Spironolactone nanocrystals for oral administration: Different pharmacokinetic performances induced by stabilizers

Mu, Simeng; Li, Mo; Guo, Meng; Yang, Wenqian; Wang, Yongjun; Li, Jingru; Fu, Qiang; Zhang, He

doi:10.1016/j.colsurfb.2016.07.051

Cited by 16 publications

(7 citation statements)

References 30 publications

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“…However, Mu et al. investigated the pharmacokinetic performances of spironolactone nanocrystals with similar particles size and different stabilizers F127 or F68 or HPMC-E5 and found that stabilizers can affect in vivo performances (Mu et al., 2016 ). It was interesting that the surface characterization, such as charge, can be different for different particles size even though prepared SLNs with same stabilizer F68 (Sanjula et al., 2009 ).…”

Section: Resultsmentioning

confidence: 99%

“…For example, Liu et al prepared PTX/F127 (1/5) nanocrystals with 105.8 nm and PTX/TPGS (1/5) nanocrystals with 77.84 nm and found that they had no significant differences in biodistribution in major organs and in tumor-bearing mice (Liu et al, 2016), and besides, Elnaggar et al fabricated daidzein complex-loaded self-emulsifying phospholipid preconcentrates (SEPPs) with or without surfactant Tween-80/ Transcutol HP and both of them had no significant differences in oral bioavailability, revealing surfactant Tween-80/ Transcutol HP having no effect on the absorption of daidzein complex-loaded SEPPs (Elnaggar et al, 2017). However, Mu et al investigated the pharmacokinetic performances of spironolactone nanocrystals with similar particles size and different stabilizers F127 or F68 or HPMC-E5 and found that stabilizers can affect in vivo performances (Mu et al, 2016). It was interesting that the surface characterization, such as charge, can be different for different particles size even though prepared SLNs with same stabilizer F68 (Sanjula et al, 2009).…”

Section: Preparation Of Nlcs With Different Particle Sizesmentioning

confidence: 99%

See 1 more Smart Citation

Repaglinide-loaded nanostructured lipid carriers with different particle sizes for improving oral absorption: preparation, characterization, pharmacokinetics, and in situ intestinal perfusion

Zhao

et al. 2019

Drug Delivery

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Section: Resultsmentioning

confidence: 99%

Section: Preparation Of Nlcs With Different Particle Sizesmentioning

confidence: 99%

Repaglinide-loaded nanostructured lipid carriers with different particle sizes for improving oral absorption: preparation, characterization, pharmacokinetics, and in situ intestinal perfusion

Zhao

et al. 2019

Drug Delivery

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“…Ionic stabilizers may not be sufficient to stabilize drug nanocrystals alone, as they may induce aggregation and agglomeration of drug crystals when passing through the gastrointestinal tract, experiencing the different pH levels. 52 In the current study, presence of poloxamer, a nonionic stabilizer, minimizes particle aggregation and enhances wettability and facilitates the GBD dissolution process. Furthermore, nanoparticles were proven to possess higher adhesiveness to absorption tissues in the GIT.…”

Section: Bioavailabilitymentioning

confidence: 87%

<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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“…For similar reasons, DSC thermograms clearly show a distinct melting endotherm, albeit with a melting point depression and reduced fusion enthalpy, as compared with as-received drug and physical mixtures [ 22 , 27 , 213 ]. Freeze-drying of drug nanosuspensions prepared by top-down approaches could either preserve drug crystallinity or result in some reduction in crystallinity, depending on the concentration/type of dispersant used [ 179 , 182 , 190 ]. Freeze drying of drug nanosuspensions prepared via LASP tends to result in a pronounced loss of crystallinity, and even complete amorphization [ 194 , 214 , 215 ].…”

Section: Preparation Characterization and Formulation Of Drug-lamentioning

confidence: 99%

Bioavailability Enhancement of Poorly Water-Soluble Drugs via Nanocomposites: Formulation–Processing Aspects and Challenges

et al. 2018

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Drug nanoparticles embedded in a dispersant matrix as a secondary phase, i.e., drug-laden nanocomposites, offer a versatile delivery platform for enhancing the dissolution rate and bioavailability of poorly water-soluble drugs. Drug nanoparticles are prepared by top-down, bottom-up, or combinative approaches in the form of nanosuspensions, which are subsequently dried to prepare drug-laden nanocomposites. In this comprehensive review paper, the term “nanocomposites” is used in a broad context to cover drug nanoparticle-laden intermediate products in the form of powders, cakes, and extrudates, which can be incorporated into final oral solid dosages via standard pharmaceutical unit operations, as well as drug nanoparticle-laden strip films. The objective of this paper is to review studies from 2012–2017 in the field of drug-laden nanocomposites. After a brief overview of the various approaches used for preparing drug nanoparticles, the review covers drying processes and dispersant formulations used for the production of drug-laden nanocomposites, as well as various characterization methods including quiescent and agitated redispersion tests. Traditional dispersants such as soluble polymers, surfactants, other water-soluble dispersants, and water-insoluble dispersants, as well as novel dispersants such as wet-milled superdisintegrants, are covered. They exhibit various functionalities such as drug nanoparticle stabilization, mitigation of aggregation, formation of nanocomposite matrix–film, wettability enhancement, and matrix erosion/disintegration. Major challenges such as nanoparticle aggregation and poor redispersibility that cause inferior dissolution performance of the drug-laden nanocomposites are highlighted. Literature data are analyzed in terms of usage frequency of various drying processes and dispersant classes. We provide some engineering considerations in comparing drying processes, which could account for some of the diverging trends in academia vs. industrial practice. Overall, this review provides rationale and guidance for drying process selection and robust nanocomposite formulation development, with insights into the roles of various classes of dispersants.

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Spironolactone nanocrystals for oral administration: Different pharmacokinetic performances induced by stabilizers

Cited by 16 publications

References 30 publications

Repaglinide-loaded nanostructured lipid carriers with different particle sizes for improving oral absorption: preparation, characterization, pharmacokinetics, and in situ intestinal perfusion

Repaglinide-loaded nanostructured lipid carriers with different particle sizes for improving oral absorption: preparation, characterization, pharmacokinetics, and in situ intestinal perfusion

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

Bioavailability Enhancement of Poorly Water-Soluble Drugs via Nanocomposites: Formulation–Processing Aspects and Challenges

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