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( Thiagarajan Madheswaran ),( Rengarajan Baskaran ),( Raj Kumar Thapa ),( Jeong Yeon Rhyu ),( Hye Yoon Choi ),( Jong Oh Kim ),( Chul Soon Yong ),( Bong Kyu Yoo ) 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
In this study, liquid crystalline nanoparticles (LCN) have been proposed as new carrier for topical delivery of finasteride (FNS) in the treatment of androgenetic alopecia. To evaluate the potential of this nanocarrier, FNS-loaded LCN was prepared by ultrasonication method and characterized for size, shape, in vitro release, and skin permeation-retention properties. The particle size ranged from 153.8 to 170.2 nm with a cubical shape and exhibited controlled release profile with less than 20% of the drug released in the first 24 h. The release profile was significantly altered with addition of different additives. Formulation with lower monoolein exhibited higher skin permeation with a flux rate of 0.061±0.005 μg cm(-2) h(-1) in 24 h. The permeation however, significantly increased with glycerol, propylene glycol, and polyethylene glycol 400, while it declined for the addition of oleic acid. A similar trend was observed with skin retention study. In conclusion, FNS-loaded LCN could be advocated as a viable alternative for oral administration of the drug.
( Thiagarajan Madheswaran ),( Rengarajan Baskaran ),( Chul Soon Yong ),( Bong Kyu Yoo ) 영남대학교 약품개발연구소 2014 영남대학교 약품개발연구소 연구업적집 Vol.24 No.0
The aim of this study was to investigate the capability of two surfactants, Cremophor RH 40 (RH) and Cremophor EL (EL), to prepare liquid crystalline nanoparticles (LCN) and to study its influence on the topical delivery of finasteride (FNS). FNS-loaded LCN was formulated with the two surfactants and characterized for size distribution, morphology, entrapment efficiency, in vitro drug release, and skin permeation/retention. Influence of FNS-loaded LCN on the conformational changes on porcine skin was also studied using attenuated total reflectance Fourier-transform infrared spectroscopy. Transmission electron microscopical image confirmed the formation of LCN. The average particle size of formulations was in the range of 165.1-208.6 and 153.7-243.0 nm, respectively. The formulations prepared with higher surfactant concentrations showed faster release and significantly increased skin permeation. Specifically, LCN prepared with RH 2.5% presented higher permeation flux (0.100 ± 0.005 μgcm(-2)h(-1)) compared with lower concentration (0.029 ± 0.007 μgcm(-2)h(-1)). Typical spectral bands of lipid matrix of porcine skin were shifted to higher wavenumber, indicating increased degree of disorder of the lipid acyl chains which might cause fluidity increase of stratum corneum. Taken together, Cremophor surfactants exhibited a promising potential to stabilize the LCN and significantly augmented the skin permeation of FNS.
( Thiagarajan Madheswaran ),( Rengarajan Baskaran ),( Raj Kumar Thapa ),( Jeong Yeon Rhyu ),( Hye Yoon Choi ),( Jong Oh Kim ),( Chul Soon Yong ),( Bong Kyu Yoo ) 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
SCOPE: Increasing evidence indicates that polyphenols may protect against metabolic disease through activating AMP-activated protein kinase (AMPK). The aims of our study were to provide new data on the molecular mechanism(s) underlying the role of the phenolic compound, 3-caffeoyl, 4-dihydrocaffeoylquinic acid (CDCQ) from Salicornia herbacea, in the prevention of high glucose-induced lipogenesis in human HepG2 cells. METHODS AND RESULTS: Nile red staining assays were used to demonstrate lipid accumulation in the cells. Expression of sterol regulatory element-binding protein-1c (SREBP-1c) and fatty acidsynthase (FAS) gene at the levels of promoter activity, mRNA, and protein was demonstrated using transient transfection assays, quantitative RT-PCR, and Western blot analyses, respectively. We found that CDCQ suppressed high glucose-induced lipid accumulation in HepG2 cells. CDCQ strongly inhibited high glucose-induced FAS expression by modulating SREBP-1c activation. Moreover, the use of both a specific inhibitor and liver kinase B1 (LKB1)-siRNA transfected HepG2 cells showed that CDCQ activated AMPK via silent information regulator T1 (SIRT1) or LKB1 in HepG2 cells. CONCLUSION: These results indicate that CDCQ prevented lipid accumulation by blocking the expression of SREBP-1c and FAS through LKB1/SIRT1 and AMPK activation in HepG2 cells, suggesting that CDCQ plays a potential role in the prevention of lipogenesis by AMPK activation.
Thiagarajan Madheswaran,Rengarajan Baskaran,Pasupathi Sundaramoorthy,유봉규 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.4
The objective of this study is to enhance skinpermeation of finasteride and dutasteride for the treatmentof androgenetic alopecia using surface-modified liquidcrystalline nanoparticle (sm-LCN) dispersion. LCNentrapped with the drugs was prepared by using monooleinas a liquid crystal former, and surface modification wasperformed by treatment of the LCN dispersion with samevolume of 1 % v/v acetic acid solution containing chitosan. Physicochemical properties of the LCN’s were studied withregard to particle size, polydispersity index, zeta potential,and release of the drugs. Skin permeation of drugsentrapped into the LCN and sm-LCN was investigated withporcine abdominal skin using Franz diffusion cell. Cytotoxicityof the LCN’s was also studied using human skinkeratinocytes. The particle size and zeta potential of theLCN were 197.9 ± 2.5 nm and -20.2 ± 1.9 mV, respectively,and sm-LCN showed slightly bigger size and positivezeta potential due to the presence of thin coating on thesurface of the nanoparticles. Compared to LCN, sm-LCNresulted in significantly enhanced skin permeation of thedrugs whereas in vitro release was significantly reduced. Cell viability as a measure of cytotoxicity was above 80 %up to 20 lg/ml concentration of both LCN and sm-LCN. Inconclusion, sm-LCN may provide a strategy to maximizetherapeutic efficacy minimizing unwanted systemic sideeffects associated with the use of the drugs for the treatmentof androgenetic alopecia.
( Raj Kumar Thapa ),( Rengarajan Baskaran ),( Thiagarajan Madheswaran ),( Jong Oh Kim ),( Chul Soon Yong ),( Bong Kyu Yoo ) 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
The use of liquid crystalline nanoparticles is a novel approach in the field of controlled drug delivery. Tacrolimus, being a highly lipophilic dug, is easily incorporated in the hydrophobic core of these nanoparticles, which are prepared using monoolein, distilled water, and varying ratios of poloxamer 407. Characterization, including transmission electron microscopy (TEM) images, particle size, and entrapment efficieney analysis suggested the formation of cubosomes with a particke size ranging from 140 to 155 nm and entrapment level of tacrolimus as high as 99% or above. In vitro release studies, revealed a sustained release of tacrolimus for 2 weeks, with a high stability profile of nanoparticles and incorporated drug during the storage period. Therefore, it suggests the possible use of tacrolimus-loaded formulation for intradermal delivery can be useful in the treatment of locally affecting autoimmune skin disease such as psoriasis.