Jirapornchai Suksaeree

Deproteinized natural rubber film forming polymeric solutions for nicotine transdermal delivery

Film forming polymeric solutions were prepared from DNRL blended with MC, PVA, or SAG, together with dibutylphthalate or glycerine used as plasticizers. These formulations were easily prepared by simple mixing. In a preliminary step, in situ films were prepared by solvent evaporation in a Petri-dish. Their mechanical and physicochemical properties were determined. The in vitro release and skin permeation of nicotine dissolved in these blended polymers were investigated by a modified Franz diffusion cell. The formulations had a white milky appearance, and were homogeneous and smooth in texture. Their pH was suitable for usage in skin contact. The mechanical property of in situ films depended on the ingredients but all compatible films were in an amorphous phase. The DNRL/PVA was shown to be the most suitable mixture to form completed films. The in vitro release and skin permeation studies demonstrated a biphasic release that provided an initial rapid release followed by a constant release rate that fitted the Higuchi’s model. Nicotine loaded DNRL/PVA series were selected for the stability test for 3 months. These formulations needed to be kept at 4°C in tight fitting containers. In conclusion, film forming polymeric solutions could be developed for transdermal nicotine delivery systems.

Quantitative analysis and formulation development of a traditional Thai antihypertensive herbal recipe

The health benefits of herbs and herbal products are gaining more attention in southeast Asia. The World Health Organization (WHO) has been supporting countries to promote application of traditional medicines so that this valuable resource is utilized safely and effectively. In Thailand, many traditional herbal recipes have been established since ancient times. Since then, they have been carefully modified, based on the wisdom of traditional Thai medicine practitioners. For this study, a traditional Thai antihypertensive herbal recipe (TTAH) was selected and studied in detail. According to WHO guidelines, both analysis of a sizeable chemical constituent, and formulation data of a product, are a requirement to support a clinical trial for an herbal recipe. Therefore, high-performance liquid chromatography–mass spectrometry (LC–MS) was used to investigate the chemical fingerprints, chemical constituents, and putative active ingredients of the TTAH. Eight chemical fingerprints were established. Metabolic profiling of 10 possible compounds was also identified and all were shown to be active pharmaceutical compounds. An attempt was also made to prepare a suitable formulation of the TTAH, to standardize the amount of active ingredients per dose, and to improve patient compliance. All evaluated parameters guided us to prepare the TTAH as a capsule. This informative data can be included in part of the chemistry–manufacturing–control guidance prior to phase 1/2 clinical trials.

Formulation, physicochemical characterization, and in vitro study of chitosan/HPMC blends-based herbal blended patches.

The current work prepared chitosan/hydroxypropyl methylcellulose (HPMC) blends and studied the possibility of chitosan/HPMC blended patches for Zingiber cassumunar Roxb. The blended patches without/with crude Z. cassumunar oil were prepared by homogeneously mixing the 3.5% w/v of chitosan solution and 20% w/v of HPMC solution, and glycerine was used as plasticizer. Then, they were poured into Petri dish and produced the blended patches in hot air oven at 70u2009±u20092°C. The blended patches were tested and evaluated by the physicochemical properties: moisture uptake, swelling ratio, erosion, porosity, Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction, and photographed the surface and cross-section morphology under SEM technique. Herbal blended patches were studied by the in vitro release and skin permeation of active compound D. The blended patches could absorb the moisture and became hydrated patches that occurred during the swelling of blended patches. They were eroded and increased by the number of porous channels to pass through out for active compound D. In addition, the blended patches indicated the compatibility of the blended ingredients and homogeneous smooth and compact. The blended patches made from chitosan/HPMC blends provide a controlled release and skin permeation behavior of compound D. Thus, the blended patches could be suitably used for herbal medicine application.

Transdermal nicotine mixed natural rubber-hydroxypropylmethylcellulose film forming systems for smoking cessation: in vitro evaluations

Abstract Novel film forming polymeric dispersions for transdermal nicotine delivery were prepared from deproteinized natural rubber latex (DNRL) blended with hydroxypropylmethylcellulose (HPMC) and dibutyl phthalate (DBP) or glycerin (GLY) as plasticizer. The preliminary molecular compatibility of ingredients was observed by Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry characterizations. All film forming polymeric dispersions were elegant in appearance and smooth in texture without agglomeration. Their pH was 7–8. In addition, their viscosity and spreadability showed good characteristics depended on HPMC and plasticizers blended. The transparent in situ dry films with good strength and elasticity were also confirmed by peeling-off. The nicotine release from them revealed an initial fast release that was similar to the release from a concentrated nicotine solution, and followed by slow release pattern from the in situ films. GLY blended formulation produced a higher amount of nicotine permeation through the in vitro pig skin than DBP blends. Ethanol mixing also enhanced nicotine permeation, but it affected the integrity of in situ films. The nicotine release and skin permeation kinetics were by a diffusion mechanism that was confirmed by the Higuchis model. These formulations were safe without producing any severe skin irritation. However, for the stability they needed to be stored at 4u2009°C in tightly sealed containers.

