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      • KCI등재

        PLGA Microsphere Addition to 1-Hydroxy-2-napthoic Acid Enhances the Sustained Release of Escitalopram

        강석희,김보연,권혁일,김혜민,조선항,박정숙,한희동,신병철 대한화학회 2019 Bulletin of the Korean Chemical Society Vol.40 No.8

        Escitalopram (ET), a selective serotonin reuptake inhibitor, has been utilized for the treatment of depression and anxiety. However, ET has serious side effects such as nausea, leading to an increased therapeutic dose, needing multiple administrations. Therefore, to overcome these issues, we developed ET encapsulated poly (d,l-lactic-co-glycolic acid) (PLGA) microspheres (PLGA-MS) as a sustained release carrier to maintain therapeutic efficacy. The mean particle size of the PLGA-MSs was measured by microscopy. Loading efficiency was measured by high performance liquid chromatography (HPLC). Morphologies were determined by microscopy and scanning electron microscopy (SEM). Differential scanning calorimetry (DSC) was used for thermal analysis and glass transition temperature determination. Mean particle size of the ET-loaded PLGA-MSs was 129?±?14??m, loading efficiency was 36.8?±?9.1%, and encapsulation efficiency was up to 70.6?±?6.8%. Loading efficiency and encapsulation efficiency were increased by the addition of 1-hydroxy-2-naphthoic acid (HNA). ET was released from PLGA-MS for 4?weeks, which was longer than ET release from PLGA-MS without the addition of HNA. Taken together, we demonstrate the optimum condition for sustained release of ET from PLGA-MS with the addition of HNA, and that this approach may be useful for depression therapy.

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        Dual Functional Gd(III)-DOTA Liposomes for Cancer Therapy and Diagnosis as a Theragnostic Carrier

        한희동,정석현,성하수,조선항,신병철 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.1

        Development of dual functional liposome has been studied for cancer theragnostics. Therefore, we focused on ultrasound-sensitive liposomes with doxorubicin (DOX) and gadolinium (Gd) as a theragnostic carrier having a potential for cancer therapy and diagnosis. In this study, Gd(III)-DOTA-modified sonosensitive liposomes (GL) was developed using chemically synthesized Gd(III)-DOTA-DPPE lipid. Sonosensitivity of GL to 1 MHz ultrasound induced 25% of DOX release. The relaxivities (r1) of GL were 7.33-10.34 mM−1s−1, which was higher than that of MR-bester®. Intracellular delivery of DOX from GL by ultrasound irradiation was evaluated according to ultrasound intensity, resulting in increase of uptake of DOX released from ultrasoundtriggered GLs compared to GL3 or Doxil® without ultrasound. Taken together, this study shows that the paramagnetic and sonosensitive liposomes, GL, is a novel and highly effective delivery system for drug with the potential for broad applications in human disease.

      • Controlled Release of BCNU from Locally Implanted Polymeric Wafer for the Treatment of Brain Tumor

        이진수,김문석,이해방,채강수,김선화,조선항,강길선 한국생체재료학회 2003 생체재료학회지 Vol.7 No.4

        The localized delivery of anticancer agents using polymeric implants is an alternative to the systemic administration for the treatment of malignant glioma. The purpose in the present study was to develop an implantable polymeric device, which can release intact BCNU for short-term period from day 4 to day 7 depending on drug loading amount, and to evaluate its in vitro anti-tumor activity against XF 498 human CNS tumor cells and in vivo anti-tumor activity against tumor-bearing animal model of L1210 mouse leukemia cells with the parameter of mean survival time of animals. In vitro release of BCNU in pH 7.4 phosphate buffered saline (PBS) was prolonged up to 1 week after initial burst release. Anti-tumor activity of BCNU-loaded poly(D,L-lactide-co-glycolide) (PLGA) wafer against XF 498 human CNS tumor cells continued over 10 days and, PLGA only did not affect the growth of the cells. Meanwhile, the cytotoxicity of BCNU powder disappeared within 12 h. For in vivo anti-tumor activity of BCNU-loaded PLGA wafer against tumor-bearing animal model of L1210 mouse leukemia cells, the interstitial release of BCNU implanted in the flank of mice resulted in 5-fold increased survival, compared with a 1.2-fold increased survival after systemic administration of BCNU. These results suggested that this short-term delivery of BCNU from PLGA wafers may be useful in the development of implantable polymeric device for malignant glioma and clinical trials.

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