Rod shaped nanocrystals exhibit superior in vitro dissolution and in vivo bioavailability over spherical like nanocrystals: A case study of lovastatin

Guo, Meng; Fu, Qiang; Wu, Chunnuan; Guo, Zhibin; Mo, Li; Sun, Jin; Zhang, He; Yang, Li

doi:10.1016/j.colsurfb.2015.02.039

Cited by 54 publications

(23 citation statements)

References 50 publications

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“…Drug NCs are usually prepared by two methods, top-down and bottom-up methods 35,36. In the top-down method, the particle size of drugs is reduced by high-pressure homogenization or milling 37–39.…”

Section: Introductionmentioning

confidence: 99%

Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

Choi¹,

Park²

2016

DDDT

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The purpose of this study was to develop the surface modification of docetaxel nanocrystals (DTX-NCs) with apo-Transferrin human (Tf) for improving the cellular uptake and cytotoxicity of DTX. DTX-NCs were prepared by a nanoprecipitation method, and the surface modified with Tf by an adsorption method (Tf-DTX-NCs). The morphology and particle size of DTX-NCs and Tf-DTX-NCs were characterized using a field emission scanning electron microscope and zetasizer. An in vitro drug release study was performed in phosphate-buffered saline containing 0.5% (w/v) Tween 80 for 24 hours. Cellular uptake was studied at 0.5, 1, and 2 hours. A cytotoxicity study was performed using the A549 (human lung cancer) cell line after 24-, 48-, and 72-hour treatments. The mean sizes were 295±97 and 398±102 nm for DTX-NCs and Tf-DTX-NCs, respectively. Tf-DTX-NCs and DTX-NCs exhibited rapid drug release, whereas DTX (pure) was slowly released. Tf-DTX-NCs showed higher cellular uptake than DTX-NCs in confocal microscopic and quantitative studies. Moreover, at DTX concentration of 100 µg/mL, Tf-DTX-NCs (82.6%±0.8%) showed higher cytotoxicity than DTX-NCs (77.4%±4.1%) and DTX (pure; 20.1%±4.6%) for 72-hour treatment. In conclusion, Tf-DTX-NCs significantly improved the cellular uptake and cytotoxicity of DTX in the A549 cell line.

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Section: Introductionmentioning

confidence: 99%

Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

Choi¹,

Park²

2016

DDDT

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“…Badawi et al [79] [68], artemisinin [69] and quercetin [70]. Oven-drying was used to isolate many nanosized API crystals such as CRS 74 (a new antiretroviral drug) [80], indomethacin [72], lovastatin [62] and cefixime [71].…”

Section: Accepted Manuscriptmentioning

confidence: 99%

“…Then, Lleucine was employed to prepare aggregations of the resultant budesonide nanoparticles suitable for pulmonary delivery, and with an improved dissolution rate in comparison to the commercial budesonide. Rod-shaped sonoprecipitated nanosized APIs showed a superior dissolution behaviour in comparison to milled nanocrystals[62,94]. Agglomerates of rod-shaped sonoprecipitated nanosized theophylline with a mean size suitable for inhalation (2.47 µm) were also prepared[94].…”

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confidence: 99%

Recent advances in the engineering of nanosized active pharmaceutical ingredients: Promises and challenges

Kaialy

Shafiee

2016

Advances in Colloid and Interface Science

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The advances in the field of nanotechnology have revolutionized the field of delivery of poorly soluble active pharmaceutical ingredients (APIs). Nanosized formulations have been extensively investigated to achieve a rapid dissolution and therefore pharmacokinetic properties similar to those observed in solutions. The present review outlines the recent advances, promises and challenges of the engineering nanosized APIs. The principles, merits, demerits and applications of the current 'bottom-up' and 'top-down' technologies by which the state of the art nanosized APIs can be produced were described. Although the number of research reports on the nanoparticle engineering topic has been growing in the last decade, the challenge is to take numerous research outcomes and convert them into strategies for the development of marketable products.

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“…However, the low oral bioavailability (<5%) resulting from its insolubility and first-pass effect limits the clinical application [6]. In the previous investigation [7], a LOV nanosuspension (LOV-NS) was developed to improve its bioavailability. Subsequently, the pharmacokinetic behavior of this novel preparation should be estimated.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous determination of lovastatin and its metabolite lovastatin acid in rat plasma using UPLC–MS/MS with positive/negative ion-switching electrospray ionization: Application to a pharmacokinetic study of lovastatin nanosuspension

Guo

Zhao

et al. 2016

Journal of Chromatography B

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Rod shaped nanocrystals exhibit superior in vitro dissolution and in vivo bioavailability over spherical like nanocrystals: A case study of lovastatin

Cited by 54 publications

References 50 publications

Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

Development of docetaxel nanocrystals surface modified with transferrin for tumor targeting

Recent advances in the engineering of nanosized active pharmaceutical ingredients: Promises and challenges

Simultaneous determination of lovastatin and its metabolite lovastatin acid in rat plasma using UPLC–MS/MS with positive/negative ion-switching electrospray ionization: Application to a pharmacokinetic study of lovastatin nanosuspension

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