04. October 2018
n recent years there has been a growing interest in solid lipid-based systems, particularly in solid lipid microparticles (SLMs); however, only very few studies deeply investigated the dissolution behaviour of orally delivered-SLMs. The present study provides new insights about the release performance in different gastrointestinal fluids of SLMs containing a freely water soluble drug (caffeine, as BCS class I drug). Three different formulations of SLMs were prepared by spray congealing using...
02. October 2018
The formulation of amorphous solid dispersions (ASDs) is an effective way to improve the bioavailability of poorly water-soluble active pharmaceutical ingredients (APIs). The combination of an amorphous state of the drug and the presence of crystallization-inhibiting polymers retains a high amount of dissolved API over time. ASDs with ketoconazole and different polymers were manufactured by spray drying and their characteristics as well as performance were analyzed. Dissolution tests with a...
01. October 2018
The controlled release of caffeine from the casein gel tablets has been achieved over release periods lasting from a few minutes to over a few days. A novel casein gel has been acidified at pH of 1.0 as the insoluble controlled-release matrix and spray-dried with coffee for microencapsulation. The optimal inlet temperature of spray drying for the casein-coffee mixtures has been found to be 150 °C. The elastic casein-coffee tablets have been engineered without denaturing the components (as...
29. September 2018
Tobramycin (TOB) and clarithromycin (CLA) can potentially be used synergistically for the treatment of respiratory infections caused by Pseudomonas aeruginosa (P. aeruginosa) in cystic fibrosis (CF) patients. This study aimed to develop a novel combination proliposome formulation (TOB/CLA-CPROLips) containing both hydrophilic TOB and hydrophobic CLA via a core-carrier approach. The combination proliposomes were produced by spray drying a suspension comprising spray-driedmannitol (SD-MAN, 0.45...
13. September 2018
The study aimed at investigating the potential of spray drying method for encapsulation of protein drugs into solid lipid microparticles (MP) and evaluating effects of excipients on encapsulation and release of protein from MP. After transformation of model protein insulin to insulin-phospholipid complex, it was dissolved together with lipid excipients in organic solvent, which was spray-dried to form solid lipid MP. Polymeric MP with D, L-lactic-co-glycolic acid (PLGA) were prepared similarly....
04. September 2018
A decrease in the release rate over time is typically encountered when dealing with hydrophilic matrix systems for oral prolonged release due to progressive increase of the distance the drugmolecules have to cover to diffuse outwards and reduction of the area of the glassy matrix at the swelling front. In order to solve this issue, a novel formulation approach based on non-uniformdistribution of the active ingredient throughout the swellable polymer matrix was proposed and evaluated. Various...
31. August 2018
Combined micro- and nanosystems are appealing for pulmonary protein delivery, fulfilling the specific physiological requirements for efficient outcomes in-vivo. However, fabrication of protein formulations may impose stresses perturbing protein conformational stability and, hence, biological activity. Herein, a protein, insulin (INS), was nanoencapsulated inside chitosan nanoparticles (CS NPs) by ionic gelation. By spray drying, the resultant protein-loaded NPs were further encapsulated with a...
26. August 2018
The aim of this study was to develop roflumilast dry powder inhaler (DPI) formulations by spray drying using hydroxypropyl-β-cyclodextrin (HPβCD) and to determine their suitability for pulmonary delivery. Different feed solution concentrations, solvent systems and spray drying parameters were used to obtain the formulations which were characterized using X-ray powder diffraction, thermal analysis, scanning electron microscopy, particle size distribution, bulk and tapped density, specific...
16. August 2018
Chlortetracycline hydrochloride (CTC) has been reported as having low aqueous solubility, leading to a limitation in its administration in treatments. This study demonstrated a strategy to enhance the supersaturated solubility of CTC by amorphous solid dispersion (SD). CTC-SDs were prepared with hydrophilic polymers, polyvinylpyrrolidone (PVP) and copovidone using various preparation methods: water bath evaporation, speed vacuum evaporation, and spray drying. Physicochemical properties and...
04. August 2018
In this paper, we explain the crystallization process of mannitol during convective droplet drying based on the crystallization kinetics calculated from two mathematical models coupled with experimental investigations. A novel differential-reaction engineering approach was developed, correlating the mannitol crystallization behavior to the deviation of droplet drying kinetics at different drying temperatures. The model was compared with a conventional glass transition-based model and the...