Relationship and improvement strategies between drug nanocarrier characteristics and hemocompatibility: What can we learn from the literature

Guo, Shiwei; Shi, Yanan; Yu, Lintao; Liu, Lanze; Sun, Kaoxiang; Li, Youxin

doi:10.1016/j.ajps.2020.12.002

Cited by 51 publications

(23 citation statements)

References 152 publications

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“…The hemocompatibility of SNEDDS was determined by a hemolysis test [ 53 ]. Blood from a healthy Wistar rat was collected in an anti-coagulant tube and washed three times with normal saline and centrifuged at 3000 rpm for 10 min [ 54 ]. RBCs pellets were washed continuously until the clear supernatant was observed.…”

Section: Methodsmentioning

confidence: 99%

Solid Self-Nano Emulsifying Nanoplatform Loaded with Tamoxifen and Resveratrol for Treatment of Breast Cancer

et al. 2022

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The solid self-nanoemulsifying drug delivery system (s-SNEDDS) is a growing platform for the delivery of drugs via oral route. In the present work, tamoxifen (TAM) was loaded in SNEDDS with resveratrol (RES), which is a potent chemotherapeutic, antioxidant, anti-inflammatory and P-gp inhibitor for enhancing bioavailability and to obtain synergistic anti-cancer effect against breast cancer. SNEDDS were developed using capmul MCM as oil, Tween 80 as surfactant and transcutol-HP as co-surfactant and optimized by central composite rotatable design. Neusilin US2 concentration was optimized for adsorption of liquid SNEDDS to prepare s-SNEDDS. The developed formulation was characterized and investigated for various in vitro and cell line comparative studies. Optimized TAM-RES-s-SNEDDS showed spherical droplets of a size less than 200 nm. In all in vitro studies, TAM-RES-s-SNEDDS showed significantly improved (p ˂ 0.05) release and permeation across the dialysis membrane and intestinal lumen. Moreover, TAM-RES-s-SNEDDS possessed significantly greater therapeutic efficacy (p < 0.05) and better internalization on the MCF-7 cell line as compared to the conventional formulation. Additionally, oral bioavailability of TAM from SNEDDS was 1.63 folds significantly higher (p < 0.05) than that of combination suspension and 4.16 folds significantly higher (p < 0.05) than TAM suspension. Thus, findings suggest that TAM- RES-s-SNEDDS can be the future delivery system that potentially delivers both drugs to cancer cells for better treatment.

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Section: Methodsmentioning

confidence: 99%

Solid Self-Nano Emulsifying Nanoplatform Loaded with Tamoxifen and Resveratrol for Treatment of Breast Cancer

et al. 2022

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“…The hemolysis test evaluates the ability of the studied compound to cause the destruction of human red blood cells and illustrates its toxic effect on the internal environment of the body. There is no standard preclinical in vivo testing method to comprehensively evaluate the hemolytic response of pharmaceuticals, so the in vitro hemolytic activity test is taken into account in toxicity studies [ 39 ].…”

Section: Resultsmentioning

confidence: 99%

Calix[4]Resorcinarene Carboxybetaines and Carboxybetaine Esters: Synthesis, Investigation of In Vitro Toxicity, Anti-Platelet Effects, Anticoagulant Activity, and BSA Binding Affinities

Morozova

Gilmullina

Voloshina

et al. 2022

IJMS

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As a result of bright complexation properties, easy functionalization and the ability to self-organize in an aqueous solution, amphiphilic supramolecular macrocycles are being actively studied for their application in nanomedicine (drug delivery systems, therapeutic and theranostic agents, and others). In this regard, it is important to study their potential toxic effects. Here, the synthesis of amphiphilic calix[4]resorcinarene carboxybetaines and their esters and the study of a number of their microbiological properties are presented: cytotoxic effect on normal and tumor cells and effect on cellular and non-cellular components of blood (hemotoxicity, anti-platelet effect, and anticoagulant activity). Additionally, the interaction of macrocycles with bovine serum albumin as a model plasma protein is estimated by various methods (fluorescence spectroscopy, synchronous fluorescence spectroscopy, circular dichroic spectroscopy, and dynamic light scattering). The results demonstrate the low toxicity of the macrocycles, their anti-platelet effects at the level of acetylsalicylic acid, and weak anticoagulant activity. The study of BSA–macrocycle interactions demonstrates the dependence on macrocycle hydrophilic/hydrophobic group structure; in the case of carboxybetaines, the formation of complexes prevents self-aggregation of BSA molecules in solution. The present study demonstrates new data on potential drug delivery nanosystems based on amphiphilic calix[4]resorcinarenes for their cytotoxicity and effects on blood components.

