Abstract
An amphiphilic core/shell-type polymer-based drug carrier system (HPAE- PCL-b -MPEG), composed of hyperbranched poly(aminoester)-based polymer (HPAE) as the core building block and poly(ethylene glycol)-b - poly(ε-caprolactone) diblock polymers (MPEG-b -PCL) as the shell building block, was designed. The synthesized polymers were characterized with FTIR, 1 H NMR, 13 C NMR, and GPC analysis. Monodisperse HPAE-PCL-b - MPEG nanoparticles with dimensions of < 200 nm and polydispersity index of < 0.5 were prepared by nanoprecipitation method and characterized with SEM, particle size, and zeta potential analysis. 5-Fluorouracil was encapsulated within HPAE-PCL-b -MPEG nanoparticles. In vitro drug release profiles and cytotoxicity of blank and 5-fluorouracil-loaded nanoparticles were examined against the human colon cancer HCT116 cell line. All results suggest that HPAE-PCL-b - MPEG nanoparticles offer an alternative and effective drug nanocarrier system for drug delivery applications.
Highlights
The poor solubility and short lifetime of pharmaceutical drugs restrict their development and clinical application due to complicating factors associated with their manufacturing, poor absorption, stability, and bioavailability [1,2,3]
The degree of branching (DB) of hyperbranched poly(aminoester)-based polymer (HPAE) was calculated according to Eq (4) as follows: DB = (D + T) / (D + L + T) (4) Here, L is the number of linear groups, T is the number of terminal groups, and D is the number of dendritic groups
The DB values of the HPAE polymer calculated on the basis of these three peaks (Figure 2C) using the definition of Hawker and Fréchet was found to be 0.84, which confirms the formation of highly branched products
Summary
The poor solubility and short lifetime of pharmaceutical drugs restrict their development and clinical application due to complicating factors associated with their manufacturing, poor absorption, stability, and bioavailability [1,2,3] To overcome these challenges, nanoparticles can provide a promising and alternative strategy for the encapsulation of various molecules with improved efficacy and reduced side effects. We have designed an amphiphilic core-shell multifunctional polymeric nanocarrier (HPAE-PCL-b-MPEG) by grafting poly(ethylene glycol)-b-poly( ε -caprolactone) diblock polymers (MPEG- bPCL) on the hyperbranched poly(aminoester)-based polymer (HPAE) backbone to evaluate their effectiveness for drug delivery applications. For this purpose, HPAE-PCL-b-MPEG polymer was synthesized as a result of a series of reactions and characterized. HPAE-PCL-b-MPEG nanoparticles were found to be an alternative and effective drug nanocarrier system for drug delivery applications
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