• YAKHAK HOEJI
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• v.44 no.4
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• pp.293-299
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• 2000

Biodegradable microspheres made from poly-lactide-co-glycolide polymers have been considered as a new delivery system for single-dose vaccine. Purified tetanus toxoid (TT) was encapsulated in poly-lactide(PLA) and poly-lactide-co-glycolide (PLGA) microparticles using a solvent evaporation method in a multiple emulsion system (water-in oil-in water). The morphology of 77-loaded microparticles was spherical and the suface of them was smooth. The particle size was in a range of 2-10. Protein loading efficiency was 68-97.8%. PLGA (85:15) microparticle showed the highest efficiency. Protein release pattern was influenced by polymer molecular weight and composition. The release rate of PLA(Mw 100,000) microsphere was higher than any other microspheres. In consequence of the hydrolysis of PLGA(50:50) microspheres, environmental pH decreased from 7.4 to 5.0. The PLA, PLGA (75:25) and PLGA (85:15) microshperes showed no significant pH change. The antigenicity or n in microshperes was assayed by indirect sandwich ELISA using equine polyclonal tetanus antitoxin for capture antibody and human polyclonal tetanus antitoxin for primary antibody. The antigenicity of TT in PLA (Mw 100,000), PLGA(50:50, Mw 100,000) and PLGA (75:25, Mw 73,300) after 30 days incubation showed 54, 40.9 and 76.7%, respectively.

• Journal of Pharmaceutical Investigation
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• v.26 no.4
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• pp.273-280
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• 1996

Chondroitin sulfate/gelatin microspheres containing dexamethasone 21-acetate were prepared by complex coacervation method and their release patterns were examined in vitro. Microspheres prepared with a small amount of crosslinking agent had smooth surface and few pores, but those with a large amount of crosslinking agent were more porous and less spherical. In vitro release patterns were varied by changing polymer/drug weight ratio and amount of crosslinking agent. The release rate of dexamethasone 21-acetate in the presence of collagenase was faster than that in the absence of collagenase. Anti-inflammatory effect of dexamethasone 21-acetate microspheres was more efficient than that of dexamethasone 21-acetate solution in carrageenan-induced arthritis in the rat. On the basis of the above results, we might expect the degradation and drug release rate of these microspheres to be regulated by the degree of crosslinking and the level of enzymes. In patients with severe rheumatoid arthritis who have high concentration of collagenase, more drug would be released from the microspheres. An intra-articular injection therapy of rheumatoid arthritis with desired release kinetics could be developed to enhance patient compliance and therapeutic index.

• YAKHAK HOEJI
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• v.55 no.1
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• pp.69-74
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• 2011

Hyaluronic acid (HA) is a natural polymer consisting of disaccharide units of D-glucuronic acid and N-acetyl-D-glucosamine. It has a great potential and success in cosmetic and biomedical applications. However, native HA is highly soluble and easily metabolized by enzymes such as hyaluronidase. Thus, various studies have been reported on modifying the physicochemical properties of HA, while maintaining its biocompatibility. For controlled drug delivery, many trials for fabricating HA microspheres were achieved under chemical reaction. The HA microspheres fabricated to improve the physical stability of HA using adipic acid dihydrazide (ADH) by cross-linking reaction has been reported earlier, however it lacks the desired physical stability and rapidly decomposes by swelling or enzymes. Therefore, we prepared double cross-linked HA microspheres (DC-HA microspheres) and alginate containing HA microspheres (AC-HA microspheres) to enhance its physicochemical properties. DC-HA microspheres were prepared using trisodium trimetaphosphate (STMP) under crosslinking reaction after ADH cross-linking reaction. AC-HA microspheres were prepared by adding alginate as a networking polymer. These microspheres were characterized by morphology, particle size, zeta potential, stability against hyaluronidase. Results showed that the DC-HA and AC-HA microspheres are more stable than that of HA microspheres.

