Screened peptides from one-bead one-compound technique extend half-life of peptide drugs in circulation through binding to albumin

Peptide drugs are known for their high biological safety.However,compared with small molecule drugs,peptide drugs are easily oxidized and hydrolyzed as well as short in half-life.Herein,inspired by the long circulation of albumin in blood,we screened albumin binding peptides(ABPs)from a one-bead one-compound(OBOC)peptide library to increase the half-life of peptide drugs.Beads displaying random peptides were screened using fluorescent labeled human serum albumin.Fluorescent beads with specific binding to albumin were isolated for sequencing.The selected ABPs can effectively bind to albumin,thus possessing the long circulation of albumin.The dissociation constant(K_(D))of ABPs to albumin is up to 1×10^(-8)mol/L.Once one of ABPs(ABP2)was coupled to triptorelin,the circulation half-life of triptorelin in mice was significantly prolonged to 263.50 h much longer than that of triptorelin alone(179.07 h).In addition,the combination therapy using ABP-conjugated triptorelin and doxorubicin(DOX)can effectively inhibit the proliferation of tumor cells in mice.The OBOC screening strategy and resulting ABPs showed great potential for enhancing the delivery efficiency of peptide drugs.

Recent advances of transformable nanoparticles for theranostics

In recent years,various transformable nanoparticles（NPs）were successfully prepared and widely utilized for biomedical applications.The sizes,surface charges or morphologies of transformable NPs would affect their behavior in physiological/pathological conditions including circulation,penetration,accumulation and retention etc.The other way round,the NPs could be precisely modulated in the specific physiological/pathological condition for precision theranostics of diseases.Herein,we summarized recent advances of transformable NPs for disease diagnostics and therapy.In this review,the transformation of NPs was divided into three groups including changes in size,surface charge and morphology,which was induced by internal stimuli,such as p H,enzyme,receptor or external stimuli,such as light,temperature etc.Moreover,we focused on the characterization of structural transformation in vivo,as well as the transformation-induced biological effects for theranostics of disease.

Live Cells Process Exogenous Peptide as Fibronectin Fibrillogenesis In Vivo

The human body is one of the most sophisticated material systems.It is still a considerable challenge to biomimic the“life-design”process to construct a part of“life”in vivo.Herein,we mimicked the natural fibronectin(FN)fibrillogenesis system using ligand–receptor interaction-induced self-assembly to construct in situ artificial fibrous FN in vivo,based on exogenous FN mimic peptide(FNMP).We performed the in vivo study with a tumor-bearing mouse model,to which the particle formulated FNMP raw materials were delivered with high efficiency to the tumor site through intravenous(iv)administration.In the tumor,the presence of overexpressed integrin receptors on the cell surface induced the self-assembly of the FNMP into fibrous structures,thereby,creating an artificial fibrous FN.However,the FNMP-based artificial fibrous FN showed different biological functionality from the natural fibrous FN,inhibiting the growth and migration of cells,making our constructed FN able to inhibit tumor growth,invasion,and metastasis.Thus,this study opens an avenue for the precise construction of biomimetic materials for in vivo biomedical applications.