ORCID Profile
0000-0002-1697-5107
Current Organisation
Yeungnam University College of Pharmacy
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Publisher: Informa UK Limited
Date: 08-07-2013
DOI: 10.3109/02652048.2013.805837
Abstract: This study was designed to optimize a fenofibrate-loaded self-microemulsifying drug delivery system (SMEDDS) by using a response surface methodology. Box-Behnken design (BBD) and its desirability function were used to optimize the SMEDDS. The independent factors were the amounts of Labrafil M 1944 CS, Labrasol, and Capryol PGMC and the dependent variables were droplet size, cumulative percentage of drug released in 30 min and equilibrium solubility of fenofibrate in SMEDDS. Various response surface graphs were used to understand the effects of each factor, and the desirability function was then adjusted to optimize SMEDDS formulation. The experimental values of optimized formulation were in close agreement with predicted values. Furthermore, in vivo pharmacokinetic study of the optimized formulation showed significant increase in relative oral bioavailability compared to that of the powder suspension. In conclusion, the BBD demonstrated its effectiveness in optimizing the SMEDDS formulation and in identifying the effects of formulation variables.
Publisher: Elsevier BV
Date: 08-2013
DOI: 10.1016/J.IJPHARM.2013.05.034
Abstract: The main purpose of this study was to investigate the potential of self-nano-emulsifying drug delivery system (SNEDDS) in improving the bioavailability of docetaxel (DCT) and its chemotherapeutic effect. The DCT-loaded SNEDDS was prepared by employing rational blends of capryol 90, labrasol, and transcutol HP using ternary phase diagram. The liquid nano-emulsion was spray-dried into solid SNEDDS (D-SNEDDS) using an inert porous carrier, colloidal silica. The optimized formulation was characterized in terms of physico-chemical and pharmacokinetic parameters. Furthermore, anti-tumor efficacy of D-SNEDDS was compared with commercial marketed product, Taxotere(®). The various compositions of SNEDDS were screened and found optimal at a volume ratio of 10/75/15 for capryol 90, labrasol, and transcutol HP, respectively. We observed a high oral bioavailability of 17% DCT for D-SNEDDS than compared to only 2.6% for pure DCT solution. Notably, D-SNEDDS exhibited an augmented anti-tumor efficacy with a reduced toxicity profile when compared with intravenously administered Taxotere(®), the commercialized formulation of DCT. Taken together, D-SNEDDS could be a potential candidate for an oral dosage form of DCT with enhanced antitumor activity and reduced toxicity.
Publisher: Oxford University Press (OUP)
Date: 24-07-2013
DOI: 10.1111/JPHP.12115
Abstract: To develop and optimize the novel self-microemulsifying drug delivery system (SMEDDS) formulation for enhanced water solubility and bioavailability of telmisartan (TMS) using the Box–Behnken design (BBD) and desirability function. TMS-SMEDDS formulation consisted of the mixture of oil (Peceol), surfactant (Labrasol), co-surfactant (Transcutol), TMS and triethanolamine. A three-level BBD was applied to explore the main effect, interaction effect and quadratic effect of three independent variables, including the amount of Peceol (X1), Labrasol (X2) and Transcutol (X3). Determined conditions were 20 & X1 & 40, 50 & X2 & 80 and 5 & X3 & 30. The response variables were droplet size (Y1), polydispersity index (Y2) and dissolution percentage of TMS after 15 min (Y3). The optimized conditions were 28.93, 80 and 28.08 (mg) for X1, X2 and X3, respectively, and the response variables were predicted to be 159.8 nm, 0.241 and 85.8% for Y1, Y2 and Y3, respectively. The actual values from the optimized formulation showed good agreement with predicted values. The optimized TMS-SMEDDS formulation showed faster drug dissolution rate and higher bioavailability than TMS powder. Our results suggest that response surface methodology using BBD and desirability function is a promising approach to understand the effect of SMEDDS variables and to optimize the formulation.
Publisher: Elsevier BV
Date: 09-2012
DOI: 10.1016/J.IJPHARM.2012.05.039
Abstract: The objective of the present study was to enhance solubility and bioavailability of itraconazole by a combined use of membrane emulsification and spray drying solidification technique. A shirasu-porous-glass (SPG) membrane with a mean pore size of 2.5 μm was used to produce monodispersed microemulsions of itraconazole consisting of methylene chloride as the dispersed phase, a mixture of Transcutol HP and Span 20 as a stabilizer, and dextran as solid carrier dissolved in water as the continuous phase. The dispersed phase permeated through the SPG membrane into the continuous phase at an agitator speed of 150 rpm, a feed pressure of 15 kPa and a continuous phase temperature of 25°C and the resultant emulsion was solidified using spray-drying technique. Solid state characterizations of the solid emulsion showed that the crystal state of itraconazole in solid emulsion was converted from crystalline to amorphous form. The solid emulsion of itraconazole displayed a significant increase in the dissolution rate than that of pure itraconazole. Furthermore, the solid emulsion after oral administration gave about eight-fold higher AUC and about ten-fold higher C(max) in rats than pure itraconazole powder (p<0.05), indicating this formulation greatly improved the oral bioavailability of drug in rats. Thus, these results demonstrated that the SPG membrane emulsification system combined with spray-drying technique could be used as a promising technique to develop solid formulation of itraconazole with enhanced solubility and bioavailability.
No related grants have been discovered for Jeonghwan Kim.