Enhanced intestinal lymphatic absorption of saquinavir through supersaturated self-microemulsifying drug delivery systems

Jo, Kanghee; Kim, Hyeongmin; Khadka, Prakash; Jang, Taejun; Kim, Soo Jin; Hwang, Seong-Ha; Lee, Jaehwi

doi:10.1016/j.ajps.2018.11.009

Cited by 35 publications

(22 citation statements)

References 28 publications

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“…Pseudo-ternary phase diagrams give information on the phase behaviors of mixtures with various component concentrations [ 13 , 36 ]. Based on the results of the solubility screening test, the pseudo-ternary phase diagrams were drawn using olive oil, water, and Tween 80 or Labrasol; Figure 2 depicts the diagram with water, olive oil and each surfactant, and the gray areas on the diagram represent nanoemulsion zone that have a transparent appearance.…”

Section: Resultsmentioning

confidence: 99%

“…These findings also suggest that studies on lymphatic targeting and migration of anticancer drugs are crucial, and, in fact, researchers have studied a number of targeting strategies and benefits based on the structural and physiological characteristics of the lymphatic system related to drug delivery [ 6 , 7 , 8 , 9 ]. Researchers have also reported on improving bioavailability and efficacy through formulations of conventional drugs [ 10 , 11 , 12 , 13 ]. Formulation with polyaminoacid nanocapsule has been attempted to improve lymphatic delivery of docetaxel as an anticancer drug [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

“…Formulation with polyaminoacid nanocapsule has been attempted to improve lymphatic delivery of docetaxel as an anticancer drug [ 10 ]. In addition to anticancer drugs, there were several studies to formulate nanostructured lipid carriers [ 11 ], solid lipid nanoparticles [ 12 ], and self-microemulsifying drug delivery systems [ 13 ] to improve lymphatic delivery for mebendazole, quetiapine, and saquinavir, respectively.…”

Section: Introductionmentioning

confidence: 99%

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Enhanced Lymphatic Delivery of Methotrexate Using W/O/W Nanoemulsion: In Vitro Characterization and Pharmacokinetic Study

2020

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Methotrexate, which is widely used in the treatment of cancer and immune-related diseases, has limitations in use because of its low bioavailability, short half-life, and tissue toxicity. Thus, in this study, a nano-sized water-in-oil-in-water (W/O/W) double emulsion containing methotrexate was prepared to enhance its lymphatic delivery and bioavailability. Based on the results from solubility testing and a pseudo-ternary diagram study, olive oil as the oil, Labrasol as a surfactant, and ethanol as a co-surfactant, were selected as the optimal components for the nanoemulsion. The prepared nanoemulsion was evaluated for size, zeta potential, encapsulation efficiency, pH, morphology, and in vitro release profiles. Furthermore, pharmacokinetics and lymphatic targeting efficiency were assessed after oral and intravenous administration of methotrexate-loaded nanoemulsion to rats. Mean droplet size, zeta potential, encapsulation efficiency, and pH of formulated nanoemulsion were 173.77 ± 5.76 nm, −35.63 ± 0.78 mV, 90.37 ± 0.96%, and 4.07 ± 0.03, respectively. In vitro release profile of the formulation indicated a higher dissolution and faster rate of methotrexate than that of free drug. The prepared nanoemulsion showed significant increases in maximum plasma concentration, area under the plasma concentration-time curve, half-life, oral bioavailability, and lymphatic targeting efficiency in both oral and intravenous administration. Therefore, our research proposes a methotrexate-loaded nanoemulsion as a good candidate for enhancing targeted lymphatic delivery of methotrexate.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Enhanced Lymphatic Delivery of Methotrexate Using W/O/W Nanoemulsion: In Vitro Characterization and Pharmacokinetic Study

2020

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“…The supernatant was collected and diluted with phosphate buffer (pH 6.8). and quantified by spectrophotometrically at λmax of 238 nm [12,13]…”

Section: Solubility Screening Studymentioning

confidence: 99%

“…It determines the self-emulsifying region by taking the different ratios of oil and mixture of surfactant and co-surfactant [Oil: (S-COS) mix] from 9:1 to 1:9. The water was titrated into the mixture with constant stirring to observe the formation of o/w microemulsion The pseudo ternary phase diagram was constructed using software Chemix School (ternary software) [13].…”

