ABSTRACT
Purpose: To investigate the active ingredients of walnut ointment (WO) and its mechanism in repairing wounds. Methods: The ingredients of WO were detected by gas chromatographymass spectrometry. The effect of linoleic acid (LA) was tested by in vitro Alamar Blue (AB) reagent. Image J software, histological and immunohistochemical analysis were used to confirm the healing effect of LA in the porcine skin model. The animals were euthanized after the experiment by injection of pentobarbital sodium. Results: LA, 24% in WO, promotes keratinocytes and fibroblasts proliferation, which were 50.09% and 15.07% respectively higher than control (p < 0.05). The healing rate of the LA group (96.02% ± 2%, 98.58% ± 0.78%) was higher than the saline group (82.11% ± 3.37%, 88.72% ± 1.73%) at week 3 and week 4 (p < 0.05). The epidermal thickness of the LA was 0.16 ± 0.04 mm greater and the expression of the P63 and CK10 proteins was stronger in the LA group than the control (p < 0.05). Conclusions: LA, which is the main components in WO can promote full-thickness burning wounds (FBWs) by stimulating cell proliferation and differentiation.
Subject(s)
Ointments/chemistry , Wound Healing/drug effects , Keratinocytes/drug effects , Linoleic Acid/therapeutic use , Nuts/chemistry , Burns/therapy , FibroblastsABSTRACT
Effect of rubbing application on the skin permeation of a hydrophilic drug caffeine (CAF) and lipophilic drug rhododendrol (RD) from lotion and cream were investigated. Skin permeation of CAF was markedly increased by rubbing action independent of the formulation type. In addition, the skin penetration-enhancement effect was affected by the rubbing direction: rubbing application against the direction of hair growth showed the highest permeation compared with rubbing applications along the direction of hair growth and in a circular pattern on the skin. On the other hand, no enhancement effect was observed by the rubbing actions on the skin permeation of RD, regardless of formulation type. Change in the infundibula orifice size of hair follicles by the rubbing and following skin stretching may be related to the higher skin permeation for CAF. In contrast, high RD distribution into the stratum corneum may be a reason why no enhancement effect was observed by the rubbing action. These results can be helpful to predict safety and effectiveness of topically applied formulations.
Subject(s)
Butanols/pharmacology , Caffeine/pharmacology , Ointments/pharmacology , Skin Cream/pharmacology , Skin/drug effects , Animals , Butanols/chemistry , Caffeine/chemistry , Hydrophobic and Hydrophilic Interactions , Ointments/chemistry , Permeability/drug effects , Skin Absorption/drug effects , Skin Cream/chemistry , SwineABSTRACT
BACKGROUND: Skin rejuvenation can be achieved with minimally invasive treatments using energy-based devices that feature reduced side effects and downtime. Post-treatment care is key to minimize any potential side effects and skin reactions such as erythema, dryness, or dyschromia. OBJECTIVE: The objective of this study was to evaluate the efficacy and patient satisfaction of a novel carboxytherapy gel mask compared with petroleum-based lanolin-containing ointment to accelerate wound healing facial post-nanofractional radiofrequency treatment. METHODS AND MATERIALS: Ten subjects were enrolled in this pilot, prospective, randomized, single-blind study and randomized into two arms. One arm received one nanofractional radiofrequency treatment with ointment right after and four consecutive days of ointment applications twice a day, while the second arm followed this regimen with a carboxytherapy gel mask application right after and four consecutive days after treatment. Investigator, safety, and patient assessments were conducted at 24 hours and one-week post treatment. Safety was monitored throughout. The primary endpoint was defined as the degree of investigator global assessment (IGA) in photodamage, pigmentation, and wrinkles using standardized photographs. Secondary endpoints included investigator-rated degree of erythema, edema, crusting, exudation, percentage healing, improvement of skin quality, and patient satisfaction. RESULTS: Nine patients completed the study. There was improvement of one degree in IGA for photodamage, pigmentation and wrinkles in all patients using the carboxytherapy gel mask at the one-week follow up. Blinded investigator ratings showed significant improvement of dryness, erythema, edema, crusting, and percentage healing at the 24-hour follow up, with all patients remaining the same a week post treatment. All patients in the carboxytherapy group were satisfied with the treatment and had no adverse effects. Three patients in the petroleum-based lanolin-containing group experienced mild edema and acne breakout that resolved two weeks after treatment. CONCLUSION: Carboxytherapy delivered via a gel mask after skin rejuvenation procedures is a safe and effective strategy to improve clinical outcomes and reduce post-treatment side effects. J Drugs Dermatol. 20(4):461-465. doi:10.36849/JDD.5856.
