Pharmacokinetics study of a supersaturatable self-microemulsifying drug delivery system for ellagic acid by UHPLC-Q-TOF-MS

Abstract To evaluate the bioavailability of ellagic acid loaded super-saturatable self-microemulsifying drug delivery system (S-SMEDDS), its pharmacokinetic properties were studied in rats with an ultra-high performance liquid chromatography-quadrupole time-of-flight tandem mass spectrometry. The plasma samples were treated by solid-phase extraction method, and gallic acid was used as the internal standard when determining the concentration of ellagic acid. Results showed that the established analytical method was sensitive and accurate, which is applicable to the pharmacokinetic study of ellagic acid. The drug was found to be absorbed rapidly in vivo, and the plasma concentration-time curve showed double peaks, indicating that ellagic acid were reabsorbed by entero-hepatic circulation after oral administration. Compared with ellagic acid suspension, the apparent clearance of ellagic acid-loaded S-SMEDDS and SMEDDS reduced significantly, and the AUC 0~t of them were 4.7 and 5.8-fold increase, respectively. Therefore, the bioavailability of ellagic acid-loaded S-SMEDDS was higher than that of the suspension and SMEDDS.

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Self-Nanoemulsifying Drug Delivery System of Tetrandrine for Improved Bioavailability: Physicochemical Characterization and Pharmacokinetic Study

BioMed Research International ◽

10.1155/2018/6763057 ◽

2018 ◽

Vol 2018 ◽

pp. 1-10 ◽

Cited By ~ 3

Author(s):

Chunxia Liu ◽

Li Lv ◽

Wei Guo ◽

Lan Mo ◽

Yaoxing Huang ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Pharmacokinetic Study ◽

Oral Bioavailability ◽

Ternary Phase Diagram ◽

Physicochemical Characterization ◽

Fold Increase ◽

Study Results

The main purpose of this study was to investigate the potential of self-nanoemulsified drug delivery system (SNEDDS) to improve the oral bioavailability of tetrandrine (Tet). SNEDDS was developed by using rational blends of excipients with good solubilizing ability for Tet which was selected based on solubility studies. Further ternary phase diagram was constructed to determine the self-emulsifying region. The optimal formulation with the best self-nanoemulsified and solubilization ability consisted of 40% (w/w) oleic acid as oil, 15% (w/w) SPC and 30% (w/w) Cremophor RH-40 as surfactant, and 15% (w/w) PEG400as cosurfactant. The average droplet size and zeta-potential of the optimal Tet SNEDDS were 19.75±0.37 nm and 1.87±0.26 mv, respectively. The dissolute rate of Tet SNEDDS in various dissolution media was remarkably faster than Tet commercial tablet. Moreover, in vivo pharmacokinetic study results show that significant increase (p≤ 0.05) in the peak concentration (Cmax) and the area under the curve (AUC) of Tet was observed after the oral administration of Tet SNEDDS and the absorption of Tet from SNEDDS resulted in approximately 2.33-fold increase in oral bioavailability compared with the commercial tablet. Our research suggests that the prepared Tet SNEDDS could be a good candidate for improved the dissolution and oral bioavailability of Tet.

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Glucan particles as anti-inflammatory agent and drug delivery system for natural compounds in experimentally induced intestinal inflammation in vivo

10.1055/s-0037-1608375 ◽

2017 ◽

Author(s):

D Rotrekl ◽

Z Vochyánová ◽

L Paráková ◽

I Saloň ◽

P Šalamúnová ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Intestinal Inflammation ◽

Natural Compounds ◽

Inflammatory Agent ◽

Anti Inflammatory ◽

Experimentally Induced

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Development and Evaluation of Floating Pulsatile Drug Delivery System Using Meloxicam

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v7i04.10647 ◽

2017 ◽

Vol 7 (04) ◽

Author(s):

ShirishaG. Suddala ◽

S. K. Sahoo ◽

M. R. Yamsani

Keyword(s):

