A highly stable oil-in-water nanoemulsion for topical applications, containing mangostins extract... more A highly stable oil-in-water nanoemulsion for topical applications, containing mangostins extracted from the pericarp of mangosteen (Garcinia mangostana L.), is a promising strategy to protect mangostins as well as to improve penetration of these important antioxidants through the skins. Nanoemulsions consisted of virgin coconut oil as the oil phase, Tween-80 and Span-80 as surfactants, and xanthan gum as the thickening agent, were prepared using the high-energy and low-energy emulsification methods. The nanoemulsions that were stable up to 28 days had oil droplet diameter of 220 nm to 353 nm and zeta potential of-46.9 mV to-63.7 mV. The accelerated stability test showed that the most stable nanoemulsions were those prepared using the low-energy emulsification method with an estimated shelf life of eleven months, composed of 11% oil phase, 17% surfactant, and 72% aqueous phase. The in vitro percutaneous penetration test for the nanoemulsion with added xanthan gum provided high cumulative skin penetration of mangostins of up to 114 μg/cm 2. The results of this study indicate that virgin coconut oil-based nanoemulsions containing mangostins, prepared using the low-energy emulsification method, stabilized by xanthan gum and mixed at 40˚C can prospectively be used for topical applications.
ASEAN Journal of Chemical Engineering, Sep 14, 2019
Deep eutectic solvents (DESs) consisting of betaine as the hydrogen donor acceptor and a propaned... more Deep eutectic solvents (DESs) consisting of betaine as the hydrogen donor acceptor and a propanediol or a butanediol as the hydrogen bonding donor were used to extract vitexin from the leaves of Anredera cordifolia (Ten.) Steenis, known in Indonesia as binahong used traditionally to treat wounds. The vitexin extraction yields depend strongly on the molecular structure of the hydrogen bonding donor used and the betaine to alcohol molar ratio. The highest extraction yield of 0.024%, w/w vitexin in binahong leaves, was obtained at room temperature using the mixture of betaine and 1,3-propanediol in 1:4 mole ratio. For each set of DESs having a common HBD, the highest extraction yield was consistently obtained using the DES having betaine to alcohol molar ratio of 1:4. A higher extraction yield of 0.042% was obtained as the extraction temperature was increased to 40 C. This study shows that DESs made of betaine and polyalcohol are prospective green solvents for extraction of bioactives such as vitexin from plants.
International Journal of Technology: IJ Tech, Dec 9, 2019
The non-volatile phenolic compounds of red ginger oleoresin are known to have high antioxidant pr... more The non-volatile phenolic compounds of red ginger oleoresin are known to have high antioxidant properties to counteract a number of free radicals. Ginger oleoresin is easily degraded when exposed to air, light, water, high temperature, and low-pH conditions in the gastric area. The objective of this research was to evaluate chitosan-alginate matrices as biodegradable media for the targeted release of red ginger oleoresin in the gastrointestinal tract. The chitosan-alginate matrices were prepared using the ionotropic gelation method with varying weight ratios of chitosan to alginate. The encapsulation efficiencies, loading capacities, and cumulative release profiles were determined based on the total phenolic content of the samples. The in-vitro release assays of red ginger oleoresin in simulated gastrointestinal fluids showed that the chitosanalginate matrices with a weight ratio of chitosan to alginate of 2:1 had a low initial cumulative release (4.3%) in simulated gastric fluid and a moderate final release in simulated colonic fluid (40.7%). The results indicated that chitosan-alginate matrices could be formulated for targeted release of red ginger oleoresin in the gastrointestinal tract and could be used as carriers to deliver bioactive compounds to the colon via oral administration.