Subject(s)
Carbon Dioxide/administration & dosage , Cosmetic Techniques/adverse effects , Erythema/drug therapy , Radiofrequency Therapy/adverse effects , Rejuvenation , Administration, Cutaneous , Adult , Erythema/diagnosis , Erythema/etiology , Face , Female , Gels , Humans , Lanolin/administration & dosage , Middle Aged , Ointments/administration & dosage , Ointments/chemistry , Patient Satisfaction , Petroleum , Photography , Pilot Projects , Prospective Studies , Radiation Dose Hypofractionation , Radiofrequency Therapy/methods , Severity of Illness Index , Single-Blind Method , Skin/diagnostic imaging , Skin/drug effects , Skin/radiation effects , Skin Aging/radiation effects , Treatment OutcomeABSTRACT
Petrolatum ointment, which is an oleaginous ointment, is generally produced through manufacturing processes such as melting, mixing, and cooling. In this type of semisolid formulation, the manufacturing conditions of each process are empirically known to affect the quality of the resultant preparation; however, in many cases, the details of the factors are unclear. To clearly investigate the influence of the pharmaceutical properties of petrolatum ointments, we manufactured several ointments while changing the conditions of the mixing and cooling process after melting white petrolatum. As a result, the temperature at the termination was determined to influence the pharmaceutical properties of the final product. To investigate these phenomena, each petrolatum ointment sample was examined via digital microscopy and laser Raman analysis, and the distribution of the liquid-solid parts of samples was investigated. The internal structure of the ointment sample manufactured at a mixing-stop temperature of 40 °C, the needle crystals and the spherical aggregates surrounding them appropriately coexisted, while the structure exhibited a state wherein the two were linked in a semisolid phase. Meanwhile, for the ointment sample manufactured under the lowest mixing-stop temperature of 25 °C, the liquid part and the spherical aggregates were clearly separated, indicating that the liquid part was easily separated from ointments. In addition, the distribution of the hydrocarbons among the samples was measured via GC-MS; no significant difference in chemical structure was observed. In conclusion, the internal structure of the petrolatum ointment was changed by the manufacturing conditions, and this affected the pharmaceutical properties.
Subject(s)
Hydrocarbons/chemistry , Ointments/chemistry , Petrolatum/chemistry , Drug Compounding , Rheology , TemperatureABSTRACT
The objective of the study was to reinforce the applicability of the immersion cells for the in vitro release testing (IVRT) of topical formulations by using marketed acyclovir 5% cream formulation (Cream 1) as a model. The method employing the immersion cells was optimized by studying the effect of variables, such as membrane type, media temperature and volume, agitation speed, and cell size, on acyclovir release from the formulation. The in-house formulation similar to the qualitative and quantitative composition of Cream 1 and the other trial formulations with variable compositions were prepared and studied by using the immersion cells. Various other brands of acyclovir topical formulations available in the Indian market were also subjected to IVRT by using the optimized method. An increase in the media temperature from 32°C to 37°C and the stirring speed from 50 to 100 to 150 rpm led to an increase in the drug release. As the immersion cell size increased (0.5, 2 and 4 cm2 surface area), the release rate also increased. Nitrocellulose membrane showed the highest drug release and Fluoropore™the least. The optimized IVRT method could establish the differences in the drug release rates among the formulations with the altered compositions. The method could also prove its discriminatory potential for various marketed formulations. The immersion cell method could serve as a simpler, facile, and reliable aid during product development and also as a quality control tool in assessing stability, aging, and batch-to-batch uniformity of semisolid formulations.
