Abstract
Nanoparticles have been shown to be effective drug carriers in cancer therapy. Pancreatic cancer forms dense tumours which are often resistant to drug molecules. In order to overcome such multidrug resistance, new drug entities, novel delivery systems and combination therapy strategies are being explored. In this paper, we report the design and synthesis of a poly(allylamine)-based amphiphile modified with hydrophobic naphthalimido pendant groups. Bisnaphthalimide compounds have been shown to possess anticancer activity. The potential of this polymer to encapsulate, solubilize and enhance drug (5-fluorouricil and bis-(naphthalimidopropyl)-diaminooctane) cytotoxicity in BxPC-3 cells was evaluated. Our studies showed that the insoluble drugs could be formulated up to 4.3 mg mL−1 and 2.4 mg mL−1 inside the amphiphiles, respectively. Additionally, the novel poly(allylamine)-naphthalimide carrier resulted in an amplification of cytotoxic effect with drug treatment after 24 h, and was capable of reduction of 50% cell population at concentrations as low as 3 μg mL−1.
Highlights
Poor aqueous solubility or dissolution of active ingredients is one of the most significant problems hindering effective drug delivery
We propose that to a synergistic reduction cellwe viability will occur after formulation in in cell viability will occur after in this system
This study highlights the potential of a naphthalimide grafted polyallylamine as a dual functioning
Summary
Poor aqueous solubility or dissolution of active ingredients is one of the most significant problems hindering effective drug delivery. A number of solubility-enhancing strategies including co-solvents, micronization and nanonisation, amorphous solid dispersions (ASDs) [3], co-crystal formation [4], surfactants [5], complexation utilizing cyclodextrins [6] and the use of polymers [7,8,9,10]. Amphiphilic polymers have been developed as a first-rate alternative to low molecule weight surfactants for drug solubilisation. This is due to the lower excipient:drug ratios required for solubilisation and a higher degree of stability due to the decreased critical aggregation concentrations [11]. Each architecture has different physical properties, but all can be used to solubilise hydrophobic compounds
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