Section: Construction Of Pseudoternary Phase Diagrammentioning

confidence: 99%

Preparation, Characterization and Stability Studies of Solid Self Emulsifying Drug Delivery System of Nifedipine

Bindhani

Mohapatra

Kar³

2020

Int J App Pharm

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Objective: The objective of this work was to improve the solubility and dissolution rate of Nifedipine by preparing a solid-self micro emulsifying drug delivery system (Solid-smedds). Methods: Liquid-self-emulsifying drug delivery system formulations were prepared by using linseed oil as oil, tween 80 as a surfactant and PEG 400 as cosurfactant. Components were selected by solubility screening studies and the self-emulsifying region was identified by the pseudo-ternary phase diagram. Thermodynamic stability study was performed for the determination of stable liquid-smedds formulation. These formulations were evaluated for self-emulsification time, drug content analysis, robustness to dilution test, particle size analysis, in vitro diffusion study, and Stability study. Solid self-micro emulsifying formulations were prepared by using aerosil-200 at a different ratio. Lf9S (0.65:1) was selected due to its highest drug entrapment efficiency and a decrease in particle size. It was selected for further studies into DSC, SEM, FTIR, and XRD analysis. Results: DSC and XRD result shows that the drug within the formulation was in the amorphous state. From the SEM study, it was observed that the drug has been uniformly distributed and having a smooth surface. From the in vitro dissolution study, it improved the dissolution rate of nifedipine which was 98.70% of drug release where pure drug release only 6.72%. Conclusion: In conclusion, a solid self-micro emulsifying drug delivery system is improved the solubility and drug release rate but also improved the stability of the formulation.

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Preparation, In Vivo and In Vitro Evaluation, and Pharmacodynamic Study of DMY‐Loaded Self‐Microemulsifying Drug Delivery System

Wang

Chen

Adu‐Frimpong³

et al. 2021

Euro J Lipid Sci & Tech

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Hyperlipidemia has become a common disease in modern society with its prevalence becoming relatively high in the world. A series of complications that accompany hyperlipidemia are seriously threatening individuals’ health. Dihydromyricetin (DMY) is a kind of polyphenol hydroxy (OH) dihydroflavonol extracted from the stems and leaves of Ampelopsis grossedentata. It has a variety of pharmacological activities. This study aims to develop a self‐microemulsifying drug delivery system (SMEDDS) to improve the oral bioavailability of DMY, and to evaluate its hypolipidemic activity. The self‐microemulsion drug delivery system is composed of medium chain triglyceride (MCT, oil phase), Tween 80 (emulsifier), and PEG 200 (coemulsifier). The prepared DMY‐SMEDDS has stable physical and chemical properties, small droplet size (15.49 ±0.15 nm), good polydispersity index (PDI = 0.160 ± 0.010), negative zeta potential (−17.37 ± 0.09 mV), and high encapsulation efficiency (98.04 ± 0.25%). The results of in vitro dissolution and in vivo pharmacokinetics show that the prepared DMY‐SMEDDS significantly improve the solubility of DMY in aqueous medium, while its oral bioavailability is 2.34 times higher than that of free drug. In conclusion, the DMY‐SMEDDS prepared in this study prospectively improves the solubility and oral bioavailability of DMY also enhance the therapeutic effect. Practical Applications: This study is relevant in the sense that SMEDDS may be used as a new strategy to improve the oral bioavailability of hydrophobic drugs. This novel nanocarrier could increase (by 2.34 times) the relative bioavailability of oral DMY‐SMEDDS in rats comparative to dihydromyricetin (DMY) suspension. Thus, DMY‐SMEDDS may prospectively be applied in food, nutraceutical, and pharmaceutical industries in view of its biocompatible excipients and good stability.

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Enhanced intestinal lymphatic absorption of saquinavir through supersaturated self-microemulsifying drug delivery systems

Cited by 35 publications

References 28 publications

Enhanced Lymphatic Delivery of Methotrexate Using W/O/W Nanoemulsion: In Vitro Characterization and Pharmacokinetic Study

Enhanced Lymphatic Delivery of Methotrexate Using W/O/W Nanoemulsion: In Vitro Characterization and Pharmacokinetic Study

Preparation, Characterization and Stability Studies of Solid Self Emulsifying Drug Delivery System of Nifedipine

Preparation, In Vivo and In Vitro Evaluation, and Pharmacodynamic Study of DMY‐Loaded Self‐Microemulsifying Drug Delivery System

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