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The effect of spray-drying temperature on Centella asiatica extract-β cyclodextrin-maltodextrin nanoparticle characteristics and stability
Get PDFCentella asiatica extract has low solubility in water. Material modification needs to be conducted to increase the dissolution rate of Centella asiatica extract. The particle size reduction to nano-size was carried out to increase surface contact with aqueous media. High surface contact was expected to increase the solubility and absorption rate. Nanoparticles were prepared with 34% maltodextrin and 6% β-cyclodextrin as a stabilizer and dried by a spray-drying method. High temperature in the spray drying process can affect the physical and chemical characteristics of the nanoparticles, so the inlet temperature in this study was observed as parameter variations, on 140oC, 150oC, and 160oC. The formed nanoparticles then being tested on several parameters, including physical appearance, moisture content, particle size, shape, and morphology. The chemical stability of the active ingredients during the drying process was assessed from the pH value changes and the content of quercetin as an antioxidant post drying process, compared to the initial content. The test results show that the nanoparticles have been formed. The inlet temperature of 160oC produced the most physically optimum spherical nanoparticles, with a particle size of 191.533 ± 18.791 nm and relatively homogeneous with a polydispersity index (PDI) value of 0.113 ± 0.057. However, temperatures that are too high indicate poor chemical stability. The poor chemical stability can be seen from the quercetin content that decreased significantly after the drying process, until the remaining 53.87 ± 0.55% and 49.52 ± 0.97% for temperatures of 140oC and 160oC, respectively. These results indicate that the combination of β-cyclodextrin and maltodextrin can not encapsulate and maintain the stability of the active ingredients during the spray drying process. A significant reduction of inlet temperature is needed to get dry nanoparticles with the most optimum physical mixture and chemical stability
Homology modeling and mutation prediction of ACE2 from COVID-19
Get PDFSARS-CoV-2 has become a pandemic in the world. The virus binds to the Angiotensin-Converting Enzyme 2 (ACE2) receptor, which is found in epithelial cells such as in the lungs, to generate the pathology of COVID-19. It is essential to analyze the characteristics of ACE2 in understanding the development of the disease and study potential new drugs. The analysis was carried out using computer simulations to speed up protein analysis that utilized Artificial Intelligence technology, databases, and big data. Homology modeling is a method to exhibit homologous of protein families, hence the model and arrangement of protein sequences modeled are established. This research aims to determine the possibility of mutations in ACE2 by performing the mutation prediction. The result shows reliable homologous modeling with the score of GA341, MPQS, Z-DOPE, and TSVMod NO35 were 1; 1.28252; -0.47; and 0.793, respectively. Moreover, Gene Ontology (GO) analysis describes that ACE2 has a molecular transport function in cells while there are no mutations found occurred in ACE2 analyzed using SIFT and PROVEAN
Accelerated stability test of snakehead fish and kelulut honey ointment with CMC-Na as a binder
Get PDFThe extract of snakehead fish (Channa striata) and kelulut honey (Heterotrigona itama) ointment was proven to have activity in wound healing. However, previous studies showed instability in the ointment as indicated by the occurrence of phase separation. This study used CMC-Na (Carboxymethyl Cellulose Sodium) with a concentration of 3% (F1), 4.5% (F2), and 6% (F3) as a binder. The stabilizer was added to increase the stability of the ointment preparation by binding to the aqueous phase and preventing it from leaving the ointment base. The test was carried out with the accelerated stability method at a temperature of 40° ± 2° C and a humidity of 75% ± 5% for 28 days. The evaluation includes organoleptic tests, homogeneity, spreadability, adhesion, and protection power. The results showed that CMC-Na increased the stability of the ointment. The data obtained show that the higher the CMC-Na concentration used, the higher the consistency and adhesion were, but the lower the spreadability of the preparation. The results of the average spreadability and adhesion power for formulation 1 were 5.09 cm and 1797.33 seconds, formulation 2 were 4.42 cm and 1798.33 seconds, and formulation 3 were 3.69 cm and 1799 seconds. The results of the One-Way ANOVA showed that all formulations experienced a significant decrease in adhesion and increase in spreadability during 28 days of storage. The best ointment that meets the physical stability criteria is shown by the CMC-Na 3% (F1) formulation, with a soft texture, homogeneous, a good spreadability (5-7 cm), a good adhesion (more than 4 seconds), and a good protective power for 28 days of testing
Synthesis and virtual screening of bis-(4-(tert-butyl)-N-(methylcarbamothioyl) benzamide)-Iron (III) complex as an anticancer candidate
