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Title: Drug derivatization for enhancement of half life
Researcher: Gupta, Vivek
Guide(s): Agrawal, R K
Shrivastava, A K
Keywords: Pharmacy
Drug Profile
half life
Drug derivatization
Upload Date: 30-Jul-2013
University: Suresh Gyan Vihar University
Completed Date: 2011
Abstract: Some of the drugs are having very short half-life, to compensate this problem it is common practice to increase the dosage, frequency or prolongation of administration of drug to maintain effective therapeutic concentration in patient. In this study a drug delivery scaffold was designed and synthesized based on polyethylene glycol (PEG)-ethylene diamine tetra acetic acid (EDTA) based poly(amidoamine) (PAMAM) star polymer (with 16 primary amine group on surface). Cloxacillin, Cephalexin and Ciprofloxacin were used as a model drugs having short half life to conjugate with PEGylated dendrimer. These drugs were coupled to star polymer via ester bond. Fourier transform infrared spectroscopy (FT-IR) and proton nuclear magnetic resonance (1H-NMR) was used to characterize the intermediate and drug-star-polymer conjugates. In-vitro activity of derivatized drugs compared to standard drug alone, it was found that zone of inhibition obtained by both category of drugs (standard and derivatized drugs) are almost similar. That means drug derivatization does not altering the antibacterial activity of drugs. To investigate pharmacokinetic parameters, selected drugs alone and modified drugs [(Drug-PEG)16-Dendrimer] were intravenously injected into rats. All the modified drugs demonstrated a dramatic increase in half-life than drugs alone. These studies suggest the use of these new PEG based EDTA core dendrimer support as a valuable alternative for enhancing biological half-life of drugs.
Pagination: x, 226p.
Appears in Departments:Department of Pharmacy

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02_certificate.pdf63.27 kBAdobe PDFView/Open
02_declaration.pdf63.27 kBAdobe PDFView/Open
03_certificates.pdf182.21 kBAdobe PDFView/Open
04_contents.pdf10.52 kBAdobe PDFView/Open
05_acknowledgements.pdf28.12 kBAdobe PDFView/Open
06_list of figures.pdf79.62 kBAdobe PDFView/Open
07_list of tables.pdf94.19 kBAdobe PDFView/Open
08_list of abbreviations.pdf13.2 kBAdobe PDFView/Open
09_abstract.pdf9.68 kBAdobe PDFView/Open
10_chapter 1.pdf730.57 kBAdobe PDFView/Open
11_chapter 2.pdf761.55 kBAdobe PDFView/Open
12_chapter 3.pdf2.18 MBAdobe PDFView/Open
13_chapter 4.pdf497.3 kBAdobe PDFView/Open
14_chapter 5.pdf224.13 kBAdobe PDFView/Open
15_chapter 6.pdf106.2 kBAdobe PDFView/Open
16_chapter 7.pdf9.89 kBAdobe PDFView/Open
17_appendix.pdf35.2 kBAdobe PDFView/Open

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