Fabrication of spontaneous emulsifying powders for improved dissolution of poorly water-soluble drugs

Weerapol, Yotsanan; Limmatvapirat, Sontaya; Takeuchi, Hirofumi; Sriamornsak, Pornsak

doi:10.1016/j.powtec.2014.10.037

Cited by 20 publications

(10 citation statements)

References 23 publications

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“…However, in a preliminary study testing these solid carriers, calcium silicate was the most effective material. Calcium silicate is capable of absorbing a very large amount of oil (4–6 mL/g) through its numerous pores, and thus, has been commonly used for the solidification of oily formulations 26,27. In addition, the pores show a particular size distribution, which are attributed to interparticle and intraparticle pores 28…”

Section: Resultsmentioning

confidence: 99%

<p>Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate</p>

Kim¹,

Cho²,

Park³

et al. 2019

IJN

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Purpose: The objective of this study was to exploit a novel methotrexate (MTX)-loaded solid self-microemulsifying drug delivery system (SMEDDS) with enhanced bioavailability and photostability. Materials and methods: The optimized liquid SMEDDS was composed of castor oil, Tween ® 80, and Plurol ® diisostearique at a voluminous ratio of 27:63:10. The solid SMEDDS was formulated by spray drying liquid SMEDDS with the solid carrier (calcium silicate). Particle size analyzer, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and Fourier transform infrared (FTIR) spectroscopy experiments characterized the physiochemical properties of the MTX-loaded solid SMEDDS. These properties include a z-average diameter of emulsion around 127 nm and the amorphous form of the solid SMEDDS. Furthermore, their solubility, dissolution, and pharmacokinetics in Sprague-Dawley rats were analyzed in comparison with the MTX powder. Results: The final dissolution rate and required time for complete release of solid SMEDDS were 1.9-fold higher and 10 min shorter, respectively, than those of MTX powder. Pharmacokinetic analysis demonstrated 2.04- and 3.41-fold increments in AUC and Cmax, respectively in comparison to MTX powder. The AUC and C max were significantly increased in solid SMEDDS. Finally, the photostability studies revealed the substantially enhanced photostability of the MTX-loaded SMEDDS under the forced degradation and confirmatory conditions. Conclusion: This solid SMEDDS formulation could be an outstanding candidate for improving the oral bioavailability and photostability of MTX.

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Section: Resultsmentioning

confidence: 99%

<p>Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate</p>

Kim¹,

Cho²,

Park³

et al. 2019

IJN

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“…Unfortunately, these drugs may be limited in their clinical applications due to their poor solubility, adverse effects, or even toxicity. Over 70% of drugs on the current market, as well as recently discovered drugs, have been reported to be poorly water soluble [1,2,3,4,5]. These drugs require extensive research to improve their bioavailability due to low absorption or non-targeted delivery.…”

Section: Introductionmentioning

confidence: 99%

Nanoconjugation and Encapsulation Strategies for Improving Drug Delivery and Therapeutic Efficacy of Poorly Water-Soluble Drugs

Tran

2019

Pharmaceutics

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Nanoconjugations have been demonstrated to be a dominant strategy for drug delivery and biomedical applications. In this review, we intend to describe several strategies for drug formulation, especially to improve the bioavailability of poorly water-soluble molecules for future application in the therapy of numerous diseases. The context of current studies will give readers an overview of the conjugation strategies for fabricating nanoparticles, which have expanded from conjugated materials to the surface conjugation of nanovehicles. Moreover, nanoconjugates for theranostics are also discussed and highlighted. Overall, these state-of-the-art conjugation methods and these techniques and applications for nanoparticulate systems of poorly water-soluble drugs will inspire scientists to explore and discover more productive techniques and methodologies for drug development.

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“…Various porous materials, e.g., porous silicon dioxide, porous calcium silicate (PCS), have been studied as adsorbent carriers for drug delivery systems. PCS is one option for enabling improvements in the dissolution properties of drugs possessing poor water solubility [16, 17]. Previous study revealed that spontaneous emulsifying powders using PCS provided a faster dissolution of drug compared to other porous materials, i.e., fumed silica and porous silicon dioxide [18].…”

Section: Introductionmentioning

confidence: 99%

Design and optimization of resveratrol-loaded porous calcium silicate powders for dissolution and photostability enhancement

Benjasirimongkol

Piriyaprasarth

Sriamornsak

2019

Heliyon

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In this study, resveratrol (RVT) was loaded onto porous calcium silicate (PCS) powders to improve its dissolution and photostability properties. The effects of RVT/PCS powders that included varying amounts of low-methoxyl pectin (LMP), ethyl acetate (EA) and PCS on drug loading capacity, encapsulation efficiency and drug dissolution at 5-min intervals (Q 5 ) were investigated using a Box–Behnken design. The experimental results demonstrated that the EA and PCS amounts significantly influenced drug loading capacity. Encapsulation efficiency was affected by EA amount, whereas the amount of PCS had a significant effect on Q 5 . Empirical experiments demonstrated the reliability of mathematical models. A design space was established based on the criteria set for maximizing each response of the RVT/PCS powders. An optimized formulation containing 2.6% w/w LMP, 19% w/w EA and 13% w/w PCS prepared within the design space satisfied all criteria. The dissolution and photostability of RVT in the RVT/PCS powders were significantly improved. Further, the bulk density of the PCS powders in RVT/PCS was increased by LMP. The Box–Behnken design used in this study provided an improved understanding of the effects of formulation factors on RVT/PCS powder characteristics as well as the optimization of RVT/PCS powder formulations with the desired properties .

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Fabrication of spontaneous emulsifying powders for improved dissolution of poorly water-soluble drugs

Cited by 20 publications

References 23 publications

<p>Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate</p>

<p>Self-microemulsifying drug delivery system (SMEDDS) for improved oral delivery and photostability of methotrexate</p>

Nanoconjugation and Encapsulation Strategies for Improving Drug Delivery and Therapeutic Efficacy of Poorly Water-Soluble Drugs

Design and optimization of resveratrol-loaded porous calcium silicate powders for dissolution and photostability enhancement

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