pH-responsive zwitterionic polypeptide as a platform for anti-tumor drug delivery

Liu, Na; Han, Jiaming; Zhang, Xinchen; Yang, Yue; Liu, Yuan; Wang, Yanming; Wu, Guolin

doi:10.1016/j.colsurfb.2016.05.027

Cited by 34 publications

(21 citation statements)

References 40 publications

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“…The VCM-StBAclm-Qt quatsomes were further characterized to determine drug entrapment efficiency (DEE%) and drug loading capacity (DLC%). The DEE % was determined by an ultrafiltration method, as previously reported using the regression equation y = 0.0038x − 0.0031, with a linear regression coefficient (R²) of 0.9998 [ 30 , 31 ] and the details can be found in the supplementary materials .…”

Section: Methodsmentioning

confidence: 99%

Formulation of pH-Responsive Quatsomes from Quaternary Bicephalic Surfactants and Cholesterol for Enhanced Delivery of Vancomycin against Methicillin Resistant Staphylococcus aureus

et al. 2020

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Globally, human beings continue to be at high risk of infectious diseases caused by methicillin-resistant Staphylococcus aureus (MRSA); and current treatments are being depleted due to antimicrobial resistance. Therefore, the synthesis and formulation of novel materials is essential for combating antimicrobial resistance. The study aimed to synthesize a quaternary bicephalic surfactant (StBAclm) and thereof to formulate pH-responsive vancomycin (VCM)-loaded quatsomes to enhance the activity of the antibiotic against MRSA. The surfactant structure was confirmed using 1H, 13C nuclear magnetic resonance (NMR), Fourier-transform infrared spectroscopy (FT-IR), and high-resolution mass spectrometry (HRMS). The quatsomes were prepared using a sonication/dispersion method and were characterized using various in vitro, in vivo, and in silico techniques. The in vitro cell biocompatibility studies of the surfactant and pH-responsive vancomycin-loaded quatsomes (VCM-StBAclm-Qt1) revealed that they are biosafe. The prepared quatsomes had a mean hydrodynamic diameter (MHD), polydispersity index (PDI), and drug encapsulation efficiency (DEE) of 122.9 ± 3.78 nm, 0.169 ± 0.02 mV, and 52.22 ± 8.4%, respectively, with surface charge switching from negative to positive at pH 7.4 and pH 6.0, respectively. High-resolution transmission electron microscopy (HR-TEM) characterization of the quatsomes showed spherical vesicles with MHD similar to the one obtained from the zeta-sizer. The in vitro drug release of VCM from the quatsomes was faster at pH 6.0 compared to pH 7.4. The minimum inhibitory concentration (MIC) of the drug loaded quatsomes against MRSA was 32-fold and 8-fold lower at pH 6.0 and pH 7.4, respectively, compared to bare VCM, demonstrating the pH-responsiveness of the quatsomes and the enhanced activity of VCM at acidic pH. The drug-loaded quatsomes demonstrated higher electrical conductivity and a decrease in protein and deoxyribonucleic acid (DNA) concentrations as compared to the bare drug. This confirmed greater MRSA membrane damage, compared to treatment with bare VCM. The flow cytometry study showed that the drug-loaded quatsomes had a similar bactericidal killing effect on MRSA despite a lower (8-fold) VCM concentration when compared to the bare VCM. Fluorescence microscopy revealed the ability of the drug-loaded quatsomes to eradicate MRSA biofilms. The in vivo studies in a skin infection mice model showed that groups treated with VCM-loaded quatsomes had a 13-fold decrease in MRSA CFUs when compared to the bare VCM treated groups. This study confirmed the potential of pH-responsive VCM-StBAclm quatsomes as an effective delivery system for targeted delivery and for enhancing the activity of antibiotics.

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Section: Methodsmentioning

confidence: 99%

Formulation of pH-Responsive Quatsomes from Quaternary Bicephalic Surfactants and Cholesterol for Enhanced Delivery of Vancomycin against Methicillin Resistant Staphylococcus aureus

et al. 2020

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“…Similarly, quantities of prodrugs have been synthesized with the help of hydrazone bonds which are easy to be cut off in acid environments too [88] , [89] , [90] , [91] . Wu et al conjugated zwitterionic L-Lys and hydrazine grafted poly(aspartamide) (PALHy) by successive aminolysis reactions of poly(succinimide) with L-lysine and hydrazine hydrate following hydrolysis [92] . The DOX molecules were conjugated to the copolymer chemically via hydrazone bonds to form PALHy-hyd-DOX conjugates.…”

Section: Applications Of Zwitterionic Materials In Drug Delivery Systmentioning

confidence: 99%

Novel zwitterionic vectors: Multi-functional delivery systems for therapeutic genes and drugs

Zhou

Zhu

Wang

et al. 2020

Computational and Structural Biotechnology Journal

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“…[13] Many nanocarriers specifically explore the slight difference in pH between healthy tissues and the extracellular environment of tumors to afford efficient drug release. [14] …”

Section: Introductionmentioning

confidence: 99%

Functional Peptide Nanofibers with Unique Tumor Targeting and Enzyme‐Induced Local Retention Properties

Bellat

Ting

Southard

et al. 2018

Adv Funct Materials

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An effective tumoral delivery system should show minimal removal by the reticuloendothelial system (RES), promote tumor uptake and penetration, and minimize on-site clearance. This study reports the design and synthesis of advanced self-assembling peptide nanofiber precursor (NFP) analogues. The peptidic nature of NFP offers the design flexibility for on-demand customization with imaging agents and surface charges while maintaining a set size, allowing for real-time monitoring of kinetic and dynamic tumoral delivery by multimodal fluorescence/positron emission tomography/computed tomography (fluo/PET/CT) imaging, for formulation optimization. The optimized glutathione (GSH)-NFP displays a reduced capture by the RES as well as excellent tumor targeting and tissue invasion properties compared to naive NFP. Inside a tumor, GSH-NFP can structurally transform into ten times larger interfibril networks, serving as in situ depot that promotes weeks-long local retention. This nanofiber, which can further be designed to release the active pharmacophores within a tumor microenvironment, displays a superior therapeutic efficacy for inhibiting disease progression and improving the survival of animals bearing triple-negative breast cancer tumors compared to free drug and liposome formulation of the drug, in addition to a favorable toxicity profile.

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pH-responsive zwitterionic polypeptide as a platform for anti-tumor drug delivery

Cited by 34 publications

References 40 publications

Formulation of pH-Responsive Quatsomes from Quaternary Bicephalic Surfactants and Cholesterol for Enhanced Delivery of Vancomycin against Methicillin Resistant Staphylococcus aureus

Formulation of pH-Responsive Quatsomes from Quaternary Bicephalic Surfactants and Cholesterol for Enhanced Delivery of Vancomycin against Methicillin Resistant Staphylococcus aureus

Novel zwitterionic vectors: Multi-functional delivery systems for therapeutic genes and drugs

Functional Peptide Nanofibers with Unique Tumor Targeting and Enzyme‐Induced Local Retention Properties

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