• Korean Chemical Engineering Research
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• v.59 no.4
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• pp.493-502
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• 2021

We prepared and investigated a biosynthesized nanoparticulate system with high adsorption and release capacity of letrozole. Silver nanoparticles (AgNPs) were biosynthesized using olive leaf extract. Cysteine was capped AgNPs to increase the adsorption capacity and suitable interaction between nanoparticles and drug. Morphology and size of nanoparticles were confirmed using transmission electron microscopy (TEM). Nanoparticles were spherical with an average diameter of less than 100 nm. Cysteine capping was successfully confirmed by Fourier transform infrared resonance (FTIR) spectroscopy and elemental analysis (CHN). Also, the factors of letrozole adsorption were optimized and the linear and non-linear forms of isotherms and kinetics were studied. Confirmation of the adsorption data of letrozole by cysteine capped nanoparticles in the Langmuir isotherm model indicated the homogeneous binding site of modified nanoparticles surface. Furthermore, the adsorption rate was kinetically adjusted to the pseudo-second-order model, and a high adsorption rate was observed, indicating that cysteine coated nanoparticles are a promising adsorbent for letrozole delivery. Finally, the kinetic release profile of letrozole loaded modified nanoparticles in simulated gastric and intestinal buffers was studied. Nearly 40% of letrozole was released in simulated gastric fluid with pH 1.2, in 30 min and the rest of it (60%) was released in simulated intestinal fluid with pH 7.4 in 10 h. These results indicate the efficiency of the cysteine capped AgNPs for adsorption and release of drug letrozole for breast cancer therapy.

• Journal of Periodontal and Implant Science
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• v.27 no.1
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• pp.129-150
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• 1997

The purpose of this study was to evaluate the effects of tetracycline(TC}, flurbiprofen, and PDGF-BB loaded biodegradable membranes on the cell-attachment, the activity of loaded PDGF-BB, in vivo release kinetics, and guided bone regenerative potentials. To evaluate the cell attachment to membranes, the number of gingival fibroblasts attached to each membrane(10% TC, 10% flurbiprofen, $200ng/cm^2$ PDGF-BB loaded membranes, drug-unloaded membrane) was counted by coulter counter and the morphologic pattern of attached cells was examined under SEM. To determine whether the activity of loaded PDGF-BB is sustained, the cellular growth and survival rate of gingival fibroblasts was used for both standard PDGF-BB and loaded PDGF-BB. For evaluation of in vivo release kinetics, drug-loaded membranes were implanted on the dorsal skin of the rats. On 1, 3, 7, 10, 14, 21, and 28 days after implantation, the amount of remaining drugs were measured by HPLC assay for TC and flurbiprofen, and by ${\gamma}-scintillation$ counter for $PDGF-BB^{1125}$. For evaluation of guided regenerative potential, the amount of new bone in the calvarial defect(5mm in diameter) of the rat was measured by histomorphometry 1 and 2 weeks after implantation of membranes. The number of cells attached to the PDGF-BB loaded membrane was largest as compared with the other mernbranes.(p< 0.05) The activity of loaded PDGF-BB was not significantly different from the activity of standard PDGF-BB.(p<0.05) After initial burst release of drug during the first 24 hours, drugs were gradually released for 4 weeks. Especially the release rate of PDGF-BB was nearly constant during 4 weeks. PDGF-BB loaded membranes(200, $400ng/cm^2$) were effective in guided bone regeneration as compared with drug-unloaded membrane. These results implicate that drug-loaded biodegradable membranes might be a useful for guided bone regeneration.

• Journal of Pharmaceutical Investigation
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• v.23 no.2
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• pp.103-110
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• 1993

Microcapsules(Mc) of cephalexin (CEPH), using Eudragit RS, RL, L, S and polyethylene glycol 1540, were evaluated biopharmaceutically. The area under the curve of CEPH-Eudragit RS/RL Mc administered orally once was larger than that of cephalexin powder twice every 6 hrs. Controlledrelease effectiveness and the absorption rate effectiveness, two important parameters of Vallner's method, of CEPH-Eudragit RS/RL Mc indicate that these Mc can be good sustained-release preparations. And a simple pharmacokinetic model is introduced which allows the gastric emptying and intestinal-transit rates of a drug itself and a solid-state drug contained in Mc. Decreasing $K_r$, without change in $K_a$, showed that the rate-limiting step of absorption moved from absorption step to releasestep.

