• Journal of Pharmaceutical Investigation
• /
• v.38 no.4
• /
• pp.229-234
• /
• 2008

In the present study, chitosan-glycerophosphate sodium salt solution as a thermosensitive system (TSS) was used to formulate a temperature-sensitive drug delivery system (TSDDS) containing acetaminophen (AAP). The optimized TSS was prepared by measuring gelation temperature, gelation time and rheological properties of TSS. The optimized gelation temperature and time of TSS were $36^{\circ}C$ and 100 seconds, respectively. The viscosity of TSS was also suitable for maintaining gel structure at $37.2^{\circ}C$. The release profiles of TSDDS in PBS/pH 7.4 with various apparatuses and mass loss of TSDDS were investigated. The time required to release 50% of AAP from TSDDS ($t_{50%}$) was 120 min with the formation of pore on the surfaces, which was 2 times longer than that from AAP-chitosan gel. In addition, TSDDS was degraded approximately 80% within 4 hr and then degraded slowly for 20 hrs. In conclusion, AAP-TSS (TSDDS) formulated in this study might be suitable for some specific uses such as subcutaneous injection and rectal formulation.

• The Korean Journal of Urological Oncology
• /
• 제15권3호
• /
• pp.178-186
• /
• 2017

Purpose: Poloxamer 407 (P407) thermo-sensitive hydrogel formulations were developed to enhance the retention time in the urinary bladder after intravesical instillation. Materials and Methods: P407 hydrogels (P407Gels) containing 0.2 w/w% fluorescein isothiocyanate dextran (FD, MW 4 kDa) as a fluorescent probe were prepared by the cold method with different concentrations of the polymer (20, 25, and 30 w/w%). The gel-forming capacities were characterized in terms of gelation temperature (G-Temp), gelation time (G-Time), and gel duration (G-Dur). Homogenous dispersion of the probe throughout the hydrogel was observed by using fluorescence microscopy. The in vitro bladder simulation model was established to evaluate the retention and drug release properties. P407Gels in the solution state were administered to nude mice via urinary instillation, and the in vivo retention behavior of P407Gels was visualized by using an in vivo imaging system (IVIS). Results: P407Gels showed a thermo-reversible phase transition at $4^{\circ}C$ (refrigerated; sol) and $37^{\circ}C$ (body temperature; gel). The G-Temp, G-Time, and G-Dur of FD-free P407Gels were approximately $10^{\circ}C-20^{\circ}C$, 12-30 seconds, and 12-35 hours, respectively, and were not altered by the addition of FD. Fluorescence imaging showed that FD was spread homogenously in the gelled P407 solution. In a bladder simulation model, even after repeated periodic filling-emptying cycles, the hydrogel formulation displayed excellent retention with continuous release of the probe over 8 hours. The FD release from P407Gels and the erosion of the gel, both of which followed zero-order kinetics, had a linear relationship ($r^2=0.988$). IVIS demonstrated that the intravesical retention time of P407Gels was over 4 hours, which was longer than that of the FD solution (<1 hour), even though periodic urination occurred in the mice. Conclusions: FD release from P407Gels was erosion-controlled. P407Gels represent a promising system to enhance intravesical retention with extended drug delivery.

• Journal of Pharmaceutical Investigation
• /
• v.35 no.3
• /
• pp.151-155
• /
• 2005

A drug delivery system(DDS) for practically insoluble meloxicam was developed and evaluated by dissolution study. A novel DDS is two layered system, where the first layer is consisted of gas-forming agent for an immediate release and the second layer is composed of metolose SR(HPMC) for sustained release. This bilayered tablets were manufactured by using manual single punch machine. The results of dissolution study showed an initial burst release followed by sustained release for the experimental period time. From a pharmaceutical point of view, the designed DDS for meloxicam would be informative system in terms of poorly soluble analgesic medicines.

• Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
• /
• 2002.11a
• /
• pp.448-451
• /
• 2002

The possibility of using polypyrrole as a drug delivery system(DDS) has been studied using indicate (Phenol red) and substance with therapeutic activity(Sodium salicylate). In aqueous solution, negative potential is applied to polypyrrole then anion(with therapeutic activity) of sodium salicylate is released by redox processes of polypyrrole. The release amount of anionic drugs from polypyrrole is measured by UV-visible spectrometer which can measure UV-absorbance of materials. Electrode area that use for release amount measurement is$50mm^{2}(5{\times}10mm)$,and thickness of polypyrrole membrane is $15{\mu}m$. DC 1V applied in saline solution, the release amount according to time increased gradually. In various electrode area, release amount of anionic drug is directly to electrode area.

• Journal of Pharmaceutical Investigation
• /
• v.27 no.1
• /
• pp.71-77
• /
• 1997

With the aim of improving periodontal regeneration efficacy, as a biodegradable local drug delivery device, drug releasing chitosan beads were prepared. Chitosan beads were prepared through the formation of intermolecular or intramolecular ionic interaction bewteen chitosan and sodium tripolyphosphate and were loaded with flurbiprofen. The mean diameter of the beads was $250\;{\mu}m$. Drug loading efficiency was improved by regulating the pH of tripolyphosphate solution. The drug release kinetics mainly depended upon the hydrophobic properties of the flurbiprofen, that is, the release of flurbiprofen showed initial burst with rapid release for the first day followed by a levelling off of the release rate. However, the release rate could be controlled by the formulation factor including the pH, concentration of the tripolyphosphate solution, gelation time, drug contents. From these results, flurbiprofen loaded chitosan beads were anticipated as biodegradable local drug delivery devices for periodontal regeneneration.

• Journal of Pharmaceutical Investigation
• /
• v.23 no.3
• /
• pp.41-50
• /
• 1993

The iontophoretic delivery across rat skin of quaternary ammonium salts (isopropamide: ISP, pyridostigmine: PS), which are positively charged over a wide pH range, was measured ill vitro. The study showed that: (a) iontophoresis significantly enhanced delivery of ISP and PS compared to respective passive transport; (b) delivery of ISP and PS was directly proportional to the applied continuous direct current density over the range of $0-0.69\;mA/cm^2;$ (c) delivery of ISP and PS was also proportional to the drug concentration in the donor compartment over the range of $0-2{\time}l0^{-2}M:$ (d) sodium ion in the donor compartment inhibited the drug transport possibly due to decreasing the electric transference number of the drug; (e) delivery of ISP and PS increased as the pH of the donor solution increased over the pH range 2-7 suggesting permselective nature of the epidermis, and inhibition of the transference number of the drugs by hydronium ion; (f) some organic anions such as taurodeoxycholate, salicylate and benzoate which form lipophilic ion-pair complexes with ISP inhibited the delivery of ISP. The degree of inhibition by the organic anions was linearly proportional to the extraction coefficient $(K_e)$ of ISP from the partition system with each counteranion between phosphate buffer (pH 7.4) and n-octanol. For PS, however, taurodeoxycholate, but not salicylate and benzoate inhibited the iontophoretic delivery. It suggests that not only sodium ion and hydronium ion but also the counteranions which form lipophilic ion-pairs with quaternary ammonium drugs are not favorable components in formulating the donor solution of the drugs to achieve an effective iontophoretic delivery.

• Journal of Pharmaceutical Investigation
• /
• v.22 no.3
• /
• pp.211-217
• /
• 1992

Stabilization of liposomes against degradation by bile salts has been investigated in order to develop a liposomal model system for oral drug delivery. Two polysaccharides, amylopectin (AP) and chitin (CT), were employed to coat both empty liposomes and bromthymol blue (BTB)-encapsulated liposomes by adsorption-coating techniques. Turbidity changes and BTB-release characteristics in pH 5.6 buffer solutions with or without bile salts, sodium cholate and sodium glycocholate, were observed to compare the differences between uncoated liposomes and polysaccharide-coated liposomes. Initial turbidities of both uncoated and polysaccharide-coated liposomes in buffer solution were kept constant within 3% range during 4 hours of experiments. But they were decreased in a different manner in bile salts-containing buffer solutions, showing 10% or less decrease for polysaccharide-coated liposomes and 25% or more decrease for uncoated liposomes. BTB release from uncoated liposomes has been greatly increased upto 90% after 4 hours in bile salts-containing buffer solution, which is a clue for breakdown of liposomal vesicles. However, polysaccharide-coated liposomes showed the controlled-release pattern which is proportional to square-root of time, followed by around 50% release for the same time period. Consequently, it is possible to conclude that these polysaccharide-coated liposomes might be an available system for oral delivery of a drug which is unstable in gut environment.

