Application of supercritical antisolvent method in drug encapsulation: a review

Kalani, Mahshid; Yunus, Robiah

doi:10.2147/ijn.s19021

Cited by 115 publications

(85 citation statements)

References 75 publications

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“…The effect of density on solubility is more considerable at higher densities. 13 SEM micrographs of products in different pressures at 30°C are shown in Figure 4. The same results occur with other pressures (Figure 5).…”

Section: Structure Of Nanoparticlesmentioning

confidence: 99%

Effect of supercritical fluid density on nanoencapsulated drug particle size using the supercritical antisolvent method

Kalani¹

2012

IJN

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Abstract:The reported work demonstrates and discusses the effect of supercritical fluid density (pressure and temperature of supercritical fluid carbon dioxide) on particle size and distribution using the supercritical antisolvent (SAS) method in the purpose of drug encapsulation. In this study, paracetamol was encapsulated inside L-polylactic acid, a semicrystalline polymer, with different process parameters, including pressure and temperature, using the SAS process. The morphology and particle size of the prepared nanoparticles were determined by scanning electron microscopy and transmission electron microscopy. The results revealed that increasing temperature enhanced mean particle size due to the plasticizing effect. Furthermore, increasing pressure enhanced molecular interaction and solubility; thus, particle size was reduced. Transmission electron microscopy images defined the internal structure of nanoparticles. Thermal characteristics of nanoparticles were also investigated via differential scanning calorimetry. Furthermore, X-ray diffraction pattern revealed the changes in crystallinity structure during the SAS process. In vitro drug release analysis determined the sustained release of paracetamol in over 4 weeks.

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Section: Structure Of Nanoparticlesmentioning

confidence: 99%

Effect of supercritical fluid density on nanoencapsulated drug particle size using the supercritical antisolvent method

Kalani¹

2012

IJN

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“…[13][14][15] The supercritical antisolvent process has been widely utilized to fabricate drug-loaded polymer microparticles. [16][17][18] In the supercritical antisolvent process, an organic solution is sprayed into supercritical CO 2 to effect immediate contact between the two media. Extremely rapid extraction of the organic solvent into supercritical CO 2 leads to higher supersaturation of the solution, creating fast nucleation and growth, and finally micronization of the solute.…”

Section: Introductionmentioning

confidence: 99%

Formation of methotrexate-PLLA-PEG-PLLA composite microspheres by microencapsulation through a process of suspension-enhanced dispersion by supercritical CO2

Chen¹,

Wang²,

Wang³

et al. 2012

IJN

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Background:The aim of this study was to improve the drug loading, encapsulation efficiency, and sustained-release properties of supercritical CO 2 -based drug-loaded polymer carriers via a process of suspension-enhanced dispersion by supercritical CO 2 (SpEDS), which is an advanced version of solution-enhanced dispersion by supercritical CO 2 (SEDS). Methods: Methotrexate nanoparticles were successfully microencapsulated into poly (L-lactide)-poly(ethylene glycol)-poly(L-lactide) (PLLA-PEG-PLLA) by SpEDS. Methotrexate nanoparticles were first prepared by SEDS, then suspended in PLLA-PEG-PLLA solution, and finally microencapsulated into PLLA-PEG-PLLA via SpEDS, where an "injector" was utilized in the suspension delivery system. Results: After microencapsulation, the composite methotrexate (MTX)-PLLA-PEG-PLLA microspheres obtained had a mean particle size of 545 nm, drug loading of 13.7%, and an encapsulation efficiency of 39.2%. After an initial burst release, with around 65% of the total methotrexate being released in the first 3 hours, the MTX-PLLA-PEG-PLLA microspheres released methotrexate in a sustained manner, with 85% of the total methotrexate dose released within 23 hours and nearly 100% within 144 hours. Conclusion: Compared with a parallel study of the coprecipitation process, microencapsulation using SpEDS offered greater potential to manufacture drug-loaded polymer microspheres for a drug delivery system.

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“…A small change in the precipitation temperature can lead to considerable density changes, especially near the critical point. 25 The increased in temperature caused decreased density of scCO 2 , thus resulting in a decrease of the antisolvent effect of scCO 2 . Therefore, achieving supersaturation was slowed and a bigger particle was formed.…”

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confidence: 99%

Formation of curcumin nanoparticles via solution-enhanced dispersion by supercritical CO2

Zhao¹,

Xie²,

Li³

et al. 2015

IJN

132

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In order to enhance the bioavailability of poorly water-soluble curcumin, solution-enhanced dispersion by supercritical carbon dioxide (CO 2 ) (SEDS) was employed to prepare curcumin nanoparticles for the first time. A 2 4 full factorial experiment was designed to determine optimal processing parameters and their influence on the size of the curcumin nanoparticles. Particle size was demonstrated to increase with increased temperature or flow rate of the solution, or with decreased precipitation pressure, under processing conditions with different parameters considered. The single effect of the concentration of the solution on particle size was not significant. Curcumin nanoparticles with a spherical shape and the smallest mean particle size of 325 nm were obtained when the following optimal processing conditions were adopted: P =20 MPa, T =35°C, flow rate of solution =0.5 mL·min −1 , concentration of solution =0.5%. Fourier transform infrared (FTIR) spectroscopy measurement revealed that the chemical composition of curcumin basically remained unchanged. Nevertheless, X-ray powder diffraction (XRPD) and thermal analysis indicated that the crystalline state of the original curcumin decreased after the SEDS process. The solubility and dissolution rate of the curcumin nanoparticles were found to be higher than that of the original curcumin powder (approximately 1.4 μg/mL vs 0.2 μg/mL in 180 minutes). This study revealed that supercritical CO 2 technologies had a great potential in fabricating nanoparticles and improving the bioavailability of poorly water-soluble drugs.

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Application of supercritical antisolvent method in drug encapsulation: a review

Cited by 115 publications

References 75 publications

Effect of supercritical fluid density on nanoencapsulated drug particle size using the supercritical antisolvent method

Effect of supercritical fluid density on nanoencapsulated drug particle size using the supercritical antisolvent method

Formation of methotrexate-PLLA-PEG-PLLA composite microspheres by microencapsulation through a process of suspension-enhanced dispersion by supercritical CO2

Formation of curcumin nanoparticles via solution-enhanced dispersion by supercritical CO2

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