The novel IR-SET can be promising as a fast-releasing SEDDS tablet of IBU for fast onset of action.

Research in this paper focuses on the kinetic evaluation of swelling of the liquid crystalline phases of glyceryl monooleate (GMO). Swelling of the lamellar and cubic liquid crystalline phases of GMO was studied using two in vitro methods, a total immersion method and a Franz cell method. The swelling of the lamellar phase and GMO having 0 %w/w initial water content was temperature dependent. The swelling ratio was greater at 20 degrees C than 37 degrees C. The water uptake increased dramatically with decreasing initial water content of the liquid crystalline phases. The swelling rates obtained using the Franz cell method with a moist nylon membrane to mimic buccal drug delivery situation were slower than the total immersion method. The swelling was studied by employing first-order and second-order swelling kinetics. The swelling of the liquid crystalline phases of GMO could be described by second-order swelling kinetics. The initial stage of the swelling (t < 4 h) followed the square root of time relationship, indicating that this model is also suitable for describing the water uptake by the liquid crystalline matrices. These results obtained from the current study demonstrate that the swelling strongly depends on temperature, the initial water content of the liquid crystalline phases and the methodology employed for measuring the swelling of GMO.

In order to enhance the dissolution profile and oral bioavailability of megestrol acetate (MA), solid dispersions of MA (MASDs) were formulated with copovidone and crystal sugar as a hydrophilic polymeric carrier and an inert core bead, respectively. Solvent evaporation method and fluidized bed coating technique were employed. MASDs were categorized as crystalline solid dispersion by the characterization of differential scanning calorimetry and X-ray diffraction. The mass-median diameters of MASDs were in a range of 1.4 to 2.6 μm. Based on drug to polymer ratio, MASD (1:1) and (1:2) were considered as optimized formulations, resulting in a smooth-surfaced homogeneously coated layer with enhanced dissolution rate. Dissolution of MASD was gradually increased up to 15 min, after which it reached a plateau. For the initial period, dissolution rates were in the decreasing order of MASD (1:2) ≥ MASD (1:1) > MASD (1:3) > MASD (1:5) > MASD (1:0.5) > MA powder. In the comparative pharmacokinetic study with Megace OS, a reference drug product, MASD (1:1) showed improved bioavailability of over 220% with 2-fold higher C(max) and 30% faster T(max). We conclude that MASD (1:1) is a good candidate for the development of oral solid dosage forms.

As an initial step to develop the transdermal delivery system of glucosamine hydrochloride (GL-HCl), the permeation study across the rat skin in vitro was performed to identify the most efficient vehicle with regard to the ability to deliver GL-HCl transdermally. The GL-HCl formulations such as o/w cream, liposome suspension, liposomal gel, and liquid crystalline vehicles were prepared and compared for transdermal flux of GL-HCl. The liquid crystalline vehicles were more effective in increasing the skin permeation of GL-HCl than o/w cream and liposomal vehicles. Of the liquid crystalline vehicles tested, the permeation enhancing ability of the cubic phase was greater than that of the hexagonal phase when the nanoparticle dispersion was used. The skin permeation enhancing ability of the cubic nanoparticles for GL-HCl was further increased by employing both oleic acid and polyethylene glycol 200. Therefore, the cubic liquid crystalline nanodispersion containing oleic acid and PEG 200 can provide a possibility of clinical application of transdermal GL-HCl.

The purpose of this study was to design and evaluate a directly compressible hydrophilic poly(ethylene oxide) (PEO) matrix for the oral sustained delivery of dihydrocodeine bitartrate (DHCT). A direct compression method was used to prepare PEO matrices, and the amount of PEO in the matrices was varied to optimize in vitro DHCT release profiles. In vitro release studies indicated that the matrices containing 20%-70% w/w of PEO with molecular weight of 5.0 x 10(6) showed a similar release profile, as estimated with DT50%, to that exhibited by a marketed product, DHC Continus. In vivo bioavailability study revealed that the difference in the pharmacokinetic parameters such as AUC0-30 and Tmax of the selected sustained-release formulation containing 60% w/w of PEO 5.0 x 10(6) and DHC Continus was statistically insignificant (p > 0.05). Thus, it could be concluded that the extent of bioavailability of the sustained-release formulation developed here was similar to that of DHC Continus although Cmax values of these two preparations were significantly different (p < 0.05). From the data obtained in this research, hydrophilic PEO matrices were found to be a novel sustained-release carrier for the oral delivery of DHCT.

