RESUMEN

Hydrolyzed collagen (HC) derived from salmon (Oncorhynchus nerka) skin possesses properties that can nourish the skin, and it is one of the active ingredients used in cosmeceutical products for moisturizing the facial skin. However, HC solution gives off a fishy odor and it is gray in color that makes the product unacceptable for cosmetic purposes. This study aimed to use liposome-encapsulated hydrolyzed salmon collagen to improve its physical appearance, skin permeation, and eliminate the fishy odor. Two percent of HC and vitamin B3 (VitB3) were used as active ingredients to incorporate into liposomes. Phosphatidylcholine, cholesterol, and Tween 80 at a suitable weight ratio of 8 : 2 : 1 produced nano-sized vesicles (170.6 ± 0.70 nm) with the highest percentage of entrapment efficiency (95.72 ± 2.00%) of VitB3 and (49.63 ± 1.74%) of HC. Skin permeation and odor detection of the HC-VitB3 liposome were studied using Franz's diffusion cell and gas chromatography, respectively, and compared with HC-VitB3 solution. Subsequently, facial serums were formulated using HC-VitB3 liposomes and HC-VitB3 solutions, and a product satisfaction test was conducted with 100 volunteers to determine their preferred product. The results of the studies of HC-VitB3 liposome serum showed improved formulation appearance, enhanced skin permeation, and better odor elimination compared to the HC-VitB3 serum. Furthermore, seventy-three volunteers in the product satisfaction test preferred and selected the liposomal serum for its superior scent. From all the experimental results, it could be seen that liposomes can help increase skin penetration, and undesirable odors and colors can be masked by the appropriate lipid bilayer structure of liposomes.

RESUMEN

BACKGROUND: Lactobacillus rhamnosus SD11 is a probiotic derived from the human oral cavity and has potential being used for dental prophylaxis. The cell free supernatant (CFS) of L. rhamnosus SD11 has good antimicrobial and antioxidant effects. AIM: This study aimed to incorporate CFS of the probiotic into thermoresponsive copolymers to create a sol-gel formulation. METHODS: The sol-gel formulation was developed using Poloxamer 407 as the main polymer, which was mixed with natural polymers such as gellan gum, sodium alginate, and xyloglucan in different proportions. The sol-gel formulations were characterized based on their physicochemical parameters such as appearance, pH, viscosity, flow-ability in low temperature, antioxidant and antibacterial activity. An in vitro release study was performed using Franz's diffusion cell and the stability was determined under freeze-thaw cycle conditions. RESULTS: The combination of 15% w/v of poloxamer 407 with 0.5% w/v of sodium alginate was the best sol-gel formulation to deliver the CFS of the probiotic. CONCLUSION: This study was successful in creating a sol-gel formulation using a thermoresponsive copolymer, that could efficiently deliver CFS of the probiotic L. rhamnosus SD11.

RESUMEN

In this study, nanoemulsions for skincare products were continuously produced using a hydrodynamic cavitation reactor (HCR) designed with a rotor and stator. The key component of this research is the utilization of a 3D-printed rotor in a HCR for the production of an oil-in-water nanoemulsion. Response surface methodology was used to determine the process conditions, such as speed of the rotor, flow rate, as well as, Span60, Tween60, and mineral oil concentrations, for generating the optimal droplet size in the nanoemulsion. The results showed that a droplet size of 366.4 nm was achieved under the recommended conditions of rotor speed of 3500 rpm, flow rate of 3.3 L/h, Span60 concentration of 2.36 wt%, Tween60 concentration of 3.00 wt%, and mineral oil concentration of 1.76 wt%. Moreover, the important characteristics for consideration in skincare products, such as polydispersity index, pH, zeta potential, viscosity, stability, and niacin released from formulations, were also assessed. For the niacin release profile of emulsion and nanoemulsion formulations, different methods, such as magnetic stirring, ultrasound, and hydrodynamic cavitation, were compared. The nanoemulsion formulations provided a greater cumulative release from the formulation than the emulsion. Particularly, the nanoemulsion generated using the HCR provided the largest cumulative release from the formulation after 12 h. Therefore, the present study suggests that nanoemulsions can be created by means of hydrodynamic cavitation, which reduces the droplet size, as compared to that generated using other techniques. The satisfactory results of this study indicate that the rotor-stator-type HCR is a potentially cost-effective technology for nanoemulsion production.

