Nanocrystals: Comparison of the size reduction effectiveness of a novel combinative method with conventional top-down approaches

Salazar, Jaime Santoyo; Ghanem, Antoine; Müller, Rainer H.; Möschwitzer, Jan P.

doi:10.1016/j.ejpb.2011.12.015

Cited by 101 publications

(60 citation statements)

References 18 publications

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“…The amount of drug and organic solvent are crucial factors to be considered for lyophilization in H96 process. 8 In the last step of drug (aprepitant) synthesis, no crystallization of the drug is performed but the drug solution was made using methanol as solvent.…”

Section: H96 (Lyophilization + Hph)mentioning

confidence: 99%

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

S¹,

Deshpande²,

Attari³

et al. 2016

Adv Pharm Bull

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Section: H96 (Lyophilization + Hph)mentioning

confidence: 99%

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

S¹,

Deshpande²,

Attari³

et al. 2016

Adv Pharm Bull

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“…The SL was found to increase by threefold in all batches and this may be due to the creation of high energy surfaces when microparticles were disrupted into nanoparticles (Salazar et al, 2012). The SL also depends upon the crystallinity of the particles and exposure of lyophobic inner surfaces of the particles to the aqueous dispersion medium (Subedi et al, 2009).…”

Section: Discussionmentioning

confidence: 99%

“…This prevents the particles from aggregation, thus stabilizing the NCs (Müller et al, 2001). Soybean LEC was chosen for stabilization since it is a proven dispersant and surfactant, and is widely used in the complexation process (Salazar et al, 2012). Strong enthalpic interaction (good solvation) between the solvent and stabilizer induces steric repulsion and this factor would have also prevented the agglomeration (Wu et al, 2011).…”

Section: Discussionmentioning

confidence: 99%

“…They are generally prepared by top down (nanonization or nanosizing) or bottom up approach (precipitation) (Müller et al, 2001;Junghanns & Müller, 2008). Top-down technology can be applied by homogenization or milling by using pearl, bead or ball mills (Gülsün et al, 2009;Salazar et al, 2012). In precipitation method, drug is dissolved in a solvent and subsequently added to a non-solvent, leading to precipitation of finely dispersed drug crystals (Gassmann & List, 1994;Junghanns & Müller, 2008;Gülsün et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

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Development and characterization of lecithin stabilized glibenclamide nanocrystals for enhanced solubility and drug delivery

Kumar

Saraswathi²,

Kumar

et al. 2013

Drug Delivery

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Novel LNCs (lipid nanocrystals) were developed with an aim to improve the solubility, stability and targeting efficiency of the model drug glibenclamide (GLB). PEG 20000, Tween 80 and soybean lecithin were used as polymer, surfactant and complexing agent, respectively. GLB nanocrystals (NCs) were prepared by precipitation process and complexed using hot and cold melt technique. The LNCs were evaluated by drug loading, saturation solubility (SL), optical clarity, in vitro dissolution, solid state characterization, in vivo and stability analysis. LNCs exhibited a threefold increase in SL and a higher dissolution rate than GLB. The percentage dissolution efficiency was found to decrease with increase in PEG 20000. The average particle size was in the range of 155-842 nm and zeta potential values tend to increase after complexation. X-ray powder diffractometry and differential scanning calorimetry results proved the crystallinity prevailed in the samples. Spherical shaped particles (51000 nm) with a lipid coat on the surface were observed in scanning electron microscopy analysis. Fourier transform infrared results proved the absence of interaction between drug and polymer and stability study findings proved that LNCs were stable. In vivo study findings showed a decrease in drug concentration to pancreas in male Wistar rats. It can be concluded that LNCs are could offer enhanced solubility, dissolution rate and stability for poorly water soluble drugs. The targeting efficiency of LNCs was decreased and further membrane permeability studies ought to be carried out.

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“…Combinative technologies are a relatively new approach to improve the effectiveness of PS reduction and to reduce the process times. In general, they can be described as a combination of a bottom-up process (the building-up of particles) ) followed by a top-down technology (disintegration) (Salazar et al, 2012, Vivek et al, 2014. This method involves two steps of PS reduction.…”

Section: Combination Milling Techniquesmentioning

confidence: 99%

Application of wet milling techniques to produce micronized and nanonized drug pre-dispersions for the development of intranasal formulations

Bartos¹

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Nanocrystals: Comparison of the size reduction effectiveness of a novel combinative method with conventional top-down approaches

Cited by 101 publications

References 18 publications

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

Preparation and Characterization of Nanosuspension of Aprepitant by H96 Process

Development and characterization of lecithin stabilized glibenclamide nanocrystals for enhanced solubility and drug delivery

Application of wet milling techniques to produce micronized and nanonized drug pre-dispersions for the development of intranasal formulations

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