In vitro stabilization and in vivo improvement of ocular pharmacokinetics of the multi-therapeutic agent baicalin: Delineating the most suitable vesicular systems

Ashraf, Orchid; Nasr, Maha; Nebsen, Marianne; Said, Azza Mohamed Ahmed; Sammour, Omaima A.

doi:10.1016/j.ijpharm.2018.01.041

Cited by 61 publications

(32 citation statements)

References 82 publications

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“…The free drug was separated from the encapsulated drug using centrifugal concentration 20 at 6000 rpm for 30 minutes (Hermle cooling centrifuge, Germany) using Nanosep tubes. The amount of baicalin in the filtrate was calculated using HPLC (Agilent, USA), following a previously validated reverse phase method 28,29 . Briefly, the chromatographic conditions were C18 column (Hypersil, Thermo Scientific), mobile phase methanol:water containing 0.5% acetic acid 94:6, and a detection wavelength 279 nm.…”

Section: Methodsmentioning

confidence: 99%

Polymeric nanocapsular baicalin: Chemometric optimization, physicochemical characterization and mechanistic anticancer approaches on breast cancer cell lines

El-Gogary

Gaber

Nasr

2019

Sci Rep

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Baicalin is a multi-purpose flavonoid known for its anticancer properties, but its application is hindered by its low water solubility and bioavailability. Polymeric nanocapsules were proposed in this work as a promising system for enhancing baicalin delivery, and potentiating its anticancer properties. The characterization of nanocapsules was augmented with chemometric analysis, and the selected formulations were tested on two breast cancer cell lines (MCF-7 and MDA-MB-231), with mechanistic anticancer elucidation using MTT assay, confocal microscopy uptake, flow cytometry, mechanism of cell death, reactive oxygen species production, caspase 3/7 activity and death biomarker expression using quantitative real time PCR. Results showed that baicalin nanocapsules displayed favorable pharmaceutical properties; with the formulation variables affecting their properties elucidated using chemometric factorial analysis. Nanocapsules enhanced the anticancer activity of baicalin up to 216 times for MCF-7 cells and 31 times for MDA-MB-231 after 24 hr incubation. Cellular internalization of the fluorescently labeled nanocapsules was confirmed after 4 hr incubation for both cell lines. Apoptosis was the dominant cell death mechanism, with significant up-regulation of P53 in baicalin nanocapsules treated cells. Data here presented drive to further preclinical studies to investigate the delivery of baicalin polymeric nanocapsules and their anti-cancer activity.

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Section: Methodsmentioning

confidence: 99%

Polymeric nanocapsular baicalin: Chemometric optimization, physicochemical characterization and mechanistic anticancer approaches on breast cancer cell lines

El-Gogary

Gaber

Nasr

2019

Sci Rep

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“…Other authors developed different vesicular systems to deliver baicalin, a bioactive flavonoid with various pharmacological activities. Results revealed that all vesicular systems, including liposomes, are promising vehicles for baicalin in vitro stabilization, sterilization endurance, safety and ocular pharmacokinetic (Ashraf, Nasr, Nebsen, Said, & Sammour, 2018). Some advantages of liposomes are biocompatibility, biodegradability, low toxicity and multi-compounds encapsulation.…”

Section: Liposomesmentioning

confidence: 99%

Advances in nutraceutical delivery systems: From formulation design for bioavailability enhancement to efficacy and safety evaluation

Gonçalves

Martins

Duarte

et al. 2018

Trends in Food Science & Technology

181

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Background: Aiming at the enhancement of food products' nutritional and health value, the incorporation of nutraceuticals has attracted increasing interest in the last years. However, they often exhibit low water solubility and stability, limiting their direct incorporation into food products. Also, they show very low bioavailability due to limited bioaccessibility, poor absorption and/or chemical transformation within the gastrointestinal tract. This renders their health benefits extremely difficult to be realized by the consumers. Scope and approach: In the present review the recent innovations regarding the formulation and design of biobased micro and nano-delivery systems to encapsulate nutraceuticals is discussed; it also gives an overview of the challenges associated to their development; and highlights some strategies to enhance nutraceuticals' bioavailability. An insight about delivery systems' potential toxicity (in particular at nano-scale) is also provided. Key findings and conclusions: Recent developments in the design of bio-based delivery systems offer the possibility of stabilizing and enhancing nutraceuticals' functionality within food products. In fact, different strategies can be used to enhance nutraceuticals' bioavailability: i) nano-delivery systems, besides showing a huge potential for the protection of valuable nutraceuticals during food processing/digestion, can be used to increase their bioavailability; ii) absorption enhancement technologies have been successfully used to increase nutraceuticals' membrane permeation; and iii) excipient foods have been shown to improve nutraceuticals' biological activity. However, the application of these enabling technologies to food is hindered by very pertinent issues that can be summarized in the effective preservation/maximization of the nutraceuticals' bioactivity and safety, once inside the human body.

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“…The release of curcumin from the microemulsion was performed using membrane dialysis [15][16][17]. One ml of curcumin microemulsion was placed in a cylinder and attached to the shaft of USP dissolution apparatus (Pharma Test, Germany).…”

Section: In Vitro Release Of Curcumin From the Prepared Microemulsionmentioning

confidence: 99%

Exploring the unique anticancer properties of curcumin nanoparticles

Makhlouf¹,

Almajali²,

Awadallah³

et al. 2019

COR

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The aim of the current work was to elucidate whether the encapsulation of curcumin in nanoparticles (of microemulsion type) would allow its exertion of anticancer activity on several cancer cell lines or not. Curcumin microemulsion was prepared using the water dilution method, in which oleic acid constituted the oily phase, and tween 20, ethanol constituted the surfactant and cosurfactant respectively. The microemulsion was tested for its particle size, charge, morphology using transmission electron microscopy, in vitro curcumin release, stability and anticancer activity on HCT-116 colon cancer line, A549 lung cancer cell line, and PC3 prostate cancer cell line. The safety of the formulation was tested on fibroblasts cell line. Results revealed that curcumin microemulsion was successfully prepared with a particle size of 11.45±0.21 nm, and a negative charge of -9.07 mV, and it was able to sustain the release of drug for 24 hours with a cumulative percent released of 66.72%. Its spherical morphology was confirmed using transmission electron microscopy. No significant changes in particle size or charge were observed upon storage, suggesting the physical stability of the microemulsion. Curcumin microemulsion was proven safe on the normal fibroblasts cell line, and it preserved the anticancer activity of curcumin against A549, HCT116, and PC3 cell lines. Results of this study delineate that microemulsion is a suitable nanodelivery system for curcumin, which needs to be tested on animal tumor models for verification of the anticancer properties in vivo.

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In vitro stabilization and in vivo improvement of ocular pharmacokinetics of the multi-therapeutic agent baicalin: Delineating the most suitable vesicular systems

Cited by 61 publications

References 82 publications

Polymeric nanocapsular baicalin: Chemometric optimization, physicochemical characterization and mechanistic anticancer approaches on breast cancer cell lines

Polymeric nanocapsular baicalin: Chemometric optimization, physicochemical characterization and mechanistic anticancer approaches on breast cancer cell lines

Advances in nutraceutical delivery systems: From formulation design for bioavailability enhancement to efficacy and safety evaluation

Exploring the unique anticancer properties of curcumin nanoparticles

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