Freeze drying or lyophilisation method was selected for preparing chitosan-alginate matrices load... more Freeze drying or lyophilisation method was selected for preparing chitosan-alginate matrices loaded with the extract of mangosteen pericarp for oral administration. The objective of this research was to obtain chitosan-alginate matrices for colon targeted drug delivery system that had a high content of mangostins by using a freeze drying method. Various compositions of matrices consisting of chitosan, alginate and mangostins have been used to study the effect of alginate and mangostin content on the release property of freeze dried matrices. Sharp X-ray diffraction peaks of the crystalline phase in pure chitosan and pure alginate, vanished in the chitosan-alginate matrices. The infrared spectroscopy spectra of matrices showed that mangostins were entrapped in the matrices. Release of mangostin from the chitosan-alginate freeze dried matrices was affected by the proportions of alginate and mangostins in the formulations. The in-vitro release assays in simulated gastrointestinal fluids showed the mangostin was burst released from the chitosan-alginate matrices prepared by freeze drying method. The chitosan extract-alginate matrix with mass ratios of 1:0.1:0.5 showed low release of mangostin in simulated gastric fluid, but high release in simulated intestinal and simulated colonic fluids. The freeze drying method facilitates high bioactive loading, and with a proper proportion of chitosan and alginate, it should be possible to obtain matrices that can be used for colon targeted oral drug delivery.
The aim of the study is to investigate the relationship between the phytochemical content of the ... more The aim of the study is to investigate the relationship between the phytochemical content of the fruit rind of Garcinia mangostana Linn with antioxidant activity and cytotoxicity of different fractions (ethyl acetate, n-butanol, water) of the xanthones extract. The ethyl acetate fraction showed the highest total xanthones as quercetin equivalent and α-mangostin equivalent, total xanthones as a-mangostin, and, total polyphenol content. High antioxidant activity and cytotoxicity were also shown from the ethyl acetate fraction with 55.8 μg/ml and 0.0029 μg/ml for IC50 and LC50 values, respectively. The linear correlations were confirmed between the total phenolic content and antioxidant activity as well as cytotoxicity of the xanthones extracts. The results of bioactivity assays and photochemical analysis of different fractions of xanthones extract showed that the ethyl acetate fraction of xanthones extract can be considered as a promising source of anticancer bioactives to be used in controlled release formulations.
Mangosteen pericarp contains -mangostin, the most abundant xanthone that is useful as an antioxi... more Mangosteen pericarp contains -mangostin, the most abundant xanthone that is useful as an antioxidant. Deep eutectic solvent (DES) was used in this study as a green solvent for extraction of -mangostin. Our previous study shows that a DES, consisting of betaine as the hydrogen bond acceptor and 1,2-propanediol as the hydrogen bond donor, having the highest extraction yields compared to other betain-based DESs. In this study, the operating condition of the solvent extraction process has been optimized using the response surface methodology approach, based on the Box-Behnken design. The highest calculated -mangostin extraction yield obtained was 4.2% (w/w), corresponding to an extraction temperature of 56.5 C, mangosteen powder to DES mass ratio of 0.12, and extraction time of 6.9 hours. The optimum temperature was found to be the combined effect of enhanced leaching of the mangosteen pericarp matrix by the DES and -mangostin degradation at higher temperatures.
The aim of the present research work was to formulate and characterize gastroretentive mucoadhesi... more The aim of the present research work was to formulate and characterize gastroretentive mucoadhesive tablets of lacidipine (LCDP) intended for the treatment of gastroparesis. Polymers such as sodium alginate, HPMC K4M, carbopol 974P, and chitosan were utilized in LCDP formulation to ensure gastric retention up to 8 h. Direct compression method was adopted in preparation of mucoadhesive tablets. Prior to compression, powder blends were evaluated in order to check their flow and compression properties. Fourier transform infrared spectroscopy and differential scanning calorimetry measurements were performed to assess the compatibility of LCDP with polymers. Tablets were characterized with respect to the uniformity of weight, hardness, friability, drug content, swelling index, surface pH and in-vitro drug release. All formulations exhibited acceptable physicochemical properties. Formulation F4 exhibiting in-vitro drug release of 95.510% was selected as the optimized formulation and was further characterized by scanning electron microscopy. In vitro dissolution data was fitted to various kinetic models, and formulation F4 was found to display non-Fickian mechanism of drug release. No major change was observed in drug release and drug content upon storage of optimized formulation under accelerated aging conditions. The obtained results revealed that carbopol 974P and chitosan can be used in combination to formulate gastroretentive mucoadhesive LCDP tablets.
