Dissolution enhancement of indomethacin-chitosan hydrochloride composite particles produced using supercritical assisted atomization

Wu, Hsien-Tsung; Yang, Ching‐Chieh; Huang, Shih-Chang

doi:10.1016/j.jtice.2016.08.012

Cited by 14 publications

(6 citation statements)

References 21 publications

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“…The XRD results showed a reduction in the intensity of the characteristic peaks (19.2°, 23.4°) of all the LTSAA-PEG particles, compared to those of the as-receive PEG, which in turn suggested the presence of amorphous polymer and/or metastable folded forms in the LTSAA-PEG powder samples. Similar decreased crystallinity has been observed, mainly in SAA-related polymer particles, e.g., PMMA, PLLA, chitosan, and IMC-CH composite [3,12,15,31]. However, the presence of crystalline particles produced by the SAA process was still observed in some materials, e.g., mannitol and PEG, and was attributed to the crystallization rate being higher than the evaporation rate [13,32].…”

Section: Resultssupporting

confidence: 61%

“…In pharmaceutical applications, PEG has been used as laxatives, ointments, fillings for gelatin capsules, solubilizers, tablet excipients, and carriers to improve the dissolution rate of drug. Such enhanced dissolution properties were achieved by the micronization of the drugs, transformation of the drug into a crystalline or amorphous form, the formation of a solid dispersion, and the increase of the wettability of the drug through the use of a water-soluble carrier in composite particles [2,3,4,5]. In addition, hydrophilic PEG can mask the surface of hydrophobic materials and prevent recognition by the immune system, resulting in prolonged system circulation and bypass of the RES (reticuloendothelial system) [6,7].…”

Section: Introductionmentioning

confidence: 99%

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Formation of Polyethylene Glycol Particles Using a Low-Temperature Supercritical Assisted Atomization Process

Tsai

2019

Molecules

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Polyethylene glycol (PEG) particles were prepared using low-temperature supercritical assisted atomization (LTSAA) with carbon dioxide as the spraying medium or the co-solute and acetone as the solvent. The effects of several key factors on the particle size were investigated. These factors included the concentration of the PEG solution, precipitator temperature, saturator temperature, ratio of the volumetric flow rate of carbon dioxide to the PEG solution, and the molecular weight of PEG. Spherical and non-aggregated PEG particles, with a mean size of 1.7–3.2 µm, were obtained in this study. The optimal conditions to produce fine particles were found to be a low concentration of the PEG solution, a low precipitator temperature, and low molecular weight of the PEG. The phase behavior of the solution mixture in the saturator presented a qualitative relationship. At the optimized volumetric flow rate ratios, the composition of CO2 in the feed streams was near the bubble points of the saturator temperatures. X-ray and differential scanning calorimetry analyses indicated that LTSAA-treated PEG had a reduced degree of crystallinity, which could be modulated via the precipitator temperature. PEG microparticles prepared by a LTSAA process would be promising carriers for drug-controlled formulations of PEG-drug composite particles.

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Section: Resultssupporting

confidence: 61%

Section: Introductionmentioning

confidence: 99%

Formation of Polyethylene Glycol Particles Using a Low-Temperature Supercritical Assisted Atomization Process

Tsai

2019

Molecules

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“…Water, ethanol, methanol, and acetone are mainly employed, pure or mixed, to process active compounds using the SAA technique. However, until now, sub-micrometric particles have mostly been prepared by SAA [136][137][138][139], while pharmaceutical nanoparticles have been produced in few papers [36,133,140]. Briefly, SAA is based on the solubilization of a controlled amount of scCO 2 in a liquid solution consisting of the solvents and solutes to be nanonized.…”

Section: Production Of Nanoparticles By Using Co 2 As a Co-solutementioning

confidence: 99%

“…When operating at low GLR values, as well as at low temperatures in the precipitator, the time required for the complete evaporation of the liquid solvents increases; thus, the precipitation of the solute/solutes occurs slowly. A GLR value of 1.8 has often been found to be the most effective for the attainment of spherical particles by SAA [133,136,137,139,141]. The concentration of the solute/solutes in the liquid solution can also strongly influence the particle size [133,138,142].…”

