title: Drug delivery investigations of quaternised poly(propylene imine) dendrimer using nimesulide as a model drug.
abstract: This study describes the demonstration of quaternized poly(propylene imine) dendrimer of generation-3, QPPI (G3) as a drug carrier for poorly soluble drug nimesulide (NMD, an anti-inflammatory drug). QPPI (G3) was prepared by treating the surface amine groups of poly(propylene imine) dendrimer with glycidyltrimethyl ammonium chloride and it was characterized with FTIR, (1)H and (13)C NMR and MALDI-TOF mass spectral techniques. The drug carrying potential of QPPI (G3) was assessed by analyzing drug solubility, in vitro release and cytotoxicity studies. The observed results reveal that the aqueous solubility of NMD has been dramatically increased in the presence of QPPI (G3) and also can sustain the release of NMD. It is further noticed that the complexation of NMD with QPPI (G3) is responsible for increased solubility and sustained release. This complexation was evidenced through NMR ((1)H & 2D) and UV-vis spectral techniques, DSC and DLS studies. Cytotoxicity study through MTT assay on Vero and HBL-100 cell lines reveal that this dendrimer increase the biocompatibility and the tolerance concentration of NMD in drug-dendrimer formulations. The observed results prove that the QPPI (G3) is one of the new promising candidate for effective delivery of NMD.
authors.affiliation: Department of Physical Chemistry, School of Chemical Sciences, University of Madras, Maraimalai Campus, Guindy, Chennai 600 025, TamilNadu, India. Electronic address: dr.e.murugan@gmail.com.
authors.forename: E
authors.initials: E
authors.lastname: Murugan
authors.affiliation: Department of Physical Chemistry, School of Chemical Sciences, University of Madras, Maraimalai Campus, Guindy, Chennai 600 025, TamilNadu, India.
authors.forename: D P
authors.initials: DP
authors.lastname: Geetha Rani
authors.affiliation: Department of Physical Chemistry, School of Chemical Sciences, University of Madras, Maraimalai Campus, Guindy, Chennai 600 025, TamilNadu, India.
authors.forename: V
authors.initials: V
authors.lastname: Yogaraj
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D016923:Cell Death / Q000187:drug effects; D002460:Cell Line; D050091:Dendrimers / Q000138:chemical synthesis / Q000737:chemistry*; D016503:Drug Delivery Systems; D005612:Freeze Drying; D008027:Light; D009682:Magnetic Resonance Spectroscopy; D011126:Polypropylenes / Q000138:chemical synthesis / Q000737:chemistry*; D012542:Scattering, Radiation; D012995:Solubility; D012996:Solutions; D013056:Spectrophotometry, Ultraviolet; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D050091:Dendrimers; D011126:Polypropylenes; D012996:Solutions; D013449:Sulfonamides; C443641:poly(propyleneimine); C012655:nimesulide
keywords: Cytotoxicity; Drug carrier; In vitro release; Nimesulide; Poly(propylene imine) dendrimer; Solubility