Naresuan University Journal: Science and Technology (NUJST), Sep 24, 2018
A reversed-phase HPLC method for the simultaneous determination gallic acid, gallocatechin, catec... more A reversed-phase HPLC method for the simultaneous determination gallic acid, gallocatechin, catechin, epicatechin and epigallocatechin gallate in banana peel extract was developed. The separation was achieved using a reversed-phase (C18) analytical column and an isocratic elution using a mobile phase of acetonitrile-formic acid (15:85 v/v, pH 2.5). The detection wavelength was set at 275 nm. The chromatographic parameters such as peak asymmetry, capacity factor, selectivity factor and resolution factor were determined. Optimization of parameters such as the detection wavelength, the amount of acetonitrile for a mobile phase and the methanol concentration on stability of standard solution was carried out. Under the optimum conditions, the order of elution was gallic acid, gallocatechin, catechin, epicatechin and epigallocatechin gallate, respectively, with the analysis time of 20 min per chromatogram. The validation parameters such as linearity, range, limit of detection, limit of quantitation, selectivity, precision and accuracy, were evaluated. Linear calibration graphs were in range of 0.25-20 mg L-1 for gallic acid and 0.50-30 mg L-1 for gallocatechin, catechin, epicatechin and epigallocatechin gallate, respectively. The proposed HPLC method was simple and rapid, and successfully applied to real samples of banana peel (ripe and green) extracts. Acceptable precisions (%RSD) and recoveries (%Rec) were obtained in the ranges of 0.3-5.9 % and 83±1-128±1 %, respectively, by spiking all samples with a mixed standard solution of five analytes. Banana peel extracts contains many phenolic compounds, especially gallic acid, catechin, epicatechin and epigallocatechin gallate.
ABSTRACT Abstract Previous studies in our laboratories showed that a novel nonionic liposome form... more ABSTRACT Abstract Previous studies in our laboratories showed that a novel nonionic liposome formulation composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10) at a weight ratio composition of 57:15:28 delivered more cyclosporin-A (CsA) into and through the skin than phospholipid-based liposomal formulations and more conventional formulations that were tested. Since only a single GDL:CH:POE-10 composition was tested, we initiated studies to determine if it would be possible to control the rate and extent of drug uptake by varying the ratios of the liposome-forming components of the formulation. This report describes how the GDL to POE-10 ratio (CH being held constant at 15 wt%) influences the rate and extent of uptake of CsA following topical application of nonionic liposomal formulations to hairless mouse skin mounted on Franz diffusion cells. The results indicate that the rate and extent of CsA uptake is highest between GDL/POE-10 ratios of about 1 to 1.5 and decreases steadily at ratios above and below this range. The effect of liposomal composition on CsA deposition is probably the result of a number of complex and interrelated factors including partitioning of CsA from the formulation into the skin and permeation enhancer effects.
Clinical, Cosmetic and Investigational Dermatology, May 1, 2019
Objective: We compared the efficacy of an antiacne hydrogel formulated with a combination of Aloe... more Objective: We compared the efficacy of an antiacne hydrogel formulated with a combination of Aloe barbadensis leaf extract, Garcinia mangostana peel extract, and Camellia sinensis leaf extract (AGC) at a ratio of 50:25:1 with a marketed 1% clindamycin gel (CG) formulation on antiacne and antiblotch activities. Methods: A single-center, parallel-arm, randomized controlled trial was performed from November 2017 to April 2018. Sixty subjects with mild-moderate acne severity according to the the American Academy of Dermatology were enrolled for the study. Outcome end points were total acne lesions (TALs) and acne-severity index (ASI) by counting the inflamed lesions and comedones and skin colors using erythema and melanin values. Results: For TALss, a decrease (P<0.0001) in the number of total inflamed lesions from baseline was evidenced in AGC group, but not in the CG group. Higher reduction in mean ASI in the AGC group was seen than in the CG group. However, there was no statistically significant difference regarding reduction in ASI between the AGC and CG groups. For erythema, a remarked reduction in skin redness from baseline was clearly seen at day 3 (P<0.05) in the AGC group. No significant decrease in erythema values from baseline was seen in the CG group. A significant decrease (P=0.037) in mean melanin value from baseline was seen in the AGC group after 14 days of twice-daily use, but not in the CG group. Both products were well tolerated, with no reports of severe adverse events. Conclusion: An anti-acne hydrogel containing a combination of mangosteen rinds, aloe vera gel, and green tea-leaf extracts was superior to 1% clindamycin gel in antiacne and antiblotch activities when measured by TALs and erythema and melanin values.