Subject(s)
Acyclovir/chemistry , Antiviral Agents/chemistry , Ointments/chemistry , Acyclovir/administration & dosage , Administration, Topical , Antiviral Agents/administration & dosage , Drug Compounding , Drug Liberation , Humans , Membranes, Artificial , Ointments/administration & dosageABSTRACT
This paper reports a pioneering study of an unknown historical drug formulation preserved in the Spezieria of Santa Maria della Scala in Rome, founded at the end of the seventeenth century by the Discalced Carmelites. Due to limited literature related to pharmaceutical remedies and drugs of the Early Modern Era (between the XV and XVIII centuries) and the complexity in their formulations, the study of these drugs represents a great challenge. The untargeted nature of the selected drug required a multi-analytical approach with complementary techniques to formulate a compositional hypothesis: FT-IR spectroscopy, gas chromatography-associated/mass spectrometry (GC-MS) and nuclear magnetic resonance (NMR) were successfully employed to identify different organic compounds. Systematic archaeobotanical research was performed as well, allowing us to acquire data related to the possible genus of plants from which these natural compounds derive and their geographical origin. The unknown drug formulation turned out to be a complex mixture used as an ointment with an anti-inflammatory purpose. It mainly contains a mixture of Venetian turpentine; a Pine resin (colophony) from the Pinaceae family; an exudate of a plant from South America, whose identified components are triterpenic compounds such as alpha- and beta-amyrins, betulin and lupeol; and saturated fatty acids which act as carriers and/or to reduce the viscosity of abovementioned exudates and resins. The study of historical drugs is important not only in order to know the practices handed down by the speziali in the past but also to reconstruct historical recipes, which can inspire new dermatological, cosmetic, hygienic and current healing products.Graphical abstract.
Subject(s)
Drug Compounding , Gas Chromatography-Mass Spectrometry , Magnetic Resonance Spectroscopy , Pharmaceutical Preparations/chemistry , Pinaceae/chemistry , Spectroscopy, Fourier Transform Infrared , Anti-Inflammatory Agents/chemistry , Drug Compounding/history , Gas Chromatography-Mass Spectrometry/methods , History, 15th Century , History, 16th Century , History, 17th Century , History, 18th Century , Magnetic Resonance Spectroscopy/methods , Ointments/chemistry , Ointments/history , Pharmaceutical Preparations/history , Resins, Plant/analysis , Rome , Spectroscopy, Fourier Transform Infrared/methods , Triterpenes/analysis , Turpentine/analysisABSTRACT
Patient satisfaction and outcomes can be optimized by identifying preferences for topical vehicles by age, gender, and ethnicity. Our study sought to identify variations in preferences for creams, lotions, and ointments among different age groups, genders, and ethnicities. Each demographic group revealed statistically significant differences in vehicle preference (P < .05).
Subject(s)
Ointments/chemistry , Patient Satisfaction , Pharmaceutical Vehicles/chemistry , Skin Cream/chemistry , Administration, Cutaneous , Adult , Age Factors , Ethnicity/statistics & numerical data , Female , Humans , Male , Middle Aged , Sex FactorsSubject(s)
Education, Pharmacy , Ointments/chemistry , Pain , Administration, Topical , Analgesics , Humans , Pain/physiopathologyABSTRACT
Effects of repeated annealing treatments (8 cycles, 12 h each) or continuous annealing treatments (12-96 h) at 50 °C on structural, physicochemical, and digestive properties of normal and waxy wheat starches were investigated. Wheat starches retained the original crystalline structure of A-type after annealing. Annealing treatments increased crystallinity, short chain of amylopectin, viscosity, and gelatinization temperatures of starch. However, molecular weight, long chain of amylopectin, solubility, and swelling power of starch decreased after annealing. Additionally, annealing reduced the in vitro digestibility of wheat starches. The changes in properties of starch varied depending on starch type, normal or waxy, and annealing methods, repeated or continuous. The repeated annealing was found to be more effective in modification of normal wheat starch properties. However, continuous annealing efficiently modified properties of the waxy wheat starch. The obtained results may help in choosing appropriate applications of annealed wheat starches in the food industry.
