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41 results on '"Jansakul, Chaweewan"'

1. Insights into the formulation properties, biocompatibility, and permeability of poorly water-soluble methoxyflavones with PEG400 and propylene glycol

Author

Eze Fredrick Nwude, Jansakul Chaweewan, and Srichana Teerapol

Subjects
methoxyflavones, compatibility, permeability, peg 400, pre-formulation study, Pharmaceutical industry, HD9665-9675
Abstract

Herein, thermal and non-thermal techniques were used to elucidate the putative physical and chemical interactions between poorly water-soluble Kaempferia methoxyflavones and PEG400/propylene glycol. Additionally, the biocompatibility of methoxyflavone-glycol solutions was evaluated using Caco-2 cells whereas the absorptive transport was investigated by measuring the apparent permeability coefficient (Papp) of the methoxyflavones and transepithelial electrical resistance (TEER) of the Caco-2 cell monolayer. Data from differential scanning calorimetry, Fourier-transform infrared (FTIR), and proton nuclear magnetic resonance (1H NMR) spectroscopic analysis revealed physico-chemical compatibility between the three methoxyflavones and PEG400/propylene glycol. Furthermore, PEG400 and propylene glycol solutions of the methoxyflavones were shown to be compatible with Caco-2 cells at pharmacologically effective concentrations. In vitro transport studies across the Caco-2 cell monolayer revealed high Papp values of 24.07 × 10–6 to 19.63 × 10–6 cm s–1 for PEG400 solutions of the methoxyflavones. The TEER values of the Caco-2 cell monolayers indicated that the increased drug transport was partly due to increased tight junction openings, but without compromising the epithelial barrier integrity. The good pharmaceutical and biocompatibility profiles, as well as improved transport of the methoxyflavones in PEG400 and propylene glycol solutions, are suggestive of the worthiness of this approach for further consideration pertaining to the development of these drugs into oral liquid dosage forms.

Published
2023
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2. Insights into the formulation properties, biocompatibility, and permeability of poorly water-soluble methoxyflavones with PEG400 and propylene glycol

Author

EZE, FREDRICK NWUDE, JANSAKUL, CHAWEEWAN, SRICHANA, TEERAPOL, EZE, FREDRICK NWUDE, JANSAKUL, CHAWEEWAN, and SRICHANA, TEERAPOL

Abstract

Herein, thermal and non-thermal techniques were used to elucidate the putative physical and chemical interactions between poorly water-soluble Kaempferia methoxyflavones and PEG400/propylene glycol. Additionally, the biocompatibility of methoxyflavone-glycol solutions was evaluated using Caco-2 cells whereas the absorptive transport was investigated by measuring the apparent permeability coefficient (Papp) of the methoxyflavones and transepithelial electrical resistance (TEER) of the Caco-2 cell monolayer. Data from differential scanning calorimetry, Fourier-transform infrared (FTIR), and proton nuclear magnetic resonance (1H-NMR) spectroscopic analysis revealed physicochemical compatibility between the three methoxyflavones and PEG400/propylene glycol. Furthermore, PEG400 and propylene glycol solutions of the methoxyflavones were shown to be compatible with Caco-2 cells at pharmacologically effective concentrations. In vitro transport studies across the Caco-2 cell monolayer revealed high Papp values of 24.07 × 10–6 to 19.63 × 10–6 cm s–1 for PEG400 solutions of the methoxyflavones. The TEER values of the Caco-2 cell monolayers indicated that the increased drug transport was partly due to increased tight junction openings, but without compromising the epithelial barrier integrity. The good pharmaceutical and biocompatibility profiles, as well as improved transport of the methoxyflavones in PEG400 and propylene glycol solutions, are suggestive of the worthiness of this approach for further consideration pertaining to the development of these drugs into oral liquid dosage forms.

