Preparation of Daidzein Microparticles through Liquid Antisolvent Precipitation Under Ultrasonication

Molecules with poor aqueous solubility are difficult to formulate using conventional approaches and are associated with many formulation delivery issues. To overcome these obstacles, nanosuspension technology can be one of the promising approaches. Hence, in this study, the feasibility of mefenamic acid (MA) oral nanosuspension was investigated for pediatric delivery by studying the role of excipients and optimizing the techniques. Nanosuspensions of MA were prepared by adopting an antisolvent precipitation method, followed by ultrasonication with varying concentrations of polymers, surfactants, and microfluidics. The prepared nanosuspensions were evaluated for particle size, morphology, and rheological measures. Hydroxypropyl methylcellulose (HPMC) with varying concentrations and different stabilizers including Tween® 80 and sodium dodecyl sulfate (SLS) were used to restrain the particle size growth of the developed nanosuspension. The optimized nanosuspension formula was stable for more than 3 weeks and showed a reduced particle size of 510 nm with a polydispersity index of 0.329. It was observed that the type and ratio of polymer stabilizers were responsive on the particle contour and dimension and stability. We have developed a biologically compatible oral nanoformulation for a first-in-class drug beautifully designed for pediatric delivery that will be progressed toward further in vivo enabling studies. Finally, the nanosuspension could be considered a promising carrier for pediatric delivery of MA through the oral route with enhanced biological impact.

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Goodbye fouling: A unique coaxial lamination mixer (CLM) enabled by two-photon polymerization for the stable production of monodisperse drug carrier nanoparticles

Lab on a Chip ◽

10.1039/d1lc00047k ◽

2021 ◽

Author(s):

Peer Erfle ◽

Juliane Riewe ◽

Heike Bunjes ◽

Andreas Dietzel

Keyword(s):

Drug Carrier ◽

Poorly Soluble Drugs ◽

Microfluidic Systems ◽

Routes Of Administration ◽

Two Photon ◽

Antisolvent Precipitation ◽

Stable Production ◽

Poorly Soluble ◽

Two Photon Polymerization

Poorly soluble drugs can be incorporated in lipid carrier nanoparticles to achieve sufficient bioavailability and open up diverse routes of administration. Preparation by antisolvent precipitation in microfluidic systems enables excellent...

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Emamectin benzoate-loaded zein nanoparticles produced by antisolvent precipitation method

Polymer Testing ◽

10.1016/j.polymertesting.2020.107020 ◽

2021 ◽

Vol 94 ◽

pp. 107020

Author(s):

Bo Cui ◽

Jing Li ◽

Ziyang Lai ◽

Fei Gao ◽

Zhanghua Zeng ◽

...

Keyword(s):

Precipitation Method ◽

Emamectin Benzoate ◽

Antisolvent Precipitation

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Enhanced Water Solubility and Oral Bioavailability of Paclitaxel Crystal Powders through an Innovative Antisolvent Precipitation Process: Antisolvent Crystallization Using Ionic Liquids as Solvent

Pharmaceutics ◽

10.3390/pharmaceutics12111008 ◽

2020 ◽

Vol 12 (11) ◽

pp. 1008 ◽

Cited By ~ 1

Author(s):

Qilei Yang ◽

Chang Zu ◽

Wengang Li ◽

Weiwei Wu ◽

Yunlong Ge ◽

...

Keyword(s):

Oral Bioavailability ◽

High Performance ◽

Water Solubility ◽

Water Soluble ◽

Precipitation Process ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Antisolvent Precipitation ◽

Antisolvent Crystallization ◽

Artificial Gastric Juice

Paclitaxel (PTX) is a poor water-soluble antineoplastic drug with significant antitumor activity. However, its low bioavailability is a major obstacle for its biomedical applications. Thus, this experiment is designed to prepare PTX crystal powders through an antisolvent precipitation process using 1-hexyl-3-methylimidazolium bromide (HMImBr) as solvent and water as an antisolvent. The factors influencing saturation solubility of PTX crystal powders in water in water were optimized using a single-factor design. The optimum conditions for the antisolvent precipitation process were as follows: 50 mg/mL concentration of the PTX solution, 25 °C temperature, and 1:7 solvent-to-antisolvent ratio. The PTX crystal powders were characterized via scanning electron microscopy, Fourier transform infrared spectroscopy, high-performance liquid chromatography–mass spectrometry, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, Raman spectroscopy, solid-state nuclear magnetic resonance, and dissolution and oral bioavailability studies. Results showed that the chemical structure of PTX crystal powders were unchanged; however, precipitation of the crystalline structure changed. The dissolution test showed that the dissolution rate and solubility of PTX crystal powders were nearly 3.21-folds higher compared to raw PTX in water, and 1.27 times higher in artificial gastric juice. Meanwhile, the bioavailability of PTX crystal increased 10.88 times than raw PTX. These results suggested that PTX crystal powders might have potential value to become a new oral PTX formulation with high bioavailability.

