Conversion of Nanosuspensions into Dry Powders by Spray Drying: A Case Study

Chaubal, Mahesh V.; Popescu, Carmen

doi:10.1007/s11095-008-9625-0

Cited by 195 publications

(92 citation statements)

References 18 publications

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“…The nanosuspension pellets showed dissolution profiles similar to those of the original drug nanosuspensions, but with a delay of 3 minutes, which could be explained by the fact that reconstitution of the compactly coated pellets took longer. 33,34 It is concluded that the dissolution capacity of the original nanosuspensions was preserved in the solidified nanosuspensions.…”

Section: In Vitro Dissolutionmentioning

confidence: 99%

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: In Vitro Dissolutionmentioning

confidence: 99%

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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“…Such a coating would have created particle repulsions during spray-drying and inhibited the irreversible aggregation of particles. 28 However, 1% of NaTau (w/w of ITZ) seemed to insufficiently cover the entire surface of the particles and did not provide a sufficiently large charge load on the particle surfaces. Therefore, a light agglomeration still SD mannitol occurred in formulation N3.…”

Section: Physicochemical Propertiesmentioning

confidence: 99%

New inhalation-optimized itraconazole nanoparticle-based dry powders for the treatment of invasive pulmonary aspergillosis

Duret¹,

Wauthoz²,

Sebti³

et al. 2012

IJN

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Correspondence: Christophe Duret Université Libre de Bruxelles (ULB), Boulevard du triomphe campus de la plaine (accès 2), Service de pharmacie galénique et biopharmacie, bat BC niveau 6, Brussels, Belgium Tel +32 650 5331 Fax +32 650 5269 Email cduret@ulb.ac.be Purpose: Itraconazole (ITZ) dry powders for inhalation (DPI) composed of nanoparticles (NP) embedded in carrier microparticles were prepared and characterized. Methods: DPIs were initially produced by reducing the ITZ particle size to the nanometer range using high-pressure homogenization with tocopherol polyethylene 1000 succinate (TPGS, 10% w/w ITZ) as a stabilizer. The optimized nanosuspension and the initial microsuspension were then spray-dried with different proportions of or in the absence of mannitol and/or sodium taurocholate. DPI characterization was performed using scanning electron microscopy for morphology, laser diffraction to evaluate the size-reduction process, and the size of the dried NP when reconstituted in aqueous media, impaction studies using a multistage liquid impactor to determine the aerodynamic performance and fine-particle fraction that is theoretically able to reach the lung, and dissolution studies to determine the solubility of ITZ. Results: Scanning electron microscopy micrographs showed that the DPI particles were composed of mannitol microparticles with embedded nano-or micro-ITZ crystals. The formulations prepared from the nanosuspension exhibited good flow properties and better fine-particle fractions, ranging from 46.2% ± 0.5% to 63.2% ± 1.7% compared to the 23.1% ± 0.3% that was observed with the formulation produced from the initial microsuspension. Spray-drying affected the NP size by inducing irreversible aggregation, which was able to be minimized by the addition of mannitol and sodium taurocholate before the drying procedure. The ITZ NP-based DPI considerably increased the ITZ solubility (58 ± 2 increased to 96 ± 1 ng/mL) compared with that of raw ITZ or an ITZ microparticle-based DPI (,10 ng/mL). Conclusion: Embedding ITZ NP in inhalable microparticles is a very effective method to produce DPI formulations with optimal aerodynamic properties and enhanced ITZ solubility. These formulations could be applied to other poorly water-soluble drugs and could be a very effective alternative for treating invasive pulmonary aspergillosis.

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“…Recently, the spray dried nanosuspension of itraconazole was prepared. 9) The emphasis was to examine the impact of various formulation and processing parameters on redispersibility of the spray dried nanoparticles and in-vitro dissolution. The in-vivo study was not performed to demonstrate the bioavailability enhancement by nanosuspension.…”

mentioning

confidence: 99%

Physicochemical and Pharmacokinetic Characterization of a Spray-Dried Cefpodoxime Proxetil Nanosuspension

Gao

Qian²,

Zhang

2010

CHEMICAL & PHARMACEUTICAL BULLETIN

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Cefpodoxime proxetil (CP) is a prodrug, broad spectrum, third generation cephalosporin ester. This prodrug ester is absorbed from the intestinal tract after oral administration and is hydrolyzed in vivo into the active cefpodoxime.1) Although CP is designed to improve the permeability and thus bioavailability of cefpodoxime, it still has only 50% oral bioavailability, when administered orally.2) The reported explanations for the low bioavailability of CP include low solubility in aqueous solution, typical gelation behavior in acidic aqueous environments and pre-absorption luminal metabolism of cefpodoxime by the action of digestive enzymes. 3,4) Metabolism of CP into cefpodoxime inside the intestinal epithelial cell and preferential efflux of cefpodoxime into lumen is also another contribution to the low bioavailability of CP. 5)Recently, nanosuspensions have shown promising potential in drug delivery to offer a unique solution for the poor bioavailability of poorly water-and lipid-soluble drugs. Nanosuspensions are colloidal dispersions of nano-sized drug particles stabilized by suitable stabilizers. Nanosuspensions are unique because of their simplicity and the advantages they confer over other formulation strategies.6) Oral nanosuspensions have been specifically used to increase the rate and extent of the absorption of poorly water-soluble drug, to enhance the onset of action, to reduce the fed/fasted ratio, and to enhance the bioavailability. In other cases, the particulate nature of nanosuspensions can be useful in the targeting of the monocyte phagocytic system, bypassing the passage of drug through epithelial cells with improved pharmacokinetic consequences.7) Nanosuspensions can also be used in controlled drug delivery systems. 8)Nanosuspension is generally prepared to be a liquid form. In order to prepare the solid dosage form for the purpose of better physical and chemical stability, spray drying is one of the commonly used techniques for solidification. However, research literature that discusses the use of spray drying for nanosuspension is limited. Recently, the spray dried nanosuspension of itraconazole was prepared.9) The emphasis was to examine the impact of various formulation and processing parameters on redispersibility of the spray dried nanoparticles and in-vitro dissolution. The in-vivo study was not performed to demonstrate the bioavailability enhancement by nanosuspension.As a solid product, solid spray-dried cefpodoxime proxetil nanosuspension (SDN) will be reconstituted in aqueous solution to form the liquid state prior to administration. It's better for SDN to regain its original state. For a heterogeneous disperse system, the rheological and thixotropic properties are important for its physical stability and clinical use. However, literature for the rheological and thixotropic properties of nanosuspensions is lacking.The main objective of the present study is to characterize the physicochemical properties of the liquid nanosuspension prepared by high pressure homogenization and SDN. I...

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Conversion of Nanosuspensions into Dry Powders by Spray Drying: A Case Study

Cited by 195 publications

References 18 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

New inhalation-optimized itraconazole nanoparticle-based dry powders for the treatment of invasive pulmonary aspergillosis

Physicochemical and Pharmacokinetic Characterization of a Spray-Dried Cefpodoxime Proxetil Nanosuspension

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