Section: Production Of Nanoparticles By Using Co 2 As a Co-solutementioning

confidence: 99%

Nanoparticles and Nanocrystals by Supercritical CO2-Assisted Techniques for Pharmaceutical Applications: A Review

Franco

Marco

2021

Applied Sciences

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Many active ingredients currently prescribed show limited therapeutic efficacy, mainly due to their dissolution rate inadequate to treat the pathology of interest. A large drug particle size creates an additional problem if a specific site of action in the human body has to be reached. For this reason, active ingredient size reduction using micronization/nanonization techniques is a valid approach to improve the efficacy of active compounds. Supercritical carbon-dioxide-assisted technologies enable the production of different morphologies of different sizes, including nanoparticles and nanocrystals, by modulating operating conditions. Supercritical fluid-based processes have numerous advantages over techniques conventionally employed to produce nanosized particles or crystals, such as reduced use of toxic solvents, which are completely removed from the final product, ensuring safety for patients. Active compounds can be processed alone by supercritical techniques, although polymeric carriers are often added as stabilizers, to control the drug release on the basis of the desired therapeutic effect, as well as to improve drug processability with the chosen technology. This updated review on the application of supercritical micronization/nanonization techniques in the pharmaceutical field aims at highlighting the most effective current results, operating conditions, advantages, and limitations, providing future perspectives.

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“…In general, the production of smaller particles with a spherical crystal habit, which provides an enhanced dissolution profile and superior powder flowability, is favorable for drug design and development. In addition, the application of supercritical fluid crystallization, a nonconventional 2 of 11 crystallization technique, for the micronization and particle design of APIs has also been discussed and reviewed in the literature [7][8][9].…”

Section: Introductionmentioning

confidence: 99%

Recrystallization and Production of Spherical Submicron Particles of Sulfasalazine Using a Supercritical Antisolvent Process

2018

Crystals

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Abstract:In this study, the recrystallization and production of spherical submicron particles of sulfasalazine, an active pharmaceutical ingredient (API), were performed using the supercritical antisolvent (SAS) process, a nonconventional crystallization technique. Sulfasalazine was dissolved in tetrahydrofuran (THF), and supercritical carbon dioxide (CO 2 ) served as the antisolvent. The effects of operating parameters on the SAS process, including the operating pressure, solution concentration, solution flowrate, CO 2 flowrate, and spraying nozzle diameter, at two operating temperatures were examined. The solid-state characteristics of sulfasalazine before and after the SAS process, including particle size, crystal habit, and crystal form, were analyzed using a scanning electron microscope (SEM), powder X-ray diffractometer (PXRD), and differential scanning calorimeter (DSC). A higher operating temperature, intermediate operating pressure, higher CO 2 flowrate, and lower solution flowrate are recommended to obtain spherical particles of sulfasalazine. The effects of the solution concentration and spraying nozzle diameter on the SAS process were negligible. Under optimal conditions, spherical sulfasalazine crystals with a mean size of 0.91 µm were generated, and this study demonstrated the feasibility for tuning the solid-state characteristics of API through the SAS process.

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Dissolution enhancement of indomethacin-chitosan hydrochloride composite particles produced using supercritical assisted atomization

Cited by 14 publications

References 21 publications

Formation of Polyethylene Glycol Particles Using a Low-Temperature Supercritical Assisted Atomization Process

Formation of Polyethylene Glycol Particles Using a Low-Temperature Supercritical Assisted Atomization Process

Nanoparticles and Nanocrystals by Supercritical CO2-Assisted Techniques for Pharmaceutical Applications: A Review

Recrystallization and Production of Spherical Submicron Particles of Sulfasalazine Using a Supercritical Antisolvent Process

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