• Polymer(Korea)
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• v.28 no.4
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• pp.291-297
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• 2004

Water-soluble chitosan micro spheres were prepared by emulsification of chitosan solution in mineral oil followed by cross linking reaction with different amount of the cross linking agent (glutraraldehyde), different chitosan concentration. Then, the physicochemical properties such as morphological change by degradation, drug loading efficiency, and drug release profiles were investigated with the drug loaded water-soluble chitosan microspheres. Norfloxacin loaded water-soluble chitosan micro spheres showed excellent drug entrapping capacities without burst release caused by surface bound drug. The absence of the surface bound drug also confirmed by X-ray diffraction study. Degradation and drug release studies showed that the amount of the crosslinking agent played a crucial role for drug loading, release and degradation. The water-soluble chitosan micro spheres showed more sustained drug release profiles with slower degradation and larger particle size by increasing crosslinking agent.

• Polymer(Korea)
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• v.34 no.4
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• pp.321-325
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• 2010

Fibroin is a biopolymer available in large quantity from silk fiber and has a long history of use as a suture proving biocompatibility. In this report, fibroin microspheres has been fabricated for biomaterial applications. W/O emulsion of regenerated fibroin droplets in a continuous phase of decane with mixed surfactants was dried to facilitate fibroin gelation and the condensed fibroin microspheres were harvested. The ratio of mixed surfactants and their proportions to decane were determined to prepare a stable W/O emulsion. A spherical form of fibroin gels was obtained from the W/O emulsion agitated at 600 rpm. Scanning electron microscopy revealed that number average sizes of the fibroin microspheres were 21.6 and 8.5 ${\mu}m$ when dried under ambient conditions or under vacuum, respectively. Tomography of the spheres revealed that their internal structures are packed or hollowed. Hollow and hemispherical forms of microspheres were also prepared by using porogen.

• Polymer(Korea)
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• v.34 no.4
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• pp.341-345
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• 2010

Effects of modification of silver nanoparticles on the polymerization rate and morphology of poly(methyl methacrylate)(PMMA)/silver microspheres prepared by suspension polymerization of MMA were investigated. The silver nanoparticles and their surface hydrophilicity played an important role in the polymerization rate and the morphology of poly(methyl methacrylate) (PMMA)/silver microspheres. The polymerization rate increased slightly with modified silver nanoparticles. PMMA/silver microspheres with conversion up to 85% were obtained in spite of the low polymerization temperature. Due to the change of hydrophilicity of silver nanoparticles, different appearances of the microspheres having golf ball-like convex surfaces or concave surfaces were observed. As the hydrophilicity of silver was decreased, stable nanocomposites were prepared.

• Journal of the Society of Cosmetic Scientists of Korea
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• v.30 no.3 s.47
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• pp.295-305
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• 2004

Colloid and surface chemistry have been focused on surface area and surface energy. Local surface properties such as surface density, interaction, molecular orientation and reactivity have been one of interesting subjects. Systems of such surface energy being important would be listed as association colloid, emulsion, particle dispersion, foam, and 2-D surface and film. Such nanoparticle systems would be applied to drug delivery systems and functional cosmetics with biocompatible and degradable materials, while nanoparticles having its size of several nm to micron, and wide surface area, have been accepted as a possible drug carrier because their preparation, characteristics and drug loading have been inves-tigated. The biocompatible carriers were also used for the solubilization of insoluble drugs, the enhancement of skin absorption, the block out of UV radiation, the chemical stabilization and controlled release. Nano/micro emulstion system is classified into nano/microsphere, nano/microcapsule, nano/microemulsion, polymeric micelle, liposome according to its prep-aration method and size. Specially, the preparation method and industrial applications have been introduced for polymeric micelles self-assembled in aqueous solution, nano/microapsules controlling the concentration and activity of high concen-tration and activity materials, and monolayer or multilayer liposomes carrying bioactive ingredients.

• International Journal of Molecular Medicine
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• v.43 no.6
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• pp.2409-2419
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• 2019

