• Applied Chemistry for Engineering
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• v.32 no.5
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• pp.509-515
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• 2021

In this study, poly lactic-co-glycolic acid (PLGA) nanoparticles (PNP) were prepared through double (w/o/w) emlusion and emulsifying solvent-evaporation technique using PLGA, which has biocompatibility and biodegradability. To maximize stability and bioavailability of the particles, chitosan-coated PLGA nanoparticles (CPNP) were prepared by charge interaction between PNP and chitosan. We demonstrated that CPNP can be utilized as a drug carrier of oral administration. The chemical structure of CPNP was analyzed by ¹H-NMR and FT-IR, and all characteristic peaks appeared, confirming that it was successfully prepared. In addition, particle size and zeta potential of CPNP were analyzed using dynamic light scattering (DLS) while morphological images were obtained using transmission electron microscope (TEM). Thermal decomposition behavior of CPNP was observed through thermogravimetric analysis (TGA). In addition, the cytotoxicity of CPNP was confirmed by MTT assay at HEK293 and L929 cell lines, and it was proved that there is no toxicity confirmed by the cell viability of above 70% at all concentrations. These results suggest that the CPNP developed in this study may be used as an oral drug delivery carrier.

• Archives of Pharmacal Research
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• v.25 no.6
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• pp.964-968
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• 2002

Colon drug delivery is advantageous in the treatment of colonic disease and oral delivery of drugs unstable or suceptible to enzymatic degradation in upper GI tract. In this study, multilayer coated system that is resistant to gastric and small intestinal conditions but can be easily degraded by colonic bacterial enzymes was designed to achieve effective colon delivery of prednisolone. Variously coated tablets containing prednisolone were fabricated using chitosan and cellulose acetate phthalate (CAP) as coating materials. Release aspects of prednisolone in simulated gastrointestinal fluid and rat colonic extracts (CERM) were investigated. Also, colonic bacterial degradation study of chitosan was performed in CERM. From these results, a three layer (CAP/Chitosan/CAP) coated system exhibited gastric and small intestinal resistance to the release of prednisolone in vitro most effectively. The rapid increase of prednisolone in CERM was revealed as due to the degradation of the chitosan membrane by bacterial enzymes. The designed system could be used potentially used as a carrier for colon delivery of prednisolone by regulating drug release in stomach and the small intestine.

• Bulletin of the Korean Chemical Society
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• v.32 no.5
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• pp.1587-1592
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• 2011

The aim of the present study was to improve the solubility and bioavailability of a poorly water-soluble drug in human body, using a solid dispersion technique (hot melt extrusion). The solid dispersion was prepared by cooling the hot melt of the drug in the carrier (Vitamin E TPGS and PVP). The dissolution rate of formulation 1 from a novel formulation prepared by solid dispersion technique was equal to release of formulation 6 (40% of eprosartan mesylate is in contrast to teveten$^{(R)}$) within 60 min (Table 1). The oral bioavailability of new eprosartan mesylate tablet having vitamin E TPGS and PVP K29 was tested on rats and dogs. Of the absorption enhancer and polymer tested, vitamin E TPGS and PVP K29, resulted in the greatest increases of AUC in animals (about 2.5-fold increase in rat and dog). When eprosartan mesylate was mixed with the absorption enhancer and polymer in a ratio of 2.94:2:1, vitamin E TPGS and PVP K29 improved eprosartan mesylate bioavailability significantly compared with the conventional immediate release (IR) tablet Teveten$^{(R)}$ (formulation 7). These results show that solid dispersion using vitamin E TPGS and PVP K29 is a promising approach for developing eprosartan mesylate drug products.