Asunto(s)

Hidrodinámica , Impresión Tridimensional , Emulsiones

RESUMEN

Rhodomyrtone, a plant-derived principal compound isolated from Rhodomyrtus tomentosa (Myrtaceae) leaf extract, was assessed as a potential natural alternative for the treatment of acne vulgaris. The clinical efficacy of a 1% liposomal encapsulated rhodomyrtone serum was compared with a marketed 1% clindamycin gel. In a randomized and double-blind controlled clinical trial, 60 volunteers with mild to moderate acne severity were assigned to two groups: rhodomyrtone serum and clindamycin gel. The volunteers were instructed to apply the samples to acne lesions on their faces twice daily. A significant reduction in the total numbers of acne lesions was demonstrated in both treatment groups between weeks 2 and 8 (p < 0.05). Significant differences in acne numbers compared with the baseline were evidenced at week 2 onwards (p < 0.05). At the end of the clinical trial, the total inflamed acne counts in the 1% rhodomyrtone serum group were significantly reduced by 36.36%, comparable to 34.70% in the clindamycin-treated group (p < 0.05). Furthermore, a commercial prototype was developed, and a clinical assessment of 45 volunteers was performed. After application of the commercial prototype for 1 week, 68.89% and 28.89% of volunteers demonstrated complete and improved inflammatory acne, respectively. All of the subjects presented no signs of irritation or side effects during the treatment. Most of the volunteers (71.11%) indicated that they were very satisfied. Rhodomyrtone serum was demonstrated to be effective and safe for the treatment of inflammatory acne lesions.

RESUMEN

Characteristics of liposomal encapsulated ethanolic coconut husk extract (LE-ECHE) prepared using two levels of lipid phase (LP) containing soybean phosphatidylcholine/cholesterol mixture of 4:1 mol ratio (60 and 80 µmol/mL) and two ECHE concentrations (1% and 2%) were investigated. Poly-dispersity index, zeta-potential, and particle size of LE-ECHE samples were 0.22% to 0.28%, -70.4 to -53.63 mV, and 232 to 697.65 nm, respectively. Encapsulation efficiency of all samples was 75.25% to 90.11%. LE-ECHE prepared with LP content of 60 µmol/mL and 1% ECHE (LP60-EC1) was milky, whereas UN-EC1 (un-encapsulated ECHE) was brownish in color. ECHE retained its antioxidant activity even after entrapment in liposome, although higher activity was recorded for UN-EC1. Encapsulation of ECHE in liposome enhanced antibacterial properties of ECHE. Hence, LP60-EC1 showed promising potential as a delivery based system for lowering dark color, a drawback associated with ECHE as well as improving the antibacterial properties of ECHE. PRACTICAL APPLICATION: Ethanolic coconut husk extract (ECHE) contains polyphenols with diverse biological activities such as antimicrobial and antioxidant properties. However, there are limited applications of ECHE in food industries, mainly because of its distinctive dark brown color. A homogeneous and stable liposomal system was demonstrated to be an efficient delivery based system for ECHE. Remarkably, antimicrobial property of ECHE was enhanced with liposomal encapsulation, whereas antioxidant activities of ECHE were retained. Also, liposomal encapsulation was shown as the potential technique to mask the undesirable dark brown, a drawback associated with ECHE for wider application.

