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Cho, Jae-Pyoung,Cho, Jin-Cheol,Oh, Eui-Chaul The Korean Society of Pharmaceutical Sciences and 2008 Journal of Pharmaceutical Investigation Vol.38 No.6
A propofol delivery system was prepared using two biocompatible polymeric surfactants, poloxamer 407 and PEG 400. The nanoparticular stability of the micellar system was evaluated in terms of temperature change, storage time and composition. The particle size of the system was slightly increased with elevating temperature from $4^{\circ}C$ to $25^{\circ}C$, but its distribution was unimodal. At $40^{\circ}C$, the system presented a bimodal particle size distribution and the increase in the fraction of particles larger than 15 nm. This result might be due to the expansion of the nanoparticles through micellar swelling at the high temperature. It was found that propofol was gradually come out of the system, stored for a month at three different temperatures (4, 25 and $40^{\circ}C$). The drug loss was apparently dependent on temperature and the system composition. Increasing temperature induced the acceleration of the drug loss of $7{\sim}10%$ at $4^{\circ}C$ and $14{\sim}16 %$ at $40^{\circ}C$. This may be owing to the high diffusivity resulting from the swelling of the hydrophilic surface of the nanoparticle at high temperature. However, the addition of PEG 400 to the system led to the reduction of the drug loss. This result is associated with the previous investigation that PEG coverage decreased diffusion coefficient because of the formation of the denser structure on the surface of nanoparticulate. Nevertheless, the limited amount of PEG, less than 2% (w/v), should be used to prevent the precipitation and discoloration of the system.
Budesonide Microemulsions for Enhancing Solubility and Dissolution Rate
Piao, Hong-Mei,Cho, Hyun-Jong,Oh, Eui-Chaul,Chung, Suk-Jae,Shim, Chang-Koo,Kim, Dae-Duk The Korean Society of Pharmaceutical Sciences and 2009 Journal of Pharmaceutical Investigation Vol.39 No.6
Budesonide belongs to Class II in the Biopharmaceutics Classification System (BCS) for its high permeability and poor aqueous solubility. The purpose of this study was to improve the solubility and dissolution rate of budesonide using an o/w microemulsion system in order to develop a nasal formulation. Based on the results of the solubility study and pseudo ternary phase diagrams, microemulsions of about 80 nm in mean diameter were formulated using isopropyl myristate and Labrasol$^{(R)}$ as an oil phase and a surfactant, respectively. Solubility of budesonide in the microemulsions increased up to 6.50 mg/mL, which is high enough for a nasal formulation. In vitro release profiles of budesonide significantly increased from the microemulsions compared to that of the budesonide powder. These results suggest that the microemulsions of budesonide could further be developed into a clinically useful nasal formulation.
Preparation and Stability Evaluation of Docetaxel-Loaded Oral Liposome
Chon, Chong-Run,Kim, Hyun-Mi,Lee, Pung-Sok,Oh, Eui-Chaul,Lee, Ma-Se The Korean Society of Pharmaceutical Sciences and 2010 Journal of Pharmaceutical Investigation Vol.40 No.2
Docetaxel-loaded liposomes were prepared by emulsion-solvent evaporation method, then coated with chitosan at room temperature and lyophilized. This system was designed in order to improve solubility and stability of docetaxel in the GI tract for oral drug delivery. The solubilizing effect of some frequently used solubilizers and/or liposome was determined. Among the results docetaxel-loaded liposomes prepared with 0.5% TPGS as a solubilizer showed 100-fold higher solubility than docetaxel. In a stability test, mean particle size of different liposome formulations was measured by a particle size analyzer in simulated gastric fluid (SGF) and in simulated intestinal fluid (SIF). The particle size of uncoated liposomes was significantly increased compared with that of chitosan-coated liposomes in SGF, however, there was no significant difference between coated and uncoated liposome in SIF. It is evident that chitosan-coated liposomes were more stable in GI conditions. The release characteristics of docetaxel-loaded liposomes were also investigated in three buffer solutions (pH 1.2, 4.0, 6.8). Docetaxel release did not occur in pH 1.2 for 4 hrs. However, in pH 4.0 and 6.8 conditions, docetaxel was gradually released over 24 hrs as a sustained release. It seems that aggregation and precipitation of particles by electrostatic interaction might protect docetaxel from being released. In Conclusion, the results from this study show that the chitosan-coated liposomes may be useful in enhancing solubility and GI stability of docetaxel.