The aim of this study was to investigate the effects of different levels of Hermetia illucens (HI) and Protaetia brevitarsis seulensis (PBS) powder on breast meat of broilers during storage. A total of 400 1-d-old Arbor Acres broilers were randomly divided into four treatments; each treatment group included four replicate pens with 25 birds per pen. Broilers were fed basal diets supplemented with 0.5%, and 1% HI powder or 1.5% PBS powder or only basal diets without HI or PBS. Traits such as meat quality, color, and antioxidant effects were evaluated. The different levels of HI and PBS powder did not enhance meat quality and color during storage. On day 0, thiobarbituric acid reactive substance (TBARS) values were not significantly affected by different levels of HI and PBS (p > 0.05). However, a significant decrease in TBARS values on day 7 was observed with 0.5% HI and 1.5% PBS treatment compared to values obtained with other treatments (p < 0.05). The reduction in TBARS values with 0.5%, and 1% HI or 1.5% PBS treatments on day 7 was 75.4%, 63.1% and 76.9%, respectively. Between the different levels of HI and PBS treatment, no significant differences in 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging were observed after 7 days of storage. However, addition of HI and PBS powder to broiler diets had a significant effect (p < 0.05) on DPPH radical scavenging in broiler breast meat on day 0. These results indicate that addition of 0.5% HI and 1.5% PBS to broiler diets improves the antioxidant activity of broiler breast meat during storage.

Ssanghwa-tang (SHT) is a traditional Korean herbal medicine widely prescribed to decrease fatigue following an illness. The purpose of this study was to investigate the effects of SHT on osteoclast differentiation in vitro, and on bone loss in ovariectomized (OVX) rats in vivo. SHT significantly reduced the receptor activator for the nuclear factor kB (NF-kB) ligand (RANKL)-induced tartrate-resistant acid phosphatase (TRAP) activity, and multinucleated osteoclast formation in RAW264.7 cells without affecting cell viability. In addition, SHT significantly attenuated RANKL-induced mRNA expression levels of c-Src and cathepsin K. To examine the in vivo effect of SHT on OVX-induced bone loss in OVX rats, we administered SHT (0.6 g/kg BID) orally to OVX rats for 12 weeks. SHT administration significantly blocked OVX-induced decrease of femoral bone mineral density (BMD) and femoral trabeculae in OVX rats. In conclusion, these results suggest that SHT treatment effectively prevents OVX-induced bone loss, and this effect may result from its inhibitory effect on osteoclast differentiation.

The following study was presented to investigate the anti-inflammatory effect of peel extracts (PE) from three citrus fruits: Citrus unshiu, Citrus limonia Osbeck and Citrus hallabong. According to this study, cytotoxicity, NO-production and protein levels of iNOS (inducible nitric oxide synthase) in macrophage cell were analyzed, which had been incubated in murine macrophage cell line RAW 264.7 cell of PE from those three citrus fruits. According to Citrus unshiu peel extracts (CUP), Citrus limonia Osbeck peel extracts (CHP) and Citrus hallabong peel extracts (CLP) treatment, the result showed that there was no cell growth inhibited below 2 mg/mL. Comparing the NO-production of the cell with LPS (100 ng/mL) and the treatment without LPS, significant increase of NO-production was detected. However NO-production also showed decrease trend, as the concentration increased. For each treatment, at the concentration of 1 mg/mL, NO-ihibitory activity showed significant result with following order: CUP > CHP > CLP. According to the result from Western blot, the inhibitory activities of iNOS protein from CUP and CHP showed fairly similar performances. Also inhibitory activity of COX-2 showed the following order: CUP > CHP> CLP. There was no doubt that all the treatments of CUP, CHP and CLP have anti-inflammatory effect and also that the inhibitory activity of the CUP treatment was the strongest among those three.