Asunto(s)

Antibacterianos/química , Antioxidantes/química , Cocos/química , Composición de Medicamentos/métodos , Liposomas/química , Extractos Vegetales/química , Antibacterianos/farmacología , Antioxidantes/farmacología , Frutas/química , Tamaño de la Partícula , Extractos Vegetales/farmacología , Residuos/análisis

RESUMEN

AIM: Antifungal activity, skin permeation and skin retention of water-in-oil microemulsion (ME) and microemulsion-based gel (MBG) containing clotrimazole (CTZ) were evaluated in comparison to a conventional CTZ cream. METHODS: CTZ-ME and CTZ-MBG containing 1% w/w of CTZ were produced. Antifungal activity against Trichophyton mentagrophytes was assessed by the agar diffusion method. Pig skin was used in the in vitro penetration study using modified Franz diffusion cells. Drug amounts which permeated into the receptor fluid, retained in the skin membrane and remained in the donor compartment were analyzed by a validated HPLC technique. RESULTS: CTZ-ME and CTZ-MBG exhibited inhibition zones against T. mentagrophytes whereas the conventional cream did not reveal any inhibition zone in the assay. While no CTZ was detected in the receptor fluid up to 24 h following the in vitro penetration study from all tested formulations, the amount of CTZ retained in the skin membrane when applying CTZ-ME and CTZ-MBG was remarkably higher than that when applying the cream. CONCLUSION: Results revealed the capacity of ME and MBG in improving skin bioavailability of CTZ while reducing the risk of systemic side effects. Thereby, ME and MBG could increase the efficacy of CTZ for dermatophytosis treatment in comparison to conventional cream.

Asunto(s)

Antifúngicos/administración & dosificación , Clotrimazol/administración & dosificación , Piel/metabolismo , Trichophyton/efectos de los fármacos , Animales , Animales Recién Nacidos , Emulsiones , Geles , Piel/parasitología , Porcinos , Tiña/tratamiento farmacológico

RESUMEN

OBJECTIVES: Plant-derived compounds are a good source of therapeutic agents and inhibitors of inflammatory process. Dental caries, periodontal diseases and candidiasis are common oral infections caused by virulent biofilms. The objectives of this study were to develop oral spray containing plant-derived compounds; α-mangostin (α-MG) and/or lawsone methyl ether (2-methoxy-1,4-naphthoquinone) (LME) and determine its antimicrobial, anti-biofilm, and anti-inflammatory activities. DESIGN: Oral spray formulations were prepared containing α-MG (5 mg/ml) and/or LME (250 µg/ml). Antimicrobial activity against Candida albicans, Streptococcus mutans, and Porphyromonas gingivalis and anti-biofilm formation activities were determined as well as cytotoxicity and anti-inflammatory effects. RESULTS: The oral spray demonstrated antimicrobial activity against all three of the oral pathogens tested with stronger effects on C. albicans and S. mutans than P. gingivalis. The formulation containing α-MG (2.5 mg/ml) and LME (125 ug/ml) reduced growth of the microorganisms about 1-2 Log CFU/ml at 1-3 h and the killing effects were complete at 24 h. Based on biofilm assay, the oral spray containing both α-MG and LME showed greater inhibitory effects than those with α-MG or LME. In addition, the oral spray containing both α-MG and LME demonstrated more inhibition of nitric oxide production than α-MG alone. All the formulations were safe and demonstrated greater anti-inflammatory activity at lower concentration (<6.25 µg/ml) than at a higher concentration. CONCLUSION: Oral spray containing α-MG and/or LME is effective against common oral pathogens without significant cytotoxicity. Thus, it has the potential to prevent the infections and may serve as adjunctive treatment to conventional therapy.

