Adsorption of pharmaceutical excipients onto microcrystals of siramesine hydrochloride: Effects on physicochemical properties

Zimmermann, Anne; Millqvist‐Fureby, Anna; Elema, Michiel Ringkjøbing; Hansen, T.N.; Müllertz, Anette; Hovgaard, Lars

doi:10.1016/j.ejpb.2008.06.014

Cited by 72 publications

(47 citation statements)

References 31 publications

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“…Adsorption of polymeric excipients and surfactants to the surface of the newly formed particles can hinder their agglomeration through steric or electrostatic stabilization of the formed suspension [34,35]. This effect is predominant when the particles are smaller than 1 mm.…”

Section: Antisolvent Crystallization With the Addition Of Stabilizersmentioning

confidence: 95%

An innovative antisolvent precipitation process as a promising technique to prepare ultrafine rifampicin particles

Viçosa¹,

Letourneau²,

Espitalier³

et al. 2012

Journal of Crystal Growth

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a b s t r a c tMany existing and new drugs fail to be fully utilized because of their limited bioavailability due to poor solubility in aqueous media (BCS drug classes II and IV). In this work, for accelerating dissolution of this kind of poorly water-soluble drugs, an antisolvent precipitation method that does not require the use of conventional volatile organic solvents is proposed. To demonstrate this technique, ultrafine particles of rifampicin were prepared using a room temperature ionic liquid (1-ethyl 3-methyl imidazolium methyl-phosphonate) as an alternative solvent and a phosphate buffer as an antisolvent.Rifampicin solubility was measured in various solvents (1-ethyl 3-methyl imidazolium methylphosphonate, water and phosphate buffer), showing the RTIL good solvency for the model drug: rifampicin solubility was found to be higher than 90 mg/g in RTIL at 30 1C and lower than 1 mg/g in water at 25 1C. Additionally, it was demonstrated that introduction of rifampicin solution in 1-ethyl 3-methyl imidazolium methyl-phosphonate into the aqueous solution antisolvent can produce particles in the submicron range with or without hydroxypropyl methylcellulose as the stabilizer. The ultrafine particles (280-360 nm) are amorphous with enhanced solubility and faster dissolution rate. To our knowledge, this is the first published work examining the suitability of using RTILs for ultrafine drug nanoparticles preparation by an antisolvent precipitation process.

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Section: Antisolvent Crystallization With the Addition Of Stabilizersmentioning

confidence: 95%

An innovative antisolvent precipitation process as a promising technique to prepare ultrafine rifampicin particles

Viçosa¹,

Letourneau²,

Espitalier³

et al. 2012

Journal of Crystal Growth

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show abstract

“…Table 1 shows the PS of lyophilized GNA-NS powder increased from 198.8 to 203.7 nm at 4 C and to 209.1 nm at 25 C during 3 months of storage, accompanied with no obvious changes of zeta potential. Here, the growth inhibition and agglomeration prevention of particles thank to the presence of stabilizers which adsorption at the surface of particles through steric stabilization (Matteucci et al, 2006;Zimmermann et al, 2009). The powder is more stable than liquid form formulation (Supplementary Table S1) which indicated that the GNA-NS could be converted into solid dosage form.…”

Section: X-ray Powder Diffractionmentioning

confidence: 99%

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

Yuan

Zhang

et al. 2015

Drug Delivery

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Nanosuspensions (NS) can enhance the saturation solubility and dissolution velocity of poorly soluble drugs. PEG as a non-ionic surfactant plays an important role in surface modification of nanoparticles for prolonging in vivo circulation. In this study, anti-solvent precipitation method was introduced to prepare gambogenic acid nanosuspensions (GNA-NS) with PVPK30 and PEG2000 as stabilizers to settle the disadvantages of GNA. The obtained nanoparticles were spherical with a mean particle size of 183.7 nm and a zeta potential of À22.8 mV.The entrapment efficiency and drug loading of the resultant formulation were 97.3 and 29.73%. X-ray diffraction analysis confirmed the amorphous phase of GNA in NS. Fourier transform infrared indicated there may be hydrogen bond interaction between the drug and excipients. After lyophilization of GNA-NS, the freeze-dried powder displayed sufficient longterm physical stability at 4 and 25 C. In comparison to GNA solution, in vitro studies of GNA-NS showed much slower release and higher cytotoxicity in HepG2 cells. What's more, the pharmacokinetic study in rats revealed that the AUC 0-1 and t 1/2 of GNA-NS were increased 2.63-and 1.77-fold than that of the reference formulation. Taken together, in vitro/in vivo evaluations showed NS would be an effectively strategy to change the poor aqueous solubility and prolong the half-life for GNA. The GNA-NS with enhanced bioavailability and drug efficacy provided a promising delivery system for the application of GNA. KeywordsCytotoxicity, gambogenic acid, in vivo pharmacokinetics, in vitro release, nanosuspensions History

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“…20 In another work, it has been reported that cellulose ethers containing hydrophobic groups (as HPMC) adsorbed onto hydrophobic siramesine surfaces while more hydrophilic derivates (as HEC) show a lower tendency for adsorbing onto the solid-liquid interface. 21 Moreover, the stability of the polymeric nanoparticles was also correlated to the affinity of the stabilizers for the droplets surface.…”

mentioning

confidence: 99%

Agglomeration of Celecoxib by Quasi Emulsion Solvent Diffusion Method: Effect of Stabilizer

Maghsoodi

Nokhodchi

2016

Adv Pharm Bull

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Adsorption of pharmaceutical excipients onto microcrystals of siramesine hydrochloride: Effects on physicochemical properties

Cited by 72 publications

References 31 publications

An innovative antisolvent precipitation process as a promising technique to prepare ultrafine rifampicin particles

An innovative antisolvent precipitation process as a promising technique to prepare ultrafine rifampicin particles

Nanosuspensions as delivery system for gambogenic acid: characterization and in vitro/in vivo evaluation

Agglomeration of Celecoxib by Quasi Emulsion Solvent Diffusion Method: Effect of Stabilizer

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