• Proceedings of the KOSOMBE Conference
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• v.1997 no.05
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• pp.11-15
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• 1997

We used the photoreactive poly(allylamie) (PPA) as the hydrophilic membrane to control the release of drug from polyurethane(PU). PPA was covalently bonded onto PU surface through the highly reactive nitrene intermediate upon UV light irradiation $(3.3mW/cm^2)$ at 254nm for 5min. Thus the release rate of rifampicin from PU surface was controlled. To know the characteristics of PU surface bonded with PPA, we measured the ATR-FTIR, ESCA, Static Contact Angle and SEM. From these, we suggest that PPA as a hydrophilic membrane is enable to control the release rate of a hydrophobic drug from polymer without the change of bulk property.

• Journal of Pharmaceutical Investigation
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• v.39 no.4
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• pp.269-273
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• 2009

The objective of this investigation was to develop a gastro-retentive(GR) dosage form of gabapentin and was to evaluate of its dissolution characteristics. GR tablet consists of expandable core tablet matrix and semi-permeable membrane coating. Poloxamer 407 and sodium bicarbonate were used to prepare the core matrix. Polyvinly acetate dispersion (Kollicoat $SR30D^{(R)}$) and polyvinyl alcohol-polyethylene glycol copolymer ((Kollicoat $IR^{(R)}$)) were employed to form the semi-permeable membrane. The GR tablets significantly expanded up to fivefold in simulated gastrointestinal fluids with no apparent damage of the coating membrane over 12 hours. Also, the swelling rate was controllable with the amount of sodium bicarbonate. The drug release was observed to be substantially sustained based on coating level. The release rate of gabapentin from the GR tablet was gradually slowed down as the coasting amount was increased. The gabapentin GR tablet with 8% coating level showed a pseudo-zero order release kinetics over 12 hours. These results suggest that this swellable GR tablet system having semi-permeable membrane coating can be applicable for hydrophilic drug substances like gabapentin.

• Asian-Australasian Journal of Animal Sciences
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• v.20 no.2
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• pp.194-199
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• 2007

Effects of recombinant bovine somatotropin (bST) on plasma hormonal concentration, embryo quality, and pregnancy rate were examined during the superovulation and synchronization treatment in donor and recipient cows. Hanwoos (Korean native beef cattle) were treated with controlled internal drug release (CIDR) combined with bST (CIDR+bST) or without bST (CIDR) as donor cows. The embryos recovered from donors were transferred into Holstein recipient heifers treated with bST (CIDR+bST) or without bST (CIDR) for synchronization. The correlation between IGF-I and P4 showed a positive pattern in the CIDR+bST group (r=0.44, p<0.01), but a negative pattern was shown in the CIDR group (r = -0.59, p<0.02) at day 7 of estrous cycles. Although the number of recovered, transferable, and degenerated embryos was not different, quantities of grade 1 (excellent) embryos in CIDR+bST group were significantly higher than those of the CIDR group (p<0.01). The pregnancy rate was higher in the CIDR+bST recipient group compared to CIDR group (p<0.05), when the embryos were recovered from the donors treated with CIDR. However, the pregnancy was maintained highly in both recipient groups, when the embryos were produced by CIDR+bST treated donors. It can be concluded that bST administration combined with CIDR is an effective method for superovulation and synchronization treatment to stabilize plasma hormonal levels, to obtain excellent quality of embryos, and to get higher pregnancy rate.

• Journal of Pharmaceutical Investigation
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• v.40 no.2
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• pp.73-78
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• 2010

Hydrogels are thought to be a promising delivery carrier for protein drugs because of their favorable aqueous environment compared with nano/micro-particles of hydrophobic polymer such as PLGA. In this study, nano-sized hydrogels (nanogels) were fabricated using inverse-miniemulsion polymerization method. The mean size of nanogels in range of 90-160nm and affected by the preparation parameters such as sonication time and concentration of monomer. While longer sonication time and lower concentration of acrylamide monomer showed a tendency to produce smaller nanogels and to have lower lysozyme activity, variation of bis-methylene acrylamide concentration made no difference. Although both longer soncaton time and lower acrylamide concentration increased in vitro release rate, acrylamide concentration was more effectively affected to the control of protein release rate, which indicated that the release rate of protein from nanogels affected by not only their size but also internal structure. In conclusion, nanogels prepared by inverse-miniemulsion can be a useful carrier for application of protein drug, because of simple process, minimum contact of organic solvent and high protein activity.

