• Korean Chemical Engineering Research
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• 제61권4호
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• pp.570-575
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• 2023

Targeted anticancer drug delivery systems are needed to enhance therapeutic efficacy by selectively delivering drugs to tumor cells while minimizing off-target effects, improving treatment outcomes and reducing toxicity. In this study, a silica-based nanocarrier capable of targeting drug delivery to cancer cells was developed. First, silica nanoparticles were synthesized by the Stöber method using the surfactant cetyltrimethylammonium bromide (CTAB). Increasing the ratio of EtOH in the solvent produced uniformly spherical silica nanoparticles. Washing the nanoparticles removed unreacted residues, resulting in a non-toxic carrier for drug delivery in cells. Upon surface modification, the pH-responsive polymer, polyethyleneimine (PEI) exhibited slow doxorubicin release at pH 7.4 and accelerated release at pH 5.5. By exploiting this feature, we developed a system capable of targeted drug release in the acidic tumor microenvironment.

• Journal of Pharmaceutical Investigation
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• 제41권6호
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• pp.347-354
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• 2011

Repeated oral administration of loxoprofen can induce many side effects such as gastric disturbances and acidosis. Therefore, we considered alternative routes of administration for loxoprofen to avoid such adverse effects. The aim of this study was to develop an ethylene-vinyl acetate (EVA) matrix system containing a permeation enhancer for enhanced transdermal delivery of loxoprofen. The EVA matrix containing loxoprofen was fabricated and the effects of drug concentration, temperature, enhancer and plasticizer on drug release were studied from the loxoprofen-EVA matrix. The solubility of loxoprofen was highest at 40% (v/v) PEG 400. The release rate of drug from drug-EVA matrix increased with increased loading dose and temperature. The release rate was proportional to the square root of loading dose. The activation energy (Ea), which was measured from the slope of log P versus 1000/T, was 5.67 kcal/mol for a 2.0% loaded drug dose from the EVA matrix. Among the plasticizer used, diethyl phthalate showed the highest release rate of loxoprofen. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancing effect. In conclusion, for the enhanced controlled transdermal delivery of loxoprofen, the application of the EVA matrix containing plasticizer and penetration enhancer could be useful in the development of a controlled drug delivery system.

• 한국재료학회지
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• 제33권11호
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• pp.458-464
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• 2023

In order to develop catechin patches for skin regeneration at wound sites, patches with varying concentrations of catechin and chitosan were manufactured. An optimal composition ratio was determined by adjusting the drug release rate and amount, to maximize efficiency. The catechin used in this study was extracted from green tea leaves using a solvent/ultrasonication method, and its characteristics were confirmed through Fourier transform-infrared spectroscopy (FT-IR) and high-performance liquid chromatography (HPLC) analyses. Patches were prepared with different concentrations of catechin and chitosan, and various properties were analyzed using techniques such as FT-IR, water contact angle analysis, and UV-Vis spectroscopy. It was observed that as the chitosan concentration increased, the release of catechin slowed down or almost ceased. A patch manufactured with 1.5 mg/cm² of catechin at a 1 % chitosan concentration exhibited a high initial release rate over 24 h and demonstrated cellular biocompatibility. Consequently, these patches, with tailored release characteristics based on the concentrations of chitosan and catechin, hold promise for use as drug delivery systems in wound healing applications.

• 한국고분자학회:학술대회논문집
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• 한국고분자학회 2006년도 IUPAC International Symposium on Advanced Polymers for Emerging Technologies
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• pp.258-258
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• 2006

Electrospun fibers of poly(vinyl alcohol) (PVA) were successfully prepared and applied as drug carriers for transdermal drug delivery system. Sodium Salicylate (SS) was the model drug and it was incorporated in the PVA fibers by adding 20 % of SS in a PVA solution prior to electrospinning. Electrospinning of SS-containing PVA solution resulted in the formation of beaded fibers. In order to control the rate of SS release and decrease water solubility of PVA, the SS-loaded electrospun PVA mat was cross-linked by either glutaraldehyde or glyoxal vapor. The morphology, thermal behavior, swelling behavior, release characteristic, kinetics of drug release and also toxicity of the cross-linked sample were investigated.

• Archives of Pharmacal Research
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• 제19권1호
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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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• 제38권1호
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• pp.63-72
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• 2008

Meloxicam-loaded microspheres were prepared with poly(D,L-lactic acid)(PLA) by a solvent-emulsion evaporation method. The morphology, particle size, drug loading capacity, drug entrapment efficiency (EE) and release patterns of drug were investigated in vitro. Various batches of micro spheres with different size and drug content were obtained by changing the ratio of meloxicam to $PLA^{\circ}{\AE}s$ with different molecular weight, PLA concentration in the dispersed phase and stirring rate. Meloxicam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. Microspheres prepared with smaller molecular weight produced faster drug release rate. The release rate of meloxicam for long-acting injectable delivery system in vitro, which would aid in predicting in vivo release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres. Blood concentration-time profile of meloxicam after intramuscular injection of meloxicam-loaded microspheres in rabbits showed possibility of long term application of this system in clinical settings.

