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Background: It has been reported that children are already practicing self-medication. Indeed, at the children's age, they are not allowed to self-medicate due to limited knowledge regarding self-medication, leading to inappropriate drug therapy or self-toxicity becoming problems in public health. Objective: This study aimed to determine how school-age adolescents carry out self-medication behavior. Methods: The study was designed as a cross-sectional in which data were collected using questionnaire methods. There were 195 students recruited in this study, consisting of SDN Keputih-245 Elementary School students, SMPN 19 Surabaya Junior High School, and SMAN 11 Surabaya Senior High School. Results: The results showed that most of the students had purchased medicine independently without a doctor's prescription. The primary source of information regarding self-medication by school students is family. Although most of the respondents stated they always inform their parents or doctors, it has been found that the practice of self-medication by school-age teenagers without informing their parents or doctors exists. Moreover, less than 50% of student respondents believe that self-medication is safe. Conclusion: The role of pharmacists is urgently needed to provide proper education related to drug information and self-medication to increase school-age students' knowledge.
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Background Wound healing shows a unique interaction of several cells, growth factors and cytokines. The healing of chronic plantar ulcer of leprosy is influenced by various factors, one of which is the concentration of growth factors and cytokines related to the pathogenesis of impaired wound healing. Growth factors and cytokines can be found in the secretome of adipose mesenchymal stem cells. Aim To compare the effectiveness of topical adipose mesenchymal stem cell-conditioned medium and framycetin gauze dressing only on the healing of chronic plantar ulcer of leprosy. Methods In this randomised controlled trial, 32 patients with chronic plantar ulcer of leprosy were recruited. After detailed clinical and initial debridement, patients were randomised to two groups to receive either topical adipose mesenchymal stem cell-conditioned medium (n = 16) or framycetin gauze dressing only (n = 16) applied every three days for up to eight weeks, following which the ulcer size, adverse reactions and complications if any were monitored weekly. Results Healing percentage increased each week in all groups. Statistical differences between groups (P < 0.05) were observed from week 2 onwards for ulcer mean size reduction and from week 3 onwards for ulcer mean depth reduction. There were no adverse reactions or complications. Limitations Off-loading on subjects were not performed. Conclusion Adipose mesenchymal stem cell-conditioned medium is a potential therapeutic agent in the management of chronic plantar ulcer of leprosy.
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Úlcera del Pie , Lepra , Células Madre Mesenquimatosas , Humanos , Úlcera del Pie/terapia , Úlcera del Pie/etiología , Framicetina , Medios de Cultivo Condicionados/farmacología , Úlcera/complicaciones , Vendajes/efectos adversos , Obesidad/complicaciones , Lepra/complicaciones , Lepra/diagnóstico , Lepra/terapia , CitocinasRESUMEN
Ursolic acid (UA) is a pentacyclic triterpene carboxylic acid which produces various effects, including anti-cancer, hepatoprotective, antioxidant and anti-inflammatory. However, UA demonstrates poor water solubility and permeability. Niosomes have been reported to improve the bioavailability of low water-soluble drugs. This study aimed to investigate the protective action of UA-niosomes with chitosan layers against liver damage induced by N-Nitrosodiethylamine (NDEA). UA niosomes were prepared using a thin layer hydration method, with chitosan being added by vortexing the mixtures. For the induction of liver damage, the mice were administered NDEA intraperitoneally (25 mg/kgBW). They were given niosomes orally (11 mg UA/kgBW) seven and three days prior to NDEA induction and subsequently once a week with NDEA induction for four weeks. The results showed that chitosan layers increased the particle sizes, PDI, and ζ-potentials of UA niosomes. UA niosomes with chitosan coating reduced the SGOT and SGPT level. The histopathological evaluation of liver tissue showed an improvement with reduced bile duct inflammation and decreasing pleomorphism and enlargement of hepatocyte cell nuclei in UA niosomes with the chitosan coating treated group. It can be concluded that UA niosomes with chitosan coating improved the efficacy of preventive UA therapy in liver-damaged mice induced with NDEA.
