Stabilized amorphous glibenclamide nanoparticles by high-gravity technique

Yu, Lei; Li, Caixia; Le, Yuan; Chen, Jianfeng; Zou, Hai‐Kui

doi:10.1016/j.matchemphys.2011.06.049

Cited by 28 publications

(21 citation statements)

References 30 publications

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“…One challenge in realizing a practical method is overcoming the high kinetic barrier imparted by the thermal constraints of orbital symmetry (7). The use of activated alkenes (8) and substrates that have the appropriate redox potentials to interact with photocatalysts (9, 10) have been described that overcome these challenges, and examples with high degrees of regio-and stereoselectivity have recently been reported (11,12).…”

Section: Acknowledgmentsmentioning

confidence: 99%

Production of amorphous nanoparticles by supersonic spray-drying with a microfluidic nebulator

Amstad

Gopinadhan

Holtze

et al. 2015

Science

114

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Amorphous nanoparticles (a-NPs) have physicochemical properties distinctly different from those of the corresponding bulk crystals; for example, their solubility is much higher. However, many materials have a high propensity to crystallize and are difficult to formulate in an amorphous structure without stabilizers. We fabricated a microfluidic nebulator that can produce amorphous NPs from a wide range of materials, even including pure table salt (NaCl). By using supersonic air flow, the nebulator produces drops that are so small that they dry before crystal nuclei can form. The small size of the resulting spray-dried a-NPs limits the probability of crystal nucleation in any given particle during storage. The kinetic stability of the a-NPs—on the order of months—is advantageous for hydrophobic drug molecules.

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Section: Acknowledgmentsmentioning

confidence: 99%

Production of amorphous nanoparticles by supersonic spray-drying with a microfluidic nebulator

Amstad

Gopinadhan

Holtze

et al. 2015

Science

114

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“…HGAP technology has been successfully applied to prepare nanosized armorphous drugs such as cefuroxime axetil, 24 itraconazole, 25 and glibenclamide. 26 However, the supersaturation generation and saturation solubility properties of these nanoparticles were not mentioned. Cefixime (CFX), an oral third generation cephalosporin antibiotic, issued to treat infections caused by bacteria such as pneumonia, bronchitis, and gonorrhea and ear, lung, throat, and urinary tract infections.…”

Section: Introductionmentioning

confidence: 99%

Large-Scale Preparation of Amorphous Cefixime Nanoparticles by Antisolvent Precipitation in a High-Gravity Rotating Packed Bed

Kuang

Zhang²,

Xie³

et al. 2015

Ind. Eng. Chem. Res.

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To enhance the solubility and dissolution rate, and thus potentially improve the oral bioavailability of cefixime (CFX), amorphous CFX nanoparticles were prepared via high-gravity antisolvent precipitation (HGAP) without the aid of any pharmaceutical additives in a rotating packed bed (RPB). The effects of operating variables on particle size and distribution were investigated. Compared to raw CFX, the mean size of prepared nanoparticles decreased greatly from about 2.1 μm to 57 nm, and the saturation solubility increased tremendously from 0.289 to 0.951 mg/mL. CFX nanoparticles showed good stability and were capable of generating a maximum supersaturation level, reaching up to ∼22.8 times of raw CFX's saturation solubility. Further, CFX nanoparticles achieved 100% drug dissolution within 2 min, while the raw drug did not dissolve completely after 45 min, suggesting that the solubility and dissolution properties of CFX nanoparticles were significantly improved. Since the drug recovery ratio achieved 99.9%, and the production capacity of lab-scale RPB with a continuous operation reached 1.8 kg/h, the HGAP method might offer a general and facile platform for mass production of CFX nanoparticles.

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“…Most of the previous reports about the use of different formulative strategies to improve the dissolution properties of GLI [18,53,10,61,11,12,3,58,33,47] do not provide data about the actual consequent improvement of in vivo bioavailability and therapeutic efficacy of the drug from such formulations. On the other hand, an increase in GLI bioavailability has been reported for its solid dispersions in Gelucire or PEG 6000 with respect to a commercial formulation (Daonil tablets (Hoechst)), but without any effect on the duration of the antiglycemic action [52].…”

Section: In Vivo Studies Of Anti-glycemic Effect Of Gli-loaded Slnmentioning

confidence: 99%

“…The very poor water-solubility of the drug is responsible for its limited and variable oral bioavailability [34], as well as for problems of nonbio-equivalence among its different commercial tablets [6]. Therefore, various approaches have been applied over the last years aimed at improving the solubility and dissolution properties of glibenclamide, including formation of binary [52,53] or ternary [11] solid dispersions in hydrophilic polymers, complexation with cyclodextrins [18,10], combined use of cyclodextrins and polymers [61,12], formulation as liquid SMEDDS [3] or solid SMEDDS [33], or even as microparticles [35] or nanoparticles [58,47].…”

Section: Introductionmentioning

confidence: 99%

Development of solid lipid nanoparticles as carriers for improving oral bioavailability of glibenclamide

Gonçalves

Maestrelli

Mannelli

et al. 2016

European Journal of Pharmaceutics and Biopharmaceutics

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a b s t r a c tA solid lipid nanoparticle (SLN) formulation was developed with the aim of improving the oral bioavailability and the therapeutic effectiveness of glibenclamide (GLI), a poorly water-soluble drug used in the treatment of type 2 diabetes. The SLN was prepared using different lipid components (Precirol Ò and Compritol Ò) and preparation procedures. Precirol-based SLN, obtained with the emulsion of solvent evaporation technique gave the best results and was selected for drug loading. Addition of lecithin to the SLN core or PEG coating was effective in increasing the nanoparticles stability in simulated gastric solution. Both such formulations were stable after one month storage at 5 ± 3°C, exhibited the absence of in vitro cytotoxicity, and presented a similar in vitro prolonged-release, reaching 100% release after 24 h. The lecithin-containing GLI-loaded SLN formulation, selected for in vivo studies in virtue of its higher EE% than the PEG-coated formulation (70.3% vs 19.6%), showed a significantly stronger hypoglycemic effect with respect to the drug alone, in terms of both shorter onset time and longer duration of the effect. These positive results indicated that the proposed SLN approach was successful in improving GLI oral bioavailability, confirming its potential as an effective delivery system for a suitable therapy of diabetes.

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Stabilized amorphous glibenclamide nanoparticles by high-gravity technique

Cited by 28 publications

References 30 publications

Production of amorphous nanoparticles by supersonic spray-drying with a microfluidic nebulator

Production of amorphous nanoparticles by supersonic spray-drying with a microfluidic nebulator

Large-Scale Preparation of Amorphous Cefixime Nanoparticles by Antisolvent Precipitation in a High-Gravity Rotating Packed Bed

Development of solid lipid nanoparticles as carriers for improving oral bioavailability of glibenclamide

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