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( Thiruganesh Ramasamy ),( Ju Yeon Choi ),( Hyuk Jun Cho ),( Subbaih Kandasamy Umadevi ),( Beom Soo Shin ),( Han Gon Choi ),( Chul Soon Yong ),( Jong Oh Kim ) 영남대학교 약품개발연구소 2015 영남대학교 약품개발연구소 연구업적집 Vol.25 No.-
Purpose Irinotecan (IRI) is a broad spectrum chemotherapeutic agent used individually or in combination to treat multiple malignancies. Present study aimed at developing polypeptide-based block ionomer complex (BIC) micelles to improve the pharmacokinetic and antitumor response of IRI. Methods Irinotecan-loaded BIC micelles (IRI-BIC) was prepared and evaluated in terms of various physicochemical and biological parameters including size, shape, release, cytotoxicity, and pharmacokinetic analysis. In vivo antitumor efficacy was investigated in SCC-7 bearing xenograft tumor model. Results IRI was successfully incorporated into the ionic cores of poly(ethylene glycol)-b-poly(aspartic acid) (PEG-b-PAA) with a high drug loading capacity (~80%). The electrostatically assembled BIC micelles were nanosized (~50 nm) with uniform size distribution pattern (PDI~0.1). The BIC micelles exhibited pHsensitiveness with limited release of IRI at physiological conditions and significantly enhanced the release rate at acidic conditions, making it an ideal delivery system for tumor targeting. The IRI-BIC showed a dose-dependent cytotoxicity in SCC-7 and A-549 cancer cell lines. Pharmacokinetic studies clearly showed that BIC micelles improved the IRI blood circulation time and decreased its elimination rate constant, while that of free IRI, rapidly eliminated from the central compartment. Moreover, IRI-BIC showed superior therapeutic performance with no toxicity in BALB/c nude xenograft mice. The micelle treated group showed an inhibition rate of ~66% compared to free IRI treated group. Conclusions Taken together, BIC micelles could be a potentially useful nanovehicle with promising applicability in systemic tumor treatment.
Hima Bindu Ruttala,Thiruganesh Ramasamy,Thiagarajan Madeshwaran,Tran Tuan Hiep,Umadevi Kandasamy,오경택,최한곤,용철순,김종오 대한약학회 2018 Archives of Pharmacal Research Vol.41 No.2
The development of novel drug delivery systemsbased on well-defined polymer therapeutics has led tosignificant improvements in the treatment of multiple disorders. Advances in material chemistry, nanotechnology,and nanomedicine have revolutionized the practices ofdrug delivery. Stimulus-responsive material-based nanosizeddrug delivery systems have remarkable propertiesthat allow them to circumvent biological barriers andachieve targeted intracellular drug delivery. Specifically,the development of novel nanocarrier-based therapeutics isthe need of the hour in managing complex diseases. In thisreview, we have briefly described the fundamentals of drugtargeting to diseased tissues, physiological barriers in thehuman body, and the mechanisms/modes of drug-loadedcarrier systems. To that end, this review serves as acomprehensive overview of the recent developments instimulus-responsive drug delivery systems, with focus ontheir potential applications and impact on the future of drugdelivery.
( Thiruganesh Ramasamy ),( Bijay Kumar Poudel ),( Himabindu Ruttala ),( Ju Yeon Choi ),( Truong Duy Hieu ),( Kandasamy Umadevi ),( Yu Seok Youn ),( Han Gon Choi ),( Chul Soon Yong ),( Jong Oh Kim ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
Nanofabrication of polymeric micelles through self-assembly of an ionic block copolymer and oppositely charged small molecules has recently emerged as a promising method of formulating delivery systems. The present study therefore aimed to investigate the interaction of cationic drugs doxorubicin (DOX) and mitoxantrone (MTX) with the anionic block polymer poly(ethylene oxide)-block-poly(acrylic acid) (PEO-b-PAA) and to study the influence of these interactions on the pharmacokinetic stability and anti-tumor potential of the formulated micelles in clinically relevant animal models. To this end, individual DOX and MTX-loaded polyelectrolyte complex micelles (PCM) were prepared, and their physicochemical properties and pH-responsive release profiles were studied, MTX-PCM and DOX-PCM exhibited a differ-ent release profile under all pH conditions tested. MTX-PCM exhibited a monophasic release profile with no initial burst, while DOX-PCM exhibited a biphasic release, DOX-PCM showed a higher cellular uptake than that shown by MTX-PCM in A-549 cancer cells. Furthermore, DOX-PCM induced higher apoptosis of cancer cells than that induced by MTX-PCM, Importantly, both MTX-PCM and DOX-PCM showed pro-longed blood circulation. MTX-PCM improved the AUC<sub>all</sub> of MTX 4-fold compared to a 3-fold increase by DOX-PCM for DOX, While a definite difference in blood circulation was observed between MTX-PCM and DOX-PCM in the pharmacokinetic study, both MTX-PCM and DOX-PCM suppressed tumor growth to the same level as the respective free drugs, indicating the potential of PEGylated polymeric micelles as effective delivery systems. Taken together, our results show that the nature of interactions of cationic drugs with the polyionic copolymer can have a tremendous influence on the biological performance of a delivery system.