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Quitosano , Triterpenos , Ratones , Animales , Dietilnitrosamina/toxicidad , Quitosano/farmacología , Liposomas/farmacología , Triterpenos/uso terapéutico , Hígado/patología , Agua/farmacología , Ácido UrsólicoRESUMEN
<b>Background and Objective:</b> Fucoidan extract from the <i>Sargassum plagiophyllum </i>brown seaweed are renowned for its anticancer and antibacterial activities. Fucoidan is one of the ingredients of <i>S. plagiophyllum </i>that can be extracted by conventional methods and new methods, one of which is microwave assisted extraction (MAE). Research on the extraction of fucoidan from <i>S. plagiophyllum </i>was still limited. Thus, an advanced experiment on how microwave assisted extraction (MAE) of fucoidan was conducted in this study and its activities against <i>Escherichia coli </i>bacteria and HeLa cancer cells were studied. <b>Materials and Methods:</b> <i>Sargassum plagiophyllum </i>was collected from the Gunung Kidul Coast in Yogyakarta, Indonesia. Fucoidan extract of <i>S. plagiophyllum</i> was acquired by applying the MAE method at 600 W for 5 min and using hydrochloric acid as a solvent. The cytotoxicity and antibacterial assays were performed using the MTT assay and the agar plate diffusion methods, respectively. <b>Results:</b> The yield of the fucoidan extract examined was 9.90% (w/w), which consisted of 2.60% sulfate and 2.33 mg 100 g<sup>1</sup> fucose. The finding indicated that fucoidan extract exhibits no antibacterial action and the cytotoxicity against the HeLa cell line was 27.82 mg mL<sup>1</sup>. <b>Conclusion:</b> The MAE technique was proven to support the fucoidan extraction from <i>S. plagiophyllum </i>successfully. Therefore, the fucoidan extract has proven to have promise beneficial in anticancer activity.
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Sargassum , Humanos , Células HeLa , Microondas , Polisacáridos/farmacologíaRESUMEN
BACKGROUND AND PURPOSE: Ursolic acid (UA) exhibits anti-hepatocarcinoma and hepatoprotective activities, thus promising as an effective oral cancer therapy. However, its poor solubility and permeability lead to low oral bioavailability. In this study, we evaluated the effect of different ratios of Span® 60-cholesterol-UA and also chitosan addition on physical characteristics and stability of niosomes to improve oral biodistribution. EXPERIMENTAL APPROACH: UA niosomes (Nio-UA) were composed of Span® 60-cholesterol-UA at different molar ratios and prepared by using thin layer hydration method, and then chitosan solution was added into the Nio-UA to prepare Nio-CS-UA. FINDINGS/RESULTS: The results showed that increasing the UA amount increased the particle size of Nio-UA. However, the higher the UA amount added to niosomes, the lower the encapsulation efficiency. The highest physical stability was achieved by preparing niosomes at a molar ratio of 3:2:10 for Span® 60, cholesterol, and UA, respectively, with a zeta-potential value of -41.99 mV. The addition of chitosan increased the particle size from 255 nm to 439 nm, as well as the zeta-potential value which increased from -46 mV to -21 mV. Moreover, Nio-UA-CS had relatively higher drug release in PBS pH 6.8 and 7.4 than Nio-UA. In the in vivo study, the addition of chitosan produced higher intensities of coumarin-6-labeled Nio-UA-CS in the liver than Nio-UA. CONCLUSION AND IMPLICATIONS: It can be concluded that the ratio of Span® 60-cholesterol-UA highly affected niosomes physical properties. Moreover, the addition of chitosan improved the stability and drug release as well as oral biodistribution of Nio-UA.