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Physicochemical Properties and In Vitro Dissolution of Spiramycin Microparticles Using the Homogenate-Antisolvent Precipitation Process

Applied Sciences ◽

10.3390/app7010010 ◽

2016 ◽

Vol 7 (1) ◽

pp. 10 ◽

Cited By ~ 5

Author(s):

Xiaonan Zhang ◽

Xia Wu ◽

Fengying Xie ◽

Zhongjiang Wang ◽

Xiuling Zhang ◽

...

Keyword(s):

Physicochemical Properties ◽

In Vitro Dissolution ◽

Precipitation Process ◽

Antisolvent Precipitation

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Nanocrystalline cerium oxide produced by supercritical antisolvent precipitation as a support for high-activity gold catalysts

Journal of Catalysis ◽

10.1016/j.jcat.2007.04.016 ◽

2007 ◽

Vol 249 (2) ◽

pp. 208-219 ◽

Cited By ~ 68

Author(s):

Z TANG ◽

J EDWARDS ◽

J BARTLEY ◽

S TAYLOR ◽

A CARLEY ◽

...

Keyword(s):

High Activity ◽

Cerium Oxide ◽

Gold Catalysts ◽

Antisolvent Precipitation ◽

Supercritical Antisolvent ◽

Supercritical Antisolvent Precipitation

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Photocatalytic degradation of atrazine under visible light using Gd-doped ZnO prepared by supercritical antisolvent precipitation route

Catalysis Today ◽

10.1016/j.cattod.2021.09.025 ◽

2021 ◽

Author(s):

Paola Franco ◽

Wanda Navarra ◽

Olga Sacco ◽

Iolanda De Marco ◽

Antonietta Mancuso ◽

...

Keyword(s):

Visible Light ◽

Photocatalytic Degradation ◽

Antisolvent Precipitation ◽

Supercritical Antisolvent ◽

Supercritical Antisolvent Precipitation ◽

Doped Zno

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PREPARATION AND CHARACTERIZATION OF NANOCRYSTALS FOR SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF PALIPERIDONE USING DIFFERENT HYDROPHILIC CARRIERS: IN VITRO-IN VIVO STUDY

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i4.24964 ◽

2018 ◽

Vol 11 (4) ◽

pp. 393

Author(s):

Moon Rajkumar ◽

Gattani Surendra

Keyword(s):

Dissolution Rate ◽

Antipsychotic Agent ◽

Aqueous Solubility ◽

In Vivo Study ◽

Scanning Calorimetry ◽

Antisolvent Precipitation ◽

Enhanced Solubility ◽

Pure Drug

Objective: The objective of this study was to increase the solubility and dissolution rate of paliperidone (PAL) by preparing its nanocrystals using different hydrophilic carriers by antisolvent precipitation technique.Methods: The nanoparticles (NP) were characterized for aqueous solubility, drug content, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, particle size, and in vitro-in vivo analysis.Results: The results showed improved solubility and dissolution rate of NPs when compared to pure drug and physical mixture (PM). Solubility data showed a linear graph giving an indication that there is a gradual increase in the solubility profile of the drug with an increase in concentration of the carriers. At highest concentration, the solubility of NPs with Plasdone S630, Povidone K-25, and PVP K-30 found to be increased by 12 folds, 9 folds and 6 folds, respectively, as compared to pure drug. The release profile of NPs with Plasdone S630 in terms of dissolution efficiency at 60 min (DE60), initial dissolution rate (IDR), amount release in 15 min (Q15 min), and time for 75% release (t75%) shows better results when compared to pure drug, PM, and also NPs with povidone 25 and povidone 30. In vivo study reveals that optimized NPs elicited significant induction of cataleptic behavior which is the indication of antipsychotic agent(s) effect.Conclusion: The process antisolvent precipitation under constant stirring may be a promising method to produce stable PAL NPs with markedly enhanced solubility and dissolution rate due to nanonization with the increased surface area, improved wettability, and reduced diffusion pathway.

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