Evaluation of the Interaction and Drug Release from ,β-Polyaspartamide Derivatives to a Biomembrane Model

Author： Castelli F. Messina C. Craparo E. Mandracchia D. Pitarresi G.

ISSN： 1521-0464

Source： Drug Delivery, Vol.12, Iss.6, 2005-11, pp. : 357-366

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Abstract

This Article reports on a comparative study on the ability of various polymers, containing hydrophilic and/or hydrophobic groups, to interact with a biomembrane model using the differential scanning calorimetry (DSC) technique. Multilamellar vesicles of mixed dimyristoylphosphatidylcholine (DMPC) and dimyristoylphosphatidic acid (DMPA) were chosen as a model of cell membranes. The investigated samples were a water soluble polymer, the ,β-poly(N-2-hydroxyethyl)-DL-aspartamide (PHEA) and its derivatives partially functionalized with polyethylene glycol (PEG 2000 ) to obtain PHEA-PEG 2000 , with hexadecylamine (C 16 ) to obtain PHEA-C 16 , and with both compounds to obtain PHEA-PEG 2000 -C 16 . These polymers are potential candidates to prepare drug delivery systems. In particular, some samples give rise to polymeric micelles able to entrap hydrophobic drugs in an aqueous medium. The migration of drug molecules from these micelles to DMPC/DMPA vesicles also has been evaluated by DSC analysis, by using ketoprofen as a model drug.