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Intense efforts to develop alternative materials for gelatine as a drug-delivery system are progressing at a high rate. Some of the materials developed are hard capsules made from alginate, carrageenan, hypromellose and cellulose. However, there are still some disadvantages that must be minimised or eliminated for future use in drug-delivery systems. This review attempts to review the preparation and potential of seaweed-based, specifically carrageenan, hard capsules, summarise their properties and highlight their potential as an optional main component of hard capsules in a drug-delivery system. The characterisation methods reviewed were dimensional analysis, water and ash content, microbial activity, viscosity analysis, mechanical analysis, scanning electron microscopy, swelling degree analysis, gel permeation chromatography, Fourier-transform infrared spectroscopy and thermal analysis. The release kinetics of the capsule is highlighted as well. This review is expected to provide insights for new researchers developing innovative products from carrageenan-based hard capsules, which will support the development goals of the industry.
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It has been known that in respiratory disease, antibiotic is selected for respiratory diseases or lung infections and this research focused on ciprofloxacin HCl as a model. The aim was to evaluate the effect of kappa-carrageenan polymer concentrations on characteristics, release, and drug deposition in the lung. Ciprofloxacin HCl-carrageenan microspheres were produced with kappa carrageenan (0.75%, 0.50%, and 0.25%) as polymer and KCl (1.5%) as crosslinker. Physical characteristics were included morphology, size, moisture content, swelling index, mucoadhesivity, drug loading, entrapment efficiency, and yield. Freeze-dried microspheres were inhaled by animal, and drug deposition was observed. Results showed that dried, smooth, and spherical microspheres of size of 1.34 to 1.70 µm and loading of 15.63% to 38.72%. Entrapment efficiency and yield were 25.38%-51.61% and 52.53%-63.19%, respectively. Mucoadhesivity was 0.0059-0.0096 kg force, and release in 24 h was 74.38%-81.02%. Release kinetics demonstrated Higuchi mechanism. Increasing carrageenan concentration affected size, loading, and efficiency but did not influence adhesivity, yield, and release. Higher amount of polymer caused the lower deposit on the lungs. Respirable size of ciprofloxacin HCl-kappa carrageenan microspheres was successfully achieved target site and prolonged residence time in lungs.
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OBJECTIVES: This study aimed to determine the effect of different components and ratios of oil, surfactant, and cosurfactant on E. palmifolia extract-loaded SNEDDS. METHODS: E. palmifolia extract loaded SNEDDS was formulated from virgin coconut oil, Miglyol 812 as oil, using Tween 80 and Transcutol as surfactants, as well as propylene glycol and PEG 400 as cosurfactants. The optimization design formula consisted of eight design formulas in five ratio formulas, thus a total of 40 formulas were optimized using different components and ratios of oil, surfactant, and cosurfactant. These ratios used were 1:1:1, 1:2:1, 1:3:1, 1:4:1, as well as 1:5:1, and the formula's components were determined based on the optimization results. RESULTS: The optimal formula of E. palmifolia extract loaded SNEDDS had the ratio 1:1:1 (formula A) of Miglyol 812:Tween 80:PEG 400 and 1:3:1 (formula E) of Miglyol 812:Tween 80:propylene glycol. Meanwhile, the optimal formulation characteristics showed a transmittance value above 90%, pH range of 5.10-5.20, 2.21-14.51 cP viscosity, emulsification time below 120 s, and particle size of 24.71-136.77 nm. CONCLUSIONS: The optimal formula of E. palmifolia extract-loaded SNEDDS, were obtained using different components and ratios. These are Miglyol:Tween 80:PEG 400 at a component ratio of 1:1:1 (formula A) and Miglyol 812:Tween 80:propylene glycol at a component ratio of 1:3:1 (formula E).
