title: Designing and in-vitro characterization of micelle forming amphiphilic PEGylated rapamycin nanocarriers for the treatment of gastric cancer.
abstract: The present study aims to develop and explore the use of PEGylated rapamycin (RP-MPEG) micelles for the treatment of gastric cancer. RP-MPEG was synthesized and characterized by using IR, H(1) NMR and C(13) NMR. RP-MPEG was prepared in the form of micelles and characterized by using field emission scanning electron microscopy, dynamic light scattering, zeta sizer, chromatographic analyses and photostability studies. The cytotoxicity studies of RP-MPEG micelles were conducted on specific CRL 1739 human gastric adenocarcinoma and CRL 1658 NIH-3T3 mouse embryonic fibroblast cell lines. RP-MPEG micelles showed the particle size distribution of 125±0.26 nm with narrow size distribution (polydispersity index 0.127±0.01). The surface charge of RP-MPEG micelles was found to be -12.3 mV showing enhanced anticancer activity against the CRL 1739 human gastric adenocarcinoma cell lines with an IC50 value of 1 mcg/ml.
authors.forename: Palanirajan Vijayaraj
authors.initials: PV
authors.lastname: Kumar
authors.affiliation: Faculty of Pharmaceutical Sciences, No: 1, Jalan Menara Gading, UCSI University (South Campus), Taman Connaught, Cheras 56000, Kuala Lumpur. Malaysia. vijayarajkumar_p@yahoo.com.
authors.forename: Bontha Venkata Subrahmanya
authors.initials: BV
authors.lastname: Lokesh
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy / Q000473:pathology; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D049109:Cell Proliferation / Q000187:drug effects; D002478:Cells, Cultured; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers / Q000138:chemical synthesis* / Q000737:chemistry; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D008823:Micelles; D041681:NIH 3T3 Cells; D053758:Nanoparticles / Q000737:chemistry; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry*; D020123:Sirolimus / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D013274:Stomach Neoplasms / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship; D013499:Surface Properties; D013501:Surface-Active Agents / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; D013501:Surface-Active Agents; D011092:Polyethylene Glycols; D020123:Sirolimus