Long-term drug release is needed to treat ocular diseases, especially in the posterior region whe... more Long-term drug release is needed to treat ocular diseases, especially in the posterior region where the retina is located. Dexamethasone, an anti-inflammation drug, was encapsulated in biocompatible and biodegradable polylactic acid/polylactic-co-glycolic acid (PLA, PLGA 90:10, PLGA 50:50) nanoparticles prepared using the solvent evaporation method. The surface of the nanoparticles was modified with didodecyldimethylammonium bromide (DDAB), a cationic surfactant, to increase the residence time in the vitreous, by contacting the nanoparticles with various surfactant solutions (PVA, DDAB-1%, PVA-DDAB-0.5%, PVA-DDAB-1%). Those modified using DDAB-1% solution exhibit the highest positive zeta potential (52.7±9.3 mV) and the smallest particle size (329±44 nm). Dexamethasone released into a buffer release media (45°C, 100 rpm) from nanoparticles with higher lactic acid content (PLA and PLGA 90:10) showed zero- order release profile up to 48 days with 30-70% accumulative release. On the other hand, the DDAB release profiles show that after 6-12 days, the cationic surfactant was detached from the surface of the nanoparticles.
A simple method of encapsulation of bioactive compounds that does not involve washing, heating, a... more A simple method of encapsulation of bioactive compounds that does not involve washing, heating, and degradation of active substance is desired. The encapsulation of red ginger oleoresin in the chitosan-alginate matrix was developed using the freeze drying method to achieve higher matrix yield and loading capacity in the matrix. Bioactive substances that are encapsulated in the chitosan-alginate matrix aim to be released in the colon. Oleoresin red ginger extract was obtained from maceration of dried rhizome powder in ethanol. A mixed solution consisting of chitosan, oleoresin extract, Tween 80 as a surfactant and alginate was lyophilized at -50 C at a vacuum pressure of about 20 atm for 48-72 hours. The X-ray diffraction pattern of the formed matrix shows that the crystalline chitosan and alginate peaks disappear in the chitosan-alginate matrix which shows compatibility. In the Infra Red matrix spectrum the interaction between chitosan and alginate in the matrix is shown by the change of peak height at 1520 and 1385 cm−1. Release assay showed that the matrix with a weight ratio of chitosan: alginate of 1: 0.5 slightly released phenolic compounds from oleoresin in the simulated gastric fluid but highly released in the simulated intestinal and colon fluids.
International Journal of Technology: IJ Tech, Nov 20, 2020
Mangosteen pericarp extract contains a high amount of xanthones, which are secondary plant metabo... more Mangosteen pericarp extract contains a high amount of xanthones, which are secondary plant metabolites that exhibit high antioxidant activities as well as beneficial pharmacological properties, but low bioavailabilities. In this study, xanthones extracted from the pericarp of soursop fruit were encapsulated in chitosan-alginate microparticles by ionic gelation, and the microparticles were subsequently formulated into antioxidant supplement tablets by direct compression. One of the tablet formulations satisfied the requirements for weight and size uniformity as well as friability, but not hardness. Dissolution test results revealed similar release profiles characterized by a burst release that occurs in the first 60 min of immersion in simulated gastrointestinal fluids and a complete release of xanthones in 120 min. The results obtained herein demonstrated the potential of the tested tablet formulations for the delivery of xanthones into the gastrointestinal tract. If a targeted release to a specific area in the gastrointestinal tract is desirable, the composition of the excipients in the present formulation should be modified.
Polylactic acid (PLA) nanoparticles could provide extended release of drugs, reducing the frequen... more Polylactic acid (PLA) nanoparticles could provide extended release of drugs, reducing the frequency of injection and increasing the compliance diabetic retinopathy patients. This requires nanoparticles with a mean diameter of approximately 200 nm to facilitate penetration of small and narrow blood vessels in the retina. Mean diameter of PLA particles prepared using the emulsification-evaporation method was found to depend linearly on the speed of the high speed homogenizer, based on the data taken in the range of 1,000-10,000 rpm. PLA nanoparticles with a mean particle diameter of 190 nm with a spherical morphology could be obtained using a homogenizer speed of 10,000 rpm, allowing the use of PLA nanoparticles for extended release of drugs in the retina.
