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Antioxidant, analgetic, and anti-inflammatory activity test of purple leaf ethanol extract (Graptophyllum pictum L. Griff) in vitro and in vivo
Get PDFPurple leaves are one of the plants that are widely used as medicine. Purple leaves have 3 types of plant varieties, namely purple leaves, green leaves, and white mottled leaves. Purple leaves have pharmacological activities that can be used as medicine, including antioxidants (improving the deterioration of cells in the body), anti-inflammatory (reducing or suppressing inflammation), antidiabetic (lowering blood glucose levels), analgesics (relieving pain), immunomodulators (increasing the work of the immune system in the body), antihemorrhoids (treating symptoms and complaints of hemorrhoids), and antibacterial (as an antiseptic). The purpose of this study was to determine the antioxidant activity of purple leaf ethanol extract (Graphtophyllum pictum (L.) Griff) in vitro using the DPPH method and to determine its effectiveness as an analgesic and anti-inflammatory against Wistar rats.The results showed that antioxidant activity showed an IC50 value of 72.31 ppm (strong antioxidant). Meanwhile, in the analgetic test, the highest percentage of analgesic effectiveness was found at a dose of 100 mg/kg BW (129.64%) and showed anti-inflammatory activity at a dose of 100 mg/kgBW with a percentage decrease in edem volume of 28.73% at the sixth hour
Application of vegetable oils as pharmaceutical ingredient: the impact of liquid lipid type on the characteristics of nanostructured lipid carrier
Get PDFRecently, drug encapsulation using a Nanostructured Lipid Carrier (NLC) has gained attention in formulation studies due to its high loading capacity and prevent drug expulsion during storage. Drug loading capacity is mainly affected by lipid type and composition, especially liquid lipids. Therefore, this research aims to evaluate the potential of avocado oil as a liquid lipid of NLC replacing pure oleic acid. All components including oil, glyceryl monostearate, Tween 20®, and Span 60® were processed to NLC by solvent injection method. The colloidal characteristics of NLC dispersion in water and 20 mM PBS pH 7 were determined, including transmittance, particle size, size distribution, zeta potential, loading capacity (LC), and loading efficiency (LE) of capsanthin in NLC. The results showed that NLC containing oleic acid (Fola) and avocado oil (Favo) dispersion in PBS exhibited a similar transmittance and zeta potential of 69-74% and -51 to -58 mV, respectively, whereas the particle size and size distribution of Favo were significantly higher than Fola. Moreover, the 1.3-fold higher LC and LE of Favo compared to Fola was insignificant (p>0.05). Additionally, the Tween 20® and Span 60® ratio of Favo should be improved to obtain an ideal particle size and size distribution as in Fola. In conclusion, avocado oil indicated the potential to be utilized as a liquid lipid of NLC formulation regarding zeta potential and drug loading. However, the surfactant composition should be adjusted to reduce the particle size of the NLC, leading to permeability enhancement in delivery, particularly oral administration
Phytochemical and antibacterial analyses of essential oils extracted from the leaves of Euodia suaveolens scheff
Get PDFEuodia suaveolens is one of the plants that ancient people in Indonesia used due to its manifold benefits. Earlier research on this plant was mostly done on its potency as a mosquito repellent. This present study aims to determine the phytochemical and antibacterial analyses of the essential oils (EOs) extracted from the leaves of E. suaveolens. The EOs of the leaves of E. suaveolens were extracted by steam distillation method and were analyzed phytochemically utilizing the GC-MS technique to determine the chemical constituents. The chemical components were tested on four pathogenic bacteria Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis utilizing the diffusion agar method. The results showed that the main compounds extracted from the EOs were delta curcumene, evodone, globulol, limonene, linalool, longipinenepoxide, menthofuran, and p-mentha-1,8-diene. The antibacterial analysis of these compounds showed potential activities to inhibit the growth of four pathogenic bacteria tested, but the inhibition zones formed were still lower compared to commercial antibiotic kanamycin. E. suaveolens EOs exhibited diameter of zone of inhibition as follows 2.03 plus minus 0.22, 0.50 plus minus 0.49, 1.38 plus minus 0.10, 1.40 plus minus 0.27 cm to E. coli, P. aeruginosa, S. aureus, and S. epidermidis while kanamycin showed 3.43 plus minus 0.08, 3.25 plus minus 0.08, 3.38 plus minus 0.12, and 3.18 plus minus 0.24 cm respectively. These results recommend that the main compounds extracted from the EOs of the leaves of E. suaveolens be explored further to determine their potencies as new antibiotic medications.