Rheumatoid Arthritis ◽

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Lag Time ◽

Oral Dosage ◽

Lag Phase ◽

Pulsatile Drug Delivery

Objective: The objective of this research work was to develop and evaluate the floating– pulsatile drug delivery system (FPDDS) of meloxicam intended for Chrono pharmacotherapy of rheumatoid arthritis. Methods: The system consisting of drug containing core, coated with hydrophilic erodible polymer, which is responsible for a lag phase for pulsatile release, top cover buoyant layer was prepared with HPMC K4M and sodium bicarbonate, provides buoyancy to increase retention of the oral dosage form in the stomach. Meloxicam is a COX-2 inhibitor used to treat joint diseases such as osteoarthritis and rheumatoid arthritis. For rheumatoid arthritis Chrono pharmacotherapy has been recommended to ensure that the highest blood levels of the drug coincide with peak pain and stiffness. Result and discussion: The prepared tablets were characterized and found to exhibit satisfactory physico-chemical characteristics. Hence, the main objective of present work is to formulate FPDDS of meloxicam in order to achieve drug release after pre-determined lag phase. Developed formulations were evaluated for in vitro drug release studies, water uptake and erosion studies, floating behaviour and in vivo radiology studies. Results showed that a certain lag time before drug release which was due to the erosion of the hydrophilic erodible polymer. The lag time clearly depends on the type and amount of hydrophilic polymer which was applied on the inner cores. Floating time and floating lag time was controlled by quantity and composition of buoyant layer. In vivo radiology studies point out the capability of the system of longer residence time of the tablets in the gastric region and releasing the drug after a programmed lag time. Conclusion: The optimized formulation of the developed system provided a lag phase while showing the gastroretension followed by pulsatile drug release that would be beneficial for chronotherapy of rheumatoid arthritis and osteoarthritis.

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Design and In Vivo Characterization of Novel Pulsatile Drug Delivery System of Biguanide Anti-Diabetic

International Journal of Pharmaceutical Research ◽

10.31838/ijpr/2020.12.02.0058 ◽

2020 ◽

Vol 12 (02) ◽

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Pulsatile Drug Delivery ◽

In Vivo Characterization

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Formulation, Characterization and In Vivo Evaluation of Self-Nanoemulsifying Drug Delivery System for Oral Delivery of Valsartan

Current Nanoscience ◽

10.2174/15734137113096660107 ◽

2014 ◽

Vol 10 (2) ◽

pp. 263-270 ◽

Cited By ~ 3

Author(s):

Maulick Chopra ◽

Usha Y. Nayak ◽

Aravind Kumar Gurram ◽

M. Sreenivasa Reddy ◽

K.B. Koteshwara

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Oral Delivery ◽

In Vivo Evaluation

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Design of 99mTc radiolabeled gemcitabine polymeric nanoparticles as drug delivery system and in vivo evaluation

Materials Chemistry and Physics ◽

10.1016/j.matchemphys.2021.124380 ◽

2021 ◽

Vol 263 ◽

pp. 124380

Author(s):

Çiğdem İçhedef ◽

Serap Teksöz ◽

Oğuz Çetin ◽

Burcu Aydın ◽

İbrahim Sarıkavak ◽

...

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Polymeric Nanoparticles ◽

In Vivo Evaluation

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Bioactive Glass as a Nanoporous Drug Delivery System for Teicoplanin

Applied Sciences ◽

10.3390/app10072595 ◽

2020 ◽

Vol 10 (7) ◽

pp. 2595 ◽

Cited By ~ 1

Author(s):

Chih-Ling Huang ◽

Wei Fang ◽

Bo-Rui Huang ◽

Yan-Hsiung Wang ◽

Guo-Chung Dong ◽

...

Keyword(s):

Drug Delivery ◽

Bioactive Glass ◽

Drug Delivery System ◽

Delivery System ◽

Inductively Coupled Plasma ◽

High Performance ◽

Ph Value ◽

Sol Gel ◽

Phase Identification ◽

Bet Analysis

Bioactive glass (BG) was made by the sol–gel method and doped with boron (B) to increase its bioactivity. Microstructures of BG and B-doped BG were observed by scanning electron microscopy, and phase identification was performed using an X-ray diffraction diffractometer. The ion concentrations released after soaking in simulated body fluid (SBF) for 1, 4, and 7 days were measured by inductively coupled plasma mass spectrometry, and the pH value of the SBF was measured after soaking samples to determine the variation in the environment. Brunauer–Emmett–Teller (BET) analysis was performed to further verify the characteristics of mesoporous structures. High performance liquid chromatography was used to evaluate the drug delivery ability of teicoplanin. Results demonstrated that B-doped BG performed significantly better than BG in parameters assessed by the BET analysis. B-doped BG has nanopores and more rough structures, which is advantageous for drug delivery as there are more porous structures available for drug adsorption. Moreover, B-doped BG was shown to be effective for keeping pH values stable and releasing B ions during soaking in SBF. The cumulative release of teicoplanin from BG and B-doped BG reached 20.09% and 3.17% on the first day, respectively. The drug release gradually slowed, reaching 29.43% and 4.83% after 7 days, respectively. The results demonstrate that the proposed bioactive glass has potential as a drug delivery system.

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