Showing papers by "Heni Rachmawati published in 2013"

Molecular Inclusion Complex of Curcumin–β-Cyclodextrin Nanoparticle to Enhance Curcumin Skin Permeability from Hydrophilic Matrix Gel

Abstract: Curcumin (CUR) has various pharmacological effects, but its extensive first-pass metabolism and short elimination half-life limit its bioavailability. Therefore, transdermal application has become a potential alternative to delivery CUR. To increase CUR solubility for the development of a transparent homogenous gel and also enhance the permeation rate of CUR into the skin, β-cyclodextrin–curcumin nanoparticle complex (BCD–CUR-N) was developed. CUR encapsulation efficiency was increased by raising the percentage of CUR to BCD up to 20%. The mean particle size of the best CUR loading formula was 156 nm. All evaluation data using infrared spectroscopy, Raman spectroscopy, powder X-ray diffractometry, differential thermal analysis and scanning electron microscopy confirmed the successful formation of the inclusion complex. BCD–CUR-N increased the CUR dissolution rate of 10-fold (p < 0.01). In addition, the improvement of CUR permeability acrossed skin model tissue was observed in gel containing the BCD–CUR-N and was about 1.8-fold when compared with the free CUR gel (p < 0.01). Overall, CUR in the form of the BCD–CUR-N improved the solubility further on the penetration of CUR.

Curcumin nanoforms promise better therapeutic values

Abstract: There are many reports proved great potential effects of curcumin in various diseases. Curcumin exhibits antioxidant, anti inflammation, antimicrobial and anticarcinogenic activities. It’s unique ability to work through so many different pathways has a positive influence in combating almost every known disease. However, lack of its stability and solubility limits its therapeutic applications in clinic. Several approaches have been described not only in chemical modifications but also in formulation technologies to expose the therapeutic values of curcumin. This review presented an updated concise review of currently available technologies to improve the physicochemical characteristic of curcumin as well as its stability, hence showing better therapeutic effects, using different types of nanoform: nanocrystal and nanocarriers.

Labeling of the Recombinant Streptokinase Using Iodine-131 as a New Thrombolytic Agent

Abstract: Stroke and acute myocardial infarction is a disease with the highest mortality in the world. WHO has estimated in 2008, 30% of deaths from heart disease and more than 80% of this cases have been occurred in developing countries. Streptokinase (SK) as an effective thrombolytic agent has been used as a drug of choice for about forty years ago. SK is plasminogen (PG) activator that converts plasminogen to active protease, called plasmin (PN) which degrades fibrin to soluble products. Recombinant streptokinase (SKA) from genetic engineering has been developed at School of Pharmacy ITB to reduce or eliminate immunogenicity of SK. However, scientific disclosures relating to dynamic and its kinetic studies in the body have still to be proven. One method that can explain this phenomenon is the pharmacological studies using radionuclide labeled compounds. Radioiodine labeled compound is used extensively and most suitable for biological studies. This paper describes the preparation of 131 I-SKA and its characterization. The labeling conditions of SKA, such as chloramine-T as an oxidizing agent, amount of SKA, incubation time, and size of resin to purify the labeling yield have been observed. The result showed that the optimum condition of labeling (35.11%) was obtained using 10 µg of chloramine-T and 60 seconds of incubation time. The highest radiochemical purity (97.46 ± 1.14%) has also been obtained by passing through the resin chromatography column using 100 mg Dowex 1x8, size 50-100 mesh. The characterization of 131 I-SKA with SDS PAGE method and autoradiography showed the similar performance with unlabeled-SKA. Received: 04 December 2012; Revised: 20 December 2012; Accepted: 21 December 2012

HEPATOPROTECTIVE ACTIVITY OF SAPONIN FRACTION OF OYONG SEED FLESH AND ITS COMBINATION AGAINST CCl4-INDUCED CHRONIC LIVER DAMAGE IN MALE WISTAR RAT

Abstract: Saponin fraction of seed flesh of Oyong (Luffaacutangula [L.]Roxb) has been investigated to have a hepatoprotective activity in rats with fibrotic chronic liver damage. This research was conducted to evaluate whether saponin fraction of Oyongseed flesh has a hepatoprotective activity in CCl4-induced acute liver damage. Hepatoprotective activity was determined by measuring the activity of liver enzymes (SGOT, SGPT, LDH), total nitrite/nitrate level, liver index and liver histology. Saponin fraction of Oyong flesh seeds 10mg/kg BW and meniran extract 400mg/kg BW alone showed hepatoprotective activity. Administration of saponin fraction 10mg/kb BB decreased SGPT and LDH significantly over untreated group. Group given meniran extract at dose of 200mg/kg BW showed decreased on LDH, while at dose of 400mg/kg BW decreased SGPT, SGOT, and LDH significantly. Hystological observation revealed any improvement in liver morphology especially after treated with saponin fraction 10mg/kg BWand meniran extract at dose of 400mg/kg BW. However, all groups treated with combination of saponin and meniran did not show improvement both at biochemical parameter and liver histology. In conclusion, saponin extract with dose of 10mg/kg BW and meniran extract at dose of 400mg/kg BW showed hepatoprotector activity. In contrast, combination of both did not show any hepatoprotective effect and it was suspected that they have antagonist effects. Key words:hepatoprotective, CCl4-induced liver fibrosis, Luffaacutangula, Phyllanthusniruri