World Academy of Science, Engineering and Technology, International Journal of Medical, Health, Biomedical, Bioengineering and Pharmaceutical Engineering, Oct 2, 2016
ABSTRACT Abstract In a previous report (1), we showed that the rate and extent of uptake of cyclo... more ABSTRACT Abstract In a previous report (1), we showed that the rate and extent of uptake of cyclosporin-A (CsA) following topical application of nonionic liposomal formulations composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10) into and through hairless mouse skin mounted on Franz diffusion cells could be controlled by varying the ratios of GDL to POE-10 (CH being held constant at 15 wt%). However, the pathways of transport as well as the dominant factors that control drug delivery from these formulations are not well understood. In this report, we describe results from studies similar in design to that reported earlier but using the melted form of the lipid components as a vehicle for transport of CsA into and through hairless mouse skin. The results suggest that the transport of CsA from liposomal formulations into and through the skin occurs as a result of dehydration of the liposomes followed by melting of the lipid components on the skin. Microautoradiographic studies suggest that CsA is predominantly transported via the pilosebaceous pathway.
ABSTRACT Abstract In a previous report (1), we showed that the rate and extent of uptake of cyclo... more ABSTRACT Abstract In a previous report (1), we showed that the rate and extent of uptake of cyclosporin-A (CsA) following topical application of nonionic liposomal formulations composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10) into and through hairless mouse skin mounted on Franz diffusion cells could be controlled by varying the ratios of GDL to POE-10 (CH being held constant at 15 wt%). However, the pathways of transport as well as the dominant factors that control drug delivery from these formulations are not well understood. In this report, we describe results from studies similar in design to that reported earlier but using the melted form of the lipid components as a vehicle for transport of CsA into and through hairless mouse skin. The results suggest that the transport of CsA from liposomal formulations into and through the skin occurs as a result of dehydration of the liposomes followed by melting of the lipid components on the skin. Microautoradiographic studies suggest that CsA is predominantly transported via the pilosebaceous pathway.
Background: Andrographolide has a potent antiviral effect in the treatment of coronavirus disease... more Background: Andrographolide has a potent antiviral effect in the treatment of coronavirus disease (COVID-19). However, there are no in vivo studies of andrographolide as an anti-COVID-19 treatment. Objective: The study aims to develop a physiologically based pharmacokinetic (PBPK) animal model and scale it up to a human model to predict andrographolide concentrations in the lungs. Method: ADAPT5 (version 5.0.58) was used to establish the PBPK model based on 24 enrolled pharmacokinetic studies. Results: The perfusion-limited PBPK model was developed in mice and extrapolated to rats, dogs, and humans. The metabolism of andrographolide in humans was described by the Michaelis-Menten equation. The saturation of the metabolism occurred at a high dose (12 g), which could not be used therapeutically. The optimized oral bioavailability in humans was 6.3%. Due to the limit of solubility, the dose-dependent absorption between 20-1000 mg was predicted by GastroPlus®. Using the extrapolated human PBPK model together with the predicted dose-dependent fraction of the dose absorbed that enters the enterocytes by GastroPlus®, the oral dosage of 200 mg q8h of andrographolide would provide a trough level of free andrographolide at a steady state over the reported IC50 value against SARS-CoV-2 in the lungs for the majority of healthy humans. Based on the reported CC50 value, toxicity might not occur at the therapeutic dosage. Conclusion: The PBPK model of andrographolide in animals and humans was successfully constructed. Once additional data is available, the model would be needed to recalibrate to gain an understanding of a dose-response relationship and optimization of dosage regimens of andrographolide.
The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several s... more The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several skin disorders, including photo-aging. Unfortunately, ATRA is susceptible to light, heat, and oxidizing agents. Thus, this study aimed to investigate the ability of polymeric micelles prepared from polyethylene glycol conjugated phosphatidylethanolamine (PEG-PE) to stabilize ATRA under various storage conditions. ATRA entrapped in polymeric micelles with various PEG and PE structures was prepared. The critical micelle concentrations were 97-243 μM, depending on the structures of the PEG and PE molecules. All of the micelles had particle diameters of 6-20 nm and neutral charges. The highest entrapment efficiency (82.7%) of the tested micelles was exhibited by ATRA in PEG with a molecular weight of 750 Da conjugated to dipalmitoyl phosphatidylethanolamine (PEG 750-DPPE) micelles. The PEG 750-DPPE micelle could significantly retard ATRA oxidation compared to ATRA in 75% methanol/ HBS solution. Up to 87% of ATRA remained in the PEG 750-DPPE micelle solution after storage in ambient air for 28 days. This result suggests that PEG 750-DPPE micelle can improve ATRA stability. Therefore, ATRA in PEG 750-DPPE micelle is an interesting alternative structure for the development of cosmeceutical formulations.
