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The Effect of Coenzyme Q10 on the Pharmacokinetic Parameters of Theophylline
Rengarajan Baskaran,용철순,최한곤,유봉규,Srinivasan Shanmugam,Santhoshkumar Nagayya-Sriraman,김주현,정태천 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.7
Interaction of a drug with other drugs and dietary supplements is becoming an emerging issue for patients and health insurance authorities due to awareness of adverse drug event. In this study, we examined the effects of coenzyme Q10 (CoQ10), one of the most popular dietary supplements, on the pharmacokinetic parameters of theophylline in rats. The pharmacokinetic parameters of theophylline changed significantly when the drug was administered after five consecutive days of pretreatment with CoQ10. Time to reach maximum plasma concentration of theophylline delayed when the drug was administered after the pretreatment with CoQ10. Maximum plasma concentration and area under the curve of theophylline were about two-fold increased and other pharmacokinetic parameters such as half-life and volume of distribution were also changed significantly. Therefore, although CoQ10 is generally considered a safe dietary supplement, it appears that patients on theophylline therapy should use caution when they take CoQ10.
Rengarajan, Thamaraiselvan,Nandakumar, Natarajan,Rajendran, Peramaiyan,Haribabu, Lingaiah,Nishigaki, Ikuo,Balasubramanian, Maruthaiveeran Periyasamy Asian Pacific Journal of Cancer Prevention 2014 Asian Pacific journal of cancer prevention Vol.15 No.4
Development of drugs from natural products has been undergoing a gradual evoluation. Many plant derived compounds have excellent therapeutic potential against various human ailments. They are important sources especially for anticancer agents. A number of promising new agents are in clinical development based on their selective molecular targets in the field of oncology. D-pinitol is a naturally occurring compound derived from soy which has significant pharmacological activitites. Therefore we selected D-pinitol in order to evaluate apoptotic potential in the MCF-7 cell line. Human breast cancer cells were treated with different concentrations of D-pinitol and cytotoxicity was measured by MTT and LDH assays. The mechanism of apoptosis was studied with reference to expression of p53, Bcl-2, Bax and NF-kB proteins. The results revealed that D-pinitol significantly inhibited the proliferation of MCF-7 cells in a concentration-dependent manner, while upregulating the expression of p53, Bax and down regulating Bcl-2 and NF-kB. Thus the results obtained in this study clearly vindicated that D-pinitol induces apotosis in MCF-7 cells through regulation of proteins of pro- and anti-apoptotic cascades.
Clinical development of photodynamic agents and therapeutic applications
Rengarajan Baskaran,이정한,양수근 한국생체재료학회 2018 생체재료학회지 Vol.22 No.4
Background: Photodynamic therapy (PDT) is photo-treatment of malignant or benign diseases using photosensitizing agents, light, and oxygen which generates cytotoxic reactive oxygens and induces tumour regressions. Several photodynamic treatments have been extensively studied and the photosensitizers (PS) are key to their biological efficacy, while laser and oxygen allow to appropriate and flexible delivery for treatment of diseases. Introduction: In presence of oxygen and the specific light triggering, PS is activated from its ground state into an excited singlet state, generates reactive oxygen species (ROS) and induces apoptosis of cancer tissues. Those PS can be divided by its specific efficiency of ROS generation, absorption wavelength and chemical structure. Main body: Up to dates, several PS were approved for clinical applications or under clinical trials. Photofrin® is the first clinically approved photosensitizer for the treatment of cancer. The second generation of PS, Porfimer sodium (Photofrin®), Temoporfin (Foscan®), Motexafin lutetium, Palladium bacteriopheophorbide, Purlytin®, Verteporfin (Visudyne®), Talaporfin (Laserphyrin®) are clinically approved or under-clinical trials. Now, third generation of PS, which can dramatically improve cancer-targeting efficiency by chemical modification, nano-delivery system or antibody conjugation, are extensively studied for clinical development. Conclusion: Here, we discuss up-to-date information on FDA-approved photodynamic agents, the clinical benefits of these agents. However, PDT is still dearth for the treatment of diseases in specifically deep tissue cancer. Next generation PS will be addressed in the future for PDT. We also provide clinical unmet need for the design of new photosensitizers.
