Nanosuspensions of poorly water-soluble drugs prepared by bottom-up technologies

Du, Juan; Li, Xiaoguang; Zhao, Huanxin; Zhou, Yuqi; Wang, Lulu; Tian, Shushu; Wang, Yancai

doi:10.1016/j.ijpharm.2015.09.021

Cited by 120 publications

(46 citation statements)

References 153 publications

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“…Therefore, the enhanced dissolution rate and plasma concentration of APIs prepared by the BC and PCC could be related to the decrease in crystallinity, as well as the size-reduction effect. However, the presence of an unstable, partially amorphous state raises concerns that the crystal structure may change during storage, which could change the dissolution properties and bioavailability (13). Small differences in the peak patterns were observed between the preparations (e.g., Fig.…”

Section: Discussionmentioning

confidence: 99%

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In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

Tahara

Nishikawa

Matsui³

et al. 2016

Pharm Res

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Section: Discussionmentioning

confidence: 99%

“…In bottom-up approaches, nanoparticles are prepared from dissolved drugs by controlled recrystallization. (5,(11)(12)(13). Crystallization is routinely used to produce fine chemicals with the desired purity and crystal polymorphs corresponding to the desired properties.…”

Section: Introductionmentioning

confidence: 99%

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

Tahara

Nishikawa

Matsui³

et al. 2016

Pharm Res

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“…16 As shown in Figure 1A, the particles were large before homogenization (367.0±5.1 nm), with a PDI value of 0.26±0.01. Homogenization significantly decreased the size to a mean diameter of ,140 nm with a PDI value of 0.18±0.02.…”

mentioning

confidence: 87%

A stabilizer-free and organic solvent-free method to prepare 10-hydroxycamptothecin nanocrystals: in vitro and in vivo evaluation

Yang¹,

Liu²,

Zhao³

et al. 2016

IJN

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10-Hydroxycamptothecin (10-HCPT) is a promising anticancer drug with a wide spectrum of antitumor activities. Due to its poor solubility, the carboxylate form that shows high water solubility but minimal anticancer activity and pharmacokinetic defects is used in the marketed 10-HCPT injections, resulting in its limited clinical application. To develop a simple, safe, and highly effective drug delivery system, a modified acid–base microprecipitation combined with a high-pressure homogenization technique was adopted to prepare 10-HCPT nanocrystals. Neither organic solvents nor stabilizers were employed throughout the preparation process. The in vitro and in vivo performances of the resulting10-HCPT nanocrystals were investigated systematically. The nanocrystals were spherical with a small size of ~130 nm, and the actual drug-loading content was as high as 75%. The nanocrystals displayed a sustained release pattern and were proven to have a higher cell uptake and antiproliferative activity than the 10-HCPT injections. The 10-HCPT nanocrystals also showed enhanced drug accumulation in tumors and better anticancer efficacy in 4T1-bearing mice. In summary, the 10-HCPT nanocrystals prepared in this study seem to be a promising delivery system for a new form of 10-HCPT dosages.

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“…A suspension of particles can in principle be formed either by a bottom-up approach from a solution (e.g. by precipitation (Du et al, 2015), solvent evaporation (Jallouli et al, 2015) or emulsion congealing (Hassan et al, 1995;Matos-Jr et al, 2015) or by a top-down approach from pre-existing solid particles (e.g. by wet milling (Afolabi et al, 2014;Li et al, 2015), high-pressure homogenisation (Möschwitzer, 2013;Tuomela et al, 2016) or their combination (Attari et al, 2016;Hatahet et al, 2016).…”

Section: Accepted M Manuscriptmentioning

confidence: 99%

Scale-up from batch to flow-through wet milling process for injectable depot formulation

Lehocký

Pěček²,

Štěpánek

2016

European Journal of Pharmaceutical Sciences

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Injectable depot formulations are aimed at providing long-term sustained release of a drug into systemic circulation, thus reducing plasma level fluctuations and improving patient compliance. The particle size distribution of the formulation in the form of suspension is a key parameter that controls the release rate. In this work, the process of wet stirred media milling (ball milling) of a poorly water-soluble substance has been investigated with two main aims: (i) to determine the parametric sensitivity of milling kinetics; and (ii) to develop scaleup methodology for process transfer from batch to flow-through arrangement. Ball milling experiments were performed in two types of ball mills, a batch mill with a 30 ml maximum working volume, and a flow-through mill with a 250 ml maximum working volume. Milling parameters were investigated in detail by methodologies of QbD to map the parametric space.Specifically, the effects of ball size, ball fill level, and rpm on the particle breakage kinetics were systematically investigated at both mills, with an additional parameter (flow-rate) in the case of the flow-through mill. The breakage rate was found to follow power-law kinetics with respect to dimensionless time, with an asymptotic d 50 particle size in the range of 200-300 nm.In the case of the flow-through mill, the number of theoretical passes through the mill was found to be an important scale-up parameter.

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Nanosuspensions of poorly water-soluble drugs prepared by bottom-up technologies

Cited by 120 publications

References 153 publications

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

A stabilizer-free and organic solvent-free method to prepare 10-hydroxycamptothecin nanocrystals: in vitro and in vivo evaluation

Scale-up from batch to flow-through wet milling process for injectable depot formulation

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