The use of finasteride for alleviating hair loss has been investigated, and it has been applied as an oral dose medication. However, due to the inconvenience of daily drug administration over long period of time, novel controllable finasteride delivery has been actively investigated. As a novel method of finasteride delivery, the development of finasteride-loaded microspheres for subcutaneous administration is becoming increasingly pharmaceutically important. Therefore, the present study aimed to use finasteride-loaded microspheres in a controlled manner in an attempt to overcome the limitations of the oral administration of finasteride and to cause fewer adverse effects. Finasteride-loaded microspheres containing poly(lactic-co-glycolic acid) and finasteride at a ratio of 4:1 were prepared, and a testosterone-induced androgenic alopecia mouse model was used. Following observation for 10 weeks, the percentage hair growth was 86.7% (total hair growth 60%, partial hair growth 26.7%) in the orally-applied finasteride-treated group as a positive control, and 93.3% (total hair growth 60%, partial hair growth 33.3%) in the finasteride-loaded microspheres-treated group. Serum dihydrotestosterone levels began to decrease at week 6 in the orally-applied finasteride- and finasteride-loaded microsphere-treated groups. In addition, the finasteride-loaded microspheres-treated group exhibited similar follicular number, follicular length, anagen/telogen ratio and hair bulb diameter values to those of the orally-applied finasteride-treated group. Furthermore, the finasteride-loaded microspheres increased the activities of phosphoinositide 3-kinase/protein kinase B and Wnt/β-catenin in relation to hair follicle cell growth signaling in mouse skin, and suppressed the apoptosis of hair follicle cells by reducing the expression of transforming growth factor-β2 and caspase-3, which are indicators of apoptosis. In conclusion, the administration of a single injection of finasteride-loaded microspheres was effective in treating testosterone-induced alopecia. Furthermore, it led to equivalent hair growth effects when compared with orally-applied finasteride, thus revealing the possibility of effective treatment via different routes of administration.

• Polymer(Korea)
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• v.27 no.1
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• pp.9-16
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• 2003

Ipriflavone (IP) stimulates proliferation and differentiation of osteoblast and also enhances calcitonin secretion in the presence of estrogen. Poly(lactide-co-glycolide) (PLCA) due to its controllable biodegradability and relatively good biocompatibility is one of the most significant candidates for the study of drug controlled release system. In this study, IP-loaded PLGA microspheres (MSs) was prepared by using conventional O/W solvent evaporation method. The size of MSs was in the range of 5~200 $mu extrm{m}$. The morphology of MSs was characterized by SEM. And, in vitro release amounts of IP were analyzed by HPLC. The highest encapsulation efficiency were obtained by using gelatin and polyvinyl alcohol (PVA) as emulsifiers. The morphology, size distribution, and in vitro release pattern of MSs were changed by several preparation parameters such as molecular weights (8, 20, 33 and 90 kg/mol), polymer concentrations (2.5, 5, 10 and 20%), emulsifier types (PVA, gelatin and Tween 80), initial drug loading amount (5, 10, 20 and 30%) and stirring speed (250, 500 and 1000 rpm). The release of IP in vitro was more prolonged over 30 days, with close to zero-order pattern by controlling the preparation parameters. The physicochemical properties of IP-loaded PLGA MSs were investigated by XRD and DSC.

• Asian Pacific Journal of Cancer Prevention
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• v.13 no.12
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• pp.6363-6368
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• 2012

Objective: The study aim was to prepare poly-DL-lactide-poly (PELA) microspheres encapsulating recombinant tissue inhibitors of metalloproteinase-1 (TIMP-1) in an adenovirus to investigate its inhibition on the proliferation of hepatocellular carcinoma cells HepG2. Methods: Microspheres were prepared by encapsulating the recombinant TIMP-1 adenovirus into biodegradable PELA. The particle size, viral load, encapsulation efficiency and in-vitro release were measured. Microspheres were used to infect HepG2 cells, then infection efficiency was examined under a fluorescent microscope and ultrastructural changes assessed by TEM. Expression of TIMP-1 mRNA in HepG2 cells was examined by semi-quantitative RT-PCR and proliferation by MTT and cell growth curve assays. Results: We successfully prepared microspheres encapsulating recombinant TIMP-1 adenovirus with a diameter of $1.965{\mu}m$, an encapsulation efficiency of 60.0%, a viral load of $10.5{\times}10^8/mg$ and approximate 60% of virus release within 120 h, the total releasing time of which was longer than 240 h. The microspheres were confirmed to be non-toxic with blank microspheres. Infected HepG2 cells could stably maintain in-vitro expression of TIMP-1, with significantly effects on biological behaviour Conclusion: PELA microspheres encapsulating a recombinant TIMP-1 adenovirus can markedly inhibit the proliferation of HepG2 cells, which provides an experimental basis for polymer/chemistry-based gene therapy of hepatocellular carcinomas.