Key Engineering Materials Vol. 901

Abstract: Azithromycin (AZM) is a potential drug for periodontitis treatment, but its poor water solubility could be problematic for local delivery to periodontal tissues. Entrapping AZM, which is a hydrophobic drug into niosomes, could effectively deliver drugs to the target site. This study aimed to design and fabricate azithromycin-loaded niosomes (NAZ) with desirable properties for intra-periodontal pocket administration. Span 60 and cholesterol were used to prepare niosomes with modified reverse phase evaporation method. NAZ were characterized and the effects of niosome composition were investigated. In vitro release and cell viability were evaluated. The results of this study indicated that with the specific ratio of Span 60 and cholesterol, the particle sizes of niosomes were in nano-sized (319 nm) with optimal zeta potential (-39.57 mV). Controlled release of AZM was achieved with release kinetic followed zero order model. NAZ exhibited low toxicity as cell viability was comparable to negative control.

Abstract: The objective of this research was to develop Mucuna pruriens jelly formula to be suitable and easily edible for Parkinson’s patients. The recipe of jelly consisted of M. pruriens seed dry extract as an active ingredient, gelatin, glycerin, citric acid, sodium benzoate, steviol, coffee flavor, and purified water. The jelly was analyzed for physical and chemical characteristics by microscopy and UV-Vis spectrophotometry. It was found that pH of the M. pruriens jelly was 4.77. The microscopic characteristics showed that the jelly texture had a consistent distribution of various components (2.53 particles/cm²), with different particles sizes. The observation of the physical macroscopic characteristics found that M. pruriens jelly had dark brown color, smooth surface, and elastic texture, hence suitable for consumption. The analysis of physical stability by observing the changes of appearance with naked eyes for 4 weeks at 30 °C and 4 °C showed that M. pruriens jelly had physical stability at 4 °C better than at 30 °C. The chemical analysis of L-dopa by UV-Vis spectrophotometry revealed that M. pruriens jelly contained a sufficient amount of L-dopa i.e. 542 mg/piece. This research could be developed to be a health product for Parkinson’s patients by taking 2 pieces per day in the morning since the therapeutic dose for Parkinson’s disease is 1000 mg of L-dopa total/day (single dose in the morning).

Abstract: Morus alba stem extract possesses several biological activities. However, skin delivery of the extract is limited by the stratum corneum. In this study, lamellar lyotropic liquid crystal (LLC) was investigated for the potential application in the skin delivery of M. alba stem extract. The four formulations were developed and incorporated with M. alba stem extract at 3% w/w. These formulations were stored at room temperature in light-protected containers for 3 months. The optical pattern under polarized light microscope, viscosity and remaining of the extract were determined. The skin penetration enhancing property of the formulations was investigated using excised porcine ear skin model. The results showed that all formulations remained stable after 3-month storage. The two formulations exhibiting good penetration enhancing properties were F3 consisting of PEG-7 glyceryl cocoate/n-Dodecane/Water/extract (55.29/19.40/22.31/3.00 %w/w) and F4 consisting of mixed Surfactant/n-Dodecane/Water/extract (48.50/4.85/43.65/3.00 %w/w). The mixed surfactant composed of PEG-7 glyceryl cocoate/PEG-40 hydrogenated castor oil/Glyceryl oleate (40/33.24/26.76 %w/w). It can be concluded that the lamellar LLC formulations developed in this study can be used as a carrier for delivering of M. alba stem extract. The components of the formulations which play important roles are the oil and the surfactant.

Abstract: Medium chain triglycerides (MCT) are important substrates of the energy metabolism and anabolic processes in mammals. In this study, MCT-rich oil was encapsulated in the mixing ratios of maltodextrin and protein by spray drying to produce spray-dried MCT-rich oil (SMCT). Spray-dried conditions were an inlet temperature of 200 °C, an outlet temperature of 90 °C, and a flow rate of 0.70 L/h. Box–Behnken experimental design and response surface methodology were applied for modeling the influence of formulation variables on powder recovery of SMCT. The key variables were concentration of maltodextrin (10-30% W/W), total protein (5–15% w/w), and MCT-rich oil (5–15% w/w). The microparticles were characterized in terms of particle morphology, yield, Carr's index, moisture content, flowability, hygroscopicity, and powder diffraction. The highest yield of SMCT was 41.19% obtained under the optimized conditions (maltodextrin concentration of 15% w/w, total protein concentration of 8% w/w, MCT-rich oil concentration of 15%). Experimentally obtained values were consistent with those predicted by the model, indicating the suitability of the employed model and the success of the model in optimizing the formulation.