ABSTRACT Abstract Our previous reports using hairless mouse skin model showed that topical delive... more ABSTRACT Abstract Our previous reports using hairless mouse skin model showed that topical delivery of cyclosporin-A (CsA) could be achieved and controlled with nonionic liposomal and nonionic lipid-based formulations composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10) at varying weight ratios (1,2). However, the distribution profiles were obtained using radiolabeled CsA and thus could represent intact drug as well as its metabolites. The present studies aim to investigate if the previously reported profiles actually represented intact CsA. The studies were carried out using a “high-pressure” liquid chromatography (HPLC) method and in vitro skin deposition studies with a metabolic inhibitor (sodium azide) incorporated in the receptor fluid. The results indicated that skin metabolism of CsA and hence its effect on percutaneous absorption of CsA is minimal and that the CsA distribution profiles obtained using radiolabeled CsA represented distribution of intact drug and not its metabolites.
ABSTRACT In an earlier report (1) we described the controlled follicular delivery of hydrophobic ... more ABSTRACT In an earlier report (1) we described the controlled follicular delivery of hydrophobic macromolecules from nonionic lipid-based formulations composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10). However, the influence of lipid composition on topical delivery of marginally hydrophobic and hydrophilic drugs from these nonionic lipid-based systems has not been investigated. In this report we describe the effect of variation of GDL to POE-10 ratio in the nonionic lipid-based formulations on the extent and route of delivery of hydrocortisone and mannitol, a marginally hydrophobic and hydrophilic model drug, respectively, into and through hairless mouse skin mounted on Franz diffusion cells. The results indicate that the extent of hydrocortisone uptake increased with increasing GDL to POE-10 weight ratio whereas mannitol uptake was quite the opposite and decreased with increasing GDL to POE-10 weight ratio. The diametrically opposite trends for the two drug markers suggests strongly that hydrocortisone and mannitol are transported into and across skin from the nonionic lipid-based formulations via two distinctly different routes. Further, the finding from microautoradiographic studies that the delivery of hydrocortisone from nonionic lipid-based lipid melt formulations was predominantly across the transfollicular route compared to its transport across both the trans-epidermal and transfollicular pathways from nonionic lipid-based liposomes, suggests that it is possible to tailor formulations for specific and targeted delivery across a certain route.
BACKGROUND Asian skin undergoing chronological aging, accumulates signs of photoaging mediated by... more BACKGROUND Asian skin undergoing chronological aging, accumulates signs of photoaging mediated by prolonged exposure to ultraviolet (UV) radiation. Although sunscreens are effective in preventing signs of photoaging, polyphenol-rich extracts e.g., grape seed extract (GSE) can provide additional protection through the broad spectrum of biological activities. AIMS To access the effectiveness of a sunscreen formulation containing GSE as an important cosmetic ingredient for the improvement of age-related changes in Asian skin using noninvasive evaluation techniques. METHODS Noninvasive methods were used to assess changes in the biophysical properties corresponding to aging signs including melanin and erythema indices, color parameters of the CIE L*a*b* system, elasticity, and hydration of the forearm skin before and after applying the sunscreen with GSE. In addition, to confirm the effectiveness of the tested product, we compared it with benchmark sunscreen, and a cream base containing either GSE or UV filters. RESULTS Twice-daily application of sunscreen containing 3% GSE significantly reduced the level of melanin and erythema and improved overall skin tone. The hydration was drastically increased after 3 hours of wearing formulation and was maintained relatively high for 5 hours. Skin elasticity parameters, including Young's modulus, retraction time, and viscoelasticity improved in participants of all age categories (35-59 years). Moreover, sunscreen with GSE, as acclaimed by participants, improved overall skin appearance. CONCLUSIONS The balancing potential of GSE on the skin, combined with the photoprotective properties of UV filters demonstrated an added value as an anti-aging agent and proved efficacy for both photoaged and chronologically aged Asian skin.