Subject(s)
Starch/analysis , Starch/chemistry , Triticum/chemistry , Waxes/chemistry , Amylopectin/analysis , Amylopectin/chemistry , Amylose/analysis , Amylose/chemistry , Chemical Phenomena , Crystallization , Gelatin/chemistry , Molecular Structure , Molecular Weight , Ointments/chemistry , Solubility , Spectroscopy, Fourier Transform Infrared , Starch/isolation & purification , Temperature , Time Factors , Viscosity , Water/chemistry , X-Ray DiffractionABSTRACT
Hot-melt extrusion (HME) has been extensively investigated for continuous manufacturing of amorphous solid dispersions, to improve the solubility of poorly water-soluble drug substances, impart abuse deterrence to controlled substances, taste masking for pediatric and geriatric formulations and development of cocrystal system. Much research has been conducted on the continuous manufacturing of solid dosage forms using HME, but its applicability in the manufacturing of semisolids remains an unexplored domain. This study aimed to explore the applicability of HME in the continuous manufacturing of topical semi-solid formulations with two active pharmaceutical ingredients (APIs). Ointments containing a combination of triamcinolone acetonide and lidocaine hydrochloride were screened based on a quality target product profile (QTPP) and established critical quality attributes (CQAs) using design of experiments (DoE). Three selected formulations, manufactured by a lab-scale fusion method and HME, were subjected to further characterization studies including work of adhesion, stiffness, apparent pH, content uniformity, differential scanning calorimetry, accelerated stability, and in vitro drug release testing. Selected formulations met design characteristics and demonstrated the applicability of HME in the continuous manufacturing of semi-solid formulations. Graphical abstract.
Subject(s)
Anti-Inflammatory Agents/chemistry , Hot Melt Extrusion Technology , Ointments/chemistry , Aged , Calorimetry, Differential Scanning , Chemistry, Pharmaceutical/methods , Drug Compounding/methods , Drug Liberation , Hot Temperature , Humans , SolubilityABSTRACT
The transdermal route of administration of drug substances allows clinicians to obtain a therapeutic effect bypassing the gastrointestinal tract, where the active substance could be inactivated. The hormonal substance used in the study-corticotropin (ACTH)-shows systemic effects. Therefore, the study of the effect of the type of ointment base and drug concentration on the release rate and also permeation rate in in vivo simulated conditions may be a valuable source of information for clinical trials to effectively optimize corticotropin treatment. This goal was achieved by preparation ointment formulation selecting the appropriate ointment base and determining the effect of ACTH concentration on the release and permeation studies of the ACTH. Semi-solid preparations containing ACTH were prepared using Unguator CITO e/s. The release study of ACTH was tested using a modified USP apparatus 2 with Enhancer cells. The permeation study was conducted with vertical Franz cells. Rheograms of hydrogels were made with the use of a universal rotational rheometer. The dependence of the amount of released and permeated hormone on the ointment concentration was found. Based on the test of ACTH release from semi-solid formulations and evaluation of rheological parameters, it was found that glycerol ointment is the most favourable base for ACTH. The ACTH release and permeation process depends on both viscosity and ACTH concentration. The higher the hormone concentration, the higher the amount of released ACTH but it reduces the amount of ACTH penetrating through porcine skin.
Subject(s)
Adrenocorticotropic Hormone/administration & dosage , Drug Liberation/physiology , Ointments/chemistry , Administration, Cutaneous , Adrenocorticotropic Hormone/pharmacology , Chemistry, Pharmaceutical , Hydrogels/chemistry , Hydrogels/pharmacology , Permeability , Rheology , Skin , ViscosityABSTRACT
Bioshell calcium oxide (BiSCaO) possesses deodorizing properties and broad microbicidal activity. This study aimed to investigate the application of BiSCaO ointment for the prevention and treatment of infection in chronic wounds in healing-impaired patients, without delaying wound healing. The bactericidal activities of 0.04, 0.2, 1, and 5 wt% BiSCaO ointment, 3 wt% povidone iodine ointment, and control (ointment only) were compared to evaluate the in vivo disinfection and healing of Pseudomonas aeruginosa-infected wounds in hairless rats. Treatment of the infected wounds with 0.2 wt% BiSCaO ointment daily for 3 days significantly enhanced wound healing and reduced the in vivo bacterial counts compared with povidone iodine ointment and control (no wound cleaning). Although 5 wt% BiSCaO ointment provided the lowest bacterial counts during 3 days' treatment, it delayed wound healing. Histological examinations showed significantly advanced granulation tissue and capillary formation in wounds treated with 0.2 wt% BiSCaO ointment for 3 days compared to wounds treated with the other ointments. This study suggested that using 0.2 wt% BiSCaO ointment as a disinfectant for infected wounds and limiting disinfection to 3 days may be sufficient to avoid the negative effects of BiSCaO on wound repair.
