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4. Solubility and Physical Stability Enhancement of Loratadine by Preparation of Co-Amorphous Solid Dispersion with Chlorpheniramine and Polyvinylpyrrolidone.

Author

Suknuntha, Krit, Khumpirapang, Nattakanwadee, Tantishaiyakul, Vimon, and Okonogi, Siriporn

Subjects
*DRUG solubility, *FOURIER transform infrared spectroscopy, *DISPERSION (Chemistry), *POVIDONE, *LORATADINE, *CHLORPHENIRAMINE
Abstract

Loratadine (LRD), a non-sedating and slow-acting antihistamine, is often given in combination with short-onset chlorpheniramine maleate (CPM) to increase efficacy. However, LRD has poor water solubility resulting in low bioavailability. The aim of this study was to improve LRD solubility by preparing co-amorphous LRD-CPM. However, the obtained co-amorphous LRD-CPM recrystallized rapidly, and the solubility of LRD returned to a poor state again. Therefore, co-amorphous LRD-CPM solid dispersions using polyvinylpyrrolidone (PVP) as a carrier were prepared. The obtained solid dispersions were characterized using X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FT-IR). The solubility, dissolution, and mechanism of drug release from the LRD-CPM/PVP co-amorphous solid dispersions were studied and compared with those of intact LRD, LRD/PVP solid dispersions, and co-amorphous LRD-CPM mixtures. The results from XRPD and DSC confirmed the amorphous form of LRD in the co-amorphous solid dispersions. The FTIR results indicated that there was no intermolecular interaction between LRD, CPM, and PVP. In conclusion, the obtained LRD-CPM/PVP co-amorphous solid dispersions can successfully increase the water solubility and dissolution of LRD and extend the amorphous state of LRD without recrystallization. [ABSTRACT FROM AUTHOR]

Published
2023
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7. The Binding of Alpinia galanga Oil and Its Nanoemulsion to Mammal GABA(A) Receptors Using Rat Cortical Membranes and an In Silico Modeling Platform

Author

Khumpirapang, Nattakanwadee, Suknuntha, Krit, Wongrattanakamon, Pathomwat, Jiranusornkul, Supat, Anuchapreeda, Songyot, Wellendorph, Petrine, Mullertz, Anette, Rades, Thomas, Okonogi, Siriporn, Khumpirapang, Nattakanwadee, Suknuntha, Krit, Wongrattanakamon, Pathomwat, Jiranusornkul, Supat, Anuchapreeda, Songyot, Wellendorph, Petrine, Mullertz, Anette, Rades, Thomas, and Okonogi, Siriporn

Abstract

The anesthetic effect of Alpinia galanga oil (AGO) has been reported. However, knowledge of its pathway in mammals is limited. In the present study, the binding of AGO and its key compounds, methyl eugenol, 1,8-cineole, and 4-allylphenyl acetate, to gamma-aminobutyric acid type A (GABA(A)) receptors in rat cortical membranes, was investigated using a [H-3]muscimol binding assay and an in silico modeling platform. The results showed that only AGO and methyl eugenol displayed a positive modulation at the highest concentrations, whereas 1,8-cineole and 4-allylphenyl acetate were inactive. The result of AGO correlated well to the amount of methyl eugenol in AGO. Computational docking and dynamics simulations into the GABA(A) receptor complex model (PDB: 6X3T) showed the stable structure of the GABA(A) receptor-methyl eugenol complex with the lowest binding energy of -22.16 kcal/mol. This result shows that the anesthetic activity of AGO and methyl eugenol in mammals is associated with GABA(A) receptor modulation. An oil-in-water nanoemulsion containing 20% w/w AGO (NE-AGO) was formulated. NE-AGO showed a significant increase in specific [H-3]muscimol binding, to 179% of the control, with an EC50 of 391 mu g/mL. Intracellular studies show that normal human cells are highly tolerant to AGO and the nanoemulsion, indicating that NE-AGO may be useful for human anesthesia.