The Journal of clinical and aesthetic dermatology, Jun 1, 2021
This study was a double-blinded, randomized, controlled, split-face trial. Neither the investigat... more This study was a double-blinded, randomized, controlled, split-face trial. Neither the investigator nor the participants knew which drugs were administered. A
Supplemental material, Supplementary Material 1, for Enhancement of Lipolysis in 3T3-L1 Adipocyte... more Supplemental material, Supplementary Material 1, for Enhancement of Lipolysis in 3T3-L1 Adipocytes by Nitroarene Capsaicinoid Analogs by Thanet Laolob, Nuntavan Bunyapraphatsara, Neti Waranuch, Sutatip Pongcharoen, Wikorn Punyain, Sirirat Chancharunee, Krisada Sakchaisri, Jaturong Pratuangdejkul, Sumet Chongruchiroj, Filip Kielar and Uthai Wichai in Natural Product Communications
Supplemental material, Supplementary Material 8, for Enhancement of Lipolysis in 3T3-L1 Adipocyte... more Supplemental material, Supplementary Material 8, for Enhancement of Lipolysis in 3T3-L1 Adipocytes by Nitroarene Capsaicinoid Analogs by Thanet Laolob, Nuntavan Bunyapraphatsara, Neti Waranuch, Sutatip Pongcharoen, Wikorn Punyain, Sirirat Chancharunee, Krisada Sakchaisri, Jaturong Pratuangdejkul, Sumet Chongruchiroj, Filip Kielar and Uthai Wichai in Natural Product Communications
Supplemental material, Supplementary Material 10, for Enhancement of Lipolysis in 3T3-L1 Adipocyt... more Supplemental material, Supplementary Material 10, for Enhancement of Lipolysis in 3T3-L1 Adipocytes by Nitroarene Capsaicinoid Analogs by Thanet Laolob, Nuntavan Bunyapraphatsara, Neti Waranuch, Sutatip Pongcharoen, Wikorn Punyain, Sirirat Chancharunee, Krisada Sakchaisri, Jaturong Pratuangdejkul, Sumet Chongruchiroj, Filip Kielar and Uthai Wichai in Natural Product Communications
This study aimed to investigate the biological activities of Tectona grandis L. f. related to hai... more This study aimed to investigate the biological activities of Tectona grandis L. f. related to hair loss treatment, including steroid 5α-reductase (S5AR) inhibition, effect on Human Follicle Dermal Papilla Cells (HFDPCs), anti-testosterone activity, cytotoxicity on macrophage cells and interleukin 1 beta (IL-1β) secretion inhibition. Among the crude extracts, T. grandis leafhexane and ethyl acetate (EtOAc) extracts possessed potent S5AR inhibitions, with IC50 values of 31.39±3.38 µg/mL and 20.92±2.59 µg/mL, respectively. T. grandis leaf-hexane extract showed lower cytotoxicity on HFDPCs than EtOAc extract. Hexane extract at 25 µg/mL had similar anti-testosterone activity with a positive control, finasteride, and exhibited 70% inhibition of IL-1β secretion in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Meanwhile, EtOAc extract had lower anti-testosterone activity at 6.25 µg/mL and exhibited 52% IL-1β secretion inhibition at 1.5 µg/mL. This discovery suggests T. grandis leaf extracts as a new source of active ingredients for the development of hair care products.
Supplementary_File_794158 for Cellulite Reduction by Modified Thai Herbal Compresses; A Randomize... more Supplementary_File_794158 for Cellulite Reduction by Modified Thai Herbal Compresses; A Randomized Double-Blind Trial by Ngamrayu Ngamdokmai, Neti Waranuch, Krongkarn Chootip, Katechan Jampachaisri, C. Norman Scholfield, and Kornkanok Ingkaninan in Journal of Evidence-Based Integrative Medicine
Centella asiatica has many applications in cosmetics, including wrinkle treatments, but its effec... more Centella asiatica has many applications in cosmetics, including wrinkle treatments, but its effectiveness remains to be clarified. This systematic review study aimed to demonstrate the efficacy and safety of C. asiatica for reducing facial wrinkles. PubMed, Excerpta Medica dataBASE (EMBASE), Cochrane Central Register of clinical trials, Allied and Complementary Medicine Database, Cumulative Index to Nursing and Allied Health Literature (CINAHL), Thai Library Integrated System, and Thai university database/journals were searched until May 2019. Five double-blinded randomised controlled trials, including 172 Asian females, were included. Endpoints were wrinkling measured by visual score, image analysis, and participant satisfaction. Two placebo-controlled studies applied gel/creams containing C. asiatica or asiaticoside for 12 w to periorbital skin. Two studies applied tretinoin or Pueraria mirifica contralaterally and by network meta-analysis C. asiatica appeared more effective than ...