A highly stable oil-in-water nanoemulsion for topical applications, containing mangostins extract... more A highly stable oil-in-water nanoemulsion for topical applications, containing mangostins extracted from the pericarp of mangosteen (Garcinia mangostana L.), is a promising strategy to protect mangostins as well as to improve penetration of these important antioxidants through the skins. Nanoemulsions consisted of virgin coconut oil as the oil phase, Tween-80 and Span-80 as surfactants, and xanthan gum as the thickening agent, were prepared using the high-energy and low-energy emulsification methods. The nanoemulsions that were stable up to 28 days had oil droplet diameter of 220 nm to 353 nm and zeta potential of-46.9 mV to-63.7 mV. The accelerated stability test showed that the most stable nanoemulsions were those prepared using the low-energy emulsification method with an estimated shelf life of eleven months, composed of 11% oil phase, 17% surfactant, and 72% aqueous phase. The in vitro percutaneous penetration test for the nanoemulsion with added xanthan gum provided high cumulative skin penetration of mangostins of up to 114 μg/cm 2. The results of this study indicate that virgin coconut oil-based nanoemulsions containing mangostins, prepared using the low-energy emulsification method, stabilized by xanthan gum and mixed at 40˚C can prospectively be used for topical applications.
ASEAN Journal of Chemical Engineering, Sep 14, 2019
Deep eutectic solvents (DESs) consisting of betaine as the hydrogen donor acceptor and a propaned... more Deep eutectic solvents (DESs) consisting of betaine as the hydrogen donor acceptor and a propanediol or a butanediol as the hydrogen bonding donor were used to extract vitexin from the leaves of Anredera cordifolia (Ten.) Steenis, known in Indonesia as binahong used traditionally to treat wounds. The vitexin extraction yields depend strongly on the molecular structure of the hydrogen bonding donor used and the betaine to alcohol molar ratio. The highest extraction yield of 0.024%, w/w vitexin in binahong leaves, was obtained at room temperature using the mixture of betaine and 1,3-propanediol in 1:4 mole ratio. For each set of DESs having a common HBD, the highest extraction yield was consistently obtained using the DES having betaine to alcohol molar ratio of 1:4. A higher extraction yield of 0.042% was obtained as the extraction temperature was increased to 40 C. This study shows that DESs made of betaine and polyalcohol are prospective green solvents for extraction of bioactives such as vitexin from plants.
International Journal of Technology: IJ Tech, Dec 9, 2019
The non-volatile phenolic compounds of red ginger oleoresin are known to have high antioxidant pr... more The non-volatile phenolic compounds of red ginger oleoresin are known to have high antioxidant properties to counteract a number of free radicals. Ginger oleoresin is easily degraded when exposed to air, light, water, high temperature, and low-pH conditions in the gastric area. The objective of this research was to evaluate chitosan-alginate matrices as biodegradable media for the targeted release of red ginger oleoresin in the gastrointestinal tract. The chitosan-alginate matrices were prepared using the ionotropic gelation method with varying weight ratios of chitosan to alginate. The encapsulation efficiencies, loading capacities, and cumulative release profiles were determined based on the total phenolic content of the samples. The in-vitro release assays of red ginger oleoresin in simulated gastrointestinal fluids showed that the chitosanalginate matrices with a weight ratio of chitosan to alginate of 2:1 had a low initial cumulative release (4.3%) in simulated gastric fluid and a moderate final release in simulated colonic fluid (40.7%). The results indicated that chitosan-alginate matrices could be formulated for targeted release of red ginger oleoresin in the gastrointestinal tract and could be used as carriers to deliver bioactive compounds to the colon via oral administration.
