Pressure Homogenization Technique Research Articles

Significantly enhanced bioavailability of niclosamide through submicron lipid emulsions with or without PEG-lipid: a comparative study

Niclosamide (NL) has demonstrated its great potential in fighting against leukaemia recently. However, either oral or systemic delivery of NL is challenged by its insoluble nature. Here, we developed two different NL-loaded submicron lipid emulsions (NL-SLEs) and compared their suitability in bioavailability enhancement. Conventional and PEGylated NL-SLEs (NL-CSLEs and NL-PSLEs) were prepared by melt dispersion/high pressure homogenisation technique. They were about 307.8 and 162.2 nm in particle size, respectively, and both of them possessed satisfactory stability and drug load (>9.0%). After oral administration, significantly enhanced bioavailability was achieved through NL-CSLEs and NL-PSLEs (441.11 and 463.55% relative to the reference). Apart from global size, NL-CSLEs and NL-PSLEs exhibited similar attributes in release, lipolysis, mucin binding, etc. Taken together, SLEs with or without PEG-lipid have shown to be promising for oral delivery of NL. PEG-lipid could significantly reduce the particle size of SLEs. But, macromolecular PEG-lipid was required to effectively stealth the lipid carriers.

Effect of four different size reduction methods on the particle size, solubility enhancement and physical stability of nicergoline nanocrystals

Nicergoline, a poorly soluble active pharmaceutical ingredient, possesses vaso-active properties which causes peripheral and central vasodilatation. In this study, nanocrystals of nicergoline were prepared in an aqueous solution of polysorbate 80 (nanosuspension) by using four different laboratory scale size reduction techniques: high pressure homogenization (HPH), bead milling (BM) and combination techniques (high pressure homogenization followed by bead milling HPH + BM, and bead milling followed by high pressure homogenization BM + HPH). Nanocrystals were investigated regarding to their mean particles size, zeta potential and particle dissolution. A short term physical stability study on nanocrystals stored at three different temperatures (4, 20 and 40 °C) was performed to evaluate the tendency to change in particle size, aggregation and zeta potential. The size reduction technique and the process parameters like milling time, number of homogenization cycles and pressure greatly affected the size of nanocrystals. Among the techniques used, the combination techniques showed superior and consistent particle size reduction compared to the other two methods, HPH + BM and BM + HPH giving nanocrystals of a mean particle size of 260 and 353 nm, respectively. The particle dissolution was increased for any nanocrystals samples, but it was particularly increased by HPH and combination techniques. Independently to the production method, nicergoline nanocrystals showed slight increase in particle size over the time, but remained below 500 nm at 20 °C and refrigeration conditions.

Formulation and Evaluation of Solid Lipid Nanoparticles of Quetiapine Fumarate and Quetiapine Hemifumarate for Brain Delivery in Rat Model

Quatiepine, an effective atypical anti psychotic administered as fumarate or hemifumarate salts by intravenous injection shows poor brain uptake due to low partitioning and/or Pgp efflux. In order to improve their brain availability, solid lipid nanoparticles (SLN) loaded with Quetiapine fumarate or hemifumarate were prepared using glyceryl monostearate (GMS), poloxamer 407 and hydrogenated soya phosphatidylcholine (HSPC) as stabilizers–using a hot melt emulsification high- pressure homogenization technique. They were characterized for physical characteristics like particle size, polydispersity (PDI), shape and entrapment efficiency (EE). Fomulation and process parameters were optimized based on particle size, PDI and EE. SLNs with a mean particle size of 101.1 nm were obtained for quetiapine fumarate and 93.6 nm for quetiapine hemifumarate. In vitro drug release study showed the release followed Higuchi kinetics model for both the formulations. In vivo studies showed a significant increase in the percentage of drug reaching the brain when administered in the form of SLN’s as compared to the respective drug solutions and the increase was greater in case of quetiapine hemifumarate salt.

Einsatz der Druckhomogenisierung zur Herstellung von zellstrukturiertem Apfelmaterial

Materials with cellular structure advantageously can be prepared from apple parenchyma using the pressure homogenisation technique on aqueous-ethanolic conditions. Compared to pure aqueous conditions homogenisation in aqueous-ethanolic environment gives higher yield of disintegrated material having an improved water-binding capacity while the necessary amounts of solvents are decreased. A procedure of 3 homogenisation steps at 60 bar in a mixture of water and ethanol leads to a material with cellular structure, 60% of which consist of particles with a size of 80 to 250 μm and a sufficient quality of colour (L-values in a range from 86 to 91). Such a homogenisation procedure doesn't result in a significant loss of water-binding capacity of the produced materials compared to preparations without homogenisation steps.