Naresuan University Journal: Science and Technology (NUJST), Sep 24, 2018
A reversed-phase HPLC method for the simultaneous determination gallic acid, gallocatechin, catec... more A reversed-phase HPLC method for the simultaneous determination gallic acid, gallocatechin, catechin, epicatechin and epigallocatechin gallate in banana peel extract was developed. The separation was achieved using a reversed-phase (C18) analytical column and an isocratic elution using a mobile phase of acetonitrile-formic acid (15:85 v/v, pH 2.5). The detection wavelength was set at 275 nm. The chromatographic parameters such as peak asymmetry, capacity factor, selectivity factor and resolution factor were determined. Optimization of parameters such as the detection wavelength, the amount of acetonitrile for a mobile phase and the methanol concentration on stability of standard solution was carried out. Under the optimum conditions, the order of elution was gallic acid, gallocatechin, catechin, epicatechin and epigallocatechin gallate, respectively, with the analysis time of 20 min per chromatogram. The validation parameters such as linearity, range, limit of detection, limit of quantitation, selectivity, precision and accuracy, were evaluated. Linear calibration graphs were in range of 0.25-20 mg L-1 for gallic acid and 0.50-30 mg L-1 for gallocatechin, catechin, epicatechin and epigallocatechin gallate, respectively. The proposed HPLC method was simple and rapid, and successfully applied to real samples of banana peel (ripe and green) extracts. Acceptable precisions (%RSD) and recoveries (%Rec) were obtained in the ranges of 0.3-5.9 % and 83±1-128±1 %, respectively, by spiking all samples with a mixed standard solution of five analytes. Banana peel extracts contains many phenolic compounds, especially gallic acid, catechin, epicatechin and epigallocatechin gallate.
ABSTRACT Abstract Previous studies in our laboratories showed that a novel nonionic liposome form... more ABSTRACT Abstract Previous studies in our laboratories showed that a novel nonionic liposome formulation composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10) at a weight ratio composition of 57:15:28 delivered more cyclosporin-A (CsA) into and through the skin than phospholipid-based liposomal formulations and more conventional formulations that were tested. Since only a single GDL:CH:POE-10 composition was tested, we initiated studies to determine if it would be possible to control the rate and extent of drug uptake by varying the ratios of the liposome-forming components of the formulation. This report describes how the GDL to POE-10 ratio (CH being held constant at 15 wt%) influences the rate and extent of uptake of CsA following topical application of nonionic liposomal formulations to hairless mouse skin mounted on Franz diffusion cells. The results indicate that the rate and extent of CsA uptake is highest between GDL/POE-10 ratios of about 1 to 1.5 and decreases steadily at ratios above and below this range. The effect of liposomal composition on CsA deposition is probably the result of a number of complex and interrelated factors including partitioning of CsA from the formulation into the skin and permeation enhancer effects.
Clinical, Cosmetic and Investigational Dermatology, May 1, 2019
Objective: We compared the efficacy of an antiacne hydrogel formulated with a combination of Aloe... more Objective: We compared the efficacy of an antiacne hydrogel formulated with a combination of Aloe barbadensis leaf extract, Garcinia mangostana peel extract, and Camellia sinensis leaf extract (AGC) at a ratio of 50:25:1 with a marketed 1% clindamycin gel (CG) formulation on antiacne and antiblotch activities. Methods: A single-center, parallel-arm, randomized controlled trial was performed from November 2017 to April 2018. Sixty subjects with mild-moderate acne severity according to the the American Academy of Dermatology were enrolled for the study. Outcome end points were total acne lesions (TALs) and acne-severity index (ASI) by counting the inflamed lesions and comedones and skin colors using erythema and melanin values. Results: For TALss, a decrease (P<0.0001) in the number of total inflamed lesions from baseline was evidenced in AGC group, but not in the CG group. Higher reduction in mean ASI in the AGC group was seen than in the CG group. However, there was no statistically significant difference regarding reduction in ASI between the AGC and CG groups. For erythema, a remarked reduction in skin redness from baseline was clearly seen at day 3 (P<0.05) in the AGC group. No significant decrease in erythema values from baseline was seen in the CG group. A significant decrease (P=0.037) in mean melanin value from baseline was seen in the AGC group after 14 days of twice-daily use, but not in the CG group. Both products were well tolerated, with no reports of severe adverse events. Conclusion: An anti-acne hydrogel containing a combination of mangosteen rinds, aloe vera gel, and green tea-leaf extracts was superior to 1% clindamycin gel in antiacne and antiblotch activities when measured by TALs and erythema and melanin values.
