Impact of Nanosizing on Solubility and Dissolution Rate of Poorly Soluble Pharmaceuticals

Murdande, Sharad B.; Shah, Dhaval A.; Dave, Rutesh H.

doi:10.1002/jps.24426

Cited by 76 publications

(38 citation statements)

References 40 publications

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“…The suspension (500 mL) was milled using the yttrium stabilized zirconium oxide beads (YTZ beads) at a milling speed of 1000 rpm in the continuous model 8 . The suspension formulation was milled for 4 h, and the particle size was measured during and following the milling process.…”

Section: Wet Millingmentioning

confidence: 99%

“…The solubility behavior of crystalline nanoparticles can be explained by the Ostwald-Frendulich equation. Based on the published reports, the thermodynamic solubility enhancement of nanocrystalline particles should be approximately 10-15% 8,15,16 . On the other hand, nanosuspensions have a very high surface-to-volume ratio and high Gibbs energy, which indicates the instability of the system.…”

Section: Introductionmentioning

confidence: 99%

“…Several formulation approaches have been suggested and reported to overcome these problems. The formulation of nanocrystals (NCs; suspension or solid) is one of the preferred approaches that has been used for the drugs which belong to the above BCS classes 7,8 . NCs offer several advantages, including enhancement in bioavailability, reduction in therapeutic dose, and elimination of the food effect [9][10][11][12][13][14] .…”

Section: Introductionmentioning

confidence: 99%

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Influence of spray drying and dispersing agent on surface and dissolution properties of griseofulvin micro and nanocrystals

Shah

Patel

Murdande

et al. 2016

Drug Development and Industrial Pharmacy

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The purpose for the current research is to compare and evaluate physiochemical properties of spray-dried (SD) microcrystals (MCs), nanocrystals (NCs), and nanocrystals with a dispersion agent (NCm) from a poorly soluble compound. The characterization was carried out by performing size and surface analysis, interfacial tension (at particle moisture interface), and in-vitro drug dissolution rate experiments. Nanosuspensions were prepared by media milling and were spray-dried. The SD powders that were obtained were characterized morphologically using scanning electron microscopy (SEM), polarized light microscopy (PLM), and Flowchem. Solid-state characterization was performed using X-ray powder diffraction (XRPD), Fourier transfer infrared spectroscopy (FT-IR), and differential scanning calorimetry (DSC) for the identification of the crystalline nature of all the SD powders. The powders were characterized for their redispersion tendency in the water and in pH 1.2. Significant differences in redispersion were noted for both the NCs in both dissolution media. The interfacial tension for particle moisture interface was determined by applying the BET (Braunauer-Emmett-Teller) equation to the vapor sorption data. No significant reduction in the interfacial tension was observed between MCs and NCs; however, a significant reduction in the interfacial tension was observed for NCm at both 25 °C and 35 °C temperatures. The difference in interfacial tension and redispersion behavior can be attributed to a difference in the wetting tendency for all the SD powders. The dissolution studies were carried out under sink and under non-sink conditions. The non-sink dissolution approach was found suitable for quantification of the dissolution rate enhancement, and also for providing the rank order to the SD formulations.

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Section: Wet Millingmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Influence of spray drying and dispersing agent on surface and dissolution properties of griseofulvin micro and nanocrystals

Shah

Patel

Murdande

et al. 2016

Drug Development and Industrial Pharmacy

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“…That said, even in the 5.0% PEG film, the d 90 value was only 556 nm, and 100% of all particles were <1 μm in size (full size distribution not shown). As such, these differences in nanoparticle size are not expected to negatively affect drug dissolution rate from films under sink conditions (Krull et al, 2016; Murdande et al, 2015). …”

Section: Resultsmentioning

confidence: 99%

Critical material attributes (CMAs) of strip films loaded with poorly water-soluble drug nanoparticles: I. Impact of plasticizer on film properties and dissolution

Krull

Patel

et al. 2016

European Journal of Pharmaceutical Sciences

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Recent studies have demonstrated polymer films to be a promising platform for delivery of poorly water-soluble drug particles. However, the impact of critical material attributes, for example plasticizer, on the properties of and drug release from such films has yet to be investigated. In response, this study focuses on the impact of plasticizer and plasticizer concentration on properties and dissolution rate of polymer films loaded with poorly water-soluble drug nanoparticles. Glycerin, triacetin, and polyethylene glycol were selected as film plasticizers. Griseofulvin was used as a model Biopharmaceutics Classification System class II drug and hydroxypropyl methylcellulose was used as a film-forming polymer. Griseofulvin nanoparticles were prepared via wet stirred media milling in aqueous suspension. A depression in film glass transition temperature was observed with increasing plasticizer concentration, along with a decrease in film tensile strength and an increase in film elongation, as is typical of plasticizers. However, the type and amount of plasticizer necessary to produce strong yet flexible films had no significant impact on the dissolution rate of the films, suggesting that film mechanical properties can be effectively manipulated with minimal impact on drug release. Griseofulvin nanoparticles were successfully recovered upon redispersion in water regardless of plasticizer or content, even after up to 6 months’ storage at 40 °C and 75% relative humidity, which contributed to similar consistency in dissolution rate after 6 months’ storage for all films. Good content uniformity (<4% R.S.D. for very small film sample size) was also maintained across all film formulations.

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“…Therefore, decreasing particle size of pesticide could effectively enhance its dissolution performance [8][9][10]. However, obvious change appears only when the particle size is in the nanoscale.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Emamectin Benzoate Solid Nanodispersion

Yang

Cui

Wang

et al. 2017

Journal of Nanomaterials

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The solid nanodispersion of 15% emamectin benzoate was prepared by the method of solidifying nanoemulsion. The mean particle size and polydispersity index of the solid nanodispersions were 96.6 ± 1.7 nm and 0.352 ± 0.041, respectively. The high zeta potential value of 31.3 ± 0.5 mV and stable crystalline state of the nanoparticles suggested the excellent physical and chemical stabilities. The contact angle and retention compared with microemulsions and water dispersible granules on rice, cabbage, and cucumber leaves indicated its improved wettability and adhesion properties. The bioassay compared with microemulsions and water dispersible granules against diamondback moths and green peach aphids provided an evidence of its enhanced biological activity. This formulation composition could avoid organic solvents and obviously reduce surfactants. It is perspective in raising bioavailability and reducing residual pollution of pesticides and further improving agricultural production and environmental safety.

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Impact of Nanosizing on Solubility and Dissolution Rate of Poorly Soluble Pharmaceuticals

Cited by 76 publications

References 40 publications

Influence of spray drying and dispersing agent on surface and dissolution properties of griseofulvin micro and nanocrystals

Influence of spray drying and dispersing agent on surface and dissolution properties of griseofulvin micro and nanocrystals

Critical material attributes (CMAs) of strip films loaded with poorly water-soluble drug nanoparticles: I. Impact of plasticizer on film properties and dissolution

Preparation and Characterization of Emamectin Benzoate Solid Nanodispersion

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