Published
2023

3. Enhanced dissolution and oral bioavailability of poorly water-soluble herb (Kaempferia parviflora) extract using solid dispersions: effect of surfactants and concentrations

Author

Weerapol, Yotsanan, Tubtimsri, Sukannika, Chairuk, Pilaipan, Jansakul, Chaweewan, and Sriamornsak, Pornsak

Abstract

Purpose: Kaempferia parviflora(KP) is a Thai traditional herb. The primary pharmacologically active substances are methoxyflavones, namely, 5,7-dimethoxyflavone, 5,7,4′-trimethoxyflavone, and 3,5,7,3′,4′-pentamethoxyflavone. These methoxyflavones are poorly soluble in water and thus have low oral absorption. Methods: In previous research, dichloromethane-extracted KP (KPD) and Kollicoat®IR (PVA-co-PEG) at a 1:1 ratio were dissolved in dichloromethane and used to produce a solid dispersion (KPD/PVA-co-PEG). In this study, the effects of surface-active agents in the solid dispersion system on dissolution and bioavailability were investigated, employing a series of concentrations (1%, 3%, and 6% w/w) of various surfactants (polysorbate 20, polysorbate 60, polysorbate 65, sorbitan ester 20, sorbitan ester 40, and sorbitan ester 80). Results: The highest dissolution profiles were found (approximately 100% dissolution) when using polysorbate 20 at a concentration of 6% w/w (PS20-6) and these corroborated with the results from the surface free energy determination. The bioavailability of methoxyflavones was studied in Wistar rats: compared to KPD, AUC of KPD/PVA-co-PEG and PS20-6, they were 3.71- and 4.88-times higher, respectively. Conclusion: These results suggest that the solid dispersion-based KPD/PVA-co-PEG may be able to modify the dissolution profiles and oral absorption, and the surfactant-in-solid-dispersion system PS20-6 can be particularly effective.

Published
2024
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11. Vascular reactivity during pregnancy in the rat

Author

Jansakul., Chaweewan

Subjects
ComputingMilieux_COMPUTERSANDEDUCATION, ComputerApplications_COMPUTERSINOTHERSYSTEMS, Uncategorized
Abstract

This thesis was scanned from the print manuscript for digital preservation and is copyright the author. Researchers can access this thesis by asking their local university, institution or public library to make a request on their behalf. Monash staff and postgraduate students can use the link in the References field.

Published
2021
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20. Enhancing oral absorption of poorly water-soluble herb (Kaempferia parviflora) extract using self-nanoemulsifying formulation.

Author

Chairuk, Pilaipan, Tubtimsri, Sukannika, Jansakul, Chaweewan, Sriamornsak, Pornsak, and Weerapol, Yotsanan

Subjects
DRUG delivery systems, CASTOR oil, PEPSIN, DIETHYLENE glycol, ABSORPTION, ORAL mucosa, HERBAL medicine
Abstract

Kaempferia parviflora, a medicinal herb, treats hypertension and promotes longevity with good health and well-being. Its bioactive component is poorly soluble in water, resulting in poor absorption. This study aimed to enhance the bioavailability of K. parviflora dichloromethane (KPD) extract using a self-nanoemulsifying drug delivery system (SNEDDS). KPD was dissolved in diethylene glycol monoethyl, polyoxyl-35 castor oil and caprylic/capric glyceride, and clear yellow SNEDDS solution was obtained. The methoxyflavone markers were used for content and dissolution analysis. Solid SNEDDS was prepared by stepwise mixing of KPD using a mortar and pestle (1:1 ratio) with five solid carriers: Aerosil® 200, Florite® RE, Neusilin® US2 (NEUS), Fujicalin®, and Neusilin® UFL2. The USP apparatus II with simulated gastric fluid USP (SGF without pepsin, pH 1.2) was used in order to perform the in vitro dissolution. The methoxyflavones dissolution at 60 min from KPD, SEDDS, and SNEDDS/NEUS were approximately 16, 92, and 73%, respectively. The pharmacokinetic profiles of methoxyflavones for oral administration were studied using Wistar rats; the areas under the curve of SNEDDS/NEUS (1.77-fold) and SNEDDS (5.38-fold) were significantly higher than that of KPD. The developed formulations showed good stability after storage for 6 months under accelerated and normal conditions. [ABSTRACT FROM AUTHOR]

Published
2020
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35. An Extract from the Medicinal PlantPhyllanthus acidusand Its Isolated Compounds Induce Airway Chloride Secretion: A Potential Treatment for Cystic Fibrosis

Author

Sousa, Marisa, primary, Ousingsawat, Jiraporn, additional, Seitz, Roswitha, additional, Puntheeranurak, Supaporn, additional, Regalado, Ana, additional, Schmidt, André, additional, Grego, Tiago, additional, Jansakul, Chaweewan, additional, Amaral, Margarida D., additional, Schreiber, Rainer, additional, and Kunzelmann, Karl, additional

Published
2006
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37. Biological Activity of Crude Extract and Saponin Pseudoginsenoside-RT 1 Derived from the Fruit of Randia siamensis.