World Academy of Science, Engineering and Technology, International Journal of Medical, Health, Biomedical, Bioengineering and Pharmaceutical Engineering, Oct 2, 2016
ABSTRACT Abstract In a previous report (1), we showed that the rate and extent of uptake of cyclo... more ABSTRACT Abstract In a previous report (1), we showed that the rate and extent of uptake of cyclosporin-A (CsA) following topical application of nonionic liposomal formulations composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10) into and through hairless mouse skin mounted on Franz diffusion cells could be controlled by varying the ratios of GDL to POE-10 (CH being held constant at 15 wt%). However, the pathways of transport as well as the dominant factors that control drug delivery from these formulations are not well understood. In this report, we describe results from studies similar in design to that reported earlier but using the melted form of the lipid components as a vehicle for transport of CsA into and through hairless mouse skin. The results suggest that the transport of CsA from liposomal formulations into and through the skin occurs as a result of dehydration of the liposomes followed by melting of the lipid components on the skin. Microautoradiographic studies suggest that CsA is predominantly transported via the pilosebaceous pathway.
ABSTRACT Abstract In a previous report (1), we showed that the rate and extent of uptake of cyclo... more ABSTRACT Abstract In a previous report (1), we showed that the rate and extent of uptake of cyclosporin-A (CsA) following topical application of nonionic liposomal formulations composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10) into and through hairless mouse skin mounted on Franz diffusion cells could be controlled by varying the ratios of GDL to POE-10 (CH being held constant at 15 wt%). However, the pathways of transport as well as the dominant factors that control drug delivery from these formulations are not well understood. In this report, we describe results from studies similar in design to that reported earlier but using the melted form of the lipid components as a vehicle for transport of CsA into and through hairless mouse skin. The results suggest that the transport of CsA from liposomal formulations into and through the skin occurs as a result of dehydration of the liposomes followed by melting of the lipid components on the skin. Microautoradiographic studies suggest that CsA is predominantly transported via the pilosebaceous pathway.
Background: Andrographolide has a potent antiviral effect in the treatment of coronavirus disease... more Background: Andrographolide has a potent antiviral effect in the treatment of coronavirus disease (COVID-19). However, there are no in vivo studies of andrographolide as an anti-COVID-19 treatment. Objective: The study aims to develop a physiologically based pharmacokinetic (PBPK) animal model and scale it up to a human model to predict andrographolide concentrations in the lungs. Method: ADAPT5 (version 5.0.58) was used to establish the PBPK model based on 24 enrolled pharmacokinetic studies. Results: The perfusion-limited PBPK model was developed in mice and extrapolated to rats, dogs, and humans. The metabolism of andrographolide in humans was described by the Michaelis-Menten equation. The saturation of the metabolism occurred at a high dose (12 g), which could not be used therapeutically. The optimized oral bioavailability in humans was 6.3%. Due to the limit of solubility, the dose-dependent absorption between 20-1000 mg was predicted by GastroPlus®. Using the extrapolated human PBPK model together with the predicted dose-dependent fraction of the dose absorbed that enters the enterocytes by GastroPlus®, the oral dosage of 200 mg q8h of andrographolide would provide a trough level of free andrographolide at a steady state over the reported IC50 value against SARS-CoV-2 in the lungs for the majority of healthy humans. Based on the reported CC50 value, toxicity might not occur at the therapeutic dosage. Conclusion: The PBPK model of andrographolide in animals and humans was successfully constructed. Once additional data is available, the model would be needed to recalibrate to gain an understanding of a dose-response relationship and optimization of dosage regimens of andrographolide.
The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several s... more The topical application of all-trans retinoic acid (ATRA) is an effective treatment for several skin disorders, including photo-aging. Unfortunately, ATRA is susceptible to light, heat, and oxidizing agents. Thus, this study aimed to investigate the ability of polymeric micelles prepared from polyethylene glycol conjugated phosphatidylethanolamine (PEG-PE) to stabilize ATRA under various storage conditions. ATRA entrapped in polymeric micelles with various PEG and PE structures was prepared. The critical micelle concentrations were 97-243 μM, depending on the structures of the PEG and PE molecules. All of the micelles had particle diameters of 6-20 nm and neutral charges. The highest entrapment efficiency (82.7%) of the tested micelles was exhibited by ATRA in PEG with a molecular weight of 750 Da conjugated to dipalmitoyl phosphatidylethanolamine (PEG 750-DPPE) micelles. The PEG 750-DPPE micelle could significantly retard ATRA oxidation compared to ATRA in 75% methanol/ HBS solution. Up to 87% of ATRA remained in the PEG 750-DPPE micelle solution after storage in ambient air for 28 days. This result suggests that PEG 750-DPPE micelle can improve ATRA stability. Therefore, ATRA in PEG 750-DPPE micelle is an interesting alternative structure for the development of cosmeceutical formulations.
