Abstract. Formation of inhalable microparticles containing rifampicin and poly(L-lactide) (L-PLA) by using supercritical anti-solvent process (SAS) was investigated. The solutions of drug and polymer in methylene chloride were sprayed into supercritical carbon dioxide. The effect of polymer content and operating conditions, temperature, pressure, carbon dioxide molar fraction, and concentration of solution, on product characteristics were studied. The prepared microparticles were characterized with respect to their morphology, particle size and size distribution, drug content, drug loading efficiency, and drug release characteristic. Discrete, spherical microparticles were obtained at high polymer:drug ratios of 7:3, 8:2, and 9:1. The shape of L-PLA microparticles became more irregular and agglomerated with decreasing polymer content. Microparticles with polymer content higher than 60% exhibited volumetric mean diameter less than 5 μm, but percent drug loading efficiency was relatively low. Drug-loaded microparticles containing 70% and 80% L-PLA showed a sustainable drug release property without initial burst release. Operating temperature level influenced on mean size and size distribution of microparticles. The operating pressure and carbon dioxide molar fraction in the range investigated were unlikely to have an effect on microparticle formation. An increasing concentration of feed solution provided larger size microparticles. Rifampicin-loaded L-PLA microparticles could be produced by SAS in a size range suitable for dry powder inhaler formulation.

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Co-spray-dried powders of theophylline and ethylcellulose were prepared using aqueous ethylcellulose dispersion. Co-spray-dried powders were directly compressed into the matrices and the release characteristics of the prepared matrices were investigated. The co-spray-dried powders exhibited good matrix formations with high hardness at rather low compression force. The concentration of ethylcellulose in the matrices was, as expected, the rate-determining factor in controlling the release rate of the drug. Increasing the weight fractions of ethylcellulose resulted in a corresponding decrease in the drug release rates in both 0.1 N HCl and phosphate buffer pH 6.8. However, at the same level of ethylcellulose content, the drug release in acidic conditions was higher than in alkaline medium. To modify release characteristics of the matrices, PVP K30 and lactose were employed as channeling agents. At concentrations of 5 and 10%, PVP K30 was found to slow the drug release when incorporated into the co-spray-dried powder formulations containing 5% ethylcellulose. Lactose at a concentration of 15% provided an increasing effect on drug release when added in the formulations. But an increase in lactose quantity from 15 to 25% did not exert much more influence on release characteristics. Higuchi plots were found to be best applicable to all release data. Scanning electron microscopic examinations on the surface and cross-section of the matrices before and after subjection to release testing revealed the formation of porous networks within the matrices by the ethylcellulose fibers. Such polymeric networks would account for the controlled diffusion of the drug from the matrices.

The objective of this study was to assess feasibility of applying shellac as a biopolymer filament for using in fused deposition modeling (FDM) 3D printing. The shellac matrices were prepared through hot melt process by heating the ground shellac samples at 80°C in a silicone oil bath under continuous stirring for 15 min. Accelerated stability testing (annealing process) was also performed in order to evaluated thermal stability by re-heating shellac matrices at 80 °C for 12 h and 24 h in a hot air oven. The shellac matrices and annealed shellac matrices were then comparatively characterized. In the present study, all shellac matrices were investigated for physical appearance, acid value, insoluble solid, moisture content and also characterized by instrument analysis including Fourier-transform infrared (FTIR) spectroscopy, powder X-ray diffractometry (PXRD) and thermal analysis. The results demonstrated that shellac with initial heat (80°C, 15 min) and annealed at 80°C for 12 h had similar properties except the annealed shellac at 80°C for 24 h which shown the lower acid value and formed insoluble solid. The melting temperature, decomposition temperature and melting enthalpy of shellac were around 63-64°C, over than 200°C and 23 J/g, respectively. Furthermore, the extruded filament based on shellac was achieved by hot melt extrusion (HME) technique. The findings revealed that the shellac properties might be suitable to fabricate FDM filaments.

The aim of our study was to evaluate the applicability of yam (Dioscorea sp.) starch and arrowroot (Maranta arundinacea) starch as suspending agents in suspension. Paracetamol was used as a model drug because of its low solubility. It was found that the optimal concentration as suspending agent in paracetamol suspension was in the range of 7-8% for yam starch and 5-6% for arrowroot starch. All formulations were stable within the period of study with pH of 5.4-6.9. These results were comparable to those obtained from the sodium carboxymethyl cellulose (sodium CMC) which is a common suspending agent. It could be concluded that yam starch and arrowroot starch showed suspending activity in paracetamol suspension and could be applied as commercial suspending agent.