Asunto(s)

Naftoquinonas/farmacología , Vaporizadores Orales , Fitoquímicos/farmacología , Exudados de Plantas/farmacología , Xantonas/farmacología , Animales , Antiinfecciosos/farmacología , Antiinflamatorios/farmacología , Biopelículas/efectos de los fármacos , Candida albicans/efectos de los fármacos , Candida albicans/crecimiento & desarrollo , Candidiasis/tratamiento farmacológico , Supervivencia Celular/efectos de los fármacos , Recuento de Colonia Microbiana , Caries Dental/tratamiento farmacológico , Ratones , Pruebas de Sensibilidad Microbiana , Naftoquinonas/uso terapéutico , Óxido Nítrico/metabolismo , Enfermedades Periodontales/tratamiento farmacológico , Fitoquímicos/uso terapéutico , Exudados de Plantas/uso terapéutico , Porphyromonas gingivalis/efectos de los fármacos , Porphyromonas gingivalis/crecimiento & desarrollo , Células RAW 264.7/efectos de los fármacos , Streptococcus mutans/efectos de los fármacos , Streptococcus mutans/crecimiento & desarrollo , Tailandia , Xantonas/uso terapéutico

RESUMEN

Topical administration of phenylethyl resorcinol (PR) has attracted much attention as skin lightening agent with potent anti-tyrosinase activity. Two novel types of elastic carriers were developed to overcome the limitation of PR as topical delivery by increasing the solubility, stability and decreasing skin irritation compared to conventional liposomes. In addition, it also promotes skin penetration of PR to reach deep skin layer at the target site. The lead formulations were obtained from the invasomes containing 1% (w/v) d-limonene mixed with 10% (v/v) absolute ethanol as the skin enhancer, and transfersomes containing 15% (w/w) sodium deoxycholate (SDC) as edge activator. All formulations gave a vesicle size < 500 nm, polydispersity index (PDI) < 0.3, high zeta potential, entrapment efficiency > 50%, and good stability on storage at 30 °C at 75% RH for 4 months. Transfersomes have a lower degree of deformability (6.63%) than invasomes (25.26%). In contrast, the liposomes as rigid vesicles do not show a deformable property. This characteristic affects the skin permeation, and thus, transfersomes with high elastic property provided a significantly higher cumulative amount, steady state flux (J ss) and permeability coefficient (Kp ) compared to other formulations. However, in vitro PR accumulation in full-thickness newborn pig skin demonstrated that the application of elastic carrier formulations gave significantly higher accumulation than liposomes, and gave anti-tyrosinase activity up to 80%. These results are straightforwardly related to the results of cellular level study. Transfersomes and invasomes showed higher tyrosinase inhibition activity and melanin content reduction when compared to liposomes in B16 melanoma cells. In addition, acute irritation test in rabbits confirmed that these formulations are safe for skin application. Therefore, elastic vesicle carriers have the efficiency to deliver PR into the deep skin in both quantity and effectiveness which are better than conventional liposomes and appropriate for a skin lightening product.

RESUMEN

The high performance liquid chromatography (HPLC) was used for quantitative determination of phenylethyl resorcinol (PR) which was loaded in the novel vesicle carriers including ethosome, invasome and transfersome formulations, and permeated into pig skin membrane and receptor fluid for skin permeation study. The reverse-phase chromatography was carried out with a C18 column (150 × 4.6 mm2, 5 µm, HypersilTM, Thermo Fisher Scientific Inc, USA) with the column temperature at 25°C. A mixture of acetonitrile-methanol-Milli-Q water in the ratio of 40:20:40%, v/v/v was used as a mobile phase by maintaining the flow rate at 0.8 mL/min. The 20 µL sample solution was injected and the absorbance was detected at 254 nm using an HPLC Agilent 1100 series. This method gave the chromatogram with symmetric peak of PR at the appropriate retention time of 4.620 min. At such retention time no interfering peaks were detected from other matrix components. All %recovery and %RSD values of PR analysis were in the range of 98-102% and not more than 2.0%, respectively. From the validation data, the method demonstrated that it had satisfactory specificity, sensitivity, linearity, accuracy and precision appropriate for analysis of PR in the presence of vesicle carriers and skin permeation study.

