freeze-drying to ensure solid state with better drug carrier capability. Addition of isomalt was advantageous in the formation of freeze-dried microspheres at low alginate concentration, which was explained by micro-CT analysis of the constructed particle structure. The internal three-dimensional network of calcium alginate demonstrated a more cancellous architecture ameliorating the roundness of microparticles

Nanoformulation of lipase from Porcine pancreas by electrospinning as a novel alternative for enzyme-based per os therapies

Pancreatic enzyme replacement therapy (PERT) treats pancreatic insufficiency, causing a lack of digestive enzymes due to pancreatic damage or dysfunction. However, traditional PERT faces challenges such as poor stability and limited efficiency of the enzymes. Lipase from Porcine pancreas (PpL) is commonly applied for PERT, however only classic formulas such as tablets or capsules produced from physical mixture of the enzyme and excipients had been developed. Electrospinning produces nanofibers that are promising as drug carriers, due to their high surface area-to-volume ratio and tunable physicochemical properties. In this study we investigated the direct nanoformulation of PpL applying polymer nanofibers. The effect of water-soluble and water-resist polymers (PVA: polyvinyl alcohol, PVP: polyvinylpyrrolidone and PLA: polylactic acid) on the physicochemical properties of precursor for electrospinning and on the nanofibers produced from them was systematically investigated. The immobilization of PpL using electrospun nanofibers by entrapment and adsorption methods was developed and compared the enzymatic activities of the nanofibrous formulas. It was found that immobilization using nanofibers in all cases caused a large increase in the enzymatic activity of PpL. Our research demonstrates that nanoformulation of PpL could be efficient by electrospinning technique and the polymer has dominant effect on the enzymatic and structural properties of formulas since PpL entrapped in PLA showed the highest enzymatic activity. Nanofibrous enzyme loaded formulations were compre- hensively studied by rheology, scanning electron (SEM) and Raman microscopy, water content determination, positron annihilation lifetime spectroscopy (PALS) and enzyme activity assay of ester hydrolysis

Evaluation of Drug Release From Coated Pellets Based on Isomalt, Sugar, and Microcrystalline Cellulose Inert Cores

The objective of the present study was to investigate the effect of the pellet core materials isomalt, sugar, and microcrystalline cellulose on the in vitro drug release kinetics of coated sustained-release pellets as well as to evaluate the influence of different ratios of polymethacrylate copolymers exhibiting different permeability characteristics on the drug release rate. For characterization of the drug release process of pellets, the effect of osmolality was studied using glucose as an osmotically active agent in the dissolution medium. The pellet cores were layered with diclofenac sodium as model drug and coated with different ratios of Eudragit® RS30D and Eudragit® RL30D (ERS and ERL; 0:1 and 0.5:0.5 and 1:0 ratio) in a fluid bed apparatus. Physical characteristics such as mechanical strength, shape, and size proved that the inert cores were adequate for further processing. The in vitro dissolution tests were performed using a USP Apparatus I (basket method). The results demonstrated that, besides the ratio of the coating polymers (ERS/ERL), the release mechanism was also influenced by the type of starter core used. Sugar- and isomalt-type pellet cores demonstrated similar drug release profiles