Optimization of self-nano emulsifying drug delivery system of rifampicin for nebulization using cinnamon oil as oil phase
Get PDFLung delivery can overcome the problems related to the effectiveness of tuberculosis treatment by increasing the drug concentration at the target site. Rifampicin as the first-line antibiotic for tuberculosis has low water solubility and is unstable in gastric which hinders its effectiveness. Self-nanoemulsifying drug delivery system (SNEDDS) is a strategy known to improve the solubility and stability of such drugs. This study aimed to obtain the optimum formula of rifampicin SNEDDS intended for lung nebulization using essential oil as an oil phase. Several essential oils are known to have effective antibacterial on Mycobacterium tuberculosis. However, a high capability to solubilize the drug is required for SNEDDS formulation. Cinnamon oil, tween 80, and transcutol P were chosen as SNEDDS components for optimization using a D-optimal mixture based on the physicochemical characteristics. The optimum formula comprised 12.65% cinnamon oil, 75.00% tween 80, and 12.35% transcutol P which dispersed easily to form a highly transparent emulsion in normal saline under 1 minute. Upon dilution with saline, the optimal SNEDDS can produce a homogenous nanometer droplet (169.2±19.771 nm, PDI of 0.258±0.070) with acceptable pH for lung administration. It also has a viscosity similar to water (0.94±0.01 cP) which allows it to be nebulized easily (aerosol output rate of 0.14±0.02 g/min). Although the diluted SNEDDS has a zeta potential of -2.533±0.268 mV, it was stable for up to 4 hours during the nebulization. These results indicate the potential of cinnamon oil-based rifampicin SNEDDS to be an alternative in the pulmonary delivery of rifampicin via nebulization
Ethanol-based solvent system for recovery antioxidant activity Centella asiatica L. Urban and its application in sleep-deprived Rats
Get PDFAntioxidants have the ability to eliminate free radicals by donating electrons to oxidants. Preclinical and clinical studies show that Centella asiatica L. Urban has antioxidant activity. Ethanol was the best solvent for extracted antioxidant compounds from Centella asiatica L. Urban. The concentration of ethanol solvents effect to the compounds extracted and its antioxidant activities. The objective of study to determine ethanol based solvent systems for best recovery of antioxidant activities and in vivo antioxidant activity of the most active extract using stress induced sleep-deprived rats with glutathione (GSH) concentration parameters. Ethanol based solvent system show different recovery antioxidant activity of Centella asiatica L. Urban. Ethanol 70% had the highest recovery of antioxidant activity with an IC50 value of 76.76 ppm. Ethanol 70% Centella asiatica L. Urban extract given in sleep-deprived rats at 300 mg/kg were not significantly different in glutathione levels from those group rats that received the positive control solution (ascorbic acid). The 70% ethanol extract of C. asiatica L. Urban has the potential to ameliorate the stress induced by sleep deprivation
Enzymatic virgin coconut oil effect on urea and creatinine levels of hypercholesterolemia-diabetics induced Wistar male rats
Get PDFCoconut (Cocos nucifera) is an Indonesian commodity that has high economic value tall. Virgin Coconut Oil (VCO) is one of the processed coconut products whose selling value is very high, because The composition of VCO consists of medium-chain fatty acids that can maintain a healthy body and prevent various diseases. The process of making VCO used in This research is an enzymatic method using pineapple weevil as a bromelain enzyme. This study aims to determine the effect of enzymatic administration of VCO and an enzymatic dose of VCO which is effective in reducing urea and creatinine levels in hypercholesterolemic-diabetic male white rats (Rattus norvegicus). This study was an experimental laboratory with a modified