Formulation optimization of solid self-microemulsifying pellets for enhanced oral bioavailability of curcumin

Sha, Kang; Ma, Qianfang; Veroniaina, Hanitrarimalala; Qi, Xiaole; Qin, Jiayi; Wu, Zhenghong

doi:10.1080/10837450.2021.1899203

Cited by 13 publications

(5 citation statements)

References 36 publications

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“…CXB had the highest solubility (418.7±7.45 mg/g) in Transcutol HP as co-emulsifier probably due to the formation of the hydrogen bond between carbonyl from CXB and the hydroxyl from Transcutol HP (fig. 2), Therefore, the Transcutol HP was selected as a co-emulsifier to improve the solubility of CXB in the system and to stabilize the microemulsion for reducing the interfacial tension as reported by others [28] . The solubility of CXB in the oil phase (Castor oil, MCT, Oleic acid)…”

Section: Resultsmentioning

confidence: 99%

Improving the Oral Absorption of Celecoxib via Solid Self-Microemulsion Drug Delivery System: Preparation and In Vitro/In Vivo Evaluation

Zhang,

Wu,

Feng

et al. 2023

IJPS

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Improving the Oral Absorption of Celecoxib via Solid Self-Microemulsion Drug Delivery SystemCelecoxib is a specific cyclooxygenase-2 inhibitor with poor solubility and low bioavailability. A solid selfmicroemulsifying drug delivery system of celecoxib was therefore developed to improve in vitro drug solubility and in vivo absorption. Solubility testing, compatibility testing and pseudo-ternary phase diagrams were employed in the design. Morphological observation, droplet size and in vitro release were used to characterize the formulation. The optimized celecoxib-liquid self-microemulsifying drug delivery system was determined as 10 % of celecoxib, 25 % of medium chain triglycerides, 56.25 % of emulsifier and 18.75 % of Transcutol HP. 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay was used to investigate the cytoxicity of active pharmaceutical ingredients, blank self-microemulsion and celecoxib liquid self-microemulsifying drug delivery system on Caco-2 cells. Celecoxib solid self-microemulsifying drug delivery system was prepared with Neusilin-US2 as a solid adsorbent and characterized using scanning electron microscopy, X-ray, Fourier-transform infrared spectroscopy, differential scanning calorimetry and in vitro release. Celecoxib liquid self-microemulsifying drug delivery system had a clear and transparent light-yellow appearance with average particle size of about 22.68 nm, zeta potential of -31.92 mv, and polydisperse coefficient of 0.141. 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide results showed that the formulations virtually had no cytotoxic effect on the cells. The results also showed that celecoxib existed in an amorphous state in celecoxib-solid self-microemulsifying drug delivery system, and the celecoxib-liquid self-microemulsifying drug delivery system and celecoxib-solid-self-microemulsifying drug delivery system had a dissolution degree of more than 90 % in different media with good stability. The pharmacokinetic studies showed that the area under curve of the liquid self-microemulsifying drug delivery system and self-microemulsifying drug delivery system increased by 6.59 and 6.37 folds, respectively, compared with celecoxib suspension. The findings showed that the developed solid self-microemulsion formulations improved the bioavailability of the drug with no cytotoxicity, hence the formulation can serve as a promising carrier for the oral delivery of celecoxib.

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Section: Resultsmentioning

confidence: 99%

Improving the Oral Absorption of Celecoxib via Solid Self-Microemulsion Drug Delivery System: Preparation and In Vitro/In Vivo Evaluation

Zhang,

Wu,

Feng

et al. 2023

IJPS

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“…This system has been utilized for the improvements in solubilities of Nrf2 modulators of low bioavailability [ [164] , [165] , [166] ], however, there are drawbacks with this technique. Despite the apparent improved dissolution rates and solubilities, animal studies have not demonstrated promising results regarding bioavailability when comparing the SMEDDS formulation of polyphenols or Nrf2 modulators to non-formulated ingredients [ 152 , 167 ]. Drug precipitation has been observed in vivo as well as limited lymphatic uptake [ [168] , [169] , [170] ].…”

Section: Challenges In the Use Of Conventional Nrf2 Activatorsmentioning

confidence: 99%

Regulation of immunomodulatory networks by Nrf2-activation in immune cells: Redox control and therapeutic potential in inflammatory diseases

Pant,

Uche,

Juric

et al. 2024

Redox Biology

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“…Jaisamut et al reported on the most successful increase in the oral bioavailability of curcumin among SMEDDS formulations in an in vivo animal model, as a 43.7-fold relative bioavailability and a 30.7-fold increase in c max (to 5.84 µg/mL), compared to non-formulated curcumin [95]. Most other SMEDDS formulations tested in in vivo animal models have shown lower increases in the oral bioavailability of polyphenols, although these have often still been by severalfold and are thus significant and promising [97][98][99].…”

Section: Self-microemulsifying Drug Delivery Systemsmentioning

confidence: 99%

Drug Delivery Strategies for Curcumin and Other Natural Nrf2 Modulators of Oxidative Stress-Related Diseases

2021

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Oxidative stress is associated with a wide range of diseases characterised by oxidant-mediated disturbances of various signalling pathways and cellular damage. The only effective strategy for the prevention of cellular damage is to limit the production of oxidants and support their efficient removal. The implication of the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway in the cellular redox status has spurred new interest in the use of its natural modulators (e.g., curcumin, resveratrol). Unfortunately, most natural Nrf2 modulators are poorly soluble and show extensive pre-systemic metabolism, low oral bioavailability, and rapid elimination, which necessitates formulation strategies to circumvent these limitations. This paper provides a brief introduction on the cellular and molecular mechanisms involved in Nrf2 modulation and an overview of commonly studied formulations for the improvement of oral bioavailability and in vivo pharmacokinetics of Nrf2 modulators. Some formulations that have also been studied in vivo are discussed, including solid dispersions, self-microemulsifying drug delivery systems, and nanotechnology approaches, such as polymeric and solid lipid nanoparticles, nanocrystals, and micelles. Lastly, brief considerations of nano drug delivery systems for the delivery of Nrf2 modulators to the brain, are provided. The literature reviewed shows that the formulations discussed can provide various improvements to the bioavailability and pharmacokinetics of natural Nrf2 modulators. This has been demonstrated in animal models and clinical studies, thereby increasing the potential for the translation of natural Nrf2 modulators into clinical practice.

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Formulation optimization of solid self-microemulsifying pellets for enhanced oral bioavailability of curcumin

Cited by 13 publications

References 36 publications

Improving the Oral Absorption of Celecoxib via Solid Self-Microemulsion Drug Delivery System: Preparation and In Vitro/In Vivo Evaluation

Improving the Oral Absorption of Celecoxib via Solid Self-Microemulsion Drug Delivery System: Preparation and In Vitro/In Vivo Evaluation

Regulation of immunomodulatory networks by Nrf2-activation in immune cells: Redox control and therapeutic potential in inflammatory diseases

Drug Delivery Strategies for Curcumin and Other Natural Nrf2 Modulators of Oxidative Stress-Related Diseases

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