Asunto(s)

Cromatografía Líquida de Alta Presión/métodos , Portadores de Fármacos , Modelos Biológicos , Resorcinoles , Absorción Cutánea , Piel , Animales , Portadores de Fármacos/análisis , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Modelos Lineales , Reproducibilidad de los Resultados , Resorcinoles/análisis , Resorcinoles/química , Resorcinoles/farmacocinética , Sensibilidad y Especificidad , Piel/química , Piel/metabolismo , Porcinos

RESUMEN

BACKGROUND: Quercus infectoria G. Olivier (Fagaceae) nutgalls have been widely employed in traditional Asian medicine for several treatments, especially wounds and skin disorders. However, the effects of this plant on wound healing have not yet been clearly elucidated. This present work was focused on utilization of Quercus infectoria (Qi) as a topical agent for chronic wound treatment. METHODS: Twenty Qi formulations (QiFs) were pharmaceutically formulated and antibacterial activity of all formulations was performed. The best formulation based on an antibacterial activity was selected for evaluation of wound healing property. Total phenolics, total flavonoids, and an anti-oxidant activity of the selected formulation were also investigated. Wound healing activity was assessed in streptozotocin-induced diabetic rats and control rats. Streptozotocin injection (50 mg/kg) was found to induce marked hyperglycaemia, compared with citrate-injected controls. Two wounds were created on the upper back of each animal. QiF was topically applied three days after wounding to one of the duplicate wounds on each animal and physiological saline (control) was applied to the other. All wounds were cleaned once a day until wound closure. RESULTS: QiF10, which exhibited antibacterial and anti-oxidant activities, had the ability to enhance the wound healing process in diabetic rats with abundant cellular infiltration, collagen deposition, and re-epithelialization when compared with the control. DISCUSSION: This study suggested that QiF10 could be a novel alternative treatment for diabetic wounds.

RESUMEN

Ethosome formulations containing phenylethyl resorcinol (PR) were developed. The formulation was produced from 0.5% w/v PR, 0.5% w/v cholesterol from lanolin, 3% w/v L-α-phosphatidylcholine from soybean, 30% v/v absolute ethanol, and water up to 100% v/v. It was characterized by a vesicular size of 389 nm, low polydispersity index of 0.266, zeta potential of -34.19 ± 0.44 mV, high PR entrapment efficiency of 71%, and good stability on storage at 4 and 30°C at 75% RH for 4 months. In vitro studies using pig skin revealed that permeation coefficient of PR from ethosomes was significantly higher than that from liposomes. In vitro retention profiles showed that PR accumulation in pig skin following application of ethosome formulations was 7.4-, 3.3-, and 1.8-fold higher than that achieved using liposomes, 20% propylene glycol solution, and 30% hydroethanolic solution, respectively. An inhibition value of around 80% was measured for antityrosinase activity of PR in pig skin. Consistently, ethosomes exhibited higher tyrosinase inhibition activity and melanin content reduction when compared to other formulations in B16 melanoma cells. Ethosomes did not cause acute dermal irritation in albino rabbits. These findings demonstrate that ethosomes are capable of delivering PR into the skin efficiently and hold promise for topical application of skin lightening products.

Asunto(s)

Compuestos de Bencidrilo , Resorcinoles , Preparaciones para Aclaramiento de la Piel , Pigmentación de la Piel/efectos de los fármacos , Animales , Animales Recién Nacidos , Compuestos de Bencidrilo/química , Compuestos de Bencidrilo/farmacología , Liposomas , Resorcinoles/química , Resorcinoles/farmacología , Preparaciones para Aclaramiento de la Piel/química , Preparaciones para Aclaramiento de la Piel/farmacología , Porcinos