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“…Lysis of RBCs caused by different nanoparticle formulations is another key factor to be considered for their in vivo use . Both peptide RΔFRGD NPs and the nanocomplex showed less than 5% hemolysis, which is under the limits prescribed by the ISO/TR 7406 guidelines for biomaterials . Further, it is also desirable that the nanocarrier system should not induce any inflammatory response .…”

Section: Discussionmentioning

confidence: 99%

“… 60 Both peptide RΔFRGD NPs and the nanocomplex showed less than 5% hemolysis, which is under the limits prescribed by the ISO/TR 7406 guidelines for biomaterials. 61 Further, it is also desirable that the nanocarrier system should not induce any inflammatory response. 62 Our results showed that RΔFRGD NPs did not elicit inflammatory cytokine response, IFN-γ.…”

Section: Discussionmentioning

confidence: 99%

Conformationally Restricted Dipeptide-Based Nanoparticles for Delivery of siRNA in Experimental Liver Cirrhosis

et al. 2022

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Liver cirrhosis is a major health problem with multiple associated complications. The presently available drug delivery systems showed moderate site-specific delivery of antifibrotic molecules to the diseased liver; therefore, research on more effective and selective delivery systems in the context of liver cirrhosis remains a necessity in clinical investigation. The aim of the present study was to develop a peptide-based targeted nanocarrier to deliver an oligonucleotide to the hepatic sinusoidal and perivascular regions of the cirrhotic liver. We have synthesized and characterized a conformationally restricted targeted pentapeptide (RΔFRGD), which contains an unnatural amino acid, α,βdehydrophenylalanine (ΔF). The RΔFRGD self-assembled into spherical nanoparticles (NPs) and was characterized by dynamic light scattering (DLS) and transmission electron microscopy (TEM). Next, we investigated the delivery potential of the pentapeptide-based NPs to make a stable complex with a well-established small interference RNA and studied its site-specific delivery in experimental liver cirrhosis. We used siNR4A1 of the orphan nuclear receptor 4A1 (NR4A1), a well-known regulatory checkpoint for controlling liver fibrosis. Peptide NPs and their complex with siNR4A1 showed high biocompatibility against various mammalian cell lines. Hepatic tissue biodistribution analysis illustrated that targeted NPs predominantly accumulated in the cirrhotic liver compared to normal rats, specifically in sinusoidal and perivascular areas. A significant downregulation of the NR4A1 mRNA expression (−70%) andlower levels of the NR4A1/GAPDH ratio (−55%) were observed in the RΔFRGD-siNR4A1 nanocomplextreated group in comparison to the RΔFRGD-vehicle group (RΔFRGD-Veh) at the gene and protein levels, respectively. In addition, in vivo inhibition of NR4A1 produced a significant aggravation in hepatic fibrosis compared with siRNA-vehicle-treated rats (+41% in the MT stain). The novel pentapeptide-based targeted delivery system can be further evaluated and validated for therapeutic purposes in various pathological conditions.

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Relationship and improvement strategies between drug nanocarrier characteristics and hemocompatibility: What can we learn from the literature

Cited by 51 publications

References 152 publications

Solid Self-Nano Emulsifying Nanoplatform Loaded with Tamoxifen and Resveratrol for Treatment of Breast Cancer

Solid Self-Nano Emulsifying Nanoplatform Loaded with Tamoxifen and Resveratrol for Treatment of Breast Cancer

Calix[4]Resorcinarene Carboxybetaines and Carboxybetaine Esters: Synthesis, Investigation of In Vitro Toxicity, Anti-Platelet Effects, Anticoagulant Activity, and BSA Binding Affinities

Conformationally Restricted Dipeptide-Based Nanoparticles for Delivery of siRNA in Experimental Liver Cirrhosis

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