A combinational supercritical CO2 system for nanoparticle preparation of indomethacin

Tozuka, Yuichi; Miyazaki, Y.; Takeuchi, Hirofumi

doi:10.1016/j.ijpharm.2009.10.044

Cited by 50 publications

(9 citation statements)

References 27 publications

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“…As shown in Figure 6A, the raw crystal powder showed diffraction peaks at 11.6, 17.3, 19.6, 21.8, and 26.6, ranging from 2.5°-50° (2θ), suggesting that the drug was highly crystalline in nature. 35,36 The same diffraction peaks were also observed in samples of the physical mixture. The diffraction peaks for the drug taken from samples of the original nanosuspensions disappeared, indicating that the drug particles were present in an amorphous state.…”

Section: Powder X-ray Diffraction and Dscsupporting

confidence: 68%

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Lü²,

Qi³

et al. 2013

IJN

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Background: Drug nanosuspensions are very promising for enhancing the dissolution and bioavailability of drugs that are poorly soluble in water. However, the poor stability of nanosuspensions, reflected in particle growth, aggregation/agglomeration, and change in crystallinity state greatly limits their applications. Solidification of nanosuspensions is an ideal strategy for addressing this problem. Hence, the present work aimed to convert drug nanosuspensions into pellets using fluid-bed coating technology. Methods: Indomethacin nanosuspensions were prepared by the precipitation-ultrasonication method using food proteins (soybean protein isolate, whey protein isolate, β-lactoglobulin) as stabilizers. Dried nanosuspensions were prepared by coating the nanosuspensions onto pellets. The redispersibility, drug dissolution, solid-state forms, and morphology of the dried nanosuspensions were evaluated. Results: The mean particle size for the nanosuspensions stabilized using soybean protein isolate, whey protein isolate, and β-lactoglobulin was 588 nm, 320 nm, and 243 nm, respectively. The nanosuspensions could be successfully layered onto pellets with high coating efficiency. Both the dried nanosuspensions and nanosuspensions in their original amorphous state and not influenced by the fluid-bed coating drying process could be redispersed in water, maintaining their original particle size and size distribution. Both the dried nanosuspensions and the original drug nanosuspensions showed similar dissolution profiles, which were both much faster than that of the raw crystals. Conclusion: Fluid-bed coating technology has potential for use in the solidification of drug nanosuspensions.

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Section: Powder X-ray Diffraction and Dscsupporting

confidence: 68%

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Lü²,

Qi³

et al. 2013

IJN

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“…Amongst these, Rapid Expansion of a Supercritical Solution into a Liquid Solvent (RESOLV) [22] and Rapid Expansion from Supercritical to Aqueous Solution (RESAS) [84,85] are the most notable ones. In RESOLV, the traditional RESS is modified by expanding the supercritical solution into a liquid solvent instead of ambient air.…”

Section: Summary Of Ress Applications For Production Of Spherical Nanmentioning

confidence: 99%

“…Presence of a stabilizer minimizes the particle aggregation by rapidly reducing the surface free energy of the primary particles generated and via steric stabilization [84]. Tozuka et al [85] successfully used 1% polyvinyl alcohol (PVA) for the same protective effect to produce indomethacin nanocrystals of 300-500 nm, via RESAS process.…”

Section: Summary Of Ress Applications For Production Of Spherical Nanmentioning

confidence: 99%

Nanoparticles in the Pharmaceutical Industry and the Use of Supercritical Fluid Technologies for Nanoparticle Production