Get PDFThiourea derivatives were much used in drug discovery and drug-making, such as for an anticancer. The formation of drug complexes can increase lipophilicity through chelation formation, and the drug action is significantly upward due to the effective permeability to the center. In another study, the alteration of the compound becomes the complex with metal will grow in its activity so recently we have synthesized the Bis-(4-(Tert-Butyl)-N-(Methylcarbamothioyl) Benzamide)-Iron (III) complex. The synthesis of Fe (III) metal with the 4-(Tert-Butyl)-N-(Methylcarbamothioyl) Benzamide in ethanol by reflux at 75oC for 7 hours. Hot Stage Microscopy, UV-Visible Spectrophotometry Infrared Spectrophotometry, and Massa Spectrophotometry were used to characterize the complex. This study concerns representing, inferring, and predicting pharmacokinetics and toxicity and molecular docking complexes. The complex weight was 0.29469 g. Its purity has been tested using the melting point determination and has obtained its range was 113o-115oC. The Characteristics of Bis-(4-(Tert-Butyl)-N-(Methylcarbamothioyl) Benzamide)-Iron(III) complex have a maximum wavelength of 260,0 nm and provide absorption of Fe-O vibrations at wavenumbers 478,2 cm-1and 588 cm-1, and the m/z complex of spectrophotometry mass was 559,31. The molecular docking process was performed using AutodockTools-1.5.6 software. It showed that Bis-(4-(Tert-Butyl)-N-(Methylcarbamo-thioyl)Benzamide)-Iron(III) complex could interact with ribonucleotide reductase enzyme, and it has better interaction than the 4-(Tert-Butyl)-N-(Methylcarbamothioyl)Benzamide with the binding affinity energy (ΔG)of  -8,52 kcal/mole and the constant inhibition (Ki ) of 568,55 nM
CYP2A6*4 allele gene high frequency associated with low-density lipoprotein cholesterol (LDL-C) among Javanese Indonesian smokers
Get PDFThe CYP2A6 gene, which codes the CYP2A6 enzyme, has known to have ahigh polymorphism. This polymorphism could decrease, increase, or eliminate the CYP2A6 enzyme activity. CYP2A6*4, an inactive allele, decreased the CYP2A6 enzyme activity. One of the CYP2A6 enzyme-specific substrates is nicotine. This inactive allele could decrease nicotine metabolism that causes high nicotine levels in the blood. In addition, it caused the increasing levels of Low-Density Lipoprotein Cholesterol (LDL-C) by expanding the lipolysis process. The purpose of this research was to evaluate the effect of the CYP2A6*4 allele gene on LDL-C levels. Respondents in this study were 31 male Javanese smokers. This research is an analytic observational study with a cross-sectional design. Polymerase chain reaction (PCR) methods use to identification the CYP2A6*4 allele gene. This study shows that a high-frequency CYP2A6*4 alleles gene among the subject was detected, with an allele frequency is 93.55%. Furthermore, this CYP2A6*4 allele gene did not impact LDL-C levels, with the Odd Ratio value was 1.636 (P-Value = 0.737). In conclusion, the CYP2A6*4 allele gene does not significantly affect the LDL-C levels in Javanese Indonesian smokers
Development of black cumin seed oil (Nigella sativa L.) SNEDDS into solid-SNEDDS and its characterization
Get PDFBlack cumin seed oil (MBJH) (Nigella sativa L.) is a well-known herb with pharmacology activities such as anticancer and anti-thrombocytopenia. The limitation of MBJH has poor absorption when using oral dosage form. The liquid SNEDDS (Self-nanoemulsifying drug delivery system) of MBJH as an alternative formulation. However, the disadvantage of liquid-SNEDDS of MJBH was the interaction between the active ingredients with soft gelatin capsules. Hence, this study proposed to develop solid-SNEDDS as a new formulation of MBJH. Solid-SNEDDS of MBJH was prepared from liquid-SEDDS of MBJH by adsorption to solid carrier method, consisting of aerosil and crospovidone as the adsorbent. The characterization of S-SNEDDS was determined by emulsification time and percent transmittance. Micromeritics properties of S-SNEDDS such as the angle of repose, bulk and tap density parameter, compressibility index, and Hausner ratio were measured  before and after stored in stress condition (40 ̊ C ± 2 ̊ C and relative humidity of 75% ± 5% for 14 days). The result showed S-SNEDDS of MBJH with aerosil absorbent had better S-SNEDDS performance in both characteristics and micromeritics properties under stress conditions than crospovidone absorbent. In conclusion, the s-SNEDDS of black cumin oil by solid aerosil carrier method is promising for future research development of S-SNEDDS dosage form
The protective effect of Phyllanthus emblica Linn. extract against doxorubicin-induced hepatotoxicity in rats
Get PDFRecently many researches have been carried out on Malacca fruit extract and its potential protective effect on in vivo organ toxicity. However, there is still no research on the protective effect of Malacca (Phyllanthus emblica L.) fruit extract on induced hepatotoxicity of anticancer drugs, especially doxorubicin in rats. The objective of this study is to determine the potential protective effect of ethanol extract of Malacca fruit (P. emblica L.) against doxorubicin-induced hepatotoxicity in rats. A preliminary phytochemical test was done followed by administration extract into doxorubicin-induced rats. Histological studies were carried out to observe the effect of the extract on liver tissue. Phytochemical test results show that the ethanol extract of Malacca fruit contains flavonoids, phenols, tannins, triterpenoids, terpenoids, and alkaloids. The increasing value of ALT and ALP of doxorubicin-induced liver tissue proved the toxicity in liver tissue caused by doxorubicin. The ethanol extract of P. emblica L. at dosage 200 mg/kg BW and dosage 400 mg/kg BW on doxorubicin-induced rats were successfully played as an antioxidant to decrease the ALT and ALPvalues and improve liver tissue doxorubicin-induced by normal hepatocytes more dominant than lysis and less mark of bleeding and congestion of blood vessels
