Capsaicin Loaded Solid SNEDDS for Enhanced Bioavailability and Anticancer Activity: In-Vitro, In-Silico, and In-Vivo Characterization

Bhagwat, Durgacharan A.; Swami, Pratik A.; Nadaf, Sameer J.; Choudhari, Prafulla B.; Kumbar, Vijay; More, Harinath N.; Killedar, Suresh G.; Kawtikwar, Pravin

doi:10.1016/j.xphs.2020.10.020

Cited by 60 publications

(20 citation statements)

References 47 publications

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“…10 mL samples were put into test tubes with lids, placed in a refrigerator at 4℃ for 12 h, and then taken out and placed in an oven at 45℃ for another 12 h. 42 The above steps were repeated three times. Through visual observation, formulations that passed through the heating and cooling cycles without flocculation, phase change, or drug precipitation were used for further study.…”

Section: Methodsmentioning

confidence: 99%

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

Miao¹,

Song²,

Zuo³

et al. 2022

DDDT

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Purpose The purpose of this work was to develop an ivacaftor self-nanoemulsion drug delivery system (IVA-SNEDDS) using the newly developed double headed miscellaneous lipid (DHML) as oil phase to reduce the food effect and inter-individual absorption variability of IVA. Methods The lipids with the greatest solubility to IVA were selected as the oil phase of IVA-SNEDDS by saturation solubility method. Then, among different surfactants and co-surfactants, those with good emulsifying ability for the selected oil phase were selected, and the proportion of surfactant and co-surfactant was further selected by pseudo-ternary phase diagram. The prepared IVA-SNEDDS were screened and evaluated in vitro and in beagle dogs. Results The optimized IVA-SNEDDS formulation consisting of DHML, Tween 80, and Transcutol HP with the weight ratio of 2:2:1 was physically stable and it was easy to disperse in water, pH 1.2 hydrochloric acid and pH 6.8 phosphate buffer solution, and generated a fine homogeneous nanoemulsion, with mean globule size less than 75 nm regardless of dilution ratio. In vitro drug release studies showed that the drug in IVA-SNEDDS could be completely released in a short time, while the drug release in IVA-suspension was less than 1% at 60 min. In vivo, using IVA-suspension (Fed) as a reference, the relative oral bioavailability of IVA-suspension (Fasted), IVA-SNEDDS (Fasted), and IVA-SNEDDS (Fed) were 23.35%, 153.63%, and 149.89%, respectively. This showed that IVA-SNEDDS could eliminate the positive food effect, improve the oral bioavailability, and reduce the IVA absorption difference between individuals. Conclusion As the oil phase of SNEDDS, DHML can significantly improve the drug solubility and drug loading of IVA-SNEDDS. Moreover, DHML was easily emulsified and can effectively form a nanoemulsion in vivo and in vitro. The prepared IVA-SNEDDS can reduce the inter-individual absorption variability of IVA, eliminate its food effect and improve its oral bioavailability.

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Section: Methodsmentioning

confidence: 99%

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

Miao¹,

Song²,

Zuo³

et al. 2022

DDDT

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show abstract

“…Optimized formulation was subjected to thermodynamic stability studies to access any phase separation and stability of the formed nanoemulsion [15].…”

Section: Thermodynamic Stability Studiesmentioning

confidence: 99%

Formulation and in Vitro Evaluation of Self Nano Emulsifying Drug Delivery System of Quercetin for Enhancement of Oral Bioavailability

Mathew¹,

Varkey²

2022

Int J Curr Pharm Sci

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Objective: The study aims to develop a Self-nanoemulsifying drug delivery system (SNEDDS) of Quercetin to enhance its oral bioavailability. Methods: In the present study, Quercetin was formulated into SNEDDS using various oils, surfactants, and co-surfactants. The developed formulations were subjected to various studies like drug content analysis, droplet size and thermodynamic stability, and in vitro drug release studies. Results: From the screening of oils, surfactant and cosurfactant, the combination of Triacetin as oil phase, Tween 20 as surfactant and Ethanol as co-surfactant was selected for the development of SNEDDS of Quercetin. The composition of the formulation was optimized using pseudo ternary phase diagram. The optimized formulation has been evaluated and found to have good physical stability and improved in vitro drug release. Conclusion: A stable SNEDDS of Quercetin was developed, and results indicated substantial enhancement in the dissolution of the drug when formulated as a self-nano emulsifying drug delivery system, indicating its potential to enhance oral solubility and bioavailability of the drug.

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“…After the treatment with complex 1 , 12.1 % of the cells have undergone apoptosis and in the case of complex 2 , 8.76 % of the cells have undergone apoptosis (Figure 10), when compared to cis‐platin only 7.5 % of the cells have undergone apoptosis (Figure 10). The presence of apoptotic cells in the late apoptotic stage (Figure 10a) indicates that complexes 1 and 2 can efficiently induce apoptosis in the cells [77–79] . Flow cytometry and DAPI staining studies show that complexes 1 and 2 cause apoptotic mode of cell death, hence the apoptotic manner of cell death is evident.…”

Section: Resultsmentioning

confidence: 96%

Fluorophore Tagged Mixed Ligand Copper(II) Complexes: Synthesis, Structural Characterization, Protein Binding, DNA Cleavage and Anticancer Activity

et al. 2021

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Two fluorophore tagged copper(II) complexes [Cu(phen)(L)(ClO4)2] (1) and [Cu(bpy)(L)(H2O)(ClO4)](ClO4) (2), (where L=2‐amino‐1H‐benzo[de]isoquinoline‐1,3‐(2H)dione (L), phen=1,10‐phenanthroline and bpy=2,2′‐bipyridine) have been synthesized and structurally characterized. Structures of the copper complexes 1 and 2 were confirmed by single‐crystal X‐ray structure determination. The coordination geometry around the copper center of complexes 1 and 2 is distorted octahedral. The plasmid DNA cleavage activity of the complexes has been investigated by agarose gel electrophoresis and the study reveals that both the complexes have high plasmid DNA photo‐cleavage activity. The binding interaction ability of the metal complexes with bovine serum albumin (BSA) was investigated using fluorescence spectroscopy. The cytotoxicity of the complexes has been evaluated by MTT (3‐[4,5‐dimethylthiazole‐2‐yl]‐2,5‐diphenyltetrazolium bromide) assay against A549 (adenocarcinoma human alveolar basal epithelial cells) and MCF‐7 (breast cancer cell line) cell lines in comparison with cis‐platin. Complexes 1 and 2 have exhibited better cytotoxic activity than cis‐platin against A549 and MCF‐7 cell lines. The cellular uptake study and localization of the complexes within the cells have been investigated by fluorescence microscopy. The cell staining and flow cytometry experiments suggest that complexes induce an apoptotic mode of cell death.

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Capsaicin Loaded Solid SNEDDS for Enhanced Bioavailability and Anticancer Activity: In-Vitro, In-Silico, and In-Vivo Characterization

Cited by 60 publications

References 47 publications

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

Reduced the Food Effect and Enhanced the Oral Bioavailability of Ivacaftor by Self-Nanoemulsifying Drug Delivery System (SNEDDS) Using a New Oil Phase

Formulation and in Vitro Evaluation of Self Nano Emulsifying Drug Delivery System of Quercetin for Enhancement of Oral Bioavailability

Fluorophore Tagged Mixed Ligand Copper(II) Complexes: Synthesis, Structural Characterization, Protein Binding, DNA Cleavage and Anticancer Activity

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