• KSBB Journal
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• v.23 no.5
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• pp.408-412
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• 2008

The rosiglitazone loaded poly (lactide-co-glycolide) (PLGA) nanoparticles (NPs) were prepared by the emulsion-evaporation method and optimized for particle size and entrapment efficiency. The optimized particles were 140-180 nm in size with narrow size distribution and 80% entrapment efficiency at 1% w/w initial drug loading when prepared with 1-3% w/v of PVA as a surfactant. These particulate carriers exhibited controlled in vitro release of rosiglitazone for 36 hrs at a nearly constant rate after 4 hrs release. In conclusion, these results indicate that PLGA NPs have greater potential for oral delivery of rosiglitazone.

• Journal of Pharmaceutical Investigation
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• v.35 no.1
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• pp.25-31
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• 2005

Depot system for local drug delivery using chitosan hydrogel has been developed to enhance the therapeutic efficacy and to prevent the severe side effect in whole body. Thus, we have prepared an injectable chitosan hydrogel containing liposomes to treat cancers clinically. Anionic liposomes incorporated to improve sustained release efficiency within chitosan hydrogel. The chitosan solution containing liposomes was designed to form a hydrogel complex at body temperature. The released behavior of doxorubicin from liposomes in chitosan hydrogel showed sustained-release caused by diffusion of doxorubicin from temperature responsive liposome into chitosan hydrogel. The chitosan hydorgel containing liposomes enhanced the therapeutic potency for the solid tumor in vivo system. Our results indicate that the liposomes in chitosan hydrogel represent a depot system for local drug delivery.

• Journal of Pharmaceutical Investigation
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• v.35 no.3
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• pp.143-150
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• 2005

Solid lipid nanoparticles(SLNs) are particulate systems for parenteral drug administration and have good biocompatibility and stability. SLNs were prepared with lauric acid, as the lipid core. Tween 20 and tween 80 were used as surfactant. 5-fluorouracil and l-benzoyl-5-fluorouracil were used as model drugs. Drug-loaded SLNs were prepared by the hot homogenization technique in order to evaluate the physical stability, entrapment efficiency of drugs as well as release profile. The particle size of SLNs was $40{\sim}600$ nm. By increasing speed, the mean particle size of SLNs was decreased. And entrapment efficiency in the case of using 1-Benzoyl-5-fluorouracil was higher than using 5-Fluorouracil. The higher surfactant concentration, the faster release rate at the range of $1.5{\sim}2.5%$.

• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.305-311
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• 2002

In order to evaluate the effect of poloxamer 407 content on the dissolution profiles of pellets, diltiazem HCl (DTL) core pellets were prepared with poloxamer 407 (50-90% w/w, with lactose as filler) using an extruder and a spheronizer. Any possible interaction between the drug and excipients was evaluated using DSC, IR and TLC. Dissolution tests were performed using USP basket method. In addition, scanning electron micrograph was performed to examine the surface roughness and cross sections. The release of DTL from the core pellets was decreased with increasing poloxamer 407 content. Cracks appeared on the surface of the core pellets with increasing the poloxamer 407 content, which may play a role on the retardation of the release of DTL from core pellets. There was no any significant interaction between the drug and excipients employed to prepare the core pellets.

• Journal of Pharmaceutical Investigation
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• v.38 no.1
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• pp.39-43
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• 2008

Cyclosporin A (CyA), a potent immunosuppressive drug used in allogeneic transplants and autoimmune disease, is a typical water-insoluble drug. Recently, nanoparticle carriers were investigated to improve the intestinal absorption of drugs. In this study, CyA-loaded nanostructured lipid carriers (NLCs) were prepared from a hot o/w emulsion using the high pressure homogenization method. The NLCs were consisted of cationic lipids, solid lipids, liquid lipids (oils), surfactant and stabilizer. Encapsulation efficiency of CyA in NLCs was approximately 71%. The average particle size and zeta potential of NLCs were below 250 nm and above +40 mV, respectively. The morphology of NLCs was confirmed by transmission electron microscopy (TEM) analysis. Compared to the CyA powder, higher in vitro release of CyA from NLCs was observed after burst release within 30 min. Thus, CyA-loaded NLCs could be applied not only for parenteral route but also for gastrointestinal administration, which needs further investigation.

• Biomolecules & Therapeutics
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• v.9 no.4
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• pp.298-306
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• 2001

To develop a novel transdermal delivery system of loxoprofen (LP), a potent antiinflammatory and analgesic agent, the effects of vehicle composition and drug loading dose on the skin permeation property were investigated. And in vivo skin absorption property studied by analysing the $C_{max}$ and AUC was investigated after applying the developed plaster systems on rabbit back skin. Addition of isopropyl myristate (IPM) and IPM-diethylene glycol monoethyl ether (DGME) cosolvent in the plaster showed higher permeation rates than those from propylene glycol laurate-DGME cosolvent systems. As the concentration of LP in the plaster increased from 0.56 mg/$\textrm{cm}^2$ to 1.19 mg/$\textrm{cm}^2$, the drug release and skin permeation rates increased linearly. At loading dose of 1.19 mg/$\textrm{cm}^2$, the flux reached 35.6 $\mu$g/$\textrm{cm}^2$/hr. New LP plasters showed a good adhesive property onto skin, and showed no crystal formation. The AU $C_{0-24hr}$ and $C_{max}$ after dermal application of LP plaster (60 mg/70 $\textrm{cm}^2$) were found to be 6951$\pm$230 ng.hr/ml and 400$\pm$44 ng/ml, respectively. And the plasma concentration maintained above 300 ng/ml up to 24 hr period. In the carrageenan-induced rat paw edema test, LP plaster showed similar inhibition rate with marketed ketoprofen (Ketoto $p^{R}$) plaster.aster.r.