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Nanopartículas , Polisorbatos , Disponibilidad Biológica , Sistemas de Liberación de Medicamentos , Emulsiones , Glicoles de Propileno , Solubilidad , TensoactivosRESUMEN
OBJECTIVES: This study aimed to evaluate the variation concentration effect of propyleneglycol, glycerin, and polyethyleneglycol 400 as a nonvolatile solvent on the physical properties and dissolution rate of the loratadine liquisolid tablet. METHODS: The tablet was formulated into 10 formulas, where nine were liquisolid and one was conventional (CT). The concentration of propyleneglycol, glycerin, and polyethyleneglycol used in liquisolid tablets were 14, 15, and 16%. Furthermore, the mixture was evaluated based on flow properties and compressibility index. The tablet was evaluated based on hardness, friability, disintegration time, and dissolution, and the data obtained was evaluated with ANOVA or Kruskal-Wallis statistic program. RESULTS: The result showed that flow properties, disintegration time, and dissolution have a significant value less than 0.05. The tablet friability for all concentration solvents, hardness at 14 and 15% solvent concentration, and compressibility index at 15 and 16% have significant value more than 0.05. The 16% propyleneglycol type solvent concentration tablet has the physical properties and contains the best solution. CONCLUSIONS: From the result, it is reasonable to conclude that F7 is the tablet with all the physical properties and the best dissolution.
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Comprimidos , Glicerol , Loratadina , Solubilidad , SolventesRESUMEN
OBJECTIVES: Chitosan is a natural polysaccharide widely used in various clinical applications including regeneration of skin tissue. Aloe vera has properties in healing burns on the skin, anti-inflammatory effect, and leaves a protective layer on the skin after drying so it provides protection to the wound. The spray gel of chitosan-A. vera was developed as a wound healing that has combined of effect of both component and easy to use. The purpose of this study was to determine the physical stability and irritability of chitosan-A. vera spray gel. METHODS: The spray gel stability test was conducted using thermal cycling and centrifugation methods. The organoleptic, viscosity, and pH of the spray were evaluated. The irritation test was performed by Draize Rabbit Test method. RESULTS: Chitosan (0.5%)-A. vera (1%) spray gel characteristics has a weak yellow color, clear, and a strong A. vera odor. The pH of the spray gel was 4.88 ± 0.01; and the viscosity was 36.50 ± 0.23 cps. The result from the chitosan (0.5%)-A. vera (1%) spray gel stability test using thermal cycling method showed a decrease of viscosity, but remained stable when evaluated using centrifugation method. There was no difference in the pH and organoleptic observation from both tests. Based on the scoring and analysis of the reaction in rabbit skin, the Primary Irritation Index (PII) obtained was 0.56. CONCLUSIONS: The spray gel of chitosan (0.5%)-A. vera (1%) was stable and according to response category from the acute dermal irritation test, it can be concluded that chitosan (0.5%)-A. vera (1%) spray gel had a slightly irritating effect.
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Aloe , Animales , Quitosano , Hojas de la Planta , Conejos , Piel , Cicatrización de HeridasRESUMEN
This study aimed to analyze the interaction of primaquine (PQ), chloroquine (CQ), and liposomes to support the design of optimal liposomal delivery for hepatic stage malaria infectious disease. The liposomes were composed of hydrogenated soybean phosphatidylcholine, cholesterol, and distearoyl-sn-glycero-3-phosphoethanolamine-N-(methoxy[polyethyleneglycol]-2000), prepared by thin film method, then evaluated for physicochemical and spectrospic characteristics. The calcein release was further evaluated to determine the effect of drug co-loading on liposomal membrane integrity. The results showed that loading PQ and CQ into liposomes produced changes in the infrared spectra of the diester phosphate and carbonyl ester located in the polar part of the phospholipid, in addition to the alkyl group (CH2) in the nonpolar portion. Moreover, the thermogram revealed the loss of the endothermic peak of liposomes dually loaded with PQ and CQ at 186.6 °C, which is identical to that of the phospholipid. However, no crystallinity changes were detected through powder X-ray diffraction analysis. Moreover, PQ, with either single or dual loading, produced the higher calcein release profiles from the liposomes than that of CQ. The dual loading of PQ and CQ tends to interact with the polar head group of the phosphatidylcholine bilayer membrane resulted in an increase in water permeability of the liposomes.