Pharmaceutical Nanotechnology Development of Curcumin Nanocrystal: Physical Aspects

Abstract: Curcumin, a naturally occuring polyphenolic phytoconstituent, is isolated from the rhizomes of Curcuma longa Linn (Zingiberaceae) It is water insoluble under acidic or neutral conditions but dissolves in alkaline environment In neutral or alkaline conditions, curcumin is highly unstable undergoing rapid hydrolytic degradation to feruloyl methane and ferulic acid Thus, the use of curcumin is limited by its poor aqueous solubility in acidic or neutral conditions and instability in alkaline pH In the present study, curcumin nanocrystals were prepared using high-pressure homogenization, to improve its solubility Five different stabilizers (polyvinyl alcohol (PVA), polyvinyl pyrrolidone (PVP), D-"-tocopherol polyethylene glycol 1000 succinate (TPGS), sodium dodecyl sulfate (SDS), carboxymethylcellulose sodium salt) possessing different stabilization mechanism were investigated The nanoparticles were characterized with regard to size, surface charge, shape and morphology, thermal property, and crystallinity A short-term stability study was performed storing the differently stabilized nanoparticles at 4 ◦ C and room temperature PVA, PVP, TPGS, and SDS successfully produced curcumin nanoparticle with the particle size in the range of 500-700 nm PVA, PVP, and TPGS showed similar performance in preserving the curcumin nanosuspension stability However, PVP is the most efficient polymer to stabilize curcumin nanoparticle This study illustrates that the developed curcumin nanoparticle held great potential as a possible approach to improve the curcumin solubility then enhancing bioavailability © 2012 Wiley Periodicals, Inc and the American Pharmacists Association J Pharm Sci 102:204-214, 2013

Study the potency of colonic pellet containing ibuprofen on the suppression of gastro duodenal ulceration in male Wistar rats

Abstract: In the previous study, the colonic release of ibuprofen pellet has been developed by using the microbial dependent release system which was successfully obtained by using the dual coatings. Pharmacokinetic study of this pellet had been done in New Zealand albino rabbit and showed delay absorption, but better bioavailability compared to conventional oral preparation. Therefore, the aim of this study is to explore the potential benefit of this formulation in minimizing the main side effect of ibuprofen: gastric duodenal ulcer. To study the suppression effect on ulcer in vivo, male Wistar rats were used and divided into 4 groups: negative control, group given ibuprofen suspension, group given uncoated ibuprofen pellet and group with coated ibuprofen pellet. All treated groups were administered orally twice a day for 14 days. Then, parameters including platelet counts and observation on gastroduodenal ulcer development both visual and histological analyses were performed. Groups receiving both suspension and uncoated pellet of ibuprofen showed ulcer development, meanwhile this condition did not occur in rats treated with coated pellet. Colonic release of ibuprofen seems to be promising in the suppression of ulceration. The efficacy of anti-inflammatory activity of the formula is now under progress.

Evaluation of adverse effects of mutein forms of recombinant human interferon alpha-2b in female swiss webster mice.

Abstract: Purpose. We successfully developed recombinant human interferon alpha-2b (rhIFN-α2b) and mutein forms through the site-directed mutagenesis technique. The mutein forms were developed by substituting cysteins at positions 2 and 99 with aspartic acids. The potential adverse effects of these rhIFN-α2bs were assessed by acute and subchronic studies. Methods. In the acute study, rhIFN-α2bs were subcutaneously administered to mice at a single dose of 97.5 μg/kg, 975 μg/kg, and 9.75 mg/kg BW and were observed for 14 days. In the subchronic study, single dose of 1.95 μg/kg and 19.5 μg/kg, respectively, was given subcutaneously every 3 days for 45 days. Results. No death as well as abnormality in body weight, behavior, presentation of main organs, and value of plasma SGPT and SGOT was observed. Wild type and mutein rhIFN-α2bs did not show significant adverse effects at dose up to 9.75 mg/kg BW. Administration of these rhIFN-α2bs given repeatedly did not induce any adverse effect. Conclusion. These results suggest that our rhIFN-α2bs are safe. However, further study is still needed to clarify the safety issue before use in clinical trial.