Published
2022

8. The Binding of Alpinia galanga Oil and Its Nanoemulsion to Mammal GABAA Receptors Using Rat Cortical Membranes and an In Silico Modeling Platform

Author

Khumpirapang, Nattakanwadee, primary, Suknuntha, Krit, additional, Wongrattanakamon, Pathomwat, additional, Jiranusornkul, Supat, additional, Anuchapreeda, Songyot, additional, Wellendorph, Petrine, additional, Müllertz, Anette, additional, Rades, Thomas, additional, and Okonogi, Siriporn, additional

Published
2022
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13. Formulation optimization, anesthetic activity, skin permeation, and transportation pathway of Alpinia galanga oil SNEDDS in zebrafish (Danio rerio)

Author

Khumpirapang, Nattakanwadee, von Gersdorff Jørgensen, Louise, Müllertz, Anette, Rades, Thomas, Okonogi, Siriporn, Khumpirapang, Nattakanwadee, von Gersdorff Jørgensen, Louise, Müllertz, Anette, Rades, Thomas, and Okonogi, Siriporn

Abstract

Alpinia galanga oil (AGO) has an anesthetic activity but its water insoluble property limits its clinical applications. The aim of the present study was to develop a self-nanoemulsifying drug delivery system of AGO (SNEDDS-AGO) to avoid the use of organic solvent and investigate AGO transportation pathway and anesthetic activity. Three optimized formulations from a contour plots of droplet size; SNEDDS-AGO-1, SNEDDS-AGO-2, and SNEDDS-AGO-3, composed of AGO, Miglyol 812, Cremophor RH 40, Capmul MCM EP, and ethanol at the ratios of 40:10:35:10:5, 40:20:15:20:5, and 60:10:15:10:5, respectively were selected as they possessed different droplet size of 62 ± 0.5, 107 ± 2.8, and 207 ± 4.3 nm, respectively. It was found that the droplet size played an important role in fish anesthesia. SNEDDS-AGO-3 showed the longest anesthetic induction time (270 sec) (p < 0.03). Transportation pathway and skin permeation of SNEDDS-AGO-2 were investigated using nile red labelled AGO and detected by fluorescence microscope. AGO was found mostly in brain, gills, and skin suggesting that the transportation pathway of AGO in zebrafish is passing through the gills and skin to the brain. SNEDDS-AGO formulations showed significantly higher permeation through the skin than AGO ethanolic solution. In conclusion, SNEDDS is a promising delivery system of AGO.

Published
2021

15. The Binding of Alpinia galanga Oil and Its Nanoemulsion to Mammal GABA A Receptors Using Rat Cortical Membranes and an In Silico Modeling Platform.

Author

Khumpirapang, Nattakanwadee, Suknuntha, Krit, Wongrattanakamon, Pathomwat, Jiranusornkul, Supat, Anuchapreeda, Songyot, Wellendorph, Petrine, Müllertz, Anette, Rades, Thomas, and Okonogi, Siriporn

Subjects
*GABA receptors, *ALPINIA, *BINDING site assay, *MOLECULAR docking, *GABA, *METHYL aspartate
Abstract

The anesthetic effect of Alpinia galanga oil (AGO) has been reported. However, knowledge of its pathway in mammals is limited. In the present study, the binding of AGO and its key compounds, methyl eugenol, 1,8-cineole, and 4-allylphenyl acetate, to gamma-aminobutyric acid type A (GABAA) receptors in rat cortical membranes, was investigated using a [3H]muscimol binding assay and an in silico modeling platform. The results showed that only AGO and methyl eugenol displayed a positive modulation at the highest concentrations, whereas 1,8-cineole and 4-allylphenyl acetate were inactive. The result of AGO correlated well to the amount of methyl eugenol in AGO. Computational docking and dynamics simulations into the GABAA receptor complex model (PDB: 6X3T) showed the stable structure of the GABAA receptor–methyl eugenol complex with the lowest binding energy of −22.16 kcal/mol. This result shows that the anesthetic activity of AGO and methyl eugenol in mammals is associated with GABAA receptor modulation. An oil-in-water nanoemulsion containing 20% w/w AGO (NE-AGO) was formulated. NE-AGO showed a significant increase in specific [3H]muscimol binding, to 179% of the control, with an EC50 of 391 µg/mL. Intracellular studies show that normal human cells are highly tolerant to AGO and the nanoemulsion, indicating that NE-AGO may be useful for human anesthesia. [ABSTRACT FROM AUTHOR]

