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作者 Devarakonda, Bharathi
書名 Poly(amidoamine) (PAMAM) dendrimers as solubility and permeation enhancers
國際標準書號 9780542068737
book jacket
說明 220 p
附註 Source: Dissertation Abstracts International, Volume: 66-04, Section: B, page: 2079
Major Professor: Melgardt M. de Villiers
Thesis (Ph.D.)--University of Louisiana at Monroe, 2005
The aim of this study was to synthesize and investigate the solubilization and permeation enhancing potential of PAMAM dendrimers with different generation sizes and functional groups. Dendrimers are highly branched and reactive three-dimensional macromolecules with all bonds emanating from a central core. Since their introduction in the mid 1980's, this novel class of polymeric materials has attracted considerable attention because of their unique structures and properties. Compared with traditional linear polymers, dendrimers have more accurately controlled structures, with a globular shape, a single molecular weight, and a large number of controllable peripheral surface functionalities
Many families of dendrimers with various core molecules and building monomers have been synthesized and are commercially available now. But, the family of dendrimers most investigated for drug delivery is the PAMAM dendrimers. PAMAM dendrimers are biocompatible, non-immunogenic, water-soluble and possess terminal-modifiable amine functional groups for binding various targeting or guest molecules. The internal cavities of PAMAM dendrimers can host metals or guest molecules because of the unique functional architecture, which contains tertiary amines and amide linkages
In the present study, the solubilization potential of PAMAM dendrimers was investigated using four practically water insoluble drugs (niclosamide, nifedipine, furosemide, and paclitaxel) as model drugs. Further, the solubilization potential of the dendrimers was compared with that of traditionally used supramolecular compounds, i.e. cyclodextrins. The permeation enhancement potential of the dendrimers was investigated after oral and topical administration of drug-dendrimer complexes, and on the permeability of paclitaxel across cancerous cells
Results showed that PAMAM dendrimers have the potential to significantly increase the aqueous solubility of these model drugs. In addition, significantly higher solubility of the drugs was observed in the presence of the dendrimers than in the presence of cyclodextrins. Also in vitro permeation studies using dendrimers as permeation/penetration enhancers showed that PAMAM dendrimers have the potential to significantly increase the permeability of drugs for oral and topical delivery and cellular entry of drugs across cancerous cells. Significant differences in the solubilization and permeation enhancement properties were observed between the PAMAM dendrimers with different generation sizes and surface functional groups (amine terminated versus ester terminated dendrimers)
School code: 1352
DDC
Host Item Dissertation Abstracts International 66-04B
主題 Chemistry, Pharmaceutical
Health Sciences, Pharmacy
0491
0572
Alt Author University of Louisiana at Monroe
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