Interaction Studies Between Indomethacin Nanocrystals and PEO/PPO Copolymer Stabilizers

Liu, Peng; Kartal-Hodzic, Alma; Liang, Huamin; Laaksonen, Timo; Hirvonen, Jouni; Peltonen, Leena

doi:10.1007/s11095-014-1491-3

Cited by 41 publications

(35 citation statements)

References 41 publications

(42 reference statements)

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“…39 This polymer folds for attachment onto the hydrophobic surface of the drug using its PPO group, whereas the PEO tails provide a thick steric layer, which stabilizes the nanosized suspension. 40 In the current study, SEM analysis showed unprocessed GBD as irregularly shaped microsized particles (Figure 2). Size characterization was confirmed by photon correlation spectroscopy analysis where the D 50 of raw GBD particles was found to be 5 µm ( Figure 3A).…”

Section: Results and Discussion Nanosizingsupporting

confidence: 51%

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Ali

Hanafy

Alqurshi

2019

IJN

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Introduction: Presenting poorly water-soluble drugs as nanoparticles has shown to be an effective technique in enhancing drug dissolution rate, intrinsic solubility, and thus oral bioavailability. Nevertheless, working with nanoparticles introduces many challenges, one of which is their physical instability. Formulating nanoparticles into a solid dosage form may overcome such challenges and thus unlock the potential benefits of nanosizing. Methods: The current work investigates the possibility of developing a novel solid dosage form, with enhanced dissolution rate, whereby nanocrystals (~400 nm) of the class II Biopharmaceutical Classification System drug, glyburide (GBD) were fabricated through combined precipitation and homogenization procedures. Using a novel, but scalable, spraying technique, GBD nanocrystals were loaded onto commonly used tablet fillers, water-soluble lactose monohydrate (LAC), and water insoluble microcrystalline cellulose (MCC). Conventional tableting processes were then used to convert the powders generated into a tablet dosage form. Results: Studies of redispersibility showed considerable preservation of size characteristics of GBD nanocrystals during downstream processing with redispersibility indices of 105 and 118 for GBD-LAC and GBD-MCC, respectively. Characterization by differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy showed that the powders generated powders contained nanosized crystals of GBD which adhered to carrier surfaces. Powder flowability was characterized using Hausner ratio (HR) and Carr's index (CI). GBD-LAC-loaded particles exhibited poor flowability with CI and HR of 37.5% and 1.60, respectively, whilst GBD-MCC particles showed a slightly improved flowability with CI and HR of 26.47% and 1.36, respectively. The novel tablet dosage form met US Pharmacopeia specifications, including drug content, hardness, and friability. Conclusion: Higher dissolution rates were observed from the nanocrystal-based tablets compared to the microsized and commercial drug formulations. Moreover, the novel nanocrystal tablet dosage forms showed enhanced in vivo performance with area under the plasma concentrationtime curve in the first 24 hours values 1.97 and 2.24 times greater than that of marketed tablets.

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Section: Results and Discussion Nanosizingsupporting

confidence: 51%

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

Ali

Hanafy

Alqurshi

2019

IJN

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“…Adsorption of polymers stabilizes crystals by providing steric hindrance (14,25,26). If there is too little polymer or slow adsorption of the polymer onto particle surfaces, then the crystal surfaces will be partly uncovered, leading to particle agglomeration through direct particle-particle interaction or polymer-assisted bridge formation (11).…”

Section: Discussionmentioning

confidence: 99%

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

Tahara

Nishikawa

Matsui³

et al. 2016

Pharm Res

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“…Secondly, we evaluated the interaction between the drugs and CGA by SPR analysis which is widely used for monitoring the interactions of molecules occurring in very close vicinity to a transducer (gold) surface. [28][29][30][31][32][33][34][35] The kinetic parameters (k a , k d , K D ) were then calculated using TraceDrawer software. Finally, we investigated the correlation between the bitterness inhibitory ratio (%) as evaluated by taste sensor output and the kinetic parameters evaluated by SPR analysis, to clarify the relation of CGA-drug interactions to bitterness suppression by CGA.…”

Section: Taste-masking Effect Of Chlorogenic Acid (Cga) On Bitter Drumentioning

confidence: 99%

Taste-Masking Effect of Chlorogenic Acid (CGA) on Bitter Drugs Evaluated by Taste Sensor and Surface Plasmon Resonance on the Basis of CGA–Drug Interactions

Shiraishi

Haraguchi

Nakamura

et al. 2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of this study was to evaluate the taste-masking effects of chlorogenic acid (CGA) on bitter drugs using taste sensor measurements and surface plasmon resonance (SPR) analysis of CGA-drug interactions. Six different bitter drugs were used: amlodipine besylate (AMD), diphenhydramine hydrochloride (DPH), donepezil hydrochloride (DNP), rebamipide (RBM), diclofenac sodium (DCF) and etodolac (ETD). Taste sensor outputs were significantly inhibited by the addition of CGA to all drugs. The inhibition ratio of the taste sensor output decreased in the following order DPH>DNP>AMD≈DCF≈RBM≈ETD. The association rate constant (k a ) for the interaction between drugs and CGA as evaluated by SPR measurement also decreased in the following order DPH>DNP>AMD>DCF≈ETD≈RBM. It was suggested that basic drugs (AMD, DNP, DPH) associate more easily with CGA than acidic drugs (DCF, RBM, ETD). The inhibition ratios (%) of the taste sensor output of bitter drugs caused by CGA and the association rate constants (k a ) between the drugs and CGA were significantly correlated (r s 0.886, p<0.05, Spearman's correlation test). Our findings suggest that the taste-masking effects of CGA are due to its direct association with the drugs. CGA may therefore be a useful taste-masking agent for basic drugs.

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Interaction Studies Between Indomethacin Nanocrystals and PEO/PPO Copolymer Stabilizers

Cited by 41 publications

References 41 publications

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

<p>Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability</p>

In Vitro and In Vivo Characterization of Drug Nanoparticles Prepared Using PureNano™ Continuous Crystallizer to Improve the Bioavailability of Poorly Water Soluble Drugs

Taste-Masking Effect of Chlorogenic Acid (CGA) on Bitter Drugs Evaluated by Taste Sensor and Surface Plasmon Resonance on the Basis of CGA–Drug Interactions

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