RESUMEN

BACKGROUND: Skin fungal infections are regular injuries suffered by people living in tropical areas. Most common pathogens are Trichophyton, Microsporum and Epidermophyton which can cause skin lesions in many parts of body. Topical antifungal phytochemicals are commonly used to avoid systemic adverse events and are more convenient for patient application than those administered by other routes. However, the effectiveness of topical treatments in eradicating fungal infection is more limited since the stratum corneum acts as the skin barrier, resulting in long treatment duration and low patient's compliance. METHODS: The goal of this work is to identify optimized drug delivery systems to improve topic clinical efficacy. Microemulsions i.e. liquid dispersions of oil and water stabilized with an interfacial film of surfactant are well known drug delivery systems. RESULTS: A thickening agent may be included to form microemulsion-based gels to increase skin adhesion. Microemulsions and microemulsion-based gels can be loaded with several hydrophilic and lipophilic drugs because they are composed of both water and oil phases. CONCLUSION: Microemulsions and microemulsion-based gels can also be used for the delivery of many drugs including antifungal drugs through stratum corneum due to their capacity to act as skin penetration enhancement. In addition to a comprehensive review of microemulsion and microemulsion-based gels as suitable carriers for skin delivery of various antifungal drugs, this review also aims to discuss the delivery of antifungal phytochemicals.

Asunto(s)

Antifúngicos/farmacología , Dermatomicosis/tratamiento farmacológico , Fitoquímicos/farmacología , Administración Tópica , Animales , Antifúngicos/administración & dosificación , Antifúngicos/química , Sistemas de Liberación de Medicamentos , Emulsiones/administración & dosificación , Emulsiones/química , Epidermophyton/efectos de los fármacos , Geles/administración & dosificación , Geles/química , Humanos , Microsporum/efectos de los fármacos , Fitoquímicos/administración & dosificación , Fitoquímicos/química , Trichophyton/efectos de los fármacos

RESUMEN

Mycophenolate mofetil (MMF) is a prodrug of mycophenolic acid (MPA) which can be metabolized by esterase. MMF has been approved by the United States Food and Drug Administration (USFDA) for treatment of psoriasis patient with skin symptoms. However, it remains unclear whether MMF is efficiently effective to treat skin symptoms developed from psoriasis. The insufficient amount of MMF penetrating through the skin results in the treatment failure due to the difficulty in MMF penetration through the stratum corneum. Skin permeation enhancers such as eucalyptol (EUL) and N-methyl-2-pyrrolidone (NMP) potentially aid in increasing skin penetration. This study aimed to investigate the effects of a concentration ratio (% w/v) between two enhancers (EUL and NMP). The results showed that EUL enhanced MMF permeation with an enhancement ratio (ER) of 3.44 while NMP was not able to promote the penetration of MMF. Interestingly, the synergistic effect of the two enhancers was observed with a suitable ratio given that the ER was 8.21. EUL and NMP are promising enhancers for the development of MMF based skin product.

RESUMEN

This study purposed to evaluate a microemulsion containing nicotinamide for its characteristics, stability, and skin penetration and retention comparing with a solution of nicotinamide in 2:1 mixture of water and isopropyl alcohol (IPA). The microemulsion system was composed of 1:1 mixture of Span80 and Tween80 as a surfactant mixture, isopropyl palmitate (IPP) as an oil phase, and 2:1 mixture of water and IPA as an aqueous phase. Nicotinamide microemulsion was prepared by dissolving the active in the aqueous phase before simply mixing with the other components. It was determined for its characteristics and stability under various conditions. The skin penetration and retention studies of nicotinamide microemulsion and solution were performed by modified Franz diffusion cells, using newborn pig skin as the membrane. The results showed that nicotinamide microemulsion could be obtained as clear yellowish liquid, was water-in-oil (w/o) type, possessed Newtonian flow, and exhibited physicochemical stability when kept at 4 °C and room temperature (≈30 ± 2 °C) during 3 months. From the skin penetration data, the microemulsion could enhance the skin penetration of nicotinamide comparing with the solution. Additionally, nicotinamide microemulsion could provide much higher amount of skin retention than that of skin penetration, resulting in suitability for a cosmeceutical product.

