Upgrading of dissolution and anti-hypertensive effect of Carvedilol via two combined approaches: self-emulsification and liquisolid techniques

Ibrahim, Tarek; Abdallah, Marwa H.; El-Megrab, Nagia A.; El-Nahas, Hanan M.

doi:10.1080/03639045.2017.1417421

Cited by 36 publications

(22 citation statements)

References 24 publications

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“…Pseudo-ternary phase diagrams provide assistance in identifying the self-dispersability potential of SEDDSs [ 30 ]. Moreover, these diagrams schematically represent the concentration range of the utilized excipients that can facilitate self-emulsification when incorporated in combination [ 57 ]. It is evident from Figure 1 that a notably large region exists on the pseudo-ternary phase diagrams for ARG, AVO, MAC and OLV SEDDSs where possible spontaneous emulsification can transpire.…”

Section: Resultsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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A quality-by-design and characterization approach was followed to ensure development of self-emulsifying drug delivery systems (SEDDSs) destined for topical delivery of the highly lipophilic clofazimine. Solubility and water-titration experiments identified spontaneous emulsification capacity of different excipient combinations and clofazimine. After identifying self-emulsification regions, check-point formulations were selected within the self-emulsification region by considering characteristics required to achieve optimized topical drug delivery. Check-point formulations, able to withstand phase separation after 24 h at an ambient temperature, were subjected to characterization studies. Experiments involved droplet size evaluation; size distribution; zeta-potential; self-emulsification time and efficacy; viscosity and pH measurement; cloud point assessment; and thermodynamic stability studies. SEDDSs with favorable properties, i.e., topical drug delivery, were subjected to dermal diffusion studies. Successful in vitro topical clofazimine delivery was observed. Olive oil facilitated the highest topical delivery of clofazimine probably due to increased oleic acid levels that enhanced stratum corneum lipid disruption, followed by improved dermal clofazimine delivery. Finally, isothermal microcalometric experiments studied the compatibility of excipients. Potential interactions were depicted between argan oil and clofazimine as well as between Span®60 and argan-, macadamia- and olive oil, respectively. However, despite some mundane incompatibilities, successful development of topical SEDDSs achieved enhanced topical clofazimine delivery.

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Section: Resultsmentioning

confidence: 99%

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

2020

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“…Vesicle size of the optimized transfersomal vesicles was carried out using Zetasizer apparatus (Mastersizer 2000 version 5.22, Malvern Instruments Ltd., Worcestershire, UK). The dynamic light scattering technique was utilized for assessing the particle size of the formulations [ 5 , 19 ].…”

Section: Methodsmentioning

confidence: 99%

Experimental Design and Optimization of Nano-Transfersomal Gel to Enhance the Hypoglycemic Activity of Silymarin

et al. 2022

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Current advancements in the research investigations focused at using natural products to generate novel dosage forms with a potential therapeutic impact. Silymarin is a natural product obtained from the herb Silybum marianum that has been shown to have remarkable hypoglycemic activity. Owing to the low enteral absorption, instability in stomach secretion, and poor solubility of Silymarin, it was better to be produced as a topical dosage form. A three-factor, three-level Box Behnken (33 BB) design was constructed to develop 15 formulations using three independent variables (phospholipid concentration, surfactant concentration, and sonication time) and two dependent variables (encapsulation efficiency and in vitro drug release). The optimized formula was added to HPMC gel and the resulting transfersomal gel was investigated for its characteristics, in vitro, ex vivo and hypoglycemic behaviors. The pH of the Silymarin-loaded transfersomal gel was 7.05, the spreadability was 55.35 mm, and the viscosity was 6.27 Pa. Furthermore, Silymarin loaded transfersomal gel had the greatest transdermal flux (92.41 µg/cm2·h), which was much greater than all other formulations. In vivo observations revealed that Silymarin loaded transfersomal gel significantly reduced blood glucose levels, compared to either Silymarin gel or oral Silymarin suspension. The findings show that the developed transfersomal gel could be an effective carrier for Silymarin transdermal delivery.

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“…Particle size of the fabricated liposomes was analyzed using Zetasizer apparatus (Malvern Instruments Ltd., Worcestershire, UK). Dynamic light scattering was used for evaluating the formulations keeping a scattering angle (90°) and temperature 25 °C [ 49 ].…”

Section: Methodsmentioning

confidence: 99%

Quality by Design for Optimizing a Novel Liposomal Jojoba Oil-Based Emulgel to Ameliorate the Anti-Inflammatory Effect of Brucine

Abdallah

Elsewedy

Lila

et al. 2021

Gels

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One of the recent advancements in research is the application of natural products in developing newly effective formulations that have few drawbacks and that boost therapeutic effects. The goal of the current exploration is to investigate the effect of jojoba oil in augmenting the anti-inflammatory effect of Brucine natural alkaloid. This is first development of a formulation that applies Brucine and jojoba oil int a PEGylated liposomal emulgel proposed for topical application. Initially, various PEGylated Brucine liposomal formulations were fabricated using a thin-film hydration method. (22) Factorial design was assembled using two factors (egg Phosphatidylcholine and cholesterol concentrations) and three responses (particle size, encapsulation efficiency and in vitro release). The optimized formula was incorporated within jojoba oil emulgel. The PEGylated liposomal emulgel was inspected for its characteristics, in vitro, ex vivo and anti-inflammatory behaviors. Liposomal emulgel showed a pH of 6.63, a spreadability of 48.8 mm and a viscosity of 9310 cP. As much as 40.57% of Brucine was released after 6 h, and drug permeability exhibited a flux of 0.47 µg/cm2·h. Lastly, % of inflammation was lowered to 47.7, which was significant effect compared to other formulations. In conclusion, the anti-inflammatory influence of jojoba oil and Brucine was confirmed, supporting their integration into liposomal emulgel as a potential nanocarrier.

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Upgrading of dissolution and anti-hypertensive effect of Carvedilol via two combined approaches: self-emulsification and liquisolid techniques

Abstract: Self-emulsifying liquisolid tablets expressed rapid onset of action with enhanced anti-hypertensive effect of Carvedilol.

Cited by 36 publications

References 24 publications

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

Experimental Design and Optimization of Nano-Transfersomal Gel to Enhance the Hypoglycemic Activity of Silymarin

Quality by Design for Optimizing a Novel Liposomal Jojoba Oil-Based Emulgel to Ameliorate the Anti-Inflammatory Effect of Brucine

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