pretest and posttest randomized controlled group design using 30 test animals which were divided into 6 treatment groups. Each group consisted of 5 test animals, namely normal control, negative control, and positive control, with doses of 0.2, 0.4, and 0.8 mL/kg BW. The data obtained were analyzed using a One Way Anova and non- parametric statistical test by Kruskal Wallis. test and followed by a further Mann Whitney test to determine differences between treatments. The results showed that enzymatic VCO at a dose of 0.8 mL/kg BW was an effective dose in reducing urea and creatinine levels with an average decrease of 17.40 mg/dL and 0.36 mg/dL. The novelty in this study showed that the enzymatic VCO had an effect on reducing urea and creatinine levels in diabetic hypercholesterolemic male white rats
In silico study of Sambiloto (Andrographis paniculata) compounds from GC-MS and LC-MS/MS as alpha-glucosidase and DPP-4 enzyme inhibitor
Get PDFDiabetes mellitus is a group of metabolic diseases characterized by hyperglycemia, impaired insulin secretion, and insulin action. To overcome this disease, some people treat it with natural ingredients. Sambiloto (Andrographis paniculata) is reported to have a wide range of pharmacological activities, one of which is anti-diabetic. Sambiloto showed activity in lowering blood glucose which has the potential as an antidiabetic. Computational methods, such as molecular docking, can increase the effectiveness and reduce the cost of searching for new active compounds. The purpose of this study was to determine the component compounds contained in the ethanol extract of Sambiloto and obtain the potential compounds to inhibit the alpha-glucosidase and DPP-4 enzymes as anti-diabetics with molecular docking method. Sambiloto leaves were macerated for 3 x 24 hours using ethanol 96% as a solvent and concentrated with an evaporator. Sambiloto extract was analyzed using LC-MS, and GC-MS. In-silico analysis includes geometry optimization and molecular docking methods. Preparation of the test ligands was carried out by the ChemBioDraw Ultra and ChemBio3D applications, then optimization by Gaussian 09 application. The crystal structures of the target proteins used were those with PDB ID 5NN8 for alpha-glucosidase and 2QOE for DPP-4. Molecular docking was performed using Autodock 4.2.3 application. From analysis with LC- MS/MS and GC-MS methods, 18 compounds were identified. Molecular docking was performed on the identified compounds. The results of molecular docking showed that the compound S17 (11-(P- Bromoanilino)-5H-Dibenzo [B,E] [1,4] Diazepine), S1 (andrographolide) and S2 (andrographanin) have the potential to inhibit the activity of alpha-glucosidase enzyme; on the other hand S17 (11-(P-Bromoanilino)-5H-Dibenzo [B,E][1,4]Diazepine) and S5 (andrographolactone) have the potential to inhibit the activity of DPP-4 enzyme. These compounds have the potential to inhibit alpha- glucosidase and DPP-4 enzymes which act as antidiabetics
In-vivo study of oleic acid and tween-80 on patch transdermal A.paniculata as anti-diabetic
Get PDFSambiloto (Andrographis paniculata) has been known empirically as a plant that has benefits as a traditional antidiabetic Javanese medicine to treat diabetes mellitus (DM). The main compound contained in sambiloto is andrographolide which has a hypoglycemia effect. Andrographolide has low solubility in water and poor bioavailability due to biotransformation by P-glycoprotein in the intestinal tract which causes andrographolide to metabolize more quickly in the duodenum and jejunum. To overcome this extract ethanol of sambiloto (EES) formulated to patch transdermal. Enhancers can affect the characteristics of transdermal patch preparations which affect the pharmacological activity of transdermal patch preparations. The critical point of transdermal patch preparation is the selection of enhancers which is one of the compounds to increase the penetration of active substances in the