Abstract: Maclura cochinchinensis (Lour.) Corner., of the Moraceae family, is a medical shrub commonly found in Thailand, and for which a wide variety of pharmacological activities have been reported, including antiviral, anti-inflammatory, antioxidant, and anticancer activities. The main bioactive compounds, oxyresveratrol and morin, are known to be found in M. cochinchinensis heartwood. In this study, we quantitatively analyzed the levels of these two active substances in M. cochinchinensis extracted with various solvents, including in various cosmetic formulations and herbs sourced from various parts of Thailand. High-performance liquid chromatography (HPLC) was performed on a C₁₈ column with an isocratic elution using 1.5% formic acid and acetonitrile at a flow rate of 1 ml/min, and detected at 352 nm. This method was validated for accuracy, precision, linearity, limits of detection, and quantification. The average percent recovery for oxyresveratrol and morin in the extracts was 100.01 ± 0.62% and 99.31 ± 2.56%, and in gel formulation was 99.65 ± 3.54% and 118.41 ± 4.70%, respectively. The relative standard deviation of intra- and inter-day precision was less than 2.0% and 2.8%, respectively. Limits of detection and quantification were 0.06 and 0.2 μg/ml, respectively. The amounts of oxyresveratrol and morin extracted from different solvents, such as acetone, 80% ethanol, 50% ethanol, methanol, and distilled water were in the range of 37.75–68.16 and 54.63–144.83 mg/g, respectively, while five samples of M. cochinchinensis heartwood collected from different regions of traditional drug stores contained in the range of 26.85–60.37 and 110.26–157.44 mg/g, respectively. Additionally, the percentage label amounts of oxyresveratrol and morin were analyzed in gel preparations, and found at 82.88% and 120.99%, respectively. This technique is convenient, simple, and reliable to effectively analyze the content of these active compounds in extracts and cosmetic products.

Abstract: Orodispersible films (ODFs) is orally pharmaceutical dosage form that rapidly disintegrates and instantly releases the drug when placed on the tongue. This study was firstly aimed to investigate physicomechanical properties of ODFs containing diclofenac sodium/β-cyclodextrin (DS/βCD) inclusion complexes prepared by solvent casting method. The influence of plasticizer, βCD and DS on hydroxypropyl metlhycellulose (HPMC) film was studied. Increasing of plasticizer concentration (e.g. PEG400 amd glycerol) resulted in decrement of disintegration time, strength and elasticity of HPMC films. When βCD was incorporated, opaque films were observed. Presence of βCD resulted in degrading of physicomechanical properties, except percentage of elongation representing the film’s elasticity. βCD films containing DS (DS/βCD films) were more brittle and transparent than blank βCD films. Amount of incorporated DS influenced on disintegration time and strength of obtained films. Cross-section scanning electron microscope (SEM) photomicrographs showed spherical particles scattered on DS/βCD films illustrating the occurrence of DS/βCD inclusion complexes during casting process. The DS/βCD inclusion complexes were then confirmed in both solid and solution. Furthermore, DS/βCD ODFs were prepared by incorporation of artificial sweeteners in DS/βCD films. It was found that DS/βCD ODFs containing xylitol were more brittle and their disintegration times were faster then those containing sucralose. Dissolution profiles were investigated then reported that release kinetic of DS/βCD films and ODFs were fitted to Higuchi model. In summary, the βCD-based ODFs containing DS were successfully developed.

Abstract: Triphala is a traditional Thai herbal formulation containing dried fruits of Phyllanthus emblica, Terminalia bellirica, and Terminalia chebula. It has wound healing, antioxidant and anti-inflammatory activities. The objective of this research was to formulate mucoadhesive films containing Triphala extract for aphthous ulcers treatment. The films were formulated using hydroxypropyl methylcellulose, HPMC, (5, 8, 10% w/w) as a film-forming polymer and glycerin (5% w/w) as a plasticizer. Triphala extract (2.5, 5, 10% w/w) was incorporated into the film during the film preparation. The films were then evaluated for the physical appearance, dissolution time, mechanical properties (strength and elasticity) and mucoadhesive capability to the porcine buccal mucosa. The antioxidant activity and anti-inflammatory activity of the films were also evaluated by DPPH assay and the proteins denaturation method, respectively. Physical properties revealed that Triphala-loaded HPMC films were transparent with brown color. All formulations showed 1-2 hr of dissolution times. Triphala films exhibited good mucoadhesive properties. Films prepared from the solution containing HPMC (10% w/w), glycerin (5% w/w), and Triphala extract (10% w/w) were the most appropriate formulation for further development due to suitable strength, elasticity, and mucoadhesive properties. Moreover, the films exhibited antioxidants and anti-inflammatory activity which may help relieve the symptom of aphthous ulcers.