Asunto(s)

Emulsiones/administración & dosificación , Emulsiones/farmacocinética , Niacinamida/administración & dosificación , Niacinamida/farmacocinética , Absorción Cutánea/efectos de los fármacos , Administración Cutánea , Animales , Animales Recién Nacidos , Evaluación Preclínica de Medicamentos/métodos , Emulsiones/química , Niacinamida/química , Técnicas de Cultivo de Órganos , Absorción Cutánea/fisiología , Porcinos , Viscosidad

RESUMEN

Psoriasis is a skin disease associated with hyperproliferation and abnormal differentiation of keratinocytes. Available approaches using synthetic drugs for the treatment of severe psoriasis may cause side effects. Alternatively, plant-derived compounds are now receiving much attention as alternative candidates for the treatment of psoriasis. In this study, the effects of rhodomyrtone, a bioactive plant extract isolated from Rhodomyrtus tomentosa leaves on the proliferation, growth arrest, and apoptosis of HaCaT keratinocytes were investigated. Percentage anti-proliferative activity of rhodomyrtone on HaCaT cells at concentrations of 2-32µg/ml after 24, 48, and 72h ranged from 13.62-61.61%, 50.59-80.16%, and 61.82-85.34%, respectively. In a scratch assay, rhodomyrtone at 2 and 4µg/ml significantly delayed closure of a wound by up to 61.78%, and 71.65%, respectively, after 24h incubation. HaCaT keratinocytes treated with rhodomyrtone showed chromatin condensation and fragmentation of nuclei when stained with Hoechst 33342. This indicated that rhodomyrtone induced apoptosis in the keratinocytes. In addition, flow cytometric analysis demonstrated an increase in the percentage of apoptosis of keratinocytes after treatment with rhodomyrtone at 2-32µg/ml from 1.2-10%, 8.2-35.4%, and 21.0-77.8% after 24, 48, and 72h, respectively, compared with the control. To further develop the compound as a potential anti-psoriasis agent, a rhodomyrtone formulation was prepared and subjected to skin irritation tests in rabbits. The formulation caused no skin irritation including such as erythema and edema. The results indicated that rhodomyrtone had the potential as a promising candidate for further development as a natural anti-psoriasis agent.

Asunto(s)

Apoptosis/efectos de los fármacos , Queratinocitos/citología , Queratinocitos/efectos de los fármacos , Xantonas/farmacología , Animales , Línea Celular , Proliferación Celular/efectos de los fármacos , Supervivencia Celular/efectos de los fármacos , Química Farmacéutica , Humanos , Magnoliopsida/química , Psoriasis/tratamiento farmacológico , Conejos , Xantonas/efectos adversos , Xantonas/química , Xantonas/uso terapéutico

RESUMEN

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 Higuchi's model. These formulations were safe without producing any severe skin irritation. However, for the stability they needed to be stored at 4 °C in tightly sealed containers.

RESUMEN

Rhodomyrtone isolated from the leaves of Rhodomyrtus tomentosa possesses antibacterial, anti-inflammatory, and anti-oxidant activities. Since rhodomyrtone is insoluble in water, it is rather difficult to get to the target sites in human body. Liposome exhibited ability to entrap both hydrophilic and hydrophobic compounds and easily penetrate to the target site. The present study aimed to develop a novel liposomal encapsulated rhodomyrtone formulations. In addition, characterization of liposome, stability profiles, and their antiacne activity were performed. Three different formulations of total lipid concentrations 60, 80, and 100 µ mol/mL were used. Formulation with 60 µ mol/mL total lipid (phosphatidylcholine from soybean and cholesterol from lanolin in 4 : 1, w/w) exhibited the highest rhodomyrtone encapsulation efficacy (65.47 ± 1.7%), average particle size (209.56 ± 4.8 nm), and ζ -potential (-41.19 ± 1.3 mV). All formulations demonstrated good stability when stored for 2 months in dark at 4°C as well as room temperature. Minimal inhibitory concentration and minimal bactericidal concentration values of liposomal formulation against 11 clinical bacterial isolates and reference strains ranged from 1 to 4 and from 4 to 64 µ g/mL, respectively, while those of rhodomyrtone were 0.25-1 and 0.5-2 µ g/mL, respectively. The MIC and MBC values of liposome formulation were more effective than topical drugs against Staphylococcus aureus and Staphylococcus epidermidis.