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Antimaláricos/química , Cloroquina/química , Vehículos Farmacéuticos/química , Fosfatidilcolinas/química , Primaquina/química , Antimaláricos/administración & dosificación , Antimaláricos/farmacocinética , Química Farmacéutica , Cloroquina/administración & dosificación , Cloroquina/farmacocinética , Colesterol/química , Composición de Medicamentos/métodos , Liberación de Fármacos , Fluoresceínas/farmacocinética , Humanos , Liposomas , Malaria/tratamiento farmacológico , Nanopartículas/química , Fosfatidiletanolaminas/química , Polietilenglicoles/química , Primaquina/administración & dosificación , Primaquina/farmacocinética , Difracción de Rayos XRESUMEN
Ursolic acid is a natural pentacyclic triterpenoid that exerts a potent anticancer effect. Furthermore, it is classified as a BCS class IV compound possessing low permeability and water solubility, consequently demonstrating limited bioavailability in addition to low therapeutic effectiveness. Nanoparticles are developed to modify the physical characteristics of drug and can often be produced in the range of 30-200 nm, providing highly effective cancer therapy due to the Enhanced Permeation and Retention (EPR) Effect. This study aims to provide a review of the efficacy and safety of various types of Ursolic Acid-loading nanoparticles within the setting of preclinical and clinical anticancer studies. This literature study used scoping review method, where the extracted data must comply with the journal inclusion criteria of within years of 2010-2020. The identification stage produced 237 suitable articles. Duplicate screening was then conducted followed by the initial selection of 18 articles that had been reviewed and extracted for data analysis. Based on this review, the use of nanoparticles can be seen to increase the anticancer efficacy of Ursolic Acid in terms of several parameters including pharmacokinetic data, survival rates and inhibition rates, as well as the absence of serious toxicity in preclinical and clinical trials in terms of several parameters including body weight, blood clinical chemistry, and organ histipathology. Based on this review, the use of nanoparticles has been able to increase the anticancer efficacy of Ursolic Acid, as well as show the absence of serious toxicity in preclinical and clinical trials. Evenmore, the liposome carrier provides development data that has reached the clinical trial phase I. The use of nanoparticle provides high potential for Ursolic Acid delivery in cancer therapy.
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OBJECTIVES: Roselle (Hibiscus sabdariffa L.) is a medicinal plant commonly used as a beverage and herbal medicine. Complex compounds in the aqueous extracts have provided good antibacterial activity by which the growth of gram-negative and -positive bacteria is inhibited. The aims of this research were to formulate hydroxypropyl methylcellulose (HPMC) 6000 gel containing the extract and investigate the inhibitory activity of the extract and its gel formula against Staphylococcus aureus ATCC 25923. MATERIALS AND METHODS: Thin layer chromatography (TLC) on silica gel GF254 was used for analyzing flavonoids and polyphenols using butanol: acetic acid: water (4:1:5) and chloroforms: ethyl acetate: formic acid (0.5:9:0.5) as eluent, respectively. A serial dilution of aqueous extract powder in citrate buffer was made to obtain 0.50, 0.25, 0.10, 0.05, and 0.02 mg/mL solution. The roselle aqueous extract (3%) was formulated as a component of gel containing HPMC 6000 in various concentrations (2%, 3%, and 4%). A diffusion agar method on two layers of nutrient agar media was applied using Staphylococcus aureus ATCC 25923 and gentamicin 25 ppm as bacterial test and standard, respectively. After incubation for 24 h at 37°C, the inhibitory effect was denoted by a clear zone around the hole and the inhibitory activity was measured as minimum inhibitory concentration (MIC). RESULTS: The aqueous extract of Hibiscus sabdariffa L. contained flavonoid and polyphenol compounds based on the TLC chromatogram profile. It was found that the gel formula containing 3% HPMC 6000 and 3% aqueous extract gave a good physical characteristic and the lowest MIC (6.0 mg/mL), equivalent to 7.58 ppm of gentamicin standard at 12.0 mg/mL concentration. CONCLUSION: The HPMC 6000 at 3% (w/w) concentration in roselle aqueous extract gel preparation gave good physical characteristics. The gel preparation exhibited inhibitory activity against Staphylococcus aureus ATCC 25923 shown by MIC 6.0 mg/mL. Formula 2 is recommended and should be further investigated for implementation in topical preparations.