• Journal of Pharmaceutical Investigation
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• 제28권2호
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• pp.87-92
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• 1998

Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of the skin irritancy and the instability against the pH, temperature, and light. In order to overcome these problems, various topical gels and multiple emulsion creams which can control the release of active ingredient, KA, were formulated employing cream bases of mineral oil with caprylic capric triglyceride and hydrophilic polymers such as chitosan, carbopol. and pluronics. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solution. Drug release from chitosan-based gels (ChitoGel) obeyed to the first order kinetics with a rapid release especially in the initial period. However, pluronic-based gels (PluGel) and carbopol-based gels (CarboGel) revealed controlled release of drug to some extent, followed by the square root-time kinetics. Moreover, the release of KA was further controlled with the W/O/W multiple emulsion creams (MultiCream), showing the apparent zero order release kinetics by virtue of dynamic ratecontrolling membrane of the oil layer. The flux $(J,\;{\mu}g/cm^2/hr)$ of ChitoGel. CarboGel. PluGel. and MultiCream in the initial period of 6hr were 73.30, 28.67. 24.04 and 7.72, respectively. On the other hand, the skin irritancy score of ChitoGel and MultiCream were observed as 2.5 and 2.3 respectively, in the rabbit skin irritation test. Although there were insignificant differences at p<0.05 between those formulations, it was possible to conclude that the W/O/W multiple emulsion creams containing KA might be a good candidate for an antimelanogenic drug delivery system due to the controlled release of acidic drug molecules.

• Archives of Pharmacal Research
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• 제10권2호
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• pp.75-79
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• 1987

Liposomes were studied as a drug delivery system. Multilamellar vesicles, small unilamellar vesicles and large unilamellar vesicles containing cytarabine were prepared using egg yolk lecithin and cholesterol. Large unilamellar vesicles showed the highest encapsulation efficiency of all and their encapsulation efficiency increased as the buffer volume decreased. Cholesterol increased the stability of liposomal drug products as drug carriers and reduced the permeability of drug across the liposomal membrane. The release rate of cytarabine increased with incubation temperature and decreased with cholesterol incorporation in liposomal membrane. The release mechanism of cytarabine from large unilamellar vesicles in vitro was chiefly due to simple diffusion across the liposomal membrane rather than liposomal rupture.

• 약학회지
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• 제32권1호
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• pp.26-39
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• 1988

Eudragit $RS^{\circledR}$ polymer was used as a wall material for the microencapsulation of aspirin by a phase separation method from chloroform-cyclohexane system with 5% polyisobutylene (PIB) in cyclohexane, and microcapsules obtained were evaluated by particle size analysis, scanning electron microscopy (SEM), drug release and drug stability test. With PIB as a coacervation inducing agent, smooth and tight microcapsules with less aggregation were obtained. Below 1 : 0.3 core-wall ratio, it was possible to coat individual particle. Variation of production conditions showed that increasing the proportion of wall material, particle size and wall thickness of microcapsules and the concentration of paraffin wax in cyclohexane as a sealant sustained drug release rates effectively. SEM confirmed that larger microcapsules after drug release did not rupture into smaller particles but contained a few small pores on the surface. Aspirin release from Eudragit $RS^{\circledR}$ coated microcapsules was independent of the pH of medium, and the mechanism of drug release from non-sealed and sealed microcapsules appeared to fit Higuchi matrix model kinetics. Aspirin in the mixture of aspirin microcapsules and sodium bicarbonate was by far more stable than that in the mixture of pure aspirin and sodium bicarbonate.

• Journal of Pharmaceutical Investigation
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• 제20권2호
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• pp.79-88
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• 1990

A numerical model for diffusion and dissolution controlled transport from dispersed matrix is presented. The rate controlling process for transport is considered to be diffusion of drug through a concentration gradient coupled with time-dependent surface change and/or disappearance of the dispersed drug in response to the dissolution. The transport behavior of drug was explained in terms of ${\nu}$ parameter: ${\nu}$ value means a ratio of diffusion time constant and dissolution time constant. This general model has wide range of application from where release is controlled by the diffusion rate to where release is governed by the dissolution rate. Based on this model, theoretical drug concentration, particle size distributions in the polymer matrix system and the resulting release rate were also investigated.