Sheth

Sandhu²,

Singhal³

et al. 2012

CDD

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Poor aqueous solubility of drug candidates is a major challenge for the pharmaceutical scientists involved in drug development. Particle size reduction appears as an effective and versatile option for solubility improvement. Nanonization is an attractive solution to improve the bioavailability of the poorly soluble drugs, improved therapies, in vivo imaging, in vitro diagnostics and for the production of biomaterials and active implants. In drug delivery, application of nanotechnology is commonly referred to as Nano Drug Delivery Systems (NDDS). In this article, commercially available nanosized drugs, their dosage forms and proprietors, as well as the methods used for preparation like milling, high pressure homogenization, vacuum deposition, and high temperature evaporation were listed. Unlike the traditional methods used for the particle size reduction, supercritical fluid-processing techniques offer advantages ranging from superior particle size control to clean processing. The primary focus of this review article is the use of supercritical CO2 based technologies for small particle generation. Particles that have the smooth surfaces, small particle size and distribution and free flowing can be obtained with particular SCF techniques. In almost all techniques, the dominating process variables may be thermodynamic and aerodynamic in nature, and the design of the particle collection environment. Rapid Expansion of Supercritical Solutions (RESS), Supercritical Anti Solvent (SAS) and Particles from Gas Saturated Solutions (PGSS) are three groups of processes which lead to the production of fine and monodisperse powders. Few of them may also control crystal polymorphism. Among the aforementioned processes, RESS involves dissolving a drug in a supercritical fluid (SCF) and passing it through an appropriate nozzle. Rapid depressurization of this solution causes an extremely rapid nucleation of the product. This process has been known for a long time but its application is limited. Carbon dioxide, which is the only supercritical fluid that is preferentially used in pharmaceutical processes, is not a good solvent for many Active Pharmaceutical Ingredients (API). Various researchers have modified the RESS process to overcome its solubilizing limitations, by introducing RESOLV, RESAS, and RESS-SC. Overall, all RESS based processes are difficult to scale up. The SAS processes are based on decreasing the solvent power of a polar organic solvent in which the substrate (API & polymer of interest) is dissolved, by saturating it with carbon dioxide (CO2) at supercritical conditions. CO2 causes precipitation and recrystalization of the drug. SAS is scalable and can be applied to a wide variety of APIs and polymers. Minor modifications of basic SAS process include GAS, ASES, SAS-DEM and SAS-EM. Processes where SCF is used as an anti solvent and dispersing agent include SEDS, SAA, and A-SAIS. The mechanisms and applications of these processes were briefly discussed. In PGSS, CO2 is dissolved in organic solutions or melted compound...

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“…The reliability of this process is demonstrated by the formation of lysozyme nanoparticles that retain the protein biological activity. An improved system using both supercritical antisolvent precipitation and rapid expansion from supercritical to aqueous solution (RESAS) was proposed to overcome the problem of low solubility of medicinal substances in supercritical CO 2 [189]. On the other hand, supercritical CO 2 methods cannot be easily applied to the production of polymer nanocarriers because of the insolubility of organic polymers in supercritical CO 2 [190].…”

Section: Nanocarriersmentioning

confidence: 99%

Targeted Delivery of Protein Drugs by Nanocarriers

2010

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Recent advances in biotechnology demonstrate that peptides and proteins are the basis of a new generation of drugs. However, the transportation of protein drugs in the body is limited by their high molecular weight, which prevents the crossing of tissue barriers, and by their short lifetime due to immuno response and enzymatic degradation. Moreover, the ability to selectively deliver drugs to target organs, tissues or cells is a major challenge in the treatment of several human diseases, including cancer. Indeed, targeted delivery can be much more efficient than systemic application, while improving bioavailability and limiting undesirable side effects. This review describes how the use of targeted nanocarriers such as nanoparticles and liposomes can improve the pharmacokinetic properties of protein drugs, thus increasing their safety and maximizing the therapeutic effect.

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A combinational supercritical CO2 system for nanoparticle preparation of indomethacin

Cited by 50 publications

References 27 publications

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Formulating food protein-stabilized indomethacin nanosuspensions into pellets by fluid-bed coating technology: physical characterization, redispersibility, and dissolution

Nanoparticles in the Pharmaceutical Industry and the Use of Supercritical Fluid Technologies for Nanoparticle Production

Targeted Delivery of Protein Drugs by Nanocarriers

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