Published
2022
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22. Self-microemulsifying drug delivery system and nanoemulsion for enhancing aqueous miscibility of Alpinia galanga oil

Author

Khumpirapang, Nattakanwadee, Pikulkaew, Surachai, Müllertz, Anette, Rades, Thomas, Okonogi, Siriporn, Khumpirapang, Nattakanwadee, Pikulkaew, Surachai, Müllertz, Anette, Rades, Thomas, and Okonogi, Siriporn

Abstract

Alpinia galanga oil (AGO) possesses various activities but low aqueous solubility limits its application particularly in aquatic animals. AGO has powerful activity on fish anesthesia. Ethanol used for enhancing water miscible of AGO always shows severe side effects on fish. The present study explores the development of self-microemulsifying drug delivery systems (SMEDDS) and nanoemulsions (NE) to deliver AGO for fish anesthesia with less or no alcohol. Pseudoternary phase diagrams were constructed to identify the best SMEDDS-AGO formulation, whereas NE-AGO were developed by means of high-energy emulsification. The mean droplet size of the best SMEDDS-AGO was 82 ± 0.5 nm whereas that of NE-AGO was 48 ± 1.6 nm. The anesthetic effect of the developed SMEDDS-AGO and NE-AGO in koi (Cyprinus carpio) was evaluated and compared with AGO ethanolic solution (EtOH-AGO). It was found that the time of induction the fish to reach the surgical stage of anesthesia was dose dependent. NE-AGO showed significantly higher activity than SMEDDS-AGO and EtOH-AGO, respectively. EtOH-AGO caused unwanted hyperactivity in the fish. This side effect did not occur in the fish anesthetized with SMEDDS-AGO and NE-AGO. In conclusion, SMEDDS and NE are promising delivery systems for AGO.

Published
2017

26. Characterization and Biological Properties of Zederone and Zedoarondiol from Rhizomes of En-Lueang (Curcumacf. amada)

Author

Anuchapreeda, Songyot, Khumpirapang, Nattakanwadee, Chiampanichayakul, Sawitree, Nirachonkul, Wariya, Saiai, Aroonchai, Usuki, Toyonobu, and Okonogi, Siriporn

Abstract

Curcumacf. amadaRoxb., also known as En-Lueang in Thailand, belongs to the Zingiberaceae family and grows from rhizomes. These rhizomes have been used in the Thai and Ayurveda systems of medicine. However, to our knowledge, no biologically active compounds isolated from En-Lueang have been reported. In this study, natural compounds were isolated from En-Lueang and their structures were determined by spectroscopic methods. The two isolated compounds were identified as zederone (1) and zedoarondiol (2) and their cytotoxicities against KG1a cells were investigated. The EtOH extract and EtOAc fraction showed stronger cytotoxic activity than n-hexane fraction against KG1a cells. In contrast, compound 1showed strong cytotoxicity against KG1a cells, but low cytotoxicity toward normal peripheral blood mononuclear cells (PBMCs). Moreover, all the extracts and 1had no effect on red blood cell hemolysis. The antioxidant properties of 1were almost 2-fold higher than that of 2, in accordance with its total phenolic content of 8.8 mg/g, which is 2-fold higher than that of 2(4.1 mg/g). In summary, two sesquiterpene compounds with leukemic cytotoxicity activity against the KG1a cell line were identified in En-Lueang extracts.

Published
2018
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