Subject(s)
Anti-Bacterial Agents/pharmacology , Calcium Compounds/pharmacology , Ointments/pharmacology , Oxides/pharmacology , Pseudomonas Infections/drug therapy , Wound Infection/drug therapy , Animal Shells/chemistry , Animals , Anti-Bacterial Agents/chemistry , Calcium Compounds/chemistry , Disinfection/methods , Male , Ointments/chemistry , Oxides/chemistry , Pectinidae/chemistry , Povidone-Iodine/pharmacology , Pseudomonas Infections/pathology , Pseudomonas aeruginosa/drug effects , Rats, Hairless , Wound Infection/microbiology , Wound Infection/pathologyABSTRACT
A simple rapid and efficient deep eutectic solvent-based magnetic colloidal gel (DES-MCG) assisted magnetic solid-phase extraction (MSPE) method followed by high performance liquid chromatography with a diode array detector (HPLC-DAD) was established for determination of four sex hormones (including ethinylestradiol, norgestrel, megestrol acetate and medroxyprogesterone acetate) in cosmetic skin care toners. The DES-MCG with the desirable advantages of high adsorbing ability was prepared by combining choline chloride/urea deep eutectic solvent and magnetic multiwalled carbon nanotubes (MMWCNTs). The synthesized DES-MCG was characterized using fourier transform infrared spectrometry (FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and vibrating sample magnetometry (VSM). The cosmetic skin care toners were concentrated by a rotary evaporator and the obtained solutions were further purified by DES-MCG assisted magnetic solid-phase extraction. Response surface methodology (RSM) was applied for efficient optimization of the main variables in the extraction procedure. Under the optimized conditions, method detection limits and method quantitation limits were in the range of 1.2-6.6 ng mL-1 and 4.4-26.6 ng mL-1, respectively. The recoveries of the four sex hormones in different cosmetic skin care toners ranged from 80.1% to 118.8% and the precisions were no more than 0.35%. The developed method was successfully applied for the determination of sex hormones in cosmetic skin care toners.
Subject(s)
Cosmetics/chemistry , Gels/chemistry , Gonadal Steroid Hormones/analysis , Ointments/chemistry , Solid Phase Extraction/methods , Solvents/chemistry , Adsorption , Chromatography, High Pressure Liquid , Cosmetics/standards , Limit of Detection , Magnetic Phenomena , Nanotubes, Carbon/chemistry , Ointments/standards , Skin CareABSTRACT
Eleven months old female patient presented to paediatric out patient with parents concerned about her facial swelling. Upon examination child's weight and height for age were normal on her percentiles, she had a cushingoid facies with plethoric cheeks (Figure-1,2) though generalized oedema was absent and there was centripetal obesity with some muscle wasting (Figure-3,4). Systemic examination was normal excluding blood pressure which was high for her age. Electrolytes and cortisol levels were normal. On further inquiry it was revealed that she had been using a nappy rash cream containing a potent steroid, i.e., fluticasone for 2 months and this was identified as a cause for her cushingoid features.
