Impact of Reverse Micelle Loaded Lipid Nanocapsules on the Delivery of Gallic Acid into Activated Hepatic Stellate Cells: A Promising Therapeutic Approach for Hepatic Fibrosis

Radwan, Shaimaa Ali Ali; El-Maadawy, Walaa H.; ElMeshad, Aliaa Nabil; Shoukri, Raguia Aly; Yousry, Carol

doi:10.1007/s11095-020-02891-z

Cited by 21 publications

(9 citation statements)

References 72 publications

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“…SP-HAECs were prepared according to D-optimal design using Design-Expert ® software (Stat-Ease, Inc., Minneapolis, MN) ( Table 2 ) to study the effect of variables on the vesicles’ properties to reduce the number of experimental runs needed for conducting the study (Nemr et al, 2021 ; Radwan et al., 2020 ).…”

Section: Methodsmentioning

confidence: 99%

Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies

et al. 2021

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Section: Methodsmentioning

confidence: 99%

Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies

et al. 2021

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“…VCZ-loaded ultradeformable elastosomes were prepared according to a 3 3 Box-Behnken design using Design-Expert® software (Stat-Ease, Inc., Minneapolis, MN) to study the effect of different variables on vesicle properties. It was chosen as it aids in reducing the number of experimental runs needed for conducting the study, hence optimizing costs and saving time (Alruwaili et al., 2020 ; Radwan et al., 2020 ). Factors, their levels and desirability constraints are listed in Table 1 .…”

Section: Methodsmentioning

confidence: 99%

Statistical optimization of hyaluronic acid enriched ultradeformable elastosomes for ocular delivery of voriconazole via Box-Behnken design: in vitro characterization and in vivo evaluation

et al. 2020

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Voriconazole (VCZ) is a well-known broad spectrum triazole antifungal, mainly used orally and intravenously. The study aimed to formulate VCZ into ultradeformable elastosomes for the topical treatment of ocular fungal keratitis. Different formulae were prepared using a modified ethanol injection method, employing a 3 3 Box-Behnken design. They were characterized by measuring their entrapment efficiency (EE%), particle size (PS), polydispersity index (PDI) and zeta potential (ZP). The optimized formula was subjected to further in vitro investigations and in vivo evaluation studies. The prepared vesicles had satisfactory EE%, PS, PDI and ZP values. The numerical optimization process suggested an optimal elastosomal formula (OE) composed of phosphatidyl choline and brij S100 at the weight ratio of 3.62: 1, 0.25%w/v hyaluronic acid and 5% (percentage from phosphatidyl choline/brij mixture) polyvinyl alcohol. It had high EE (72.6%), acceptable PS and PDI (362.4 nm and 0.25, respectively) and highly negative ZP of −41.7 mV. OE exhibited higher elasticity than conventional liposomes, with acceptable stability for three months. Transmission electron microscopy demonstrated the spherical morphology of vesicles with an external transparent coat of Hyaluronic acid. OE was expected to cause no ocular irritation or blurring in vision as reflected by pH and refractive index measurements. The histopathological study revealed the safety of OE for ocular use. The fungal susceptibility testing using Candida albicans demonstrated the superiority of OE to VCZ suspension, with greater and more durable growth inhibition. Therefore, OE can be regarded as a promising formula, achieving both safety and efficacy.

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“…The apoptotic effects of systems on the aHSCs were evaluated using DAPI fluorescent dye. 55 , 56 Briefly, the aHSC-T6 cells were seeded in 12 well culture plates (1 × 10 5 cells/well) for 24 h. The cells were then exposed to medium (control), plain CNPs, free GA, GA-ANCNP, GA-CACNP, and GA-CACNP/VA for 48 h. Next, the cells were washed with PBS and stained with 0.5 μg/mL DAPI for 5 min. The apoptosis signs of nucleus condensation or chromatin fragmentation were detected under fluorescence microscope (IX81, Olympus, Tokyo, Japan).…”

Section: Methodsmentioning

confidence: 99%

“…The mean fluorescence intensity percentage of each organ was then determined, where Rhodamine B fluorescence was detected at λ ex of 488 nm and λ em of 620 nm. 50 , 56 …”

Section: Methodsmentioning

confidence: 99%

<p>Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling</p>

Radwan¹,

El-Maadawy²,

Yousry³

et al. 2020

IJN

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Purpose Zein/phospholipid composite nanoparticles (CNPs) were developed as a delivery platform for gallic acid (GA), a polyphenolic compound with reported preclinical antifibrotic activities. However, the therapeutic applicability of GA is hampered owing to its low bioavailability and rapid clearance. Accordingly, we developed GA-loaded CNPs. The effect of their size, surface charge and targeting strategies was investigated and optimized, with the aim of enhancing their ability to deliver GA to the activated hepatic stellate cells (aHSCs) in order to suppress hepatic fibrosis progression. Methods Different CNP systems were prepared and characterized with regard to their particle size, zeta potential, and GA entrapment efficiency (EE%). Also, they were statistically optimized via response surface methodology. The optimized systems were investigated with regard to their in vitro GA release, in vitro efficacy on aHSCs, and in vivo biodistribution in healthy rats. Results The GA-loaded cationic CNPs coupled with vitamin A (GA-CACNP/VA; 192 nm) showed high GA EE% (60% w/w), highest cellular internalization via active targeting, and more selective hepatic distribution, relative to free GA solution, GA-loaded anionic, and GA-loaded cationic systems. Furthermore, GA-CACNP/VA markedly triggered the apoptosis of aHSCs, repressed collagen deposition, and inhibited HSCs’ activation to a lesser extent. Conclusion The GA-CACNP/VA was shown to be a promising candidate for specific and controlled delivery of GA to aHSCs, which may provide an effective antifibrotic therapeutic approach.

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Impact of Reverse Micelle Loaded Lipid Nanocapsules on the Delivery of Gallic Acid into Activated Hepatic Stellate Cells: A Promising Therapeutic Approach for Hepatic Fibrosis

Cited by 21 publications

References 72 publications

Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies

Spironolactone hyaluronic acid enriched cerosomes (HAECs) for topical management of hirsutism: in silico studies, statistical optimization, ex vivo, and in vivo studies

Statistical optimization of hyaluronic acid enriched ultradeformable elastosomes for ocular delivery of voriconazole via Box-Behnken design: in vitro characterization and in vivo evaluation

<p>Zein/Phospholipid Composite Nanoparticles for Successful Delivery of Gallic Acid into aHSCs: Influence of Size, Surface Charge, and Vitamin A Coupling</p>

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