Palmitoylation of octreotide for incorporation into poly(amidoamine) dendrimers

초록

Poly(amidoamine) (PAMAM) dendrimers are nano-sized carrier molecules with tremendous promise in polymeric drug delivery systems. The purpose of this study was to prepare and characterize palmitoyl-octreotide-incorporated PAMAM dendrimers. As octreotide is hydrophilic, it was difficult to be incorporated into PAMAM dendrimers. This study demonstrated that the conjugation of palmitic acid (palmitoylation) was effective for the incorporation of octreotide into PAMAM dendrimers. The site-specific palmitoylation at the N-terminal amine of octreotide was successfully performed by a reversible protection approach using maleic anhydride, and the conditions for the production of the final product were optimized. The incorporation yield of palmitoyl-octreotide into PAMAM dendrimers was significantly higher than that of octreotide. The palmitoyl-octreotide-incorporated PAMAM dendrimer has a potential as a new drug delivery system for somatostatin therapeutics.

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