• Journal of Pharmaceutical Investigation
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• v.28 no.1
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• pp.43-50
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• 1998

Niosomes are vesicles formed from synthetic non-ionic surfactants, offering an alternative to chemically unstable and expensive liposomes as a drug carrier. Non-ionic surfactant and cholesterol mixture film leads to the formation of vesicular system by hydration with sonication method. The formation of niosome was ascertained by negative staining of TEM. The entrapment efficiency of niosomal suspension was gradually increased with increasing the ratio of cholesterol to surfactant. It was found that the niosome with 6 : 4 (polyoxyethylene 2-cetyl ether: cholesterol) ratio was more stable than those with other ratios. The topical application of acyclovir(ACV) in the treatment of herpes simplex virus type 1(HSV-1) skin disease has a long history. There are an increasing number of reports, however, in which topical ACV therapy is not as effective as oral administration. Lack of efficacy with topical ACV has been hypothesized to reflect the inadequate delivery of drug to the skin. We investigated the permeation of niosome containing $[^{3}H]ACV$ in hairless mouse skin using Franz diffusion cell model. Permeation coefficient(P) of aqueous ACV was $6.7{\times}10^{-4}\;(cm/hr)$ and that of ACV in niosome was $23.4{\times}10^{-4}\;(cm/hr)$, suggesting about 3.5 times increase in the transdermal permeation.

• Biotechnology and Bioprocess Engineering:BBE
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• v.11 no.6
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• pp.526-529
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• 2006

The aim of this study was to prepare cyclosporin A-loaded liposome (CyA-Lip) as an oral delivery carrier, with their encapsulation into microspheres based on alginate or extracellular polysaccharide (EPS) p-m10356. The main advantage of liposomes in the microspheres (LIMs) is to improve the restricted drug release property from liposomes and their stability in the stomach environment. Alginate microspheres containing CyA-Lip were prepared with a spray nozzle; CyA-Liploaded EPS microspheres were also prepared using a w/o emulsion method. The shape of the LIMs was spherical and uniform, and the particle size of the alginate-LIMs ranged from 5 to $10\;{\mu}m$, and that of the EPS-LIMs was about $100\;{\mu}m$. In a release test, release rate of CyA in simulated intestinal fluid (SIF) from the LIMs was significantly enhanced compared to that in simulated gastric fluid (SGF). In addition, the CyA release rates were slower from formulations containing the liposomes compared to the microspheres without the liposome. Therefore, alginate-and EPS-LIMs have the potential for the controlled release of CyA and as an oral delivery system.

• Journal of Pharmaceutical Investigation
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• v.9 no.1
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• pp.7-14
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• 1979

The relative efficacy on the renal function of rabbits by oral administration of furosemide and 1 : 2 furosemide-PVP coprecipitate was compared by measuring the urine volume in response to maximal response and the amounts of electrolytes excreted in urine. The furosemide produced a rapid onset, short duration of diuresis, in contrast, the 1: 2 furosemide-PVP coprecipitate, a rapid onset, significantly larger magnitude, and longer duration of diuresis and therefore the bioavailability of furosemide from the coprecipitate were increased significantly. The average urine volume and the amount of sodium and potassium excreted in urine were increased about 2.9-, 14.8-, and 1.8-fold from furosemide, and about 6.2-, 24.2-, and 3.6-fold from 1 : 2 furosemide- PVP 40,000 coprecipitate, rerpectively, comparing by their control values.

• Archives of Pharmacal Research
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• v.29 no.8
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• pp.712-719
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• 2006

In this study, we prepared core-shell type nanoparticles of a poly(DL-lactide-co-glycolide) (PLGA) grafted-dextran (DexLG) copolymer with varying graft ratio of PLGA. The synthesis of the DexLG copolymer was confirmed by $^1H$ nuclear magnetic resonance (NMR) spectroscopy. The DexLG copolymer was able to form nanoparticles in water by self-aggregating process, and their particle size was around $50\;nm{\sim}300\;nm$ according to the graft ratio of PLGA. Morphological observations using a transmission electron microscope (TEM) showed that the nanoparticles of the DexLG copolymer have uniformly spherical shapes. From fluorescence probe study using pyrene as a hydrophobic probe, critical association concentration (CAC) values determined from the fluorescence excitation spectra were increased as increase of DS of PLGA. $^1H-NMR$ spectroscopy using $D_2O$ and DMSO approved that DexLG nanoparticles have core-shell structure, i.e. hydrophobic block PLGA consisted inner-core as a drug-incorporating domain and dextran consisted as a hydrated outershell. Drug release rate from DexLG nano-particles became faster in the presence of dextranase in spite of the release rate not being significantly changed at high graft ratio of PLGA. Core-shell type nanoparticles of DexLG copolymer can be used as a colonic drug carrier. In conclusion, size, morphology, and molecular structure of DexLG nanoparticles are available to consider as an oral drug targeting nanoparticles.