The Effect of Coenzyme Q10 on the Pharmacokinetic Parameters of Theophylline
Baskaran, Rengarajan,Shanmugam, Srinivasan,Nagayya-Sriraman, Santhoshkumar,Kim, Ju-Hyun,Jeong, Tae-Chun,Yong, Chul-Soon,Choi, Han-Gon,Yoo, Bong-Kyu 대한약학회 2008 Archives of Pharmacal Research Vol.31 No.7
Interaction of a drug with other drugs and dietary supplements is becoming an emerging issue for patients and health insurance authorities due to awareness of adverse drug event. In this study, we examined the effects of coenzyme Q10 (CoQ10), one of the most popular dietary supplements, on the pharmacokinetic parameters of theophylline in rats. The pharmacokinetic parameters of theophylline changed significantly when the drug was administered after five consecutive days of pretreatment with CoQ10. Time to reach maximum plasma concentration of theophylline delayed when the drug was administered after the pretreatment with CoQ10. Maximum plasma concentration and area under the curve of theophylline were about two-fold increased and other pharmacokinetic parameters such as half-life and volume of distribution were also changed significantly. Therefore, although CoQ10 is generally considered a safe dietary supplement, it appears that patients on theophylline therapy should use caution when they take CoQ10.
( 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.
( Srinivasan Shanmugam ),( Rengarajan Baskaran ),( Prabagar Balakrishnan ),( Pritam Thapa ),( Chul Soon Yong ),( Bong Kyu Yoo ) 영남대학교 약품개발연구소 2012 영남대학교 약품개발연구소 연구업적집 Vol.22 No.0
The objectives of this study was to prepare solid self-nanoemulsifying drug delivery system (S-SNEDDS) containing phosphatidylcholine (PC), an endogenous phospholipid with excellent in vivo solubilization capacity, as oil phase for the delivery of bioactive carotenoid lutein, by spray drying the SNEDDS (liquid system) containing PC using colloidal silica (Aerosil® 200 VV Pharma) as the inertsolid carrier, and to evaluate the enhanced bioavailability (BA) of lutein from S-SNEDDS. The droplet size analyses revealed droplet size of less than 100 nm. The solid state characterization of S-SNEDDS by SEM, DSC, and XRPD revealed the absence of crystalline lutein in the S-SNEDDS. The bioavailability study performed in rabbits resulted in enhanced values of C(max) and AUC for S-SNEDDS. The enhancement of C(max) for S-SNEDDS was about 21-folds and 8-folds compared with lutein powder (LP) and commercial product (CP), respectively. The relative BA of S-SNEDDScompared with CP or LP was 2.74-folds or 11.79-folds, respectively. These results demonstrated excellent ability of S-SNEDDS containing PC as oil phase to enhance the BA of lutein in rabbits. Thus, S-SNEDDS containing PC as oil phase could be a useful lipid drug delivery system for enhancing the BA of lutein in vivo.
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.
Ajay Vijayakumar,Rengarajan Baskaran,맹한주,유봉규 대한약학회 2017 Archives of Pharmacal Research Vol.40 No.7
The aim of this study was to develop a ginsenoside- modified nanostructured lipid carrier (G-NLC) dispersion containing curcumin. The NLC was prepared by melt emulsification with slight modification process. Different G-NLC dispersion systems were prepared using lipid carrier matrix composed of ginsenoside, phosphatidylcholine, lysophosphatidylcholine, and hydrogenated bean oil. TEM image of the nanoparticles in the NLC dispersion showed core/shell structure, and there was corona-like layer surrounding the particles in the G-NLC. The mean particle size of G-NLC dispersion was in the range of about 300–500 nm and stayed submicron size up to 12 months. The in vitro release of curcumin was faster in pH 1.2 compared to pH 6.8 and it showed linear release pattern after lag time of 1 h. When the G-NLC dispersion was orally administered to rats, Cmax of the free curcumin was 15.2 and 32.3 ng/mL at doses of 50 and 100 mg/kg, respectively, while it was below quantification limit when curcumin was administered as of dispersion in distilled water. Based on these results, it is certain that ginsenoside modulated the NLC dispersion, leading to enduring shelflife of the dispersion system and enhanced bioavailability. These results strongly suggest that ginsenoside holds a promising potential as a pharmaceutical excipient in the pharmaceutical industries to increase the utility of various bioactives.