Abstract
Nanoparticle (NP) compositions such as hydrophobicity and surface charge are vital to determine the presence and amount of human serum albumin (HSA) binding. The HSA binding influences drug release, biocompatibility, biodistribution, and intercellular trafficking of nanoparticles (NPs). Here, we prepared 2 kinds of nanomaterials to investigate HSA binding and evaluated drug release of HSA-bound NPs. Polysaccharides (pullulan) carboxyethylated to provide ionic derivatives were then conjugated to cholesterol groups to obtain cholesterol-modified carboxyethyl pullulan (CHCP). Cholesterol-modified pullulan (CHP) conjugate was synthesized with a similar degree of substitution of cholesterol moiety to CHCP. CHCP formed self-aggregated NPs in aqueous solution with a spherical structure and zeta potential of −19.9±0.23 mV, in contrast to −1.21±0.12 mV of CHP NPs. NPs could quench albumin fluorescence intensity with maximum emission intensity gradually decreasing up to a plateau at 9 to 12 h. Binding constants were 1.12×105 M−1 and 0.70×105 M−1 to CHP and CHCP, respectively, as determined by Stern-Volmer analysis. The complexation between HSA and NPs was a gradual process driven by hydrophobic force and inhibited by NP surface charge and shell-core structure. HSA conformation was altered by NPs with reduction of α-helical content, depending on interaction time and particle surface charges. These NPs could represent a sustained release carrier for mitoxantrone in vitro, and the bound HSA assisted in enhancing sustained drug release.
Highlights
Nanomaterials hold great promise for use in drug delivery, as image contrast agents, and for diagnostic purposes [1,2,3]
carboxyethyl pullulan (CEP) show that besides an absorption peak at 1640 cm21 (C-O stretch), the band at 1733 cm21 (C = O) confirms that the carboxyethyl group was conjugated to pullulan
cholesterol-modified carboxyethyl pullulan (CHCP) 1H-nuclear magnetic resonance (NMR) spectra analysis allowed for identifying protons corresponding to pullulan chain at: 0.40–2.40, 2.49 (DMSO-d6), and 2.53 (2 methylene groups, -OCH2CH2O-) ppm
Summary
Nanomaterials hold great promise for use in drug delivery, as image contrast agents, and for diagnostic purposes [1,2,3]. Nanoscale objects in the form of capsules, liposomes, and particles are widely used for delivering small-molecular-weight drugs and macromolecular-protein drugs by localized or targeted delivery to the tissue of interest [4,5,6,7]. Polymeric amphiphiles such as polysaccharides modified with cholesterol groups can spontaneously form the self-aggregated NPs, which have shown huge potential for controlled drug release and targeting ability in medical and pharmaceutical application [8,9,10]. The HSA binding influenced the drug release characteristic of NPs, which is meaningful for these drug carriers to be further investigated for in vivo efficacy
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