• Current Optics and Photonics
• /
• v.4 no.4
• /
• pp.368-372
• /
• 2020

We report the terahertz time-domain spectroscopy (THz-TDS) of transdermal drug delivery in human skin. The time evolution of transdermal nicotine delivery in nicotine patches was assessed by detecting the transmission coefficient of sub-picosecond THz pulses and using a semi-analytic model based on the single-layer effective medium approximation. Using commercial nicotine patches (Nicoderm CQ^®, 7 mg/24 h), THz transmission coefficients were measured to quantitatively analyze the cumulative amounts of nicotine released from the patches in the absence of their detailed specifications, including multilayer structures and optical properties at THz frequencies. The results agreed well with measurements by conventional in vitro and in vivo methods, using a diffusion cell with high-performance liquid chromatography and blood sampling respectively. Our study revealed the ability of the THz-TDS method to be an effective alternative to existing methods for noninvasive and label-free assessments of transdermal drug delivery, showing its high promise for biomedical, pharmaceutical, and cosmetic applications.

• Journal of the Korean Applied Science and Technology
• /
• v.32 no.2
• /
• pp.202-214
• /
• 2015

Stimuli-responsive biomaterials that alter their function through sensing local molecular cues may enable technological advances in the fields of drug delivery, gene delivery, actuators, biosensors, and tissue engineering. In this research, pH-responsive hydrogel which is comprised of dimethylaminoethyl methacylate (DMAEMA) and 2-hydroxyethyl methacrylate (HEMA) was synthesized for the effective delivery of doxorubicin (Dox) to breast cancer cells. Cancer and tumor tissues show a lower extracellular pH than normal tissues. DMAEMA/HEMA hydrogels showed significant sensitivity by small pH changes and each formulation of hydrogels was examined by scanning electron microscopy, mechanical test, equilibrium mass swelling, controlled Dox release, and cytotoxicity. High swelling ratios and Dox release were obtained at low pH buffer condition, low cross-linker concentration, and high content of DMAEMA. Dox release was accelerated to 67.3% at pH 5.5 for 6-h incubation at $37^{\circ}C$, while it was limited to 13.8% at pH7.4 at the same time and temperature. Cell toxicity results to breast cancer cells indicate that pH-responsive DMAEMA/HEMA hydrogels may be used as an efficient matrix for anti-cancer drug delivery with various transporting manners. Also, pH-responsive DMAEMA/HEMA hydrogels may be useful in therapeutic treatment which is required a triggered release at low pH range such as gene delivery, ischemia, and diabetic ketoacidosis.

• Proceedings of the KOSOMBE Conference
• /
• v.1995 no.11
• /
• pp.253-256
• /
• 1995

Polymers have been one of the emerging biomedical materials in the area of biomedical research which are applicable to the human body. For human applications, noninvasive characterization of the biomedical polymers has been one of the important topics, and is valuable information. Among others, the swelling rate is one of the important measurements needed for the hydrophilic polymers. NMR imaging has been a suitable method for the noninvasive study of such a material since it is sensitive to many physical and biochemical changes of the specimens. In addition, NMR techniques possess many useful intrinsic properties such as the relaxation and diffusion effects. The present study has provided a noble and noninvasive method of measuring the process of swelling as well as volumetric changes occurred in polymers and drug delivery processes in a drug delivery system (DDS) together with changes of released drug. This gives information, relating with both water ingress process, volumetric changes of polymer specimens and the visualization of sequential drug delivery process. Also, this study provides more reliable method to ascertain the time dependent swelling process compared to the conventional method. The important aspects is that the proposed method is truly noninvasive and is able to ascertain time dependent processes.