Investigation of the in vitro performance difference of drug-Soluplus® and drug-PEG 6000 dispersions when prepared using spray drying or lyophilization

Altamimi, Mohammad A.; Neau, Steven H.

doi:10.1016/j.jsps.2016.09.013

Cited by 49 publications

(25 citation statements)

References 51 publications

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“…With the strong tendency to form micelles, the interaction between EGCG and water is mitigated, which is similar with some previous results [ 52 ]. Nagy et al has succeeded in controlling the release of spironolactone via electrospinning and extrusion using Soluplus ® as a drug carrier matrix [ 53 ].…”

Section: Resultssupporting

confidence: 92%

Amorphous Solid Dispersion of Epigallocatechin Gallate for Enhanced Physical Stability and Controlled Release

2017

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Epigallocatechin gallate (EGCG) has been recognized as the most prominent green tea extract due to its healthy influences. The high instability and low bioavailability, however, strongly limit its utilization in food and drug industries. This work, for the first time, develops amorphous solid dispersion of EGCG to enhance its bioavailability and physical stability. Four commonly used polymeric excipients are found to be compatible with EGCG in water-dioxane mixtures via a stepwise mixing method aided by vigorous mechanical interference. The dispersions are successfully generated by lyophilization. The physical stability of the dispersions is significantly improved compared to pure amorphous EGCG in stress condition (elevated temperature and relative humidity) and simulated gastrointestinal tract environment. From the drug release tests, one of the dispersions, EGCG-Soluplus® 50:50 (w/w) shows a dissolution profile that only 50% EGCG is released in the first 20 min, and the remains are slowly released in 24 h. This sustained release profile may open up new possibilities to increase EGCG bioavailability via extending its elimination time in plasma.

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Section: Resultssupporting

confidence: 92%

Amorphous Solid Dispersion of Epigallocatechin Gallate for Enhanced Physical Stability and Controlled Release

2017

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“…The samples were heated from 25 to 300 °C at a rate of 10 °C/min under dry nitrogen with a flow rate of 25 ml/min. Standard aluminum sample pans and lids were used with approximate sample sizes of 5 mg (Altamimi and Neau, 2016, Altamimi and Neau, 2017).…”

Section: Methodsmentioning

confidence: 99%

In vitro dissolution and bioavailability study of furosemide nanosuspension prepared using design of experiment (DoE)

Shariare

Altamimi

Marzan

et al. 2019

Saudi Pharmaceutical Journal

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BackgroundNanotechnology can offer the advantages of increasing solubility and bioavailability of delivering drugs like Furosemide. The aim of the current study is to investigate the in vitro and in vivo performance of furosemide nanosuspensions.MethodsFurosemide nanosuspensions were prepared by antisolvent precipitation method using full factorial experimental design. Four factors were employed namely; Stirring time, Injection rate, antisolvent: solvent ratio & stabilizer: drug ratio (at two levels = high & low). The in vitro dissolution experiments were conducted to compare the representative formulation with raw drug powder. The bioavailability of nanosuspension was, also, evaluated in mice as an animal model.ResultsSolid state characterization (PXRD, DSC and FESEM) did show physical changes during preparation and optimization of the furosemide nanosuspensions. Individual material attributes showed more significant impact on the average particle size of the nanocrystals compared to process parameters. Two-way interactions between material attributes and process parameters significantly affected nanosuspension particle size distribution. Dissolution rate of furosemide nanosuspemsion was significantly higher than that observed for raw furosemide powder. The in vivo pharmacokinetics parameters of nanosuspension in comparison to pure drug showed significant increase in Cmax and AUC(0-t), about 233% and 266%, respectively. The oral bioavailability of furosemide from nanosuspension was about 2.3 fold higher as compared with the bioavailability from pure drug.ConclusionsFurosemide nanosuspensions prepared using antisolvent precipitation method enhanced the dissolution rate and oral bioavailability compared to raw furosemide powder.