ABSTRACT Abstract Our previous reports using hairless mouse skin model showed that topical delive... more ABSTRACT Abstract Our previous reports using hairless mouse skin model showed that topical delivery of cyclosporin-A (CsA) could be achieved and controlled with nonionic liposomal and nonionic lipid-based formulations composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10) at varying weight ratios (1,2). However, the distribution profiles were obtained using radiolabeled CsA and thus could represent intact drug as well as its metabolites. The present studies aim to investigate if the previously reported profiles actually represented intact CsA. The studies were carried out using a “high-pressure” liquid chromatography (HPLC) method and in vitro skin deposition studies with a metabolic inhibitor (sodium azide) incorporated in the receptor fluid. The results indicated that skin metabolism of CsA and hence its effect on percutaneous absorption of CsA is minimal and that the CsA distribution profiles obtained using radiolabeled CsA represented distribution of intact drug and not its metabolites.
ABSTRACT In an earlier report (1) we described the controlled follicular delivery of hydrophobic ... more ABSTRACT In an earlier report (1) we described the controlled follicular delivery of hydrophobic macromolecules from nonionic lipid-based formulations composed of glyceryl dilaurate (GDL), cholesterol (CH), and polyoxyethylene-10-stearyl ether (POE-10). However, the influence of lipid composition on topical delivery of marginally hydrophobic and hydrophilic drugs from these nonionic lipid-based systems has not been investigated. In this report we describe the effect of variation of GDL to POE-10 ratio in the nonionic lipid-based formulations on the extent and route of delivery of hydrocortisone and mannitol, a marginally hydrophobic and hydrophilic model drug, respectively, into and through hairless mouse skin mounted on Franz diffusion cells. The results indicate that the extent of hydrocortisone uptake increased with increasing GDL to POE-10 weight ratio whereas mannitol uptake was quite the opposite and decreased with increasing GDL to POE-10 weight ratio. The diametrically opposite trends for the two drug markers suggests strongly that hydrocortisone and mannitol are transported into and across skin from the nonionic lipid-based formulations via two distinctly different routes. Further, the finding from microautoradiographic studies that the delivery of hydrocortisone from nonionic lipid-based lipid melt formulations was predominantly across the transfollicular route compared to its transport across both the trans-epidermal and transfollicular pathways from nonionic lipid-based liposomes, suggests that it is possible to tailor formulations for specific and targeted delivery across a certain route.
BACKGROUND Asian skin undergoing chronological aging, accumulates signs of photoaging mediated by... more BACKGROUND Asian skin undergoing chronological aging, accumulates signs of photoaging mediated by prolonged exposure to ultraviolet (UV) radiation. Although sunscreens are effective in preventing signs of photoaging, polyphenol-rich extracts e.g., grape seed extract (GSE) can provide additional protection through the broad spectrum of biological activities. AIMS To access the effectiveness of a sunscreen formulation containing GSE as an important cosmetic ingredient for the improvement of age-related changes in Asian skin using noninvasive evaluation techniques. METHODS Noninvasive methods were used to assess changes in the biophysical properties corresponding to aging signs including melanin and erythema indices, color parameters of the CIE L*a*b* system, elasticity, and hydration of the forearm skin before and after applying the sunscreen with GSE. In addition, to confirm the effectiveness of the tested product, we compared it with benchmark sunscreen, and a cream base containing either GSE or UV filters. RESULTS Twice-daily application of sunscreen containing 3% GSE significantly reduced the level of melanin and erythema and improved overall skin tone. The hydration was drastically increased after 3 hours of wearing formulation and was maintained relatively high for 5 hours. Skin elasticity parameters, including Young's modulus, retraction time, and viscoelasticity improved in participants of all age categories (35-59 years). Moreover, sunscreen with GSE, as acclaimed by participants, improved overall skin appearance. CONCLUSIONS The balancing potential of GSE on the skin, combined with the photoprotective properties of UV filters demonstrated an added value as an anti-aging agent and proved efficacy for both photoaged and chronologically aged Asian skin.