• Journal of Pharmaceutical Investigation
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• v.37 no.1
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• pp.15-22
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• 2007

An oil-in-water solvent evaporation method was used to prepare the cyclosporin A (CyA)-loaded nanoparticles varying in poly (D,L-lactide-co-glycolide) (PLGA) polymer (RG 502H, RG 503H) and the amount of additive ethyl myristate (EM) or chitosan (CS). The particles were characterized for drug loading and entrapment efficiency by HPLC, surface morphology by scanning electron microscopy, particle size by dynamic light scattering and surface charge by Zetapotential. The results showed drug loadings ranging from 10.9% to 15.8% with high encapsulation efficiency (82.0-97.8%). SEM and DLS studies showed discrete and spherical particles with smooth surfaces and mean size ranging 257.6-721.7 nm. The additive EM or CS did not change the mean sizes of the nanoparticles, whereas by the coating effect of CS, the Zetapotential values of the CS-added nanoparticles were moved to the more positive direction as the amount of CS was increased. From the pharmacokinetic analysis, the nanoparticles formulations showed the higher bioavailability and MRT than $Neoral^{\circledR}$ While little adding effect of EM or CS was detected in pharmacokinetic profile when RG 503H was used as polymer carrier, more noticeable different pharmacokinetic behaviors could be observed in case of RC 502H. EM incorporation was found to elevate the $K_{el}$, whereas CS coating resulted in the decrease of F and $K_{el}$, which seems to be due to the function of CS as a barrier and a mucoadhesive coating.

• Journal of the Korean Chemical Society
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• v.60 no.3
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• pp.187-193
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• 2016

In this study, preparation of positively and negatively charged carbon nanotube (CNT)-collagen (CG) hydrogels with pH sensitive characteristic was reported. The positive and negative characteristics of the prepared hydrogels were created by introduction of positively functionalized CNT-NH₂ and negatively functionalized CNT-COOH, respectively, into the collagen hydrogel. The surface charge of CNTs (CNT-NH₂ and CNT-COOH), CG and CNTs/CG hydrogels was measured by Zetasizer. The swelling ratios of CNT-NH₂/CG and CNT-COOH/CG hydrogels in aqueous solution were checked by measuring of weight changes of the hydrogels in the range of pH 2~10. In detail, the positively charged CNT-NH₂/CG hydrogel swelled up to 5% at pH 4 in comparison to the weight at pH 7, while the negatively charged CNT-COOH/CG hydrogel swelled up to 10% at pH 10. The prepared CNT-NH₂/CG and CNT-COOH/CG hydrogels will be very useful as pH sensitive oral drug-delivering systems for gastrointestine (pH ~2) and small intestine (pH ~9), respectively.

• Journal of Periodontal and Implant Science
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• v.27 no.4
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• pp.751-765
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• 1997

Periodontal disease is a bacterially causal by disease, To remove plaque and bacteria, it has been necessary to prescribe chemical drug to patient to subjugate therapeutic unvalue by mechanical scaling. As a patient on a high dosage of the antibiotics to maintain the effective concentration may produce unfavorable side effects, this decase demands the Slow-release local drug delivery system. The object of the experiment is to study on the slow-release local drug delivery effects of calcium sulfate compounded with tetracycline that mainly used in periodontal disease. Experimental groups were divided into four classes as follow: Group 1 10% tetracycline compounded modified calcium sulfate paste. Group 2 : compounded and hardened 10% tetracycline and calcium sulfate. Group 3 : compounded 10% tetracycline and calcium sulfate, used Just before hardened. Group 4 : tetracycline-ethylene vinyl acetate fiber. In the four groups, release concentration, it's durability and the period of absorption by times are observed and concluded as follow: 1. An effective concentration($4{\mu}g/ml$) remained until 5 weeks in group 1, 9 days in group 2, 7 days in group 3, 15 days in group 4. 2. It was fully fused at 11.8 days average in group 2 and 14.8 days average in group 3. . There were no statistically significant results in tetracycline concentration until a week in group 2 and 3(p<0.05) These results suggest that tetracycline loaded calcium sulfate release sufficient tetracycline and fused in $11{\sim}14$ days, so calcium sulfate is useful carrier as slow release local drug delivery system.