• Polymer(Korea)
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• v.24 no.5
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• pp.728-735
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• 2000

Fentanyl-loaded biodegradable poly(L-lactide-co-glycolide) (75 : 25 by mole ratio of lactide to glycolide, PLGA) microspheres (MSs) were prepared to study the possibility for long-acting local anesthesia. We developed the fentanyl base (FB, slightly water-soluble)-loaded PLGA MSs by means of conventional O/W solvent evaporation method. The size of MSs was in the range of 10~150 ${\mu}{\textrm}{m}$. The morphology of MSs was characterized by SEM, and the in vitro release amounts of FB were analyzed by HPLC. The lowest porous cross-sectional morphology and the highest encapsulation efficiency were obtained by using gelatin as an emulsifier. The influences of several preparation parameters, such as emulsifier types, molecular weights and concentrations of PLGA, and initial drug loading amount, etc., have been observed in the release patterns of FB. The release of FB in vitro was more prolonged over 25 days, with close to zero-order pattern by controlling the preparation parameters. We also investigated the physicochemical properties of FB-loaded PLGA MSs by X-ray diffraction and differential scanning calorimeter.

• Macromolecular Research
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• v.14 no.4
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• pp.461-465
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• 2006

Two types of injectable system using thermosensitive chitosan (chitosan-g-NIPAAm), hydrogel and microparticles (MPs)-embedded hydrogel were developed as drug carriers for controlled release and their pharmaceutical potentials were investigated. 5-Fluorouracil (5-FU)-loaded, biodegradable PLGA MPs were prepared by a double emulsion method and then simply mixed with an aqueous solution of thermosensitive chitosan at room temperature. All 5-FU release rates from the hydrogel matrix were faster than bovine serum albumin (BSA), possibly due to the difference in the molecular weight of the drugs. The 5-FU release profile from MPs-embedded hydrogel was shown to reduce the burst effect and exhibit nearly zero-order release behavior from the beginning of each initial stage. Thus, these MPs-embedded hydrogels, as well as thermosensitive chitosan hydrogel, have promising potential as an injectable drug carrier for pharmaceutical applications.

• Journal of environmental and Sanitary engineering
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• v.17 no.1
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• pp.75-80
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• 2002

This study was carried out to investigate release characteristics of phosphorus with DO, pH and temperature, to suppose its behaviour with time using mathematical model, and to under-stand its forms with pH. Released SRP was in inversely proportional to DO and it did few release in initial aerobic conditions, but it did actively with decreasing DO concentration. Also, its release was increased with increasing pH and temperature. It was found that relation between time and released SRP concentration was zero order reaction. As compared with k values in various pH and temp., they was $k_{15}>k_{25}$ in pH 6 but was $k_{15} in pH 7 and 8. Considering forms of phosphorus with pH, Resdi.-P & NAI-P increased but Ads.-P & Apt.-P decreased with increasing pH.

• Archives of Pharmacal Research
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• v.19 no.1
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• pp.1-5
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• 1996

Laminated films composed of drug-containing reservoir layer and drug-free membrane were prepared. Zero-order drug release with lag time was achieved by laminating drug-free film onto the reservoir layer, while burst effect was observed on cast-on film. The rate controlling membrane was either attached to or cast directly into the reservoir. The release rate was independent on the reservoir composition but dependent on the composition of rate-controlling membrane. In growth inhibitory test of cephalexin from Eudragit RS film to Streptococcus Mutans, the disk even after release test for 72 hours showed more bacterial growth inhibition than that of control. Permeation of drug through rat skin was proportional to the HPC fraction in the film. We could control the release of cephalexin from the film by changing the fraction of Eudragit RS, HPC and DEP content. Consequently, Eudragit RS/HPC film was found to be very effective system for local delivery of drugs.

• Journal of Pharmaceutical Investigation
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• v.21 no.2
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• pp.91-95
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• 1991

Polyethylene glycol, polypropylene glycol and block copolymer of ethylene glycol and propylene glycol were crosslinked by triisocyanate to form water swellable, rubbery polymer. The equilibrium swelling of the hydrogels ranged from 3% to 60% according to the hydrophobic-hydrophilic properties of the prepolymers. Model drugs, sodium salicylate and prednisolone were incorporated in the polymer matrices by swelling loading. Physical properties of the drugs affected the drug release mechanisms due to the change in the swelling behaviors of the polymeric devices. Zero order release was observed in the case of relatively hydrophobic polymer matrices.