Topical anti-inflammatory effect of Ekor Naga (Rhaphidophora pinnata (L.f) Schott) leaves extract
Get PDFEkor Naga (Rhaphidophora pinnata (L.f) Schott) leaves are leaves that contain secondary metabolites which can be developed into medicine. Ekor Naga leaves have secondary metabolite compounds of flavonoids, alkaloids, triterpenoid saponins, steroids, tannins, and phenols. This metabolite compound is the basis for testing the anti-inflammatory effect of Ekor Naga leaves extract using topical methods. The purpose of this study was to determine the anti-inflammatory effect of the ethanol extract of Ekor Naga leaves by a topical method. This study used five treatment groups with five mice in each treatment. This research tested the anti-inflammatory activity of Ekor Naga leaves extract by using the combination of 2 methods; namely the method of forming airbags and the formation of artificial edema using the induction of 2% carrageenan solution with the observation parameters being the measurement of exudate volume and differentiation of the number of leukocyte cells observed under a microscope. The results showed that the Ekor Naga leaves extract had an anti-inflammatory effect. The best inflammatory effect is a concentration of 10%, followed by a concentration of 5% and 2.5%
Gastroprotective effect of Canna edulis Ker. ethanolic extract in piroxicam-induced rats
Get PDFMedications derived from plants and pure natural ingredients have far lower side effects and risks than synthetic drugs. One side effect of piroxicam is irritation of the digestive tract. One of the therapeutic preventions to minimize peptic ulcers was utilizing Canna edulis Ker. This study aims to prove that ethanolic extract of Canna edulis Ker. can be used as an alternative to prevent piroxicam-induced peptic ulcers based on ulcer index parameters and the protection ratio. The rats were divided randomly into 6 groups consisting of 5 rats. The normal group was given food and water. The negative control group was given 0.5% CMC-Na. The extract groups were given various doses of ethanolic extract of Canna edulis Ker. (50, 100, and 200 mg/kg BW). The positive control was given sucralfate at 360 mg/kg BW dose. Rats were treated orally for 14 days. One hour after the treatment on the 14th day, all groups except group I were orally administered with piroxicam dissolved in 0.5% CMC-Na at 1.8 mg/kg BW dose. Twenty-four hours later, animals were sacrificed, dissected, and their stomach organs were removed to analyze its number of ulcers. Ulcer observation was formed by giving a score and protection ratio. The mean ulcer index value was 0.33±0.58 for 50 mg/kg BW and 100 mg/kg BW ethanol extract treatment groups, while the 200 mg/kg BW group showed 0.67±0.58. The protection ratio was 83.33±28.87 in 50 mg/kg BW and 100 mg/kg BW treatment groups, while  66.67±28.87 was shown in the 200mg/kg BW group. Canna edulis Ker. ethanolic extract has the gastroprotective ability by decreasing the index of gastric ulcers and increasing the protection ratio to the stomach of piroxicam-induced rats
Composition of carbopol 940 and HPMC affects antibacterial activity of beluntas (Pluchea indica (L.)) leaves extract gel
Get PDFIndonesia is a country known for its source of biological wealth, one of which is beluntas leaves. Beluntas leaves have the potential to be an antibacterial, so it is appropriate to be formulated in the form of medicinal preparations, especially gels. This study aims to find out the influence of variations between carbopol gel base 940 and Methylcellulose Hydroxypropyl (HPMC) on the physical properties of gel preparations beluntas leaf extract (Pluchea indica (L.), and know the influence of gel of extract of beluntas leaves on antibacterial activity. The extract is obtained by the maceration method using ethanol solvent 96%. Each formula uses 15% of the extract of beluntas leaves. Gels are made in four gel base variations namely F0 (0.5% carbopol, 1% HPMC), FI (1% carbopol, 1.5% HPMC), FII (1.5% carbopol, 2.5% HPMC), and FIII (2% carbopol, 3% HPMC). Gels evaluated for their physical properties include organoleptic, viscosity, pH, homogeneity, scattering power, adhesion and Freeze-thaw cycling. Then the gel tested antibacterial activity against bacteria Staphylococcus aureus and Pseudomonas aeruginosa by cup-plate diffusion method. The data obtained were analyzed with One Way Anova and LSD with a 95% confidence level. The results showed that beluntas leaf extract gel meets the organoleptic requirements, homogeneity, good gel adhesion (> 4sec), good gel viscosity (2000-50.000 cps), and good gel pH (4.5-6.5). However, the gel does not meet the requirements of good scattering power (5-7 cm) and Freeze-thaw cycling. Based on the test results that have been done with some of the parameters above, The best composition of carbopol 940 and HPMC in the beluntas leaf extract gel which has antibacterial activity against Staphylococcus aureus and Pseudomonas aeruginosa  is 1% carbopol and 1.5% HPMC. The antibacterial activity of the formula is categorized as strong