Optimization of formulation and process parameters for the production of nanosuspension by wet media milling technique: Effect of Vitamin E TPGS and nanocrystal particle size on oral absorption

Ghosh, Indrajit; Schenck, Daniel; Bose, Sonali; Ruegger, Colleen

doi:10.1016/j.ejps.2012.08.011

Cited by 111 publications

(69 citation statements)

References 17 publications

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“…Enhanced breakage kinetics can reduce milling time required, energy consumption, and even bead wear, which can be achieved by proper selection of the milling parameters such as bead size, bead loading, drug loading, rotor speed, and suspension flow rate. Influence of these parameters on the final drug particle size has been studied previously through experiments (Afolabi et al, 2014;Cerdeira et al, 2011;Ghosh et al, 2011;Ghosh et al, 2013;Ghosh et al, 2012;Monteiro et al, 2013;Singare et al, 2010;Singh et al, 2011). However, the influence of these parameters on breakage kinetics leading to sub-100 nm drug particles with reduced energy consumption and low bead wear has not been addressed.…”

Section: Introductionmentioning

confidence: 96%

Sub-100nm drug particle suspensions prepared via wet milling with low bead contamination through novel process intensification

Yaragudi

Afolabi

et al. 2015

Chemical Engineering Science

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Section: Introductionmentioning

confidence: 96%

Sub-100nm drug particle suspensions prepared via wet milling with low bead contamination through novel process intensification

Yaragudi

Afolabi

et al. 2015

Chemical Engineering Science

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“…The samples with drug-to-stabilizer ratio 2:1 had the largest particle size (478.1 nm), which increased substantially after seven days storage (1816 nm). Sufficient quantity of stabilizers are needed to provide sufficient coverage of the surface of the drug particle, in order to establish effective steric repulsion (Ghosh et al, 2012). It is likely that the stabilizer in this sample was insufficient, resulting in inadequate steric stabilization, and hence the observed large particle size, and increase in particle size.…”

Section: Synthesis and Characterization Of Peg-pblamentioning

confidence: 99%

Formulation and characterization of biocompatible and stable I.V. itraconazole nanosuspensions stabilized by a new stabilizer polyethylene glycol-poly(β-Benzyl- l -aspartate) (PEG-PBLA)

Zong

Wang

et al. 2017

International Journal of Pharmaceutics

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Formulation and characterization of biocompatible and stable I.V.itraconazole nanosuspensions stabilized by a new stabilizer polyethylene glycolpoly(␤-Benzyl-L-aspartate) (PEG-PBLA).International Journal of Pharmaceutics http://dx.doi.org/10. 1016/j.ijpharm.2017.08.082 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain. AbstractAmphiphilic block copolymers, PEG-PBLA with different molecular weights, were synthesized and used as new stabilizers for Itraconazole nannosuspensions (ITZ-PBLA-Nanos). ITZ-PBLA-Nanos were prepared by the microprecipitation-high pressure homogenization method, and the particle size and zeta potential were measured using a ZetaSizer Nano-ZS90. Morphology and crystallinity were studied using TEM, DSC and powder X-ray. The effect of the PEG-to-PBLA ratio, and the drug-to-stabilizer ratio were investigated to obtain the optimal formulation. It was found that the optimal length of hydrophobic block was 25 BLA-NCA molecules and the optimal ratio of drug/stabilizer was 1:1, where the resulted average particle size of ITZ-PBLA-Nanos was 262.1±7.13 nm with a PDI value of 0.163±0.011. The images of TEM suggest that ITZ-PBLA-Nanos were rectangular in shape. ITZ existed as crystals in the nanoparticles as suggested by the DSC and XRD results. Compared with the crude drug suspensions, the dissolution rate of ITZ nanocrystals, was significantly increased and was similar to Sporanox ® injection. The ITZ-PBLA-Nanos also demonstrated better dilution stability and storage stability compared with ITZ-F68-Nanos. The particle size of ITZ-PBLA-Nanos did not change significantly after incubated in rat plasma for 24 h which is a good attribute for I.V. administration. Acute toxicity tests showed that ITZ-PBLA-Nanos has the highest LD50 compared with ITZ-F68-Nanos and Sporanox ® injection. ITZ-PBLA-Nanos also showed stronger inhibiting effect on the growth of Candida albicans compared with Sporanox ® injection. Therefore, PEG-PBLA has a promising potential as a biocompatible stabilizer for ITZ nanosuspensions and potentially for other nanosuspensions as well.

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“…A wide variation was seen among the observed response indicating that the independent variables had significant effect on dependent variables. For further statistical analysis, the three responses were individually fitted to the second-order polynomial model and each model was validated by analysis of variance combined with the F test (26,27). As shown in Table III, the independent variables had significant effect (p value <0.05) for all the response variables.…”

Section: Plackett-burman Screening Designmentioning

confidence: 99%

Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals

et al. 2015

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Abstract. The present investigation was carried out to design, optimize, and evaluate lurasidone hydrochloride nanocrystals for improving its solubility and dissolution characteristics. Nanocrystals were prepared by media milling technique using zirconium oxide beads with 0.1 mm diameter. Various stabilizers, viz. poloxamer 188, PVP K30, SLS, HPMC E15, and PVP S 630 D, were evaluated to stabilize the nanocrystals. The Pareto chart obtained through Plackett-Burman screening design revealed that HPMC E 15 showed the highest standardized effect (p value <0.05) on percent dissolution efficiency at 2 min. In subsequent studies, a 3 2 factorial design was employed to quantify the effect of two independent variables, namely amount of stabilizer and milling time on predetermined response variables mean particle size, saturation solubility, and percent dissolution efficiency at 2 min. Statistical analysis of the factorial design revealed that all predetermined response variables were significantly dependent (p value <0.05) on the independent variables. The observed response of the optimized batch prepared as per the desirability function was in close agreement with predicted response, and mathematical model generated was validated. The optimized batch was lyophilized, and X-ray powder diffraction studies indicated that there was no substantial change in crystallinity of the drug. The optimized formulation showed mean particle size of 228 nm and released almost all the drug within first 5 min. Since the crystallinity of the drug is maintained, improvement in saturation solubility and dissolution efficiency could be attributed to decrease in mean particle size of the drug.

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Optimization of formulation and process parameters for the production of nanosuspension by wet media milling technique: Effect of Vitamin E TPGS and nanocrystal particle size on oral absorption

Cited by 111 publications

References 17 publications

Sub-100nm drug particle suspensions prepared via wet milling with low bead contamination through novel process intensification

Sub-100nm drug particle suspensions prepared via wet milling with low bead contamination through novel process intensification

Formulation and characterization of biocompatible and stable I.V. itraconazole nanosuspensions stabilized by a new stabilizer polyethylene glycol-poly(β-Benzyl- l -aspartate) (PEG-PBLA)

Design, Optimization, and Evaluation of Lurasidone Hydrochloride Nanocrystals

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