Showing papers by "Heni Rachmawati published in 2015"

Curcumin nanoemulsion for transdermal application: formulation and evaluation.

Abstract: The aim of this work is to develop a curcumin nanoemulsion for transdermal delivery. The incorporation of curcumin inside a nanoglobul should improve curcumin stability and permeability. A nanoemulsion was prepared by the self-nanoemulsification method, using an oil phase of glyceryl monooleate, Cremophor RH40 and polyethylene glycol 400. Evaluation of the nanoemulsion included analysis of particle size, polydispersity index, zeta potential, physical stability, Raman spectrum and morphology. In addition, the physical performance of the nanoemulsion in Viscolam AT 100P gel was studied. A modified vertical diffusion cell and shed snake skin of Python reticulatus were used to study the in vitro permeation of curcumin. A spontaneously formed stable nanoemulsion has a loading capacity of 350 mg curcumin/10 g of oil phase. The mean droplet diameter, polydispersity index and zeta potential of optimized nanoemulsion were 85.0 ± 1.5 nm, 0.18 ± 0.0 and −5.9 ± 0.3 mV, respectively. Curcumin in a nanoemulsion...

The Influence of Formula and Process on Physical Properties and the Release Profile of PVA/BSA Nanofibers Formed by Electrospinning Technique

Abstract: Electrospinning is a simple versatile process to produce nanofibers. However, it requires careful approach to form appropriates fibers for different purposes. This report describes aspects influencing successful development of nanofiber containing BSA using electrospinning method. Optical and scanning electron microscopy, energy dispersive X-Ray and Fourier transformed infrared spectroscopy, differential scanning calorimetric, and X-Ray diffraction analysis of nanofiber were performed. Modification of PVA/BSA nanofiber with Eudragit L-100 was conducted by dip coating method. The presence of BSA increased the diameter of the fibers. Modification of PVA/BSA nanofiber with Eudragit L-100 delayed the release of BSA in acidic medium but promoting its release in intestinal mimicking medium.

Phytosome Containing Silymarin for Oral Administration: Formulation and Physical Evaluation

Abstract: Silymarin is a unique flavonoid complex isolated from milk thistle (Silybum marianum). It has been widely used as a hepatoprotective agent. Orally administered silymarin can be absorbed rapidly but only 20-50% of silymarin will be absorbed through gastrointestinal tract, resulting in low bioavailability. Those limitations are due to its low solubility, either in water and oil, and its low intestinal permeability. This study was aimed to develop silymarin-containing phytosome in order to improve the bioavailability of silymarin with sufficient safety and stability. This system consisted of silymarin-phospholipid complex prepared by solvent evaporation method, which was incorporated to form phytosome vesicles using thin layer method with various concentrations and molar ratios of silymarin and phospholipid. The vesicle size of phytosome was reduced with sonication. The results demonstrated that formula with 2% silymarin-phospholipid complex and molar ratio of silymarin to phospholipid of 1:5 showed the best phytosomal characteristics, with mean vesicle diameter of 133.534 ± 8.76 nm, polidispersity index of 0.339 ± 0.078, entrapment efficiency of 97.169 ± 2.412 %, and loading capacity of 12.18 ± 0.30 %. The preparation remained stable after freeze-thaw stability test. Analysis of Infrared spectroscopy and Differential Scanning Calorimetry confirmed the presence of physical and chemical interactions between silymarin and phospholipid within complex formation. Well formed and discrete vesicles were revealed by Transmission Electron Microscopy analysis, drug content measurement, and freeze-thaw stability test.

The Influence of Non-Ionic Surfactant on the Physical Characteristics of Curcumin-Loaded Nanofiber Manufactured by Electrospinning Method

Abstract: Electrospinning is one of techniques used for nanofiber fabrication as drug delivery systems. Curcumin possesses challenging properties as it has low solubility and poor absorption. Incorporation of curcumin into nanofiber is expected to enhance solubility and absorption. In this study, curcumin loaded nanofiber for oral delivery has been developed. Nanofibers were synthesized from curcumin and Polyvinylpyrrolidone (PVP) with mass ratio of 1:10 using electrospinning method. Various PVP concentration from 5 to 10 % (w/v) were used. To further assess the variation in the physical characteristics of fiber, the influence of Polysorbate 20, a nonionic surfactant, was studied. Electrospinning of curcumin-PVP nanofiber with the addition of Polysorbate 20 yielded fiber with overall diameter of 350-400 nm. In the absence of Polysorbate 20, the diameter was higher i.e 540-660 nm. The highest diameter was observed in highest PVP concentration at 10% (w/v). Drug release study showed that more than 50% of curcumin has been released within 45 minutes in all formulas. Initial rapid release occurred in the formula containing Polysorbate 20. As a summary, the presence of Polysorbate 20 reduced the diameter of curcumin-loaded PVP nanofiber and enhanced the release of curcumin from the fiber.