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The objective of this study was to determine and evaluate a controlled release implant of ciprofloxacin using bovine hydroxyapatite (BHA)-chitosan composite and glutaraldehyde or genipin as crosslinking agents. Ciprofloxacin implants were prepared using BHA, chitosan, ciprofloxacin at 30:60:10 and using three different concentrations of glutaraldehyde or genipin (0.3, 0.5, or 0.7%) as crosslinkers. Implants were formed as mini-tablet with 4.0 mm diameter weighing 100 mg using compression method. Further, the prepared ciprofloxacin implants were characterized for porosity, density, water absorption capacity, swelling, degradation, compressive strength, compatibility (Fourier transforms-infrared spectroscopy (FT-IR)), morphology (scanning electron microscope (SEM)), X-ray diffraction (X-RD), and in vitro drug release. The addition of glutaraldehyde or genipin as crosslinkers in ciprofloxacin implant showed controlled release profile of ciprofloxacin over a time period of 30 days. SEM photomicrograph revealed low porosity of the implant after crosslinking with glutaraldehyde or genipin. The FTIR study confirmed the formation of covalent imine bonds between chitosan and glutaraldehyde. Moreover, the addition of glutaraldehyde or genipin as crosslinkers caused a decrease in the mechanical strength of the implant. Increased concentration of glutaraldehyde or genipin reduced the crystallinity of BHA and chitosan, which were confirmed by X-RD studies. The results obtained from this study indicated that glutaraldehyde or genipin had the potential effect to retard ciprofloxacin release from BHA-chitosan-ciprofloxacin implant for 30 days.
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OBJECTIVES: The development of oral vaccine formulations has been widely investigated to overcome oral route problems. This research investigated the in vivo immune response of ovalbumin-alginate microspheres by uptake compared with a commercial oral vaccine product. MATERIALS AND METHODS: Ovalbumin-loaded alginate microspheres were prepared using aerosolization. Ovalbumin antigen in vivo uptake was investigated in order to understand the distribution and uptake by Peyer's plaque (PP) after oral administration using fluorescence microscopy. The histopathology of ovalbumin-alginate microspheres in the liver and kidney was also investigated. RESULTS: The use of alginate microspheres to deliver vaccines could be a promising delivery system for the development of oral vaccines because uptake by PP is an essential step in oral vaccination. CONCLUSION: Fluorescence visualization revealed the uptake of ovalbumin-loaded alginate microspheres with and without lyoprotectant maltodextrin by PP was equal to the oral vaccine product and no liver or kidney damage was found.
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The significant inhibitory action of diclofenac formulated in mixed micelles of lecithin with cholate or deoxycholate was observed on the rat hind paw edema induced by carrageenan. In the primary stage, mixed micelle formulation of deoxycholate was more effective compared with that of cholate. However, in the final term, the inhibitory action was similar in both formulations. In a previous study, the flux of diclofenac was greater in the mixed micelle formulation of deoxycholate compared with that of cholate. It was suggested that the permeation rate of diclofenac through skin was proportional to the pharmacological activity. The hind paw edema was quickly inhibited when cyclic monoterpene such as d-limonene or l-menthol was included in the formulations. All the micelle formulations significantly decreased the value of AUC estimated the hind paw thickness-time profile. This suggests that the micelle formulation of cholate in addition to deoxycholate showed significant anti-inflammatory activity to hind paw edema of rats. Incorporation of d-limonene or l-menthol was more effective on the decrease of AUC. A pharmacological study revealed that micelle formulations were able to reduce the skin irritation of chemicals.