Freeze drying or lyophilisation method was selected for preparing chitosan-alginate matrices load... more Freeze drying or lyophilisation method was selected for preparing chitosan-alginate matrices loaded with the extract of mangosteen pericarp for oral administration. The objective of this research was to obtain chitosan-alginate matrices for colon targeted drug delivery system that had a high content of mangostins by using a freeze drying method. Various compositions of matrices consisting of chitosan, alginate and mangostins have been used to study the effect of alginate and mangostin content on the release property of freeze dried matrices. Sharp X-ray diffraction peaks of the crystalline phase in pure chitosan and pure alginate, vanished in the chitosan-alginate matrices. The infrared spectroscopy spectra of matrices showed that mangostins were entrapped in the matrices. Release of mangostin from the chitosan-alginate freeze dried matrices was affected by the proportions of alginate and mangostins in the formulations. The in-vitro release assays in simulated gastrointestinal fluids showed the mangostin was burst released from the chitosan-alginate matrices prepared by freeze drying method. The chitosan extract-alginate matrix with mass ratios of 1:0.1:0.5 showed low release of mangostin in simulated gastric fluid, but high release in simulated intestinal and simulated colonic fluids. The freeze drying method facilitates high bioactive loading, and with a proper proportion of chitosan and alginate, it should be possible to obtain matrices that can be used for colon targeted oral drug delivery.
The aim of the study is to investigate the relationship between the phytochemical content of the ... more The aim of the study is to investigate the relationship between the phytochemical content of the fruit rind of Garcinia mangostana Linn with antioxidant activity and cytotoxicity of different fractions (ethyl acetate, n-butanol, water) of the xanthones extract. The ethyl acetate fraction showed the highest total xanthones as quercetin equivalent and α-mangostin equivalent, total xanthones as a-mangostin, and, total polyphenol content. High antioxidant activity and cytotoxicity were also shown from the ethyl acetate fraction with 55.8 μg/ml and 0.0029 μg/ml for IC50 and LC50 values, respectively. The linear correlations were confirmed between the total phenolic content and antioxidant activity as well as cytotoxicity of the xanthones extracts. The results of bioactivity assays and photochemical analysis of different fractions of xanthones extract showed that the ethyl acetate fraction of xanthones extract can be considered as a promising source of anticancer bioactives to be used in controlled release formulations.
Mangosteen pericarp contains -mangostin, the most abundant xanthone that is useful as an antioxi... more Mangosteen pericarp contains -mangostin, the most abundant xanthone that is useful as an antioxidant. Deep eutectic solvent (DES) was used in this study as a green solvent for extraction of -mangostin. Our previous study shows that a DES, consisting of betaine as the hydrogen bond acceptor and 1,2-propanediol as the hydrogen bond donor, having the highest extraction yields compared to other betain-based DESs. In this study, the operating condition of the solvent extraction process has been optimized using the response surface methodology approach, based on the Box-Behnken design. The highest calculated -mangostin extraction yield obtained was 4.2% (w/w), corresponding to an extraction temperature of 56.5 C, mangosteen powder to DES mass ratio of 0.12, and extraction time of 6.9 hours. The optimum temperature was found to be the combined effect of enhanced leaching of the mangosteen pericarp matrix by the DES and -mangostin degradation at higher temperatures.
The aim of the present research work was to formulate and characterize gastroretentive mucoadhesi... more The aim of the present research work was to formulate and characterize gastroretentive mucoadhesive tablets of lacidipine (LCDP) intended for the treatment of gastroparesis. Polymers such as sodium alginate, HPMC K4M, carbopol 974P, and chitosan were utilized in LCDP formulation to ensure gastric retention up to 8 h. Direct compression method was adopted in preparation of mucoadhesive tablets. Prior to compression, powder blends were evaluated in order to check their flow and compression properties. Fourier transform infrared spectroscopy and differential scanning calorimetry measurements were performed to assess the compatibility of LCDP with polymers. Tablets were characterized with respect to the uniformity of weight, hardness, friability, drug content, swelling index, surface pH and in-vitro drug release. All formulations exhibited acceptable physicochemical properties. Formulation F4 exhibiting in-vitro drug release of 95.510% was selected as the optimized formulation and was further characterized by scanning electron microscopy. In vitro dissolution data was fitted to various kinetic models, and formulation F4 was found to display non-Fickian mechanism of drug release. No major change was observed in drug release and drug content upon storage of optimized formulation under accelerated aging conditions. The obtained results revealed that carbopol 974P and chitosan can be used in combination to formulate gastroretentive mucoadhesive LCDP tablets.