Subject(s)
Cushing Syndrome/chemically induced , Hypertension/chemically induced , Skin Cream/adverse effects , Anti-Inflammatory Agents/adverse effects , Anti-Inflammatory Agents/therapeutic use , Diaper Rash/drug therapy , Female , Fluticasone/adverse effects , Fluticasone/therapeutic use , Humans , Iatrogenic Disease , Infant , Ointments/adverse effects , Ointments/chemistry , Ointments/therapeutic use , Skin Cream/chemistry , Skin Cream/therapeutic useABSTRACT
The effects of Mesona chinensis polysaccharide (MCP) on the pasting, rheological properties, granule size, and water mobility of tapioca starch (TS) were investigated at different gelatinization temperatures (75⯰C and 95⯰C). The structures of tapioca starch-Mesona chinensis polysaccharide (TM) gels formed at different gelatinization temperatures were investigated by X-ray diffraction (XRD) and scanning electron microscopy (SEM). Results showed that the peak, trough, and final viscosities of TM-95 mixtures were lower than that of TM-75 mixtures. Addition of MCP had a significant reduce (pâ¯<â¯0.05) on the granule size and transversal relaxation time of TM mixtures at the two gelatinization temperatures. Rheological analysis also showed that the addition of MCP increased the consistency indexes (K) and decreased the flow behavior indexes (n) of TM-95 and TM-75 gels. XRD results confirmed the diffraction peak of TM-95 gels became blunt and wider, and the diffraction peak at 17° and 23° of TM-75 gels could be observed after MCP added. In addition, the microstructures of TM-75 gels were more compact than that of TM-95 gels. These results can promote the development of TS-based products and application of MCP at different gelatinization temperatures.
Subject(s)
Gelatin/chemistry , Lamiaceae/chemistry , Manihot/chemistry , Ointments/analysis , Ointments/chemistry , Polysaccharides/chemistry , Starch/chemistry , Gels/chemical synthesis , Gels/chemistry , Magnetic Resonance Spectroscopy , Microscopy, Electron, Scanning , Particle Size , Rheology , Starch/ultrastructure , Temperature , Viscosity , X-Ray DiffractionABSTRACT
Common buckwheat starch (CBS) has extensive using value in the human diet. In this study, the molecular structure and physicochemical properties of CBS isolated from five cultivars collected from three regions of China were studied. Variations in molecular structure, crystalline structure, complexity, water solubility (WS), swelling power (SP), pasting properties, and thermal characteristics were recorded among the starches. The CBS had both similarities and differences in its properties by comparison with maize starch (MS) and potato starch (PS). The average molecular weight (MW) and amylopectin average chain length (ACL) of CBS ranged from 3.86 × 107 g/mol to 4.68 × 107 g/mol and from 21.29% to 22.68%, respectively. CBS and MS were divided into one subgroup and showed typical A diffraction patterns, while PS was divided into two subgroups and exhibited a typical B polymorphic pattern. The WS and SP of all the starches significantly increased with increasing temperature and had great variation at 70 °C and 90 °C. Pearson's correlation analysis showed that the molecular structure of starches greatly affected the physicochemical properties. This study revealed that the physicochemical properties of CBS could be affected by the molecular structures.
Subject(s)
Amylopectin/chemistry , Fagopyrum/chemistry , Amylopectin/analysis , Amylose/analysis , Amylose/chemistry , China , Correlation of Data , Crystallization , Flow Cytometry , Molecular Structure , Molecular Weight , Ointments/chemistry , Reference Values , Solanum tuberosum/chemistry , Solubility , Spectroscopy, Fourier Transform Infrared , Temperature , Viscosity , Water/chemistry , X-Ray Diffraction , Zea mays/chemistryABSTRACT
INTRODUCTION: The oral treatment of feline hyperthyroidism with antithyroid drugs often results in gastrointestinal side effects (10-20%). To date only oral formulations are approved although the oral application is not tolerated by all cats. Transdermal therapy can be an alternative. Nanocarriers could be used to ensure adequate transport of active agents through the skin. The present pilot study investigated the efficacy and safety of a novel dermal formulation of thiamazole for the treatment of feline hyperthyroidism. For the first time, amphiphilic dendritic core-multishell-nanocarriers were used. Cats with T4 values ≥ 4.0 µg/dl or a T4 value from 3.0-4.0 µg/dl and defined clinical findings were recruited. The euthyroid range for the T4 value was defined from ≥ 0.8 and ≤ 4.0 µg/dl. A total of 24 hyperthyroid cats were included and treated with thiamazole ointment for three weeks (24 cats) up to eight weeks (12 cats). The treatment success was 50% after three weeks and 41,7% after eight weeks. Cats that were within the euthyroid range required after three weeks a mean total dose of 1,09 mg/kg/d (0,68-1,7 mg/kg/d, 12/24) and after eight weeks 1,65 mg/kg/d (1,49-2,04 mg/kg/d, 5/12). No side effects were observed during the three resp. eight-week study period. Variations of the T4 value in companion cats in the same household were comparable to those of an independent control group. Thiamazole ointment based on nanocarriers is suitable for the treatment of feline hyperthyroidism.