• Journal of Pharmaceutical Investigation
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• v.32 no.1
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• pp.1-6
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• 2002

The mucoadhesive characteristics of [P(AA-co-PEGMM)] films by estimating the glass transition temperature $(T_g)$, analyzing surface energy and studying FT-IR was previously reported. In this study, the possibility of buccal mucoadhesive dosage form of [P(AA-co-PEGMM)] films by mucoadhesive force measurements and dissolution tests were also investigated. Mucoadhesiveness of [P(AA-co-PEGMM)] films was compared with cr-PAA and cr-PEGMM films crosslinked with 3% ethyleneglycol dimethacrylate (EGDMA). The buccal mucoadhesive force of [P(AA-co-PEGMM)] films increased with increasing content of PEGMM. [P{AA-co-PEGMM (18 mole%)}] films showed a significantly greater mucoadhesiveness than cr-PAA and cr-PEGMM films. The mucoadhesive force measured in normal saline (pH 5.0) was higher than that measured in phosphate buffer (pH 6.8) because of the pH dependence of hydrogels with carboxyl ions within the PAA. Moreover, the mucoadhesive force of [P{AA-co-PEGMM (18 mole%)}] films was at maximum after 2 hr attachment of buccal mocosa and it was maintained over $1\;N/cm^2$ for up to 10 hr. In dissolution studies, the release of butorphanol tartrate from [P(AA-co-PEGMM)] films increased with increasing PEGMM content, and films prepared with 18 mole% PEGMM gave almost zero order release kinetics.

• Korean Journal of Food Science and Technology
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• v.44 no.3
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• pp.274-279
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• 2012

The objective of this study was to develop oral matrix tablets for the sustained release of vitamin C. In this study hydroxypropyl methylcellulose (HPMC) has been utilized as an excipient, as it is one of the most widely used polymers, for use during long periods of time in formations. The vitamin C tablet formulation depends on the molecular weight and concentration of sustained-delivery in HPMC. Anti-oxidants have been added as a dissolution medium in order to prevent vitamin C degradation in water. The dissolution test was carried out in a distilled water medium, and the release model equation was applied to analyze the vitamin C release pattern. The results demonstrated that the release and lasting power of vitamin C tablets, containing HPMC, lasted for more than 12 h.

• Macromolecular Research
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• v.8 no.6
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• pp.253-260
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• 2000

Biodegradable wafers were prepared with poly (hydroxybutyrate-co-hydroxyvalerate) (PHBV;5, 10, and 15 mole% for 3-hydroxyvalerate) by simple heat pressing method for the sustained release of antibiotic agent, gentamicin sulfate (GS) to investigate the possibility of the treatment for osteomyelitis. The effects of hydroxyvalerate (HV) content, thickness of wafers, various types of additives such as sodium dodecyl sulfate (SDS), microcrystalline cellulose, polyvinylpyrrolidone, and hydroxypropylcellulose (HPC), and different initial drug loading ratio on the release profile have been investigated. In vitro release studies showed that different release patterns and rates could be achieved by simply modifying factors in the preparation conditions. PHBV wafers with 3 mm thickness, 10% of GS initial loading, 15% of HV content and addition of 5% of SDS and HPC were free from initial burst and a near-zero-order sustained release was observed for over 30 days. It might be suggested that the mechanisms of G5 release may be more predominant simple dissolution and diffusion of GS than erosion of PHBV in our system.

• Macromolecular Research
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• v.11 no.3
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• pp.183-188
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• 2003

The controlled delivery of anticancer agents using biodegradable polymeric implant has been developed to solve the problem of penetration of blood brain barrier and severe systemic toxicity. This study was performed to prepare 5-FU-loaded poly (L-lactide-co-glycolide) (PLGA) wafer fabricated microparticles prepared by two different method and to evaluate their release profile for the application of the treatment of brain tumor. 5-FU-loaded PLGA microparticles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC). SEM observation of the 5-FU-loaded PLGA microparticles prepared by rotary solvent evaporation method showed that 5-FU was almost surrounded by PLGA and significant reduction of crystallinity of 5-FU was confirmed by XRD. In case of release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by mechanical mixing, the release profile of 5-FU followed near first order release kinetics. In contrast to the above result, release profile of 5-FU from 5-FU-loaded PLGA wafer fabricated microparticles prepared by rotary solvent evaporation method followed near zero order release kinetics. These results indicate that preparation method of the 5-FU-loaded PLGA microparticles to fabricate into wafers was contributed to drug release profile.

• Macromolecular Research
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• v.10 no.5
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• pp.246-252
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• 2002

In order to the development of the delivery device of long-acting local anesthetics for postoperative analgesia and control of chronic pain of cancer patient, fentnyl-loaded poly (L-lactide-co-glycolido) (PLGA, molecular weight, 5,000 g/mole; 50 : 50 mole ratio by lactide to glycolide) microspheres (FMS) were studied. FMS were prepared by an emulsion solvent-evaporation method. The influence of several preparation parameters such as initial drug loading, PLGA concentration, emulsifier concentration, oil phase volume, and fabrication temperature has been investigated on the fentanyl release profiles. Generally, the drug showed the biphasic release patterns, with an initial diffusion followed by a lag period before the onset of the degradation phase, but there was no lag time in our system. Fentanyl was slowly released from FMS over 10 days in vitro with a quasi-zero order property. The release rate increased with increasing drug loading as well as decreasing polymer concentration with relatively small initial burst effect. From the results, FMS may be a good formulation to deliver the anesthetic for the treatment of chronic pain.