Quantitation of curcuminoid contents, dissolution profile, and volatile oil content of turmeric capsules produced at some secondary government hospitals

The aim of this work was to validate the simple and rapid isocratic reversed phase-high performance liquid chromatography using a C-18 column for the determination of curcuminoid contents, dissolution profile, and volatile oil content of turmeric capsules produced at three secondary government hospitals. The validated reversed phase-high performance liquid chromatography method for three curcuminoids (bisdemethoxycurcumin, demethoxycurcumin, and curcumin) had a good linearity (R2xa0>xa00.9990), accuracy (% recovery was 99.96-101.14%, 97.42-102.23%, and 98.01-99.12% for bisdemethoxycurcumin, demethoxycurcumin, and curcumin, respectively), precision (% relative standard deviationxa0<xa02% and < 5% for intraday and interday precision, respectively), including limit of detection, limit of quantitation, and system suitability. We found that turmeric capsules had a higher content of curcumin than bisdemethoxycurcumin and demethoxycurcumin. The total curcuminoid contents of all lots ranged from 12.02%w/w to 14.36%w/w. Dissolution profiles of curcuminoids were fitted with Higuchi model. Moreover, volatile oil content, determined using the hydrodistillation method, ranged from 7.00%v/w to 8.00%v/w. In conclusion, all nine lots of turmeric capsules from three secondary government hospitals met the standard criteria of the Thai Herbal Pharmacopoeia in the topic of curcuminoid contents, dissolution, and volatile oil content.

Improved Deproteinization Process for Protein-Free Natural Rubber Latex

Hev b1-14 type proteins in natural rubber latex (NRL) have been identified as allergens in immunogenic responses. Several methods have been developed to reduce these proteins from NRL such as enzyme treatment, centrifugation, creaming, simple or ultrasonic leaching, and chlorination. In this work, the improvement of deproteinization of NRL was developed using the combination of enzyme treatment and leaching processes. The fresh NRL was incubated with 0.2 phr proteolytic alcalase enzyme, and preserved with 2%v/v paraben concentrate in the presence of a 2%v/v sodium lauryl ether sulfate (SLES) as a surfactant at 37°C for 24 hours, and then centrifuged. The upper rubber mass was then leached for three times with either distilled water, a 1%v/v SLES solution, or a mixture of 1%v/v SLES and 2.5%v/v ethanol, and then finally re-dispersed in distilled water. It was found that the increasing process of leaching with either 1%v/v SLES or a mixture of 1%v/v SLES and 2.5%v/v ethanol had the higher efficacy to reduce the remained protein in deproteinized NRL (DNRL). The best deproteinized process was the enzyme treatment and followed by the three times leaching process with a mixture of 1%v/v SLES and 2.5%v/v ethanol, that could completely reduce the proteins in DNRL to 0%. This DNRL had the pH value, viscosity, dry rubber content, and total solid content of 7.41, 13.82 cps, 42.57%, and 44.63%, respectively. Its particle size was 626.23 nm with low polydispersity index of 0.16. The negative charge of SLES could increase the higher negative charge of DNRL to-63.20 mV that exhibited very good physical stability during storage. In conclusions, the combination of enzyme treatment and leaching process with both SLES and ethanol was successful to produce the protein-free DNRL. This DNRL could be further used for several applications including medical skin products.

Properties of Deproteinized Natural Rubber Latex/Gelatinized Starch Blended Films

This research aimed to study the compatibility and properties of deproteinized natural rubber latex (DNRL)/gelatinized starch blended films for use as transdermal patches. Various starches were previously gelatinized by heat treatment. Then, the DNRL/gelatinized starch blended films were prepared by simple mixing of DNRL with gelatinized starch and then drying at 50°C. The various parameters such as types (potato, sago, bean, corn, tapioca, rice and glutinous starches), amounts (5, 10, 15 and 20 part per hundred of rubber (phr)) and concentrations of gelatinized starch pastes (5, 10, 20 and 50%) were evaluated. It was found that all starch types could be blended as a homogeneous mixture with DNRL only in 5 phr. Bean starch also provided the good mixture in 10 and 15 phr. Rice and corn starches in the concentrations up to 20 phr could also be blended. Higher concentration of gelatinized starch pastes obtained the higher viscous liquids that were difficult to blend as a homogeneous mixture with DNRL, and provided inhomogeneous blended films. The dried films of all homogeneous DNRL/gelatinized starch mixtures were slightly yellowish transparent with good physical appearances. The tensile strength, swelling and erosion of these blended films increased when increasing amounts of gelatinized starch, but their elasticities were not different comparing to that of DNRL film itself. However, their strengths should be further improved by adding some plasticizers. Some drugs would be further loaded in these homogeneous film formulations for transdermal delivery.