INTRODUCTION: Le traitement oral de l'hyperthyroïdie féline avec des médicaments antithyroïdiens entraîne souvent des effets secondaires gastro-intestinaux (10 à 20% des cas). À ce jour, seules les formulations orales sont approuvées, bien que l'application orale ne soit pas tolérée par tous les chats. La thérapie transdermique peut être une alternative. Des nanoporteurs pourraient être utilisés pour assurer un transport adéquat des agents actifs à travers la peau. La présente étude pilote a examiné l'efficacité et l'innocuité d'une nouvelle formulation cutanée de thiamazole pour le traitement de l'hyperthyroïdie féline. Pour la première fois, des nanoporteurs à noyau multicellulaire dendritiques amphiphiles ont été utilisées. Des chats avec des valeurs T4 ≥ 4,0 µg/dl ou une valeur T4 de 3,04,0 µg/dl et un tableau clinique définis ont été recrutés. La gamme euthyroïdienne pour la valeur T4 a été définie entre ≥ 0,8 et ≤ 4,0 µg/dl. Un total de 24 chats hyperthyroïdiens ont été inclus et traités avec une pommade au thiamazole pendant une période allant de trois semaines (24 chats) jusqu'à huit semaines (12 chats). Le succès du traitement était de 50% après trois semaines et de 41,7% après huit semaines. Les chats qui se trouvaient dans la gamme euthyroïdienne avaient besoin après trois semaines d'une dose totale moyenne de 1,09 mg/kg/j (0,681,7 mg/kg/j, 12/24) et après huit semaines 1,65 mg/kg/j (1,49-2,04 mg/kg/j, 5/12). Aucun effet secondaire n'a été observé pendant les trois respectivement les huit semaines de l'étude. Les variations de la valeur T4 chez les chats vivant dans le même ménage étaient comparables à celles d'un groupe témoin indépendant. La pommade au thiamazole à base de nanoporteurs convient au traitement de l'hyperthyroïdie féline.
Subject(s)
Cat Diseases/drug therapy , Hyperthyroidism/veterinary , Thyroxine/administration & dosage , Administration, Cutaneous , Animals , Antithyroid Agents/administration & dosage , Cats , Drug Carriers , Hyperthyroidism/drug therapy , Nanotechnology , Ointments/chemistry , Ointments/therapeutic use , Pilot Projects , Treatment OutcomeABSTRACT
Gelatinization and retrogradation characteristics of starches from tigernut (Cyperus esculentus) tuber before and after various oil extraction processes were studied in this investigation. The results indicated that starches isolated from tigernut tuber after the various oil extraction processes varied significantly in gelatinization and retrogradation properties. The starches isolated from the cakes of tigernut tuber after hot press extraction exhibited higher retrogradation tendency and relatively less shear-thinning than other starch samples. The results of FT-IR, XRD, and NMR analysis indicated that oil extraction had an unfavorable influence on starch retrogradation, which may be due to structural changes caused by oil extraction processes. In particular, oil extraction led to more efficient packing of double helices in the crystalline lamella of the starches during storage. Retrogradation of the starch gels also reduced the water holding capacities of the starches. The starch sample isolated from the cake after cold press extraction exhibited the highest water absorption capacity among the five samples for all storage times. This investigation provides valuable novel information for the industrial utilization of tigernut tuber starches isolated from meals and cakes after oil extraction.