Abstract: Abstract The aim of this study was to fabricate curcumin-loaded polymeric mixed micelle which was a new nanocarrier of therpeutic agent for skin uses. Curcumin was extracted from dried turmeric rhizomes using ethanol and recrystallized. The purity of curcumin was 79±3.6 %w/w. Six curcumin-loaded polymeric micelles (PM1-PM6) were prepared by simple dissolution method using poloxamer 407 (5% and 10%) as a main core structure. PEG-40 hydrogenated castor oil (PEG-40HCO) was incorporated at two percentages (2.5% and 5.0%) to study the effect on the nanoparticle characteristics. The average particle sizes of PM1-PM6 were in the range of 33.3±6.6 nm to 171.3±52.8 nm. The entrapment efficiency and the loading capacity of curcumin were in the range of 47.45%-77.35% and 0.048%w/w-0.078%w/w, respectively. When PEG-40HCO was incorporated in to the polymeric micelles, the particle size decreased and the entrapment efficiency increased. Thus, PM4 and PM5 were selected for further study. Moisturizing antioxidant creams containing 0.005%w/w of curcumin loaded in PM4, PM5 and curcumin simply dissolved in propylene glycol (PG) were formulated. The resulted formulations showed good spreadability and good characteristics. After being subjected to accelerated test, all of the formulations remained with characteristic color, pH and showed no phase separation. The stability data showed that the moisturizing antioxidant creams were stable for the whole 3 months after storage at accelerated temperature (45°C/75%RH). The study demonstrated that polymeric mixed micelle spontaneously encapsulated a poorly water-soluble curcumin and increased the solubility up to 250 folds. The developed moisturizing cream containing 0.005%w/w of curcumin resulted a greenish-yellow color preparation. It had tolerable physicochemical properties based on curcumin content, pH and viscosity under the harsh condition. The cream also had satisfactory antioxidant activity, which can be regarded as an effective and acceptable therapeutic or skincare products for topical uses.

Abstract: Film-forming systems (FFSs) were developed by using Eudragit^® E100 as a film former. Kaempferia parviflora (black ginger) extract was used as an anti-inflammatory agent for aphthous ulcers. The FFS could rapidly form a thin film in only 5 s when it was applied to a wet surface e.g. an aphthous ulcer. When the FFS was applied to a dry surface, the FFS without extract could form a film in 2-4 min. The incorporation of this extract contributed to delaying the film-formation time in the dry state; hence, the film-forming time increased to 6-8 min. The mucoadhesive property of FFSs was verified with the wash-off method. To simulate oromucosal conditions, the FFSs were applied on a cellophane membrane coated with mucin and washed by phosphate buffer of pH 6.8. The formulations without mucoadhesive polymers could not withstand flushing with a medium for more than 8 min without dislodging. Therefore, three different mucoadhesive agents were trialed: PVP K90, HPMC E15 LV, and HPC SL. The highest adhesion results were obtained when HPMC was added at 5%(w/w) as well as, the residence time was 22 min. In vitro release of black ginger extract from FFS showed a gradual release for 2 h. This study indicated that the FFS with HPMC E15 LV was an appropriate alternative formulation as a local delivery system for an aphthous ulcer.

Abstract: Dry socket disease, a pocket wound caused by the tooth extraction that resulted in severe acute pain which requires a topical analgesic with rapidly pain reduction and suppress the pain until the wound healed. This study aimed to investigate factors affecting gelation temperature and gelation time of lidocaine hydrochloride (LH)-loaded polyelectrolyte complex (PEC) thermosensitivity gel for treating dry socket wound. The first factor was investigated the effects of the ratio of three different types of polymers as chitosan (CS), hyaluronic acid (HA) and poloxamer407 (P407) on the phase transition caused by temperature. The second factor was examined the effects of gel preparation methods. The results showed that increasing concentration of the cationic polymer as CS induced the separation of the solution to gel (sol-to-gel) system due to the charge of CS and the charge of PEC. The ratio of HA:P407 affected the gel forming which high concentration of P407 reduced the gelation temperature while low concentration of HA disturbed the sol-to-gel state causing coagulation. The viscosity, spreadability, and swelling were significantly increased due to the concomitant increased in each polymer, HA and P407. The particle of the formulation observed under microscope was found to be less than 1 µm. Phase inversion from sol-to-gel was found after a min at 23°C. Since gelation temperature of the purposed formula is supposed to form gel below 37°C within a short period of injection. The results of the study indicate the suitable sol-to-gel forming in the appropriate temperature and time which should be used for further investigation in the efficacy and safety.