Synthesis and Evaluation of Novel Dendrimers with a Hydrophilic Interior as Nanocarriers for Drug Delivery
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- 作者：Renu Singh Dhanikula and Patrice Hildgen
- 刊名：Bioconjugate Chemistry
- 出版年：2006
- 出版时间：January 2006
- 年：2006
- 卷：17
- 期：1
- 页码：29 - 41
- 全文大小：336K
- 年卷期：v.17,no.1(January 2006)
- ISSN：1520-4812
文摘
Novel polyester-co-polyether dendrimers consisting of a hydrophilic core were synthesized by a combination ofconvergent and divergent syntheses. The core was synthesized from biocompatible moieties, butanetetracarboxylicacid and aspartic acid, and the dendrons from PEO (poly(ethylene oxide)), dihydroxybenzoic acid or gallic acid,and PEG monomethacrylate. The dendrimers, Den-1-(G 2) (second generation dendrimer-1) and Den-2-(G 2)(second generation dendrimer-2) consisting of 16 and 24 allyl surface groups, respectively, were obtained bycoupling the dendrons to the core. The dendrimer (Den-1-(G 2)-OH) with hydroxyl groups at the surface wassynthesized by oxidation of the allyl functional groups of Den-1-(G 2), which was divergently coupled to thedendrons to obtain the third generation dendrimer Den-1-(G 3) consisting of 32 surface groups. The modificationsin surface groups and generation of dendrimers were shown to influence the shape of dendrimers in the AFMstudies. The aggregation as well as self-assembly of dendrimers was observed at high concentration in water bylight scattering studies; however, it was reduced on dilution and in the presence of sodium chloride. Dendrimersdemonstrated good ability to encapsulate the guest molecule, with loading of 15.80 and 6.47% w/w for rhodamineand 
-carotene, respectively. UV spectroscopy proved the absence of any 
- complexation between the dendrimerand encapsulated compounds. 1H NMR and FTIR studies showed that the physical entrapment and/or hydrogenbonding by PEO in the interior and branch of the dendrimer are the mechanisms of encapsulation. The release ofthe encapsulated compounds was found to be slow and sustained, suggesting that these dendrimers can serve aspotential drug delivery vehicles.
-carotene, respectively. UV spectroscopy proved the absence of any - complexation between the dendrimerand encapsulated compounds. 1H NMR and FTIR studies showed that the physical entrapment and/or hydrogenbonding by PEO in the interior and branch of the dendrimer are the mechanisms of encapsulation. The release ofthe encapsulated compounds was found to be slow and sustained, suggesting that these dendrimers can serve aspotential drug delivery vehicles.