Formation of PVP/nimesulide microspheres by supercritical antisolvent coprecipitation

Prosapio, Valentina; Reverchon, Ernesto; Marco, Iolanda De

doi:10.1016/j.supflu.2016.07.023

Cited by 54 publications

(29 citation statements)

References 54 publications

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“…Nimesulide (4-nitro-2-phenoxymethanesulfonamide) (NiM) is a non-steroidal anti-inflammatory drug (NSAID), widely used to ameliorate acute pain [1,2]. Its mechanism of action is associated with the inhibition of the ciclo-oxigenase-2 (COX-2) isoform [3].…”

Section: Introductionmentioning

confidence: 99%

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Optimization of nimesulide-loaded solid lipid nanoparticles (SLN) by factorial design, release profile and cytotoxicity in human Colon adenocarcinoma cell line

Campos

Fernandes

Sousa

et al. 2019

Pharmaceutical Development and Technology

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The aim of this work has been the development of a non-toxic, long-term stable solid lipid nanoparticles (SLN) formulation for the loading of Nimsulide (NiM) by a 2 2 factorial design. The optimized formulation was composed of 10 wt% of glyceryl behenate and 2.5 wt% of poloxamer 188. Immediately after production, Z-Ave of NiM-SLN was 166.1±0.114 nm, with a polydispersity index (PI) of 0.171±0051 and zeta potential nearly neutral (-3.10±0.166 mV). A slight increase of Z-Ave was recorded for NiM-SLN stored at 25ºC for a period of 15 days, whereas at 4ºC particles kept size within similar range. Long-term stability was monitored using TurbiscanLab®, showing a high stability of the nanoparticles with variations in the backscattering profiles below 10%. The release profile of NiM-SLN followed a sustained pattern with ca. 30% of drug released up to 24 h. Empty-SLN and NiM-SLN were non-toxic after exposing Caco-2 cells to the highest concentration (100 μg/mL) up to 48 hours (cell viability higher than 80%). NiM-SLN were lyophilized using different cryoprotectants, producing particles of 463.1±36.63 nm (PI 0.491±0.027) with 5% trehalose. Solid character of NiM-SLN was confirmed by DSC, recording a recrystallization index of 83% for NiM-SLN and of 74% for lyophilized SLN.

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Section: Introductionmentioning

confidence: 99%

“…Like most of the NSAIDs, NiM shows low solubility in water, which limits its bioavailability in vivo [2]. This may lead to a significant reduction of drug's efficacy which, associated to the need of higher dose and/or longterm therapy, adverse side effects usually occur [1,4].…”

Section: Introductionmentioning

confidence: 99%

Optimization of nimesulide-loaded solid lipid nanoparticles (SLN) by factorial design, release profile and cytotoxicity in human Colon adenocarcinoma cell line

Campos

Fernandes

Sousa

et al. 2019

Pharmaceutical Development and Technology

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show abstract

“…In addition, particle engineering and crystal manipulation could be performed by this method [7,8]. In addition, supercritical fluid techniques have been used for producing small and nanosized particles [9][10][11]. However, preventing the crystal growth is the biggest problem in this process.…”

Section: Introductionmentioning

confidence: 99%

Effect of high pressure homogenization on physicochemical properties of curcumin nanoparticles prepared by antisolvent crystallization using HPMC or PVP

Homayouni

Sohrabi

Amini

et al. 2019

Materials Science and Engineering: C

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“…Owing to poor solubility and rate of dissolution, the bioavailability of these pharmaceutical drugs is insubstantial. This requires high dosages of these drugs in order to bring out the required therapeutic effect with consequent detrimental effects on the patient's health . Nimesulide (4‐nitro‐2‐phenoxymethanesulfonamide) (NIM) is a comparatively COX‐2 choosy, nonsteroidal anti‐inflammatory drug (NSAID) which acts as an antipyretic, analgesic and anti‐inflammatory agent, and is widely used in treating acute pain due to various diseases such as headache, migraine, back pain and postoperative pain .…”

Section: Introductionmentioning

confidence: 99%

Continuous preparation of nimesulide nanoparticles by liquid antisolvent precipitation using spinning disc reactor

Rathod

2018

J of Chemical Tech & Biotech

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BACKGROUND: Nimesulide (NIM), a nonsteroidal anti-inflammatory drug (NSAID) acts as an antipyretic, analgesic and anti-inflammatory agent, and it is widely used in treating acute pain due to various diseases such as headache, migraine, back pain and postoperative pain. Nimesulide is reported to have poor solubility in water (0.01 mg mL −1 ). In this work, the solvent-antisolvent (S:AS) precipitation of NIM using spinning disc reactor (SDR) was investigated. RESULTS:Comparative studies were investigated between stirred tank reactor and SDR. The effects of different functional parameters of spinning disc process such as S:AS ratio and flow rate, nimesulide concentration, disc surface texture, capping agent concentration, different capping agents and speed of rotating disc were studied on the particle size of nimesulide. The average particle size of 192 nm for nimesulide was successfully achieved with a considerable particle size distribution at a 300 mL min −1 total flow rate, with the following parameters: concentration of nimesulide in ethanol 0.5 mg mL −1 ; concentration of polyvinylpyrrolidone (PVP) in deionized water 1 mg mL −1 ; S:AS ratio 1:6 and at 3000 rpm rotating disc speed. This result should be compared with 9.5 m particle size with mechanical agitated contactor at S:AS ratio 1:6 and speed of agitation 600 rpm. CONCLUSION:The NIM nanoparticles can be continuously prepared in a SDR with a control and uniform particle size. This leads to increased dissolution rate and bioavailability of poorly water soluble drugs.

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Formation of PVP/nimesulide microspheres by supercritical antisolvent coprecipitation

Cited by 54 publications

References 54 publications

Optimization of nimesulide-loaded solid lipid nanoparticles (SLN) by factorial design, release profile and cytotoxicity in human Colon adenocarcinoma cell line

Optimization of nimesulide-loaded solid lipid nanoparticles (SLN) by factorial design, release profile and cytotoxicity in human Colon adenocarcinoma cell line

Effect of high pressure homogenization on physicochemical properties of curcumin nanoparticles prepared by antisolvent crystallization using HPMC or PVP

Continuous preparation of nimesulide nanoparticles by liquid antisolvent precipitation using spinning disc reactor

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