In Vitro and In Vivo Evaluation of Core–Shell Mesoporous Silica as a Promising Water-Insoluble Drug Delivery System: Improving the Dissolution Rate and Bioavailability of Celecoxib With Needle-Like Crystallinity

Han, Chun; Zhang, Shanqiang; Huang, Haitao; Dong, Yan; Sui, Xiaoyu; Jian, Baiyu; Zhu, Wenquan

doi:10.1016/j.xphs.2019.06.011

Cited by 9 publications

(10 citation statements)

References 52 publications

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“…Nowadays, with the advent of encapsulation technologies using core-shell particles, medicines can stay active for longer periods of time. 59,60 They protect the drug against harsh conditions and provide the possibility of release under specic temperature or pH conditions; that's why these micro and nano-capsulation methods have gained more attention. [60][61][62] Core-shelling can be dened as a process for trapping one substance, usually the drug, in a shell as a physical barrier to protect the core from adverse factors and conditions.…”

Section: Core-shell Particlesmentioning

confidence: 99%

“…Also, by adding organic and inorganic materials to it, it can be given unique properties suitable for drug release. 54,56,59 In elds such as healthcare, separation, biotechnology, and biomedical sensing, silica has a wide variety of practical applications. Chemical stability, low cost, and formability are the unique characteristics of silica that allow spherical particles from nano to micrometer size to be formed.…”

Section: Core-shell Materialsmentioning

confidence: 99%

“…Nowadays, with the advent of encapsulation technologies using core–shell particles, medicines can stay active for longer periods of time. 59,60 They protect the drug against harsh conditions and provide the possibility of release under specific temperature or pH conditions; that's why these micro and nano-capsulation methods have gained more attention. 60–62 …”

Section: Core–shell Particlesmentioning

confidence: 99%

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Microfluidics for core–shell drug carrier particles – a review

et al. 2021

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Section: Core-shell Particlesmentioning

confidence: 99%

Section: Core-shell Materialsmentioning

confidence: 99%

Section: Core–shell Particlesmentioning

confidence: 99%

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Microfluidics for core–shell drug carrier particles – a review

et al. 2021

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“…It has been used as a drug delivery system to improve the solubility and increase the bioavailability of poorly water-soluble drugs [44][45][46][47][48][49][50][51][52]. In this study, a nanoporous silica entrapped lipid-drug complex (NSC) was prepared to maximize the oral absorption of the poorly water-soluble drug, DUT.…”

Section: Introductionmentioning

confidence: 99%

Nanoporous Silica Entrapped Lipid-Drug Complexes for the Solubilization and Absorption Enhancement of Poorly Soluble Drugs

2021

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This study aims to examine the contribution of nanoporous silica entrapped lipid-drug complexes (NSCs) in improving the solubility and bioavailability of dutasteride (DUT). An NSC was loaded with DUT (dissolved in lipids) and dispersed at a nanoscale level using an entrapment technique. NSC microemulsion formation was confirmed using a ternary phase diagram, while the presence of DUT and lipid entrapment in NSC was confirmed using scanning electron microscopy. Differential scanning calorimetry and X-ray diffraction revealed the amorphous properties of NSC. The prepared all NSC had excellent flowability and enhanced DUT solubility but showed no significant difference in drug content homogeneity. An increase in the lipid content of NSC led to an increase in the DUT solubility. Further the NSC were formulated as tablets using D-α tocopheryl polyethylene glycol 1000 succinate, glyceryl caprylate/caprate, and Neusilin®. The NSC tablets showed a high dissolution rate of 99.6% at 30 min. Furthermore, NSC stored for 4 weeks at 60 °C was stable during dissolution testing. Pharmacokinetic studies performed in beagle dogs revealed enhanced DUT bioavailability when administered as NSC tablets. NSC can be used as a platform to develop methods to overcome the technical and commercial limitations of lipid-based preparations of poorly soluble drugs.

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“…Drug delivery systems are used to improve the solubility and increase the bioavailability of poorly water-soluble drugs [43][44][45][46][47][48][49][50][51][52][53]. Numerous techniques have been developed in recent years to enhance the oral bioavailability of poorly water-soluble drugs, including mesoporous silica, microemulsions [54], self-nano-emulsifying drug delivery systems [55], lyotropic liquid crystalline nanoparticles, and chitosan nanoparticles [56].…”

Section: Introductionmentioning

confidence: 99%

Formation of Self-Assembled Liquid Crystalline Nanoparticles and Absorption Enhancement of Ω-3s by Phospholipids and Oleic Acids

Jeon

Jin²,

Park

2021

Pharmaceutics

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This study aimed to optimize and evaluate self-assembled liquid crystalline nanoparticles (SALCs) prepared from phospholipids and oleic acid for enhancing the absorption of ω-3s. We explored the structure and optimal formulation of SALCs, which are composed of ω-3 ethyl ester (ω-3 EE), phospholipids, and oleic acid, using a ternary diagram and evaluated the improvement in ω-3 dissolution, permeation, and oral bioavailability. The in vitro dissolution and pharmacokinetics of ω-3 SALCs were compared with those of Omacor soft capsules (as the reference). The shape of the liquid crystal was determined according to the composition of phospholipids, oleic acids, and ω-3s and was found to be in cubic, lamellar, and hexagonal forms. The dissolution rates of eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) obtained from ω-3 SALCs were 1.7 to 2.3-fold higher than those of the Omacor soft capsules. Furthermore, a pharmacokinetic study in male beagle dogs revealed that ω-3 SALCs increased the oral bioavailability of ω-3 EE by 2.5-fold for EPA and 3.1-fold for DHA compared with the reference. We found an optimal formulation that spontaneously forms liquid crystal-based nanoparticles, improving the bioavailability of EPA and DHA, not found in the existing literature. Our findings offer insight into the impact of nanoparticle phase on the oral delivery of oil-soluble drugs and provide a novel ω-3 EE formulation that improves the bioavailability of EPA and DHA.

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In Vitro and In Vivo Evaluation of Core–Shell Mesoporous Silica as a Promising Water-Insoluble Drug Delivery System: Improving the Dissolution Rate and Bioavailability of Celecoxib With Needle-Like Crystallinity

Cited by 9 publications

References 52 publications

Microfluidics for core–shell drug carrier particles – a review

Microfluidics for core–shell drug carrier particles – a review

Nanoporous Silica Entrapped Lipid-Drug Complexes for the Solubilization and Absorption Enhancement of Poorly Soluble Drugs

Formation of Self-Assembled Liquid Crystalline Nanoparticles and Absorption Enhancement of Ω-3s by Phospholipids and Oleic Acids

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