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“…SNMSD could be categorized under controlled release formulation; the use of various mathematical models in describing drug release from solid dispersion including zero-order, first-order, Higuchi, Hixson–Crowell, and Korsmeyer–Peppas models was well recognized and reported. 44 – 47 Specifically, a solid dispersion using SOL could improve dissolution due to solid-state transformation as well as micellization. The use of zero-order, first-order, Higuchi, Hixson–Crowell, and Korsmeyer–Peppas models has been successfully described for drug release from SOL-based solid dispersion.…”

Section: Methodsmentioning

confidence: 99%

“…The use of zero-order, first-order, Higuchi, Hixson–Crowell, and Korsmeyer–Peppas models has been successfully described for drug release from SOL-based solid dispersion. 47 , 48 Thus, the results obtained from the HPLC analysis were fitted into the different release kinetic models including first order, zero order, Hixson–Crowell, Higuchi matrix, and Korsmeyer–Peppas to determine the release kinetic. In addition, the release profile of native EDR and NEF was compared by calculating the dissimilarity (f1) and similarity (f2) factors to understand the impact of pH on release.…”

Section: Methodsmentioning

confidence: 99%

Self-nanomicellizing solid dispersion of edaravone: part I – oral bioavailability improvement

Parikh¹,

Kathawala²,

Tan³

et al. 2018

DDDT

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BackgroundEdaravone (EDR) is known for its free radical scavenging, antiapoptotic, antinecrotic, and anticytokine effects in neurological and non-neurological diseases. It is currently available clinically as Radicava® and Radicut®, intravenous medications, recently approved for the treatment of amyotrophic lateral sclerosis and cerebral infarction. However, the oral use of EDR is still restricted by its poor oral bioavailability (BA) due to poor aqueous solubility, stability, rapid metabolism, and low permeability. The present study reports the development of novel EDR formulation (NEF) using self-nanomicellizing solid dispersion (SNMSD) strategy with the aim to enable its oral use.Materials and methodsThe selection of a suitable carrier for the development of NEF was performed based on the miscibility study. The optimization of EDR-to-carrier ratio was conducted via kinetic solubility study after preparing SNMSDs using solvent evaporation technique. The drug–polymer carrier interaction and self-nanomicellizing properties of NEF were investigated with advanced characterization studies. In vitro permeation, metabolism, and dissolution study was carried out to examine the effect of the presence of a carrier on physico-chemical properties of EDR. Additionally, the dose-dependent pharmacokinetic study of NEF was conducted and compared with the EDR suspension.ResultsSoluplus® (SOL) as a carrier was selected based on the potential for improving aqueous solubility. The NEF containing EDR and SOL (1:5) resulted in the highest enhancement in aqueous solubility (17.53-fold) due to amorphization, hydrogen bonding interaction, and micellization. Moreover, the NEF demonstrated significant improvement in metabolism, permeability, and dissolution profile of EDR. Furthermore, the oral BA of NEF showed 10.2-, 16.1-, and 14.8-fold enhancement compared to EDR suspension at 46, 138, and 414 µmol/kg doses.ConclusionThe results demonstrated that SNMSD strategy could serve as a promising way to enhance EDR oral BA and NEF could be a potential candidate for the treatment of diseases in which oxidative stress plays a key role in their pathogenesis.

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Investigation of the in vitro performance difference of drug-Soluplus® and drug-PEG 6000 dispersions when prepared using spray drying or lyophilization

Cited by 49 publications

References 51 publications

Amorphous Solid Dispersion of Epigallocatechin Gallate for Enhanced Physical Stability and Controlled Release

Amorphous Solid Dispersion of Epigallocatechin Gallate for Enhanced Physical Stability and Controlled Release

In vitro dissolution and bioavailability study of furosemide nanosuspension prepared using design of experiment (DoE)

Self-nanomicellizing solid dispersion of edaravone: part I – oral bioavailability improvement

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Investigation of the in vitro performance difference of drug-Soluplus® and drug-PEG 6000 dispersions when prepared using spray drying or lyophilization

Cited by 49 publications

References 51 publications

Amorphous Solid Dispersion of Epigallocatechin Gallate for Enhanced Physical Stability and Controlled Release

Amorphous Solid Dispersion of Epigallocatechin Gallate for Enhanced Physical Stability and Controlled Release

In vitro dissolution and bioavailability study of furosemide nanosuspension prepared using design of experiment (DoE)

Self-nanomicellizing solid dispersion of edaravone: part I &ndash; oral bioavailability improvement

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Self-nanomicellizing solid dispersion of edaravone: part I – oral bioavailability improvement