Optimization of formulation and process parameters for the production of carvedilol nanosuspension by wet media milling

Medarević, Djordje; Djuriš, Jelena; Ibrić, Svetlana; Mitrić, Miodrag; Kachrimanis, Kyriakos

doi:10.1016/j.ijpharm.2018.02.011

Cited by 73 publications

(44 citation statements)

References 58 publications

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“…3S SSL PM) as well as for both nanosuspensions, the isoliquiritigenin endothermic melting peak showed a substantial shift of about 178°C, whereas a small shift of 197°C was observed for the isoliquiritigenin and PVP K30 physical mixture (ISL-PVP K30 PM). The observed shift in the isoliquiritigenin melting peak in both nanosuspensions may be ascribed to a reduction in particle size or high miscibility of the drug with excipients [21,26]. Additionally, Medarević et al [21] reported that wet media milling can induce formation of a polymorphic transition or disordered drug lattice, which may lower the melting point of a drug.…”

Section: Resultsmentioning

confidence: 96%

“…The observed shift in the isoliquiritigenin melting peak in both nanosuspensions may be ascribed to a reduction in particle size or high miscibility of the drug with excipients [21,26]. Additionally, Medarević et al [21] reported that wet media milling can induce formation of a polymorphic transition or disordered drug lattice, which may lower the melting point of a drug. However, a decrease in the melting point for a physical mixture, partly as a result of interaction, can occur between a drug and excipients, as reported by Gao et al [27].…”

Section: Resultsmentioning

confidence: 96%

“…In recent y, nanosuspensions have attracted great attention as an insoluble drug delivery system, owing to their small size, high drug loading capacity, ease of preparation, high dispersity, reproducibility of oral absorption, and high adhesion to biological membranes [20][21]. Generally, nanosuspensions are prepared through top-down and bottom-up techniques.…”

Section: Isoliquiritigenin Nanosuspension Enhances Cytostatic Effectsmentioning

confidence: 99%

“…Generally, nanosuspensions are prepared through top-down and bottom-up techniques. Wet media milling, a top-down method, has been used to prepare a formulation that reached market for several reasons including its ability to run continuously and its cost effectiveness [21]. Nanosuspensions have many advantages such as enhancing the solubility of insoluble drugs as well as improving the cytostatic activity of bulk drugs; however, they are unstable and tend to aggregate because of their small particle sizes and large specific surface areas.…”

Section: Isoliquiritigenin Nanosuspension Enhances Cytostatic Effectsmentioning

confidence: 99%

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Isoliquiritigenin Nanosuspension Enhances Cytostatic Effects in A549 Lung Cancer Cells

et al. 2020

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Isoliquiritigenin, a flavonoid extracted from licorice root, has been shown to be active against most cancer cells; however, its antitumor activity is limited by its poor water solubility. The aim of this study was to develop a stable isoliquiritigenin nanosuspension for enhanced solubility and to evaluate its in vitro cytostatic activity in A549 cells. The nanosuspension of isoliquiritigenin was prepared through wet media milling with HPC SSL (hydroxypropyl cellulose-SSL) and PVP K30 (polyinylpyrrolidone-K30) as stabilizers, and the samples were then characterized according to particle size, zeta-potential, SEM (scanning electron microscopy), TEM (transmission electron microscopy), DSC (differential scanning calorimetry), XRPD (X-ray powder diffraction), FTIR (Fourier transform infrared spectroscopy), XPS (X-ray photoelectron spectroscopy), and in vitro release. The isoliquiritigenin nanosuspension prepared with HPC SSL and PVP K30 had particle sizes of 238.1 ± 4.9 nm and 354.1 ± 9.1 nm, respectively. Both nanosuspensions showed a surface charge of approximately − 20 mV and a lamelliform or ellipse shape. The dissolution of isoliquiritigenin from the 2 nanosuspensions was markedly higher than that of free isoliquiritigenin. In vitro studies on A549 cells indicated that the cytotoxicity and cellular uptake significantly improved after treatment with both nanosuspensions in comparison to the isoliquiritigenin solution. Furthermore, cell apoptosis analysis showed a 7.5 – 10-fold increase in the apoptosis rate induced by both nanosuspensions compared with pure drug. However, the cytotoxicity of pure drug and nanosuspension on normal cells (HELF) was lower, which indicated both isoliquiritigenin nanosuspensions have low toxicity to normal cells. Therefore, the isoliquiritigenin nanosuspension prepared with HPC SSL and PVP K30 as stabilizers may be a promising approach to improve the solubility and cytostatic activity of isoliquiritigenin.

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Section: Resultsmentioning

confidence: 96%

Section: Resultsmentioning

confidence: 96%

Section: Isoliquiritigenin Nanosuspension Enhances Cytostatic Effectsmentioning

confidence: 99%

Section: Isoliquiritigenin Nanosuspension Enhances Cytostatic Effectsmentioning

confidence: 99%

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Isoliquiritigenin Nanosuspension Enhances Cytostatic Effects in A549 Lung Cancer Cells

et al. 2020

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“…Ion Exchange Resin (IER) nanoparticles were prepared by Top down technique, wet milling [41,42,43,44,45,46,47] . Two types of Zirconium beads were used for the experiment: a) Cerium stabilized and b) Yttrium stabilized.…”

Section: Formulation Of Ier Nanoparticlesmentioning

confidence: 99%

Formulation and Characterization of Moxifloxacin Nanoparticles with Ion Exchange Resin

Vyas¹,

Daxini²,

Patel³

2020

J. Drug Delivery Ther.

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Moxifloxacin (MOX) is a fluoroquinolone anti-infective drug, indicated for the treatment of bacterial conjunctivitis. The drug is soluble in water but still produces low ocular bioavailability due to biological barriers and so it requires dosing for two/three times a day. The present study was designed to formulate, optimize and characterize polymeric Nanoparticles MOX for ocular administration using Ion Exchange Resin (IER). IER-nanoparticles were prepared by media milling method, formulation/process parameters were optimized based on evaluation parameters such as color of nanosuspension, sedimentation behaviour, particle size and zeta potential. MOX-IER nanosuspensions were prepared at different stoichiometric ratio of MOX and IER and characterized by entrapment efficiency, pH, particle size and zeta potential of nanosuspension. In vitro release study of optimized batch MNIER3 exhibited sustained release pattern which follows Korsmeyer-Peppas model with Fickian diffusion mechanism for drug release. Based on these results optimized batch of MOX-IER nanosuspension formulated in the laboratory was found suitable for ocular delivery. Keywords: Moxifloxacin; nanoparticles, nanosuspension; media milling; stoichiometric ratio; sedimentation behaviour.

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Investigation of Formulation and Process Parameters of Wet Media Milling to Develop Etodolac Nanosuspensions

Karakucuk

Çelebi

2020

Pharm Res

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Optimization of formulation and process parameters for the production of carvedilol nanosuspension by wet media milling

Cited by 73 publications

References 58 publications

Isoliquiritigenin Nanosuspension Enhances Cytostatic Effects in A549 Lung Cancer Cells

Isoliquiritigenin Nanosuspension Enhances Cytostatic Effects in A549 Lung Cancer Cells

Formulation and Characterization of Moxifloxacin Nanoparticles with Ion Exchange Resin

Investigation of Formulation and Process Parameters of Wet Media Milling to Develop Etodolac Nanosuspensions

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