Formulation development of matrix type transdermal patches containing mefenamic acid: physicochemical characterization and in vitro release evaluation

This research prepared the matrix type transdermal patches for mefenamic acid using ethylcellulose and Eudragit®RL as matrix layer and diethyl phthalates as plasticizer. They were prepared by dissolving all ingredients in the solvent and homogeneously mixing with the mefenamic acid powder by mechanical stirrer. Then, they were sonicated and poured into a Petri dish, and subsequently dried in hot air oven at 50xa0±xa02xa0°C. The mefenamic acid-loaded transdermal patches were evaluated and characterized by differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, and in vitro release. We found that crystallization of mefenamic acid affected the patches. However, when we increased the Eudragit®RL ratio as matrix layer, we found lower crystals characteristic of mefenamic acid in matrix patches. This was due to the fact that mefenamic acid could be dissolved in Eudragit®RL polymer more than ethylcellulose. The mefenamic acid powder showed the melting temperature at 233.50xa0°C; however, all matrix patches exhibited the melting point of mefenamic acid. The release profile showed a decrease of mefenamic acid release with increased Eudragit®RL ratio as a matrix layer. Thus, when increased the Eudragit®RL ratio, these matrix patches could reduce the crystalline effect of mefenamic acid, but it showed low release behavior of mefenamic acid from patches and was difficult to build the complete patches. The release behavior of all mefenamic acid patches followed the Higuchi’s model. The mefenamic acid patches could be easily prepared by simple method; however, in the future, these matrix patches will be developed to improve the crystallization effect of mefenamic acid.Graphical abstract

Deproteinized natural rubber latex/gelatinized starch blended films as drug delivery carrier

Deproteinized natural rubber (DNR) latex was blended to each of gelatinized potato, rice, and glutinous starch (GPS, GRS, and GGS, respectively) dispersions to construct a thin film with glycerin added as plasticizer. The appropriate blended films were selected to load lidocaine and used as drug delivery. It was found that dispersions of each gelatinized starch type provided different viscosities due to their amylose/amylopectin ratios. GRS dispersion could be blended with DNR latex up to 20 part per hundred of rubber (phr) because of its lowest viscosity. All gelatinized starch dispersions could be mixed with DNR latex to provide good film at the concentration of 5xa0phr. The percentage of moisture uptake and swelling ratio of these films increased causing the blending of gelatinized starch in DNR. The higher amounts of gelatinized starch increased the swelling ratio and volumetric swelling of blended film. The ultimate tensile strengths of these blended films were not different comparing to DNR film itself, but they had a tendency to raise up when the amounts of gelatinized starch increased. At 5xa0phr of gelatinized starch, GPS provided the highest percentage of elongation at break of blended film while GGS and GRS gave the lower values, respectively. Lidocaine could be mixed in DNR and 5xa0phr GRS blended films by simple mixing during film preparation process. The compatibility of these blended films was confirmed by their morphology, fourier transform infrared spectroscopy and differential scanning calorimeter. Amorphous pattern of drug in these films was detected by X-ray diffraction. Lidocaine release profile from this film showed the slow release for up to 90% in 12xa0h.Graphical abstract

Formulation of Polyherbal Patches Based on Polyvinyl Alcohol and Hydroxypropylmethyl Cellulose: Characterization and In Vitro Evaluation

The purpose of this research was to prepare and characterize polyherbal patches made from polyvinyl alcohol (PVA) and hydroxypropylmethyl cellulose (HPMC) with glycerine as a plasticizer. Polyherbal extracts were Luk-Pra-Kob recipes extracted with 95% ethanol. They were prepared by mixing the polymer solutions and glycerine in a beaker; subsequently, the polyherbal extracts were homogeneously mixed. Then, they were transferred into a Petri dish and dried in a hot-air oven at 70u2009±u20092°C for 5xa0h. The dry polyherbal patches were evaluated for physicochemical properties by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, and a scanning electron microscope. They were studied for in vitro release and skin permeation of the marker active compound (E)-4-(3′,4′-dimethoxyphenyl)but-3-en-l-ol (compound D) using a modified Franz-type diffusion cell. The polyherbal patches made from PVA as a matrix layer were homogeneous, smooth, and compact relative to HPMC-containing polyherbal patches. The selected polyherbal patches made from PVA produced a release profile with an initial burst effect in which compound D release was 74.21u2009±u20096.13% within 8xa0h, but compound D could permeate the pig skin only 37.28u2009±u20095.52% and was highly accumulated in newborn pig skin at 35.90u2009±u20096.72%. The in vitro release and skin permeation kinetics of compound D were fitted to the Higuchi model. The polyherbal patches made from PVA could be suitably used for herbal medicine application.