• Journal of Pharmaceutical Investigation
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• v.27 no.4
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• pp.323-329
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• 1997

Ipriflavone is non-hormonal antiosteoporotic drug which inhibits bone resorption by reducing recruitment and/or differentiation of osteoclasts, and stimulates proliferation and differentiation of osteoblast, and also enhances calcitonin secretion in the presence of estrogen. Although some kinds of immediately-released preparation of ipriflavone are available in commercial market, in present study, we tried to formulate sustained-release tablet using coating method with hydrophobic and hydrophilic coating materials. In vitro dissolution test was applied to evaluate sustained-release patterns of several test preparations (Test tablet A, B and C) designed using different preparation method or different compositions. From the results of dissolution test, test tablet A which showed suitable dissolution profile was selected as the candidate of new product. Pharmacokinetic evaluation of test drug, ipriflavone sustained-release tablets, was conducted in 6 beagle dogs weighing $11.5{\pm}0.5\;Kg$ compared with $Theobon^{\circledR}$ tablet, immediately-released tablet (Kukjae Pharm. Co.) as reference drug. Two products were randomly administered to 6 beagle dogs, and after 1 week, cross-over study was conducted. From the present study, AUC and $T_{max}$ of test product were significantly different from those of reference product (p<0.05), respectively$(AUC\;:\;3646.28{\pm}472.56\;vs\;3646.28{\pm}472.56\;ng{\cdot}hr/ml,\;T_{max}\;:\;4.33{\pm}1.03\;vs\;1.42{\pm}0.38\;hr)$. But $C_{max}$ was not significantly different between two products (p>0.05) $(\;512.52{\pm}48.18\;vs\;443.97{\pm}140.53\;ng/ml)$. From the results of pharmacokinetic evaluations, it was noted that absorption amount of test product was increased, but absorption rate was delayed and $C_{max}$ of two products were not changed. And it was concluded that redesign of the sustained-release preparation which has a lower content of iprifavone rather than test tablet A must be considered.

• Polymer(Korea)
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• v.25 no.6
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• pp.884-892
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• 2001

Biodegradable wafers were prepared with poly (L-lactide-co-glycolide) (50 : 50 mole ratio of lactide to glycolide, molecular weight:5000 g/mole) by direct compression method for the sustained release of nifedipine to investigate the possibility of the treatment of hypertension. PLGA wafers were prepared by altering initial drug/polymer loading ratio, wafer thickness, and hydroxypropyl methylcellulose (HPMC) content. These wafers showed new zero-order release patterns for 11 days, and various biphasic release patterns could be obtained by altering the composition of wafers such as addition of matrix binder as HPMC to the PLGA wafer to reduce release rate of initial phase. The onset of polymer mass loss only occured after 4 days and about 40% of mass loss was observed after 11 days nifedipine release. This system had advantages in terms of simplicity in design and obviousness of drug release rate and may be useful as an implantable dosage form.

• Macromolecular Research
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• v.12 no.3
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• pp.269-275
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• 2004

To graft N-isopropylacrylamide (NIPAAm) onto alginate, varying dosages of ${\gamma}$-rays were irradiated onto alginate films in deionized water and methanol media, which are non-solvents of alginate. We investigated the hydrogels graft ratio, mechanical strength, swelling kinetics and ratio, and behavior with respect to drug release. The graft yield of NIPAAm increased upon increasing the irradiation dose. The use of the aqueous solution increased the graft yield relative to that obtained in methanol. The mechanical strength of the grafted hydrogels increased after grafting with NIPAAm. In a study of the swelling kinetics, we found that all hydrogels reached an equilibrium swollen state within 3 h. The equilibrium swelling ratio of the hydrogels decreased upon increasing the irradiation dose. The swelling ratio of the hydrogels decreased dramatically between 30 and 35$^{\circ}C$ because phase separation of NIPAAm occurred at 32$^{\circ}C$. The swelling process, with respect to the temperature change, was repeatable. An NIPAAm-grafted alginate containing a drug sustained its release rate until 3 h after an initial high drug release caused by a burst effect.