skin by disrupting the permeability of the stratum corneum. The aim of this research is to determine the effect of variations in the combination of oleic acid and tween 80 as an enhancer on the physical characteristics of EES patches.The methods of extraction sambiloto use soxhetation with ethanol 96% as solvent. The formulation of EES patch transdermal using solvent casting technique with various concentration enhancer tween-80 and oleic acid. This research was conducted by making 3 formulas, where F1 (1:1), F2 (1:3) and F3 (1:3). The evaluations include weight uniformity, thickness, water content, pH and folding endurance of the patch. The result of visual appearance the patch EES has a dark green with aroma specific of EES. The characteristics of EES transdermal patches were affected by the ratio of tween-80 and oleic acid as the enhancers. The combination of oleic acid and tween 80 as a permeation enhancer has an influence on physical characteristics (weight and thickness) of EES patches
The effect of HPMC-K15M and guar gum as polymer-coated for sustained-released tablet: disintegration and release kinetics
Get PDFPolymeric coating films are able to control tablet drug release rate depending on polymer physicochemical properties. Guar gum and HPMC-K15M (GG/HPMC-K15M) can be a coating polymer in sustained-release tablets. This study aims to characterize the disintegration and drug release kinetics on theophylline sustained-release tablets coated with GG/HPMC-K15M. The film coating was made with variations of the GG/HPMC-K15M ratio of 1:3 (F1), 1:4 (F2), and 1:5 (F3). Granules were preformulated regarding LOD, granule size distribution, packing, and flow properties. Film coating was carried out using a liquid spraying method. Coated tablets were tested for quality examination, and the drug release kinetics model was determined based on in-vitro dissolution. Granule pre-formulation result shows that the granules have excellent packing and flow properties with an LOD of 4.59–5.33% and a size of 553.28–627.28 πm. Tablets provided uniform size characteristics with a weight variation of 333.38–339.56 mg (CV 1.32–3.43% and acceptance value 6.53–13.58), hardness of 11.61–18.86 kgf, friability of 0.103–0.186%, disintegration time of 20.69–27.36 min, and drug content of 98.51–98.55%. The theophylline was dissolved by 95.24% (6h in FI), 97.04% (7h in F2), and 99.79% (8h in F3); all formulas followed zero-order kinetic (r2 ~ 1). Suitable quality theophylline tablets GG/HPMC-K15M coating have been successfully produced. Increasing the concentration ratio of HPMC-K15M in the coating solution resulted in a significant increase in disintegration time and a slowing of the drug release rate. The drug release kinetics of all formulations followed the zero-order kinetic model
Acute toxicity of the intranasal administration of Anredera cordifolia extract in Wistar Rats
Get PDFAnredera cordifolia (AC) known as binahong plant in Indonesia is commonly used for traditional medicine since ancients. AC contains of secondary metabolites such as flavonoids that have anti-oxidative, anti-inflammatory, anti-mutagenic and anti-carcinogenic properties. Many flavonoids compound that has anti-inflammatory activity were potential for treatment of nasal inflammatory such as allergic rhinitis. This study aims to evaluate the preclinical safety of acute intranasal administration of AC extract in laboratory wistar rats. Acute toxicity using the intranasal route of administration of AC extract was evaluated on 30 female wistar rats, divided five rats for control, and each five of doses 5%, 10%, 25%, 50% and 75%. Observation during 14 days for the incidence of mortality and signs of toxicity. The AC extract intranasal administration doses at 5%, 10%, 25%, 50% and 75% did not show mortality or treatment related adverse events and did not showed significantly changes on blood profile. The AC extract was found safe until 75% for nasal administration in wistar rats.