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Lee, Sang Gon,Kim, Chang Hyun,Sung, Si Woo,Lee, Eun Seok,Goh, Min Su,Yoon, Ho Yub,Kang, Myung Joo,Lee, Sangkil,Choi, Young Wook Dove Medical Press 2018 International journal of nanomedicine Vol.13 No.-
<P><B>Background</B></P><P>To facilitate selective and enhanced drug delivery to hepsin (Hpn)-expressing cancer cells, RIPL peptide (IPLVVPLRRRRRRRRC, 16-mer)-conjugated nanostructured lipid carriers (RIPL-NLCs) were developed.</P><P><B>Methods</B></P><P>NLCs were prepared using a solvent emulsification-evaporation method and the RIPL peptide was conjugated to the maleimide-derivatized NLCs via the thiol-maleimide reaction. Employing a fluorescent probe (DiI), in vitro target-selective intracellular uptake behaviors were observed using fluorescence microscopy and flow cytometry. Separately, docetaxel (DTX) was encapsulated by pre-loading technique, then cytotoxicity and drug release were evaluated. In vivo antitumor efficacy was investigated in BALB/c nude mice with SKOV3 cell tumors after intratumoral injections of different DTX formulations at a dose equivalent to 10 mg/kg DTX.</P><P><B>Results</B></P><P>RIPL-NLCs showed positively charged nanodispersion, whereas NLCs were negatively charged. DTX was successfully encapsulated with an encapsulation efficiency and drug loading capacity of 95–98% and 44-46 µg/mg, respectively. DTX release was diffusion-controlled, revealing the best fit to the Higuchi equation. Cellular uptake of DiI-loaded RIPL-NLCs was 8.3- and 6.2-fold higher than that of DiI-loaded NLCs, in Hpn(+) SKOV3 and LNCaP cells, respectively. The translocation of RIPL-NLCs into SKOV3 cells was time-dependent with internalization within 1 h and distribution throughout the cytoplasm after 2 h. DTX-loaded RIPL-NLCs (DTX-RIPL-NLCs) revealed dose-dependent in vitro cytotoxicity, while drug-free formulations were non-cytotoxic. In SKOV3-bearing xenograft mouse model, DTX-RIPL-NLCs significantly inhibited tumor growth: the inhibition ratios of the DTX solution-treated and DTX-RIPL-NLC-treated groups were 61.4% and 91.2%, respectively, compared to those of the saline-treated group (control).</P><P><B>Conclusion</B></P><P>RIPL-NLCs are good candidates for Hpn-selective drug targeting with a high loading capacity of hydrophobic drug molecules.</P>
Lee, Sangkil,Lee, Jaehwi,Choi, Young Wook Pharmaceutical Society of Japan 2008 Biological & pharmaceutical bulletin Vol.31 No.4
<P>Liquid intraurethral prostaglandin E<SUB>1</SUB> (PGE<SUB>1</SUB>) delivery system was developed using self-microemulsifying drug delivery system (SMEDDS). For this, pseudo-ternary phase diagrams were constructed and characterized. The viscosity of optimized formulation was increased gradually upon the addition of water and it was decreased from the water contents over 40%. With excessive mass of water, the present system transformed to a free flowing microemulsion. These results demonstrate that the present liquid PGE<SUB>1</SUB> SMEDDS formulation might stay in the urethra as a viscous sol or gel state with contacting the moisture of urethra and easily eliminated by urination. Draize test and long-term stability study revealed that the present system would be safe and PGE<SUB>1</SUB> would be stable for more than one year at 4 °C, respectively. In the feline animal model, SMEDDS formulation was as effective as PGE<SUB>1</SUB> intracavernosal injections in terms of ICP (intracavernosal pressure), penile length increment, and erection sustaining time was more elongated than PGE<SUB>1</SUB> injections. Therefore, SMEDDS was considered as a promising PGE<SUB>1</SUB> intraurethral liquid formulation for erectile dysfunction treatment.</P>
Sangkil Lee,Rakesh Bastola 한국약제학회 2019 Journal of Pharmaceutical Investigation Vol.49 No.3
Vaccine adjuvants enhance immunogenic responses of antigens and increase potency of vaccines. Physicochemical properties of particulate vaccine adjuvants namely, particle size, surface charge, hydrophobicity, shape and composition play an important role to determine their activity and potency. Various studies have been done using different types of particulate vaccine adjuvants to correlate their physicochemical properties with immune responses. Generally, change in particle size does not show any trend in modulation of immunogenicity, however, it directly influences on cellular uptake of particles, leading to alteration of cytokine profile and induction of Th1 and/or Th2 responses. Usually, positively charged adjuvant particles undergo higher cellular uptake than negatively charged particles and hydrophobic particles undergo cellular uptake more efficiently than hydrophilic particles. Furthermore, shape and composition of adjuvant particles also influence on immune responses. This review gives an insight into the impact of particle size, surface charge, hydrophobicity, shape and composition of particulate vaccine adjuvants in modulating immune responses.
Sangkil Lee,이재휘,최영욱 대한화학회 2007 Bulletin of the Korean Chemical Society Vol.28 No.1
To prepare freeze-dried ascorbyl palmitate (AsP)-containing liposome which can protect the drug from moisture attack and be used instantly by mixing with water for anti-aging and skin whitening therapy, AsP was encapsulated into liposomes and freeze-dried with trehalose. The freeze-dried liposome formulations were characterized by measuring water contents, particle size, time required for complete reconstitution. With the freeze-dried liposomes, we performed the stability test under accelerated conditions, skin permeation and localization test. The measurement of the time to perfect reconstitution showed that the freeze-dried liposomes can be changed to their initial state rapidly and short term stability test of AsP in reconstituted liposomes under accelerated conditions confirmed that the stability of AsP was considerably enhanced as compared to freshly prepared liposomes. The skin permeation and localization properties of AsP in reconstituted liposomes were not significantly different, indicating that the liposomal structures were maintained before and after freeze-drying. In conclusion, the freeze-drying method provided a possible way to overcome the instability issue of AsP induced by the moisture and reproduced similar skin permeation and localization properties as shown by freshly prepared liposomes.
이상길(Sangkil Lee),김성도(Sungdo Kim),이강영(Gangyoung Lee) 한국추진공학회 2008 한국추진공학회지 Vol.12 No.5
Each weapon systems muzzle velocity can be used as basic data for operating accurate automatic firing control system. Even among the same kind of ammunition, despite taking into consideration various battlefield parameters, irregular performance causes difficulties in obtaining accurate muzzle velocity data. In this study, pressure in the gun barrel was measured, the experimental relationship between chamber pressure and the projectiles base pressure was found, and a method of obtaining muzzle velocity was researched. Through this method, data regarding muzzle velocity is offered that corrects irregular performance.
포 발사 고체연료 램제트 탄의 설계 및 성능해석에 관한 연구
이상길(Sangkil Lee),김창기(Changkee Kim),이상승(Sangseung Lee) 한국추진공학회 2008 한국추진공학회지 Vol.12 No.3
In this study, the design method of a 155 mm Solid Fuel Ramjet projectile is proposed and a flight performance analysis program through mathematical modelling is developed. Through flight performance analysis, ramjet performance during flight, which is comprised of thrust, specific impulse, pressure recovery ratio, location of shock waves, and magnitude of drag, was predicted. The results show that compared to Rocket Assisted Projectile(RAP), the range was increased by 90 %. Furthermore, how variations in nozzle exit area ratio and the intake area cause variations in range was observed. This research on modeling and simulation methodology will provide useful data for future development of solid fuel ramjet projectiles.