The Journal of clinical and aesthetic dermatology, Jun 1, 2021
This study was a double-blinded, randomized, controlled, split-face trial. Neither the investigat... more This study was a double-blinded, randomized, controlled, split-face trial. Neither the investigator nor the participants knew which drugs were administered. A
Supplemental material, Supplementary Material 1, for Enhancement of Lipolysis in 3T3-L1 Adipocyte... more Supplemental material, Supplementary Material 1, for Enhancement of Lipolysis in 3T3-L1 Adipocytes by Nitroarene Capsaicinoid Analogs by Thanet Laolob, Nuntavan Bunyapraphatsara, Neti Waranuch, Sutatip Pongcharoen, Wikorn Punyain, Sirirat Chancharunee, Krisada Sakchaisri, Jaturong Pratuangdejkul, Sumet Chongruchiroj, Filip Kielar and Uthai Wichai in Natural Product Communications
Supplemental material, Supplementary Material 8, for Enhancement of Lipolysis in 3T3-L1 Adipocyte... more Supplemental material, Supplementary Material 8, for Enhancement of Lipolysis in 3T3-L1 Adipocytes by Nitroarene Capsaicinoid Analogs by Thanet Laolob, Nuntavan Bunyapraphatsara, Neti Waranuch, Sutatip Pongcharoen, Wikorn Punyain, Sirirat Chancharunee, Krisada Sakchaisri, Jaturong Pratuangdejkul, Sumet Chongruchiroj, Filip Kielar and Uthai Wichai in Natural Product Communications
Supplemental material, Supplementary Material 10, for Enhancement of Lipolysis in 3T3-L1 Adipocyt... more Supplemental material, Supplementary Material 10, for Enhancement of Lipolysis in 3T3-L1 Adipocytes by Nitroarene Capsaicinoid Analogs by Thanet Laolob, Nuntavan Bunyapraphatsara, Neti Waranuch, Sutatip Pongcharoen, Wikorn Punyain, Sirirat Chancharunee, Krisada Sakchaisri, Jaturong Pratuangdejkul, Sumet Chongruchiroj, Filip Kielar and Uthai Wichai in Natural Product Communications
This study aimed to investigate the biological activities of Tectona grandis L. f. related to hai... more This study aimed to investigate the biological activities of Tectona grandis L. f. related to hair loss treatment, including steroid 5α-reductase (S5AR) inhibition, effect on Human Follicle Dermal Papilla Cells (HFDPCs), anti-testosterone activity, cytotoxicity on macrophage cells and interleukin 1 beta (IL-1β) secretion inhibition. Among the crude extracts, T. grandis leafhexane and ethyl acetate (EtOAc) extracts possessed potent S5AR inhibitions, with IC50 values of 31.39±3.38 µg/mL and 20.92±2.59 µg/mL, respectively. T. grandis leaf-hexane extract showed lower cytotoxicity on HFDPCs than EtOAc extract. Hexane extract at 25 µg/mL had similar anti-testosterone activity with a positive control, finasteride, and exhibited 70% inhibition of IL-1β secretion in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Meanwhile, EtOAc extract had lower anti-testosterone activity at 6.25 µg/mL and exhibited 52% IL-1β secretion inhibition at 1.5 µg/mL. This discovery suggests T. grandis leaf extracts as a new source of active ingredients for the development of hair care products.
Supplementary_File_794158 for Cellulite Reduction by Modified Thai Herbal Compresses; A Randomize... more Supplementary_File_794158 for Cellulite Reduction by Modified Thai Herbal Compresses; A Randomized Double-Blind Trial by Ngamrayu Ngamdokmai, Neti Waranuch, Krongkarn Chootip, Katechan Jampachaisri, C. Norman Scholfield, and Kornkanok Ingkaninan in Journal of Evidence-Based Integrative Medicine
Centella asiatica has many applications in cosmetics, including wrinkle treatments, but its effec... more Centella asiatica has many applications in cosmetics, including wrinkle treatments, but its effectiveness remains to be clarified. This systematic review study aimed to demonstrate the efficacy and safety of C. asiatica for reducing facial wrinkles. PubMed, Excerpta Medica dataBASE (EMBASE), Cochrane Central Register of clinical trials, Allied and Complementary Medicine Database, Cumulative Index to Nursing and Allied Health Literature (CINAHL), Thai Library Integrated System, and Thai university database/journals were searched until May 2019. Five double-blinded randomised controlled trials, including 172 Asian females, were included. Endpoints were wrinkling measured by visual score, image analysis, and participant satisfaction. Two placebo-controlled studies applied gel/creams containing C. asiatica or asiaticoside for 12 w to periorbital skin. Two studies applied tretinoin or Pueraria mirifica contralaterally and by network meta-analysis C. asiatica appeared more effective than ...
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