• Bulletin of the Korean Chemical Society
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• v.23 no.6
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• pp.872-879
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• 2002

One of the improtant characteristics of core-shell type nanoparticles is the long-term storage and reuse as an aqueous injection solution when required. For this reason, reconstruction of lyophilized core-shell type nanoparticles is considered to be essential . BAB type triblock copolymers differ from AB type diblock copolymers, which contain the A block as a hydrophilic part and the B block as a hydrophobic part. by not being easily redistributed into phosphate-buffered saline (PBS, pH 7.4, 0.1 M). Therefore, lyophilized core-shell type nanoparticles of CEC triblock copolymer were reconstituted using a somication process with a bar-type sonicator in combination with a freezing-thawing process. Soncation for 30s only resuspended CEC nanoparticles in PBS; their particle size distribution showed a monomodal pattern with narrow size distribution. The bimodal size distribution pattern and the aggregates were reduced by further sonication for 120 s but these nanoparticles showed a wide size distribution. The initial burst of drug release was increased by reconstitution process. The reconstitution of CEC core-shell type nanoparticles by freezing-thawing resulted in trimodal distribution pattern and formed aggregates, although freezing-thawing process was easier than sonication . Drug release form CEC nanoparticles prepared by freezing-thawing was slower than from the original dialysis solution. Although core-shell typenanoparticles of CEC triblock copolymers were not easily performed. Cytotoxicity testing of core-shell type nanoparticles of CEC-2 triblock copolymers containing clonazepam (CNZ) was performed using L929 cells. Cytotoxicity of CNZ was decreased by incorporation into nanoparticles.

• Archives of Pharmacal Research
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• v.19 no.2
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• pp.106-111
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• 1996

Alginate microspheres were prepared by the emulsification process as a drug delivery system of ampicillin sodium (AMP-Na). The preparation parameters such as the concentration of calcium chloride, the stirring time and the amount of AMP-NA were investigated. The alginate microspheres containing hydroxypropylmethylcellulose (HPMC) were found to be generally spherical, discrete and had smoother surfaces when compared to without HPMC. However, there was no significant difference in the release profile of AMP-NA from alginate microspheres prepared with or without HPMC. The concentration of calcium chloride solution and the stirring time in the preparation of alginate microspheres influenced the aggregation of alginate microspheres. The amount of AMP-NA in alginate microspheres influenced the surface morphology and the practical drug content in microspheres.

• Journal of Pharmaceutical Investigation
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• v.27 no.2
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• pp.133-137
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• 1997

Buccal absorption test of omeprazole in human was performed to determine the permeability of the drug molecule through oral mucous membrane. Oral mucosal adhesive tablets of omeprazole were prepared by compressing the omeprazole with a mixture of sodium alginate and hydroxypropylmethyl cellulose (HPMC) as bioadhesive polymers, magnesium oxide (MgO) as a stabilizer and sodium carboxymethyl cellulose (Na CMC) or cros-carmellose sodium (Ac-Di-Sol) as disintegrants. The bioadhesive force, stability in saliva and release characteristics of the tablets were evaluated. Omeprazole was absorbed about 23% in 15 min through human buccal mucous membrane. Furthermore, omeprazole was stable in saliva for more than 8 hrs when MgO was added to the tablet as the amount of 2.5 fold of omeprazole. The release rate of omeprazole was increased with increasing the amount of sodium alginate in the tablet. From these results, it is suggested that tablets composed of [omeprazole/HPMC/sodium alginate/MgO/Ac-Di-Sol and/or Na CMC (20/6/24/50/10) (mg/tablet)] are potential candidate for buccal drug delivery system.

• Bulletin of the Korean Chemical Society
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• v.19 no.9
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• pp.962-967
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• 1998

Block copolymers consisting of poly(rbenzyl L-glutamate) (PBLG) as the hydrophobic part and poly(ethylene oxide) (PEO) as the hydrophilic part were synthesized and characterized. Polymeric micelles of the block copolymers (abbreviated GEG) were prepared by a dialysis method. The GEG block copolymers were associated in water to form polymeric micelles, and the critical micelle concentration (CMC) values of the block copolymers decreased with increasing PBLG chain length in the block copolymers. Transmission electron microscopy (TEM) observations revealed polymeric micelles of spherical shapes. From dynamic light scattering (DLS) study, sizes of polymeric micelles of GEG-1, GEG-2, and GEG-3 copolymer were 106.5±59.2 nm, 79.4±46.0 nm, and 37.9±13.3 nm, respectively. The drug loading contents of GEG-1, GEG-2 and GEG-3 polymeric micelles were 12.6, 11.9, and 11.0 wt %, respectively. These results indicated that the drugloading contents were dependent on PBLG chain length in the copolymer; the longer the PBLG chain length, the more the drug-loading contents. Release of norfloxacin (NFX) from the nanoparticles was slower in higher loading contents of NFX than in lower loading contents due to the hydrophobic interaction between PBLG core and NFX.