Preparation, characterization, and evaluation of antioxidant activity and bioavailability of a self-nanoemulsifying drug delivery system (SNEDDS) for buckwheat flavonoids

Abstract The self-nanoemulsifying drug delivery system has shown many advantages in drug delivery. In this study, a self-nanoemulsifying drug delivery system of buckwheat flavonoids was prepared for enhancing its antioxidant activity and oral bioavailability. A nanoemulsion of buckwheat flavonoids was developed and characterized, and its antioxidant, in vitro release, and in vivo bioavailability were determined. The nanoemulsion was optimized by the central composite design response surface experiment, and its particle size, polymer dispersity index (PDI), zeta potential, morphology, encapsulation efficiency, and stability were evaluated. The antioxidant activity was tested by measuring its 2,2-diphenyl-1-picrylhydrazyl scavenging activity, hydroxyl radical scavenging activity, and superoxide anion scavenging ability. In vitro release of buckwheat flavonoids nanoemulsion showed a higher cumulative release than the suspension, and the release fitting model followed the Ritger–Peppas and Weibull models. The effective concentration of the nanoemulsion was evaluated in vivo using a Wistar rat model, and the area under the plasma concentration-time curve of the buckwheat flavonoids nanoemulsion was 2.2-fold higher than that of the buckwheat flavonoid suspension. The Cmax of the nanoemulsion was 2.6-fold greater than that of the suspension. These results indicate that the nanoemulsion is a promising oral drug delivery system that can improve the oral bioavailability to satisfy the clinical requirements.

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Thermosensitive Drug Delivery System of Salmon Calcitonin: In Vitro Release, In Vivo Absorption, Bioactivity and Therapeutic Efficacies

Pharmaceutical Research ◽

10.1007/s11095-009-0015-z ◽

2009 ◽

Vol 27 (2) ◽

pp. 272-284 ◽

Cited By ~ 31

Author(s):

Yu Tang ◽

Jagdish Singh

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Salmon Calcitonin ◽

In Vitro Release ◽

In Vivo Absorption ◽

Vitro Release

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Montmorillonite-Alginate Nanocomposites as a Drug Delivery System: Intercalation and In Vitro Release of Vitamin B1 and Vitamin B6

Journal of Biomaterials Applications ◽

10.1177/0885328209344003 ◽

2009 ◽

Vol 25 (2) ◽

pp. 161-177 ◽

Cited By ~ 48

Author(s):

Bhavesh D. Kevadiya ◽

Ghanshyam V. Joshi ◽

Hasmukh A. Patel ◽

Pravin G. Ingole ◽

Haresh M. Mody ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Vitamin B6 ◽

In Vitro Release ◽

Vitamin B1 ◽

Vitro Release

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Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽

10.3390/nano11112920 ◽

2021 ◽

Vol 11 (11) ◽

pp. 2920

Author(s):

Ameeduzzafar Zafar ◽

Syed Sarim Imam ◽

Nabil K. Alruwaili ◽

Omar Awad Alsaidan ◽

Mohammed H. Elkomy ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Delivery ◽

Ex Vivo ◽

In Vitro Release ◽

System Optimization ◽

Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

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Self Nanoemulsifying Drug Delivery System of Olanzapine for Enhanced Oral Bioavailability: In vitro, In vivo Characterisation and In vitro -In vivo Correlation

Journal of Bioequivalence & Bioavailability ◽

10.4172/jbb.1000159 ◽

2013 ◽

Vol 05 (05) ◽

Author(s):

Raman Suresh Kumar Urmila Sri Syamala

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Bioavailability

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Self microemulsifying drug delivery system of lurasidone hydrochloride for enhanced oral bioavailability by lymphatic targeting: In vitro, Caco-2 cell line and in vivo evaluation

European Journal of Pharmaceutical Sciences ◽

10.1016/j.ejps.2019.105027 ◽

2019 ◽

Vol 138 ◽

pp. 105027 ◽

Cited By ~ 9

Author(s):

Mitali H. Patel ◽

Krutika K. Sawant

Keyword(s):

Drug Delivery ◽

Cell Line ◽

Drug Delivery System ◽

Delivery System ◽

Oral Bioavailability ◽

In Vivo Evaluation ◽

Lurasidone Hydrochloride ◽

Lymphatic Targeting

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Enhanced Oral Bioavailability and Improved Biological Activities of a Quercetin/Resveratrol Combination Using a Liquid Self-Microemulsifying Drug Delivery System

Planta Medica ◽

10.1055/a-1270-7606 ◽

2020 ◽

Author(s):

Patcharawalai Jaisamut ◽

Subhaphorn Wanna ◽

Surasak Limsuwan ◽

Sasitorn Chusri ◽

Kamonthip Wiwattanawongsa ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Bioavailability ◽

Biological Activities ◽

Area Under The Curve ◽

Aqueous Solubility ◽

The Self

AbstractBoth quercetin and resveratrol are promising plant-derived compounds with various well-described biological activities; however, they are categorized as having low aqueous solubility and labile natural compounds. The purpose of the present study was to propose a drug delivery system to enhance the oral bioavailability of combined quercetin and resveratrol. The suitable self-microemulsifying formulation containing quercetin together with resveratrol comprised 100 mg Capryol 90, 700 mg Cremophor EL, 200 mg Labrasol, 20 mg quercetin, and 20 mg resveratrol, which gave a particle size of 16.91 ± 0.08 nm and was stable under both intermediate and accelerated storage conditions for 12 months. The percentages of release for quercetin and resveratrol in the self-microemulsifying formulation were 75.88 ± 1.44 and 86.32 ± 2.32%, respectively, at 30 min. In rats, an in vivo pharmacokinetics study revealed that the area under the curve of the self-microemulsifying formulation containing quercetin and resveratrol increased approximately ninefold for quercetin and threefold for resveratrol compared with the unformulated compounds. Moreover, the self-microemulsifying formulation containing quercetin and resveratrol slightly enhanced the in vitro antioxidant and cytotoxic effects on AGS, Caco-2, and HT-29 cells. These findings demonstrate that the self-microemulsifying formulation containing quercetin and resveratrol could successfully enhance the oral bioavailability of the combination of quercetin and resveratrol without interfering with their biological activities. These results provide valuable information for more in-depth research into the utilization of combined quercetin and resveratrol.

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