Modified two-step emulsion solvent evaporation technique for fabricating biodegradable rod-shaped particles in the submicron size range

Bile acids are proposed as therapeutic agents for various diseases, including liver diseases and obesity. However, oral or subcutaneous administration of a solubilized version of these drugs has limited efficacy and imposes unwanted side effects. Here, we describe a gold-templating method for fabricating stable, bile salt—cholate or deoxycholate—microparticles. The gold ions’ reduction at the oil-water interface in a double emulsion solvent evaporation process enables a gold–bile salt interaction and the formation of bile salt particles. We demonstrate that composite microparticles release cholate/deoxycholate into solution via a surface erosion process. We illustrate these particles’ capability to lyse adipocytes, both in vitro and in vivo, with minimal side effects, contrary to the Food and Drug Administration–approved salt solution that leads to severe inflammation and ulceration. Overall, particle-based cholate/deoxycholate opens opportunities for localized delivery of these salts, improving efficacy while minimizing side effects associated with oral and subcutaneous use.

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“…In line with previous studies ( 20 ), the size of the hexagons varied as a function of the surfactant concentration, as shown in Fig. 2 and fig.…”

Section: Resultssupporting

confidence: 92%

Biodegradable, bile salt microparticles for localized fat dissolution

et al. 2020

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“…Fluorescent (Cy5.5-loaded) spherical and rodshaped PLGA particles of 1.5 m ESD were fabricated via a two-step emulsion solvent evaporation technique ( fig. S3A), as previously described (34). As with polystyrene particles, PLGA rods were taken up by primary human neutrophils at a ~20% higher rate than that of equivalent PLGA spheres (Fig.…”

Section: Downloaded Frommentioning

confidence: 63%

“…Rod-shaped PLGA particles were fabricated by the modified twostep emulsion solvent evaporation technique previously described (34). Briefly, 25 mg of acid-terminated 50:50 PLGA polymer and 0.5 mg of Cy5.5-conjugated PLGA were dissolved in 10 ml of chloroform.…”

Section: Fabrication Of the Cy55-loaded Plga Rods And Spheresmentioning

confidence: 99%

Neutrophils preferentially phagocytose elongated particles—An opportunity for selective targeting in acute inflammatory diseases

et al. 2020

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Polymeric particles have recently been used to modulate the behavior of immune cells in the treatment of various inflammatory conditions. However, there is little understanding of how physical particle parameters affect their specific interaction with different leukocyte subtypes. While particle shape is known to be a crucial factor in their phagocytosis by macrophages, where elongated particles are reported to experience reduced uptake, it remains unclear how shape influences phagocytosis by circulating phagocytes, including neutrophils that are the most abundant leukocyte in human blood. In this study, we investigated the phagocytosis of rod-shaped polymeric particles by human neutrophils relative to other leukocytes. In contrast to macrophages and other mononuclear phagocytes, neutrophils were found to exhibit increased internalization of rods in ex vivo and in vivo experimentation. This result suggests that alteration of particle shape can be used to selectively target neutrophils in inflammatory pathologies where these cells play a substantial role.

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“…Briefly, TMR-dextran (200 µL) was blended into a CPT-11 and GEM polymeric solutions in CHCl 3 with sonications. These emulsions were consequently blended in a PVA-PBS solution, left for solvents evaporations (Gupta et al., 2017 ; Li et al., 2017 ; Safari et al., 2018 ; Guo et al., 2019 ). The emulsions were stirred for 24 h, and they evaporated the organic solvents.…”

Section: Methodsmentioning

confidence: 99%

Combinational dual drug delivery system to enhance the care and treatment of gastric cancer patients

Xiao

Gao

et al. 2020

Drug Delivery

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Gastric cancer is a frequently occurring cancer with high mortality each year worldwide. Finding new and effective therapeutic strategy against human gastric cancer is still urgently required. Hence, we have established a new method to achieve treatment-actuated modifications in a tumor microenvironment by utilizing synergistic activity between two potential anticancer drugs. Dual drug delivery of gemcitabine (GEM) and Camptothecin-11 (CPT-11) exhibits a great anti-cancer potential, as GEM enhances the effect of CPT-11 treatment of human gastric cells by providing microenvironment stability. However, encapsulation of GEM and CPT-11 obsessed by poly(lactic-co-glycolic acid) (PLGA)-based nanoparticles (NPs) is incompetent owing to unsuitability between the binary free GEM and CPT-11 moieties and the polymeric system. Now, we display that CPT-11 can be prepared by hydrophobic covering of the drug centers with dioleoylphosphatidic acid (DOPA). The DOPA-covered CPT-11 can be co-encapsulated in PLGA NPs alongside GEM to stimulate excellent anticancer property. The occurrence of the CPT-11 suggestively enhanced the encapsulations of GEM into PLGA NPs (GEM-CPT-11 NPs). Formation of the nanocomposite (GEM-CPT-11 NPs) was confirmed by FTIR and X-ray spectroscopic techniques. Further, the morphology of GEM NPs, CPT-11 NPs, and GEM-CPT-11 NPs and NP size was examined by transmission electron microscopy (TEM), respectively. Furthermore, GEM-CPT-11 NPs induced significant apoptosis in human gastric NCI-N87 and SGC-791 cancer cells in vitro. The morphological observation and apoptosis were confirmed by the various biochemical assays (AO-EB, nuclear staining, and annexin V-FITC). In addition, evaluation of the hemolysis assay with erythrocytes of human shows excellent biocompatibility of free GEM, free CPT-11, GEM NPs, CPT-11 NPs, and GEM-CPT-11 NPs. The results suggest that GEM-CPT-11 NPs are one of the promising nursing cares for human gastric cancer therapeutic candidates worthy of further investigations.

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Modified two-step emulsion solvent evaporation technique for fabricating biodegradable rod-shaped particles in the submicron size range

Cited by 15 publications

References 32 publications

Biodegradable, bile salt microparticles for localized fat dissolution

Biodegradable, bile salt microparticles for localized fat dissolution

Neutrophils preferentially phagocytose elongated particles—An opportunity for selective targeting in acute inflammatory diseases

Combinational dual drug delivery system to enhance the care and treatment of gastric cancer patients

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