RESUMEN

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.

Asunto(s)

Nicotina/química , Goma/química , Piel/metabolismo , Administración Cutánea , Animales , Química Farmacéutica/métodos , Sistemas de Liberación de Medicamentos/métodos , Concentración de Iones de Hidrógeno , Membranas Artificiales , Nicotina/administración & dosificación , Permeabilidad , Goma/administración & dosificación , Absorción Cutánea , Soluciones/administración & dosificación , Soluciones/química , Solventes/química , Porcinos

RESUMEN

BACKGROUND: Cellulose masks obtained from natural sources such as bacteria are of interest as cosmetic devices for the treatment of dry skin because they not only improve hydration of the skin, but have low toxicity and are biodegradable. The aims of this study were to determine the in vivo effects of a cellulose mask obtained from Acetobacter xylinum on skin characteristics and to evaluate user satisfaction with the product. METHODS: Thirty healthy Thai volunteers aged 21-40 years participated in the study. The volunteers were randomly separated into a control group and an experimental group. For the control group, volunteers were assigned to apply moist towels to the face for 25 minutes. For the experimental group, the volunteers were assigned to apply the masks, ie, translucent patches which could be fitted onto the face for the same period. The following week, the groups were changed over to the alternative treatment. Skin moisture, sebum, elasticity, texture, dullness, and desquamation levels were assessed using a system used for routine skin counseling before applying the trial product and five minutes after its removal. Degree of satisfaction with use of the cellulose mask was investigated using a five-point rating scale. RESULTS: The cellulose mask increased moisture levels in the skin significantly more than moist towels (P < 0.05) after a single application. No obvious effects on other skin characteristics were found. The cellulose mask product rated around 4/5 on the satisfaction rating scale. CONCLUSIONS: A single application of the trial cellulose mask enhanced moisture uptake by facial skin. Users also reported being satisfied with the trial product.

RESUMEN

Hibiscus sabdariffa Linn, or Roselle, is a medicinal plant used extensively in traditional Thai medicine since ancient times. The extracts of Roselle calyces possess antioxidant activity and have potential for development as active ingredients in cosmetic products. However the limitations of using Roselle extracts in cosmetics are its low skin permeation and dermal irritation. Liposome technology is an obvious approach that might overcome these problems. Liposome formulations of standardized Roselle extracts were developed with various lipid components. The formulation showing the highest entrapment efficiency was selected for stability, skin permeation and dermal irritability studies. The liposome formulation with the highest entrapment efficiency (83%) and smalôlest particle size (332 mm) was formulated with phosphatidylcholine from soybean (SPC): Tween 80: deoxycholic acid (DA); 84:16:2.5 weight ratio, total lipid of 200 g/mL and 10% w/v Roselle extract in final liposomal preparation. This liposome formulation was found to be stable after storage at 4 degrees C, protected from light, for 2 months. The in vitro skin permeation studies, using freshly excised pig skin and modified Franz-diffusion cells, showed that the liposome formulation was able to considerably increased the rate of permeation of active compounds in Roselle extracts compared to the Roselle extract solution. The in vivo dermal irritability testing on rabbit skin showed that the liposome formulation dramatically decreased skin irritability compared to the unformulated extract. These results showed that the liposomes containing Roselle extracts had good stability, high entrapment efficacy, increased skin permeation and low skin irritation.

Asunto(s)

Antioxidantes/farmacología , Hibiscus/química , Extractos Vegetales/farmacología , Plantas Medicinales , Absorción Cutánea , Administración Cutánea , Administración Tópica , Animales , Antioxidantes/aislamiento & purificación , Relación Dosis-Respuesta a Droga , Flores , Liposomas , Permeabilidad , Extractos Vegetales/aislamiento & purificación , Conejos , Piel/metabolismo , Pruebas de Irritación de la Piel