Intraoral Film Containing Insulin-Phospholipid Microemulsion: Formulation and In Vivo Hypoglycemic Activity Study

Abstract: Non-invasive administration of insulin is expected for better diabetes mellitus therapy. In this report, we developed intraoral preparation for insulin. Insulin was encapsulated into nanocarrier using self-assembly emulsification process. To increase lipophilicity of insulin, it was dispersed in phospholipid resulted in insulin-phospholipid solid dispersion. The microemulsion formula was established from our previous work which contained glyceryl monooleate (GMO), Tween 20, and polyethylene glycol (PEG 400) in a ratio of 1:8:1. To confirm the formation of insulin-phospholipid solid dispersion, PXRD, FTIR spectroscopy, and Raman spectroscopy were performed. Then, the microemulsion was evaluated for droplet size and distribution, zeta potential, entrapment efficiency, physical stability, and Raman spectroscopy. In addition, microemulsion with expected characteristic was evaluated for in vitro release, in vitro permeation, and in vivo activity. The droplets size of ∼100 nm with narrow distribution and positive charge of +0.56 mV were formed. The insulin encapsulated in the oil droplet was accounted of >90%. Water-soluble chitosan seems to be a promising film matrix polymer which also functioned as insulin release controller. Oral administration of insulin microemulsion to healthy Swiss-Webster mice showed hypoglycemic effect indicating the success of this protein against a harsh environment of the gastrointestinal tract. This effectiveness significantly increased by fourfold as compared to free insulin. Taken together, microemulsion seems to be a promising carrier for oral delivery of insulin.

Tabletting Process of Pellets Containing Bioactive Fraction DLBS1033F Isolated from Lumbricus rubellus: Challenge and Strategy.

Abstract: DLBS1033 is a mixture of bioactive proteins fractinated from the earthworm Lumbricus rubellus which possesses antithrombotic and thrombolytic activities. DLBS1033 contains a potent fibrinolytic enzyme with excellent specificity for fibrin. A commercial oral enteric coated tablet for administration 3 times daily is available on the market from the DLBS manufacturer. This research aimed to develop a multiparticulate sustained-release DLBS1033 Forte (DLBS1033F) tablet (with more potent fibrinolytic activity than DLBS1033), which has targeted release in the small intestine and colon. The chemical and physical stability of the fibrinolytic enzyme was expected to be preserved in these bowel segments. The sustained-release system was designed to maintain the effective plasma concentration of the proteins and prolong the thrombolytic activity. This was done by incorporating the proteins in a multiparticulate solid that was subsequently compressed into the monolithic system of a sustained-release tablet. The challenge was to maintain pellet integrity after the compression process. A set of studies confirmed the preserved physical shape of the pellets. In addition, in vitro release studies of the multiparticulate tablet in reassembling media of the gastrointestinal tract indicated the successful formulation of DLBS1033F as an enteric as well as sustained-release solid dosage form.

Peningkatan stabilitas kurkumin melalui pembentukan kompleks kurkumin--siklodekstrin nanopartikel dalam bentuk gel

Abstract: Curcumin is a compound derived from turmeric. This compound is practically insoluble in water and has poor stability. To improve the benefit of curcumin as a potential active compound in a gel preparation, better stability are requested. Encapsulation was performed by freeze drying methods and all evaluation data confirmed that curcumin included in the -cyclodextrin forming curcumin-- cyclodextrin nanoparticle. The formula showed particle size of 156.8 ± 38.3 nm, polydispersity index of 0.174 ± 0.026, and zeta potential of -17.3  0.2 mV. The gelling agents used for formulation of gel base were HPMC, CMC-Na, carbopol 940, water-soluble chitosan, and viscolam. Viscolam showed best stability of pH and viscosity after storage at 25 and 40 oC for 28 days. The inclusion complex and curcumin were incorporated into gel. Both of the formulas showed good stability in pH and viscosity after storage at 25 and 40oC for 28 days, and the inclusion complex gel showed improvement in the chemical stability which is approximately 2.12-fold (p<0.01) and 1.41-fold (p<0.05), after storage at 25 and 40 oC, respectively.