Long-term drug release is needed to treat ocular diseases, especially in the posterior region whe... more Long-term drug release is needed to treat ocular diseases, especially in the posterior region where the retina is located. Dexamethasone, an anti-inflammation drug, was encapsulated in biocompatible and biodegradable polylactic acid/polylactic-co-glycolic acid (PLA, PLGA 90:10, PLGA 50:50) nanoparticles prepared using the solvent evaporation method. The surface of the nanoparticles was modified with didodecyldimethylammonium bromide (DDAB), a cationic surfactant, to increase the residence time in the vitreous, by contacting the nanoparticles with various surfactant solutions (PVA, DDAB-1%, PVA-DDAB-0.5%, PVA-DDAB-1%). Those modified using DDAB-1% solution exhibit the highest positive zeta potential (52.7±9.3 mV) and the smallest particle size (329±44 nm). Dexamethasone released into a buffer release media (45°C, 100 rpm) from nanoparticles with higher lactic acid content (PLA and PLGA 90:10) showed zero- order release profile up to 48 days with 30-70% accumulative release. On the other hand, the DDAB release profiles show that after 6-12 days, the cationic surfactant was detached from the surface of the nanoparticles.
A simple method of encapsulation of bioactive compounds that does not involve washing, heating, a... more A simple method of encapsulation of bioactive compounds that does not involve washing, heating, and degradation of active substance is desired. The encapsulation of red ginger oleoresin in the chitosan-alginate matrix was developed using the freeze drying method to achieve higher matrix yield and loading capacity in the matrix. Bioactive substances that are encapsulated in the chitosan-alginate matrix aim to be released in the colon. Oleoresin red ginger extract was obtained from maceration of dried rhizome powder in ethanol. A mixed solution consisting of chitosan, oleoresin extract, Tween 80 as a surfactant and alginate was lyophilized at -50 C at a vacuum pressure of about 20 atm for 48-72 hours. The X-ray diffraction pattern of the formed matrix shows that the crystalline chitosan and alginate peaks disappear in the chitosan-alginate matrix which shows compatibility. In the Infra Red matrix spectrum the interaction between chitosan and alginate in the matrix is shown by the change of peak height at 1520 and 1385 cm−1. Release assay showed that the matrix with a weight ratio of chitosan: alginate of 1: 0.5 slightly released phenolic compounds from oleoresin in the simulated gastric fluid but highly released in the simulated intestinal and colon fluids.
International Journal of Technology: IJ Tech, Nov 20, 2020
Mangosteen pericarp extract contains a high amount of xanthones, which are secondary plant metabo... more Mangosteen pericarp extract contains a high amount of xanthones, which are secondary plant metabolites that exhibit high antioxidant activities as well as beneficial pharmacological properties, but low bioavailabilities. In this study, xanthones extracted from the pericarp of soursop fruit were encapsulated in chitosan-alginate microparticles by ionic gelation, and the microparticles were subsequently formulated into antioxidant supplement tablets by direct compression. One of the tablet formulations satisfied the requirements for weight and size uniformity as well as friability, but not hardness. Dissolution test results revealed similar release profiles characterized by a burst release that occurs in the first 60 min of immersion in simulated gastrointestinal fluids and a complete release of xanthones in 120 min. The results obtained herein demonstrated the potential of the tested tablet formulations for the delivery of xanthones into the gastrointestinal tract. If a targeted release to a specific area in the gastrointestinal tract is desirable, the composition of the excipients in the present formulation should be modified.
Polylactic acid (PLA) nanoparticles could provide extended release of drugs, reducing the frequen... more Polylactic acid (PLA) nanoparticles could provide extended release of drugs, reducing the frequency of injection and increasing the compliance diabetic retinopathy patients. This requires nanoparticles with a mean diameter of approximately 200 nm to facilitate penetration of small and narrow blood vessels in the retina. Mean diameter of PLA particles prepared using the emulsification-evaporation method was found to depend linearly on the speed of the high speed homogenizer, based on the data taken in the range of 1,000-10,000 rpm. PLA nanoparticles with a mean particle diameter of 190 nm with a spherical morphology could be obtained using a homogenizer speed of 10,000 rpm, allowing the use of PLA nanoparticles for extended release of drugs in the retina.
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