Author

Jansakul, Chaweewan, Intarit, Kanokkan, Itharat, Arunporn, Phadungcharoen, Thatree, Ruangrungsi, Nijsiri, Merica, Alexandru, and Lange, Gordon L.

Subjects
*RUBIACEAE, *SAPONINS, *PHYTOCHEMICALS, *RATS, *PHYSIOLOGY, *CHEMICALS
Abstract

Ursolic acid (1), pseudoginsenoside-RP1 ( 2), and pseudoginsenoside-RT1 (3) were isolated from the fruit of Randia siamensis. 13C NMR spectroscopy was particularly useful in confirming the structures of these components. Studies with rats showed that saponin 3 caused a decrease in blood pressure, an increase in heart rate and an increase in spontaneous contractility of the uterus. Also, a crude ethanol extract of the fruit of R. siamensis exhibited acute ichthyotoxic activity. [ABSTRACT FROM AUTHOR]

Published
1999
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38. An extract from the medicinal plant Phyllanthus acidus and its isolated compounds induce airway chloride secretion: A potential treatment for cystic fibrosis.

Author

Sousa, Marisa, Ousingsawat, Jiraporn, Seitz, Roswitha, Puntheeranurak, Supaporn, Regalado, Ana, Schmidt, André, Grego, Tiago, Jansakul, Chaweewan, Amaral, Margarida D, Schreiber, Rainer, and Kunzelmann, Karl

Abstract

According to previous reports, flavonoids and nutraceuticals correct defective electrolyte transport in cystic fibrosis (CF) airways. Traditional medicinal plants from China and Thailand contain phytoflavonoids and other bioactive compounds. We examined herbal extracts of the common Thai medicinal euphorbiaceous plant Phyllanthus acidus for their potential effects on epithelial transport. Functional assays by Ussing chamber, patch-clamping, double-electrode voltage-clamp and Ca2+ imaging demonstrate activation of Cl- secretion and inhibition of Na+ absorption by P. acidus. No cytotoxic effects of P. acidus could be detected. Mucosal application of P. acidus to native mouse trachea suggested transient and steady-state activation of Cl- secretion by increasing both intracellular Ca2+ and cAMP. These effects were mimicked by a mix of the isolated components adenosine, kaempferol, and hypogallic acid. Additional experiments in human airway cells and CF transmembrane conductance regulator (CFTR)-expressing BHK cells and Xenopus laevis oocytes confirm the results obtained in native tissues. Cl- secretion was also induced in tracheas of CF mice homozygous for Phe508del-CFTR and in Phe508del-CFTR homozygous human airway epithelial cells. Taken together, P. acidus corrects defective electrolyte transport in CF airways by parallel mechanisms including 1) increasing the intracellular levels of second messengers cAMP and Ca2+, thereby activating Ca2+-dependent Cl- channels and residual CFTR-Cl- conductance; 2) stimulating basolateral K+ channels; 3) redistributing cellular localization of CFTR; 4) directly activating CFTR; and 5) inhibiting ENaC through activation of CFTR. These combinatorial effects on epithelial transport may provide a novel complementary nutraceutical treatment for the CF lung disease.

Published
2007
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41. Saponins from Fresh Fruits of Randia siamensis(Lour) Roem. & Schult. (Rubiaceae)

Author

Khwanchuea, Rapheeporn, Queiroz, Emerson Ferreira, Marston, Andrew, Jansakul, Chaweewan, and Hostettmann, Kurt

Abstract

Bioactivity-directed fractionation of the n-butanol extract of fresh fruits of Randia siamensisled to the isolation of 4 new ginsenosides: pseudoginsenosides-RT2, -RT3, -RT4and -RT5, together with 7 known compounds. Tyramine was found to be responsible for the hypertensive activity, whereas pseudoginsenosides-RT1and -RP1were responsible for the hypotensive activity. The structures were determined by spectroscopic and chemical methods.

Published
2008
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