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Junghanns, Herbert

doi:10.1007/978-3-662-00528-6_20

Cited by 9 publications

(5 citation statements)

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“…The three most important technologiesf or HPH include the microfluidizer method( DD-PTM technology), the piston-gap homogenization methodi nw ater (Dissocubes), and in-water mixture (Nanopure). [57] The Dissocubes tool, engineered by Müller and co-workers at the end of the twentiethc entury, was ab reakthrough technology. [58] It involves the application of high pressure (up to 400 MPa) to an aqueous solution in which the drug is dispersed, creatingasignificant shear stress force when the solution passest hrough at ight gap by means of ah omogenizer piston.…”

Section: High-pressure Homogenizationmentioning

confidence: 99%

“…The use of water as ad ispersant solution may hydrolyze water-sensitive drugs and create abundant foam. [57] Another methodt hat uses the piston-gap homogenizer is Nanopure technology.T his consists of homogenization of the drug dispersed in non-aqueous mediuma tl ow temperature (close to 0 8C) and even below its freezingp oint. Thea ppliedp ressure is low,p reventing cavitation phenomena.T he particles ize diminution is still acceptable,b elow 1 mm.…”

Section: High-pressure Homogenizationmentioning

confidence: 99%

“…This explains, for instance,w hy the dose of fenofibrate can be decreased by 18 % in marketed tablets of nanocrystals for the same bioequivalence of micronized fenofibrate. [57,177] In addition to the capacity of nanocrystalst oc ross the gastrointestinal epithelium, other research has shown that the enhanced bioavailability of nanocrystals comesf rom inhibition of P-glycoprotein (P-gp) in the apical membrane. [178,179] More precisely,P -gp-mediated efflux is decreased by surfactants in the nanocrystal formulations.P -gp-driven efflux acrosst he apical membrane can disrupt the rate and amount of drug traversing the basolateral membrane andi nto the bloodstream.…”

Section: Oral Deliverymentioning

confidence: 99%

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State of the Art of Pharmaceutical Solid Forms: from Crystal Property Issues to Nanocrystals Formulation

et al. 2018

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The solid‐form screening of active principal ingredients is a challenge for pharmaceutical drug development, as more than 80 % of marketed drugs are formulated in the solid form. A broad and comprehensive study of the various solid forms of drugs is needed to enhance their translation into the clinic. Therefore, the most suitable solid form must be taken into consideration regarding ex vivo and in vivo stability, targeting, solubility, dissolution rate, and bioavailability. In this review, techniques of solid‐form screening are covered, including differences in solid forms such as polymorphs, solvates, salts, co‐crystals, and amorphous particles. Moreover, solid drug size reduction is also discussed, with insight into the emergence of drug nanocrystal formulations. An overview of the smallest nanocrystals reported in the literature and on the market is also provided, along with their applications and routes of administration.

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Section: High-pressure Homogenizationmentioning

confidence: 99%

Section: High-pressure Homogenizationmentioning

confidence: 99%

Section: Oral Deliverymentioning

confidence: 99%

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State of the Art of Pharmaceutical Solid Forms: from Crystal Property Issues to Nanocrystals Formulation

et al. 2018

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“…[4] In order to obtain nanoscale crystals, the cycle needs to be repeated many times, normally over 70 cycles. [32] However, even after many cycles, there is a considerable quantity of microcrystals in the system. To overcome these obstacles, piston-gap homogenizers have been developed.…”

Section: High-pressure Homogenizationmentioning

confidence: 99%

Nanocrystallization: An Effective Approach to Enhance the Performance of Organic Molecules

2017

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Organic nanocrystals have attracted great research interest in recent years due to their superior physical and chemical properties as compared to their amorphous counterparts. Higher photoluminescence intensity, steadier dissolution, and greater structural stability are a few examples of these properties, making nanocrystals an excellent choice for a wide range of applications, like electronics, bioimaging, and pharmaceuticals. Here, the principles of the most important nanocrystallization methods for organic compounds are elaborated. The discussion comprises the most important top‐down and bottom‐up approaches reported so far, explaining their advantages and limitations. To address the limitations of these methods, a new bottom‐up concept of stress‐induced seed‐assisted nanocrystallization is proved to be universally applicable to different organic molecules. To close, the future perspectives in the field are discussed.

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“…Further, their delivery through an oral route is difficult due to poor and variable bioavailability. Over the past decade or so, several strategies have been proposed to tackle these challenges, such as particle size diminution, emulsion (micro/nano) based formulations, self‐emulsifying systems, salt formation, micronization, liposomes, micelle formation, cyclodextrin inclusion complexation, and solid dispersions …”

Section: Introductionmentioning

confidence: 99%

Low Energy Nanoemulsions as Templates for the Formulation of Hydrophobic Drugs

Badruddoza

Gupta

Myerson

et al. 2018

Advanced Therapeutics

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Most small molecule active pharmaceutical ingredients (APIs) are hydrophobic which poses formulation challenges due to their poor water solubility. Current approaches are energy intensive and involve presenting the API in a nanoparticle form that is then combined with other additives into a stable formulation. Here, a bottom-up and scalable method that formulates nanoparticles (crystalline or amorphous) of poorly water-soluble APIs directly embedded in composite hydrogel beads is presented. Using nanoemulsions prepared from a low energy method as templates, the flexible approach allows to vary the embedded API nanoparticle size from 100 to 500 nm and the hydrogel bead size from 100 to 1200 µm, and subsequently achieve control over the dissolution kinetics. To better understand the dissolution process, a physical model is build that allows to collapse the kinetic data onto a master curve and predict the dependence of release rates on size of both API nanoparticles and hydrogel beads. Lastly, it is demonstrated that the dissolution kinetics of multiple drugs embedded in the same hydrogel matrix can be tuned simultaneously, an attractive property for commercial multi-drug dosage applications. The new approach not only leads to process intensification, but also improved performance.

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U

Cited by 9 publications

References 0 publications

State of the Art of Pharmaceutical Solid Forms: from Crystal Property Issues to Nanocrystals Formulation

State of the Art of Pharmaceutical Solid Forms: from Crystal Property Issues to Nanocrystals Formulation

Nanocrystallization: An Effective Approach to Enhance the Performance of Organic Molecules

Low Energy Nanoemulsions as Templates for the Formulation of Hydrophobic Drugs

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