Abstract
We prepared two types of cholesterol hydrophobically modified pullulan nanoparticles (CHP) and carboxyethyl hydrophobically modified pullulan nanoparticles (CHCP) substituted with various degrees of cholesterol, including 3.11, 6.03, 6.91 and 3.46 per polymer, and named CHP−3.11, CHP−6.03, CHP−6.91 and CHCP−3.46. Dynamic laser light scattering (DLS) showed that the pullulan nanoparticles were 80–120 nm depending on the degree of cholesterol substitution. The mean size of CHCP nanoparticles was about 160 nm, with zeta potential −19.9 mV, larger than CHP because of the carboxyethyl group. A greater degree of cholesterol substitution conferred greater nanoparticle hydrophobicity. Drug-loading efficiency depended on nanoparticle hydrophobicity, that is, nanoparticles with the greatest degree of cholesterol substitution (6.91) showed the most drug encapsulation efficiency (90.2%). The amount of drug loading increased and that of drug release decreased with enhanced nanoparticle hydrophobicity. Nanoparticle surface-negative charge disturbed the amount of drug loading and drug release, for an opposite effect relative to nanoparticle hydrophobicity. The drug release in pullulan nanoparticles was higher pH 4.0 than pH 6.8 media. However, the changed drug release amount was not larger for negative-surface nanoparticles than CHP nanoparticles in the acid release media. Drug release of pullulan nanoparticles was further slowed with human serum albumin complexation and was little affected by nanoparticle hydrophobicity and surface negative charge.
Highlights
Many drugs with highly efficient action are dysfunctional as treatment because of the fast drug metabolism and a peak-valley reaction
We investigated the principal extracellular protein if wethe consider the other factors human body systems interacting with nanoparticles, the drug release mechanism will more in the human body systems interacting with nanoparticles, the drug release mechanism will more be complicated
The size formed and drug release of self-aggregated pullulan nanoparticles decreased with increasing cholesterol substitution
Summary
Many drugs with highly efficient action are dysfunctional as treatment because of the fast drug metabolism and a peak-valley reaction. The effect of nanoparticle hydrophobicity and surface and carboxyethyl groups on drug release.The. We measured encapsulation, loading capacityand and surface transmission electron microscopy effect ofdrug nanoparticle hydrophobicity charge on the drug loading amount and drug release in phosphate buffered saline (PBS) was studied sizes pullulan nanoparticles withdrug different properties and observed morphology viastudied charge on theofdrug loading amount and release in phosphate bufferedthe saline (PBS) was to clarify the application asmicroscopy a drug carrier. Nanoparticles with different properties charge surface weak acid and strong release media and studied HSA complexation with CHP nanoparticles. This complexation can be divided into two. Drugnano-drug slow preparation be used for further vivo efficacy study.in vivo efficacy study
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