Subject(s)
Cyperus/chemistry , Gelatin/chemistry , Plant Oils/isolation & purification , Plant Tubers/chemistry , Starch/chemistry , Chemical Fractionation/methods , Crystallization , Food Technology , Gels/chemistry , Magnetic Resonance Spectroscopy , Microscopy, Electron, Scanning , Ointments/chemistry , Plant Oils/chemistry , Rheology , Shear Strength , Spectroscopy, Fourier Transform Infrared , Starch/isolation & purification , Starch/ultrastructure , Thermogravimetry , Viscosity , Water/chemistry , X-Ray DiffractionABSTRACT
The synergistic effects of the combination of acetylated distarch adipate and sesbania gum (C-ADA-SG) with the ratio of 5:0, 4:1, 2.5:2.5, 1:4, 0:5, accounting for 5% (w/w) of the starch on gelatinization and retrogradation properties of wheat starch (WS) were studied. Scanning Electron Microscopy (SEM) showed that the microstructure of gelatinized WASs (WS added with C-ADA-SG) tended to be smoother. Based on the results of Rapid Visco-Analyzer (RVA) and Differential Scanning Calorimetry (DSC), the pasting characteristics of WS were affected and the gelatinization process was retarded by C-ADA-SG. After seven-day storage at 4⯰C, compared to WS, the gel firmness, syneresis, retrogradation enthalpy, and the relative crystallinity of WASs clearly decreased by 17.47-44.36â¯g, 11.16-17.93%, 0.22-0.80â¯J·g-1, and 4.06-8.61%, respectively. However, the band ratio 1639:1157â¯cm-1 by FTIR and loss tangent (tan δ) value were increased with C-ADA-SG addition. Meanwhile, X-Ray Diffraction (XRD) reflected that native WS showed A-type crystal structure, which transferred to Bâ¯+â¯V type after retrogradation. Furthermore, Low-Field Nuclear Magnetic Resonance (LF-NMR) declared that C-ADA-SG increased the water mobility and limited the diffusion and seepage of water during storage. Generally, ADA and SG produced a synergistic effect on retarding the gelatinization and retrogradation of WS.
Subject(s)
Adipates/chemistry , Galactans/chemistry , Gelatin/chemistry , Mannans/chemistry , Plant Gums/chemistry , Starch/chemistry , Triticum/chemistry , Acetylation , Calorimetry, Differential Scanning , Crystallization , Food Preservation/methods , Gelatin/ultrastructure , Gels/chemistry , Magnetic Resonance Spectroscopy , Microscopy, Electron, Scanning , Ointments/chemistry , Rheology , Spectroscopy, Fourier Transform Infrared , Thermodynamics , Thermography , Water/chemistry , X-Ray DiffractionABSTRACT
PURPOSE: The purpose of this study was (a) to suggest a novel dermatopharmacokinetic (DPK) approach from which pharmacokinetic parameters relevant to the bioequivalence (BE) assessment of a topical formulation can be deduced while circumventing the need for numerous measurements and assumptions, and (b) to investigate whether this approach enables the correct conclusion of BE and bioinequivalence (BIE). METHODS: Bioequivalent and bioinequivalent formulations of acyclovir were compared versus a reference product (Zovirax®). Tape Stripping was conducted at only one dose duration during the uptake phase to generate drug content in stratum corneum versus time profiles, each time point corresponding to one stripped layer. Nonlinear mixed effect modeling (ADAPT5®) (MLEM algorithm) was used to fit the DPK data and to estimate the rate (Kin) and extent (FS) of drug absorption/input into the skin. Results were evaluated using the average BE approach. RESULTS: Estimated exposure metrics were within the usual BE limits for the bioequivalent formulation (FS: 102.4 [90%CI: 97.5-107.7]; Kin: 94.2 [90%CI: 83.7-106.0]), but outside those limits for the bioinequivalent formulation (FS: 43.4 [90%CI: 27.9-67.6]; Kin: 54.5 [90%CI: 36.6-81.1]). CONCLUSIONS: The proposed novel DPK approach was shown to be successful, robust and applicable to assess BE and BIE correctly between topical formulations.