Nanoparticulation of Poorly Water Soluble Drugs Using a Wet-Mill Process and Physicochemical Properties of the Nanopowders

Tanaka, Yusuke; Inkyo, Mitsugi; Yumoto, Ryoko; Nagai, Junya; Takano, Mikihisa; Nagata, Shunji

doi:10.1248/cpb.57.1050

Cited by 51 publications

(39 citation statements)

References 27 publications

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“…The diffraction interference by water in wet sample or co-existing with PVP and SLS might weaken the peak intensities in the ultracentrifuged (B) or freeze-dried products (D), respectively. These results concluded that the current media milling process in aqueous phase might not induce a polymorphic transition and amorphization of the drug as other authors have been previously reported (Van Eerdenbrugh et al, 2008b;Kawabata et al, 2010;Tanaka et al, 2009). Consequently, the crystalline state was still kept even if the drug were broken down into nano-sized particles.…”

Section: Physicochemical Properties Of Nanoparticlessupporting

confidence: 62%

Universal wet-milling technique to prepare oral nanosuspension focused on discovery and preclinical animal studies – Development of particle design method

Niwa

Miura

Danjo

2011

International Journal of Pharmaceutics

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Section: Physicochemical Properties Of Nanoparticlessupporting

confidence: 62%

Universal wet-milling technique to prepare oral nanosuspension focused on discovery and preclinical animal studies – Development of particle design method

Niwa

Miura

Danjo

2011

International Journal of Pharmaceutics

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“…The dried particles which can be spontaneously transformed to nanodispersed suspension in aqueous fluid such as digestive juices are called "dry nanosuspension" in this paper. According to previous reports, freeze-drying is the most popular way to obtain the powder from the milled suspension (29)(30)(31). Actually, this method based on freeze and sublimation phenomena of water tends to produce the porous and bulky powder, which is highly advantageous to be soaked up by and dispersed in water.…”

Section: Concept Of Dry Nanosuspensionmentioning

confidence: 99%

Design of Dry Nanosuspension with Highly Spontaneous Dispersible Characteristics to Develop Solubilized Formulation for Poorly Water-Soluble Drugs

2011

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“…[20] As the drug is suspended in aqueous media, the thermal energy generated is considered lower than dry milling techniques and is also considered an efficient way to generate drug crystals. [21] Some products already available in the market and developed with this technique are Rapamune and Emend, launched in 2002 and 2003, respectively. Another method of producing nanocrystalline suspensions is by means of the HPH method, developed by Muller in 1999.…”

Section: Introductionmentioning

confidence: 99%

Enhanced bioavailability of danazol nanosuspensions by wet milling and high-pressure homogenization

Kanthamneni¹,

Patel²,

Xia³

et al. 2016

Int J Pharma Investig

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Introduction:The majority of drugs obtained through synthesis and development show poor aqueous solubility and dissolution velocity, resulting in reduced bioavailability of drugs. Most of these problems arise from formulation-related performance issues, and an efficient way to overcome these obstacles and to increase dissolution velocity is to reduce the particle size of drug substances to form drug nanosuspensions.Materials and Methods:Danazol nanosuspensions were prepared by wet milling (WM) and high-pressure homogenization (HPH) methods. The nanosuspensions obtained using these fabrication methods were analyzed for their particle size, surface charge, and the crystallinity of the product was assessed by X-ray diffraction (XRD) and differential scanning calorimetry techniques. To determine in vitro and in vivo performances of the prepared nanosuspensions, dissolution velocity, and bioavailability studies were performed.Results:Particle size and zeta potential analysis showed the formation of nanosized particles with a negative charge on the surface. XRD depicted the nanocrystalline nature of danazol with low diffraction intensities. With increased surface area and saturation solubility, the nanosuspensions showed enhanced dissolution velocity and oral bioavailability in rats when compared to the bulk danazol suspension.Conclusions:The results suggest that the preparation of nanosuspensions by WM or HPH is a promising approach to formulate new drugs or to reformulate existing drugs with poorly water-soluble properties.

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Nanoparticulation of Poorly Water Soluble Drugs Using a Wet-Mill Process and Physicochemical Properties of the Nanopowders

Cited by 51 publications

References 27 publications

Universal wet-milling technique to prepare oral nanosuspension focused on discovery and preclinical animal studies – Development of particle design method

Universal wet-milling technique to prepare oral nanosuspension focused on discovery and preclinical animal studies – Development of particle design method

Design of Dry Nanosuspension with Highly Spontaneous Dispersible Characteristics to Develop Solubilized Formulation for Poorly Water-Soluble Drugs

Enhanced bioavailability of danazol nanosuspensions by wet milling and high-pressure homogenization

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