Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

El-Habashy, Salma E.; Allam, Ahmed N.; El-Kamel, Amal H.

doi:10.2147/ijn.s93354

Cited by 21 publications

(4 citation statements)

References 32 publications

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“…The use of emulsification has been commonly applied to prepare polymeric nanoparticles. 23 , 44 Composite DX/HAp/PCL particles in this study were prepared using S/O/W emulsion–solvent evaporation, where DX was introduced into the system in a dispersed form. We prepared four formulations ( Table 5 ) to investigate the effect of PCL concentration in the organic phase and the presence of 4% NaCl in the aqueous phase on DX EE.…”

Section: Resultsmentioning

confidence: 99%

Biomaterial-Based Nanocomposite for Osteogenic Repurposing of Doxycycline

El-Habashy¹,

Eltaher²,

Gaballah³

et al. 2021

IJN

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Background Besides its antimicrobial action, doxycycline (DX) has lately been repurposed as a small-molecule drug for osteogenic purposes. However, osteogenic DX application is impeded by its dose-dependent cytotoxicity. Further, high-dose DX impairs cell differentiation and mineralization. Purpose Integrating DX into a biomaterial-based delivery system that can control its release would not only ameliorate its cytotoxic actions but also augment its osteogenic activity. In this work, we managed to engineer novel composite DX–hydroxyapatite–polycaprolactone nanoparticles (DX/HAp/PCL) to modify DX osteogenic potential. Methods Employing a 2 3 -factorial design, we first optimized HApN for surface-area attributes to maximize DX loading. Composite DX/HAp/PCL were then realized using a simple emulsification technique, characterized using various in vitro methods, and evaluated for in vitro osteogenesis. Results The developed HApN exhibited a favorable crystalline structure, Ca:P elemental ratio (1.67), mesoporous nature, and large surface area. DX/HAp/PCL achieved the highest reported entrapment efficiency (94.77%±1.23%) of DX in PCL-based particles. The developed composite system achieved controlled release of the water-soluble DX over 24 days. Moreover, the novel composite nanosystem managed to significantly ameliorate DX cytotoxicity on bone-marrow stem cells, as well as enhance its overall proliferation potential. Alkaline phosphatase and mineralization assays revealed superior osteodifferentiation potential of the composite system. Quantification of gene expression demonstrated that while DX solution was able to drive bone-marrow stem cells down the osteogenic lineage into immature osteoblasts after 10-day culture, the innovative composite system allowed maturation of osteodifferentiated cells. To the best of our knowledge, this is the first work to elaborate the impact of DX on the expression of osteogenic genes: RUNX2 , OSP, and BSP. Further, the osteogenicity of a DX-loaded particulate-delivery system has not been previously investigated. Conclusion Our findings indicate that repurposing low-dose DX in complementary biomaterial-based nanosystems can offer a prominent osteogenic candidate for bone-regeneration purposes.

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Section: Resultsmentioning

confidence: 99%

Biomaterial-Based Nanocomposite for Osteogenic Repurposing of Doxycycline

El-Habashy¹,

Eltaher²,

Gaballah³

et al. 2021

IJN

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“…In particular, ethyl cellulose, a biocompatible polymer used in this study is characterised by enhanced tolerability and lack of toxicity. 33 Furthermore, the spherical AXT nanoparticle with an average particle size of 185 nm falls within the optimal size range of 100-300 nm required for easy cellular penetration, bioavailability and clearance.…”

Section: Discussionmentioning

confidence: 97%

Astaxanthin inhibits hallmarks of cancer by targeting the PI3K/NF‐κΒ/STAT3 signalling axis in oral squamous cell carcinoma models

et al. 2019

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Aberrant activation of the PI3K/Akt signalling pathway, a major driving force of diverse cellular processes has been implicated in tumour development and progression. Here, we report that astaxanthin (AXT), a potent antioxidant ketocarotenoid prevents cancer hallmarks by inhibiting PI3K/Akt and the associated downstream NF‐κB and STAT‐3 signalling pathways in SCC131 and SCC4 oral cancer cells as well as in the hamster buccal pouch carcinogenesis model. Using small molecule inhibitors of NF‐κB, STAT‐3 and PI3K and by overexpression of PI3K, we provide evidence to show that AXT inhibits NF‐κB and STAT‐3 signalling and cancer hallmarks by restraining the kinase activity of PI3K/Akt. Additionally, AXT downregulated the noncoding RNAs (ncRNAs), miR‐21 and HOTAIR that influence PI3K/Akt signalling emphasising its modulatory effects on epigenetic regulation. Ethyl cellulose‐based AXT nanoparticles showed greater chemotherapeutic efficacy in the hamster oral carcinogenesis model compared to native AXT. We suggest that AXT prevents cell proliferation, apoptosis evasion, invasion and angiogenesis by intercepting the crosstalk between the PI3K/Akt, NF‐κB and STAT‐3 signalling circuits both in vitro and in vivo. Astaxanthin that abrogates the PI3K/Akt signalling axis, a central hub that orchestrates acquisition of cancer hallmarks is a promising candidate for anticancer drug development.

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“…Drug release from the CS microsphere can be controlled by utilizing a naturally existing crosslinking agent to impart a skeleton network for the pursuit of a prolonged release profile and better physiological compatibility [9]. For example, Wu and coworkers [10] reported RPG-loaded nanostructured lipid carriers with various particle sizes for enhancing oral bioavailability by solvent diffusion method.…”

Section: ■ Introductionmentioning

confidence: 99%

Improved Mucoadhesive Properties of Repaglinide-Loaded Nanoparticles: Mathematical Modelling through Machine Learning-Based Approach

Namazi

2023

Indones. J. Chem.

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This research work aims to develop a modified repaglinide-loaded chitosan-ethyl cellulose nanoparticles (RPG-ECSNPs) as a novel sustained-release dosage form with improved mucoadhesive properties using an emulsification solvent-evaporation technique. The RPG-ECSNPs with different particle sizes were prepared from various polymers containing ethyl cellulose (EC) as the internal phase and chitosan (CS) as the external phase, and the use of surfactants, including Tween 80 and poloxamer 188 as emulsifiers. In vitro drug release, drug loading amount, and entrapment efficiency have been influenced by changes in the concentrations of CS and EC. The mean droplet size and zeta potential of RPG-ECSNPs were 213 ± 8.5 nm and 16.4 ± 2.4 mV, respectively. The optimized formulation's entrapment efficiency was 66 ± 2.3%, and drug loading was 7.9 ± 1.65%. The release profile was significantly higher in PBS (90%) than in diluted hydrochloric acid (30%) during 24 h of the study. The mucoadhesive function of the particles was examined in vitro using part of rat intestines. The highest adhesive % was observed for the chitosan-coated NPs. No adhesive properties were noticed for chitosan-free NPs (P-value > 0.05). This indicated that ECSNPs can be successfully utilized for sustained and controlled drug delivery of RPG through the GIT.

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Ethyl cellulose nanoparticles as a platform to decrease ulcerogenic potential of piroxicam: formulation and in vitro/in vivo evaluation

Cited by 21 publications

References 32 publications

Biomaterial-Based Nanocomposite for Osteogenic Repurposing of Doxycycline

Biomaterial-Based Nanocomposite for Osteogenic Repurposing of Doxycycline

Astaxanthin inhibits hallmarks of cancer by targeting the PI3K/NF‐κΒ/STAT3 signalling axis in oral squamous cell carcinoma models

Improved Mucoadhesive Properties of Repaglinide-Loaded Nanoparticles: Mathematical Modelling through Machine Learning-Based Approach

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