In vivo dual-delivery of glucagon like peptide-1 (GLP-1) and dipeptidyl peptidase-4 (DPP4) inhibitor through composites prepared by microfluidics for diabetes therapy

Araújo, Francisca; Shrestha, Neha; Gomes, Maria João; Herranz-Blanco, Bárbara; Liu, Dongfei; Hirvonen, Jouni; Granja, Pedro L.; Santos, Hélder A.; Sarmento, Bruno

doi:10.1039/c6nr00294c

Cited by 64 publications

(41 citation statements)

References 51 publications

(116 reference statements)

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“…The preparation of Liraglutide loaded PLGA nanoparticles was carried out by means of the double emulsion W1/O/W2-solvent evaporation method, which is the most commonly used technique for the encapsulation of peptide drugs within PLGA NPs due to its simplicity and high encapsulation efficiency (15,16). The amount of PLGA (30 or 60 mg) was dissolved in ethyl acetate at room temperature to form the organic phase.…”

Section: Methodsmentioning

confidence: 99%

“…Based on our careful evaluation of literature regarding the emerging developments in oral delivery of antidiabetic peptides (10,11), we found out that PLGA nanoparticles showed promising results in improving the stability of peptides through the GIT in addition to other merits of nanocarrier systems, which can all lead to enhancing the oral bioavailability of these peptides (12). Among the applied techniques for preparing PLGA NPs, the double emulsion solvent evaporation method was found to be the most preferable one, which has been efficiently used for encapsulating peptides and proteins (13–15). Nevertheless, the physicochemical properties of nanoparticles may be affected by various formulation and process parameters, which influence the product quality.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Statistical Optimization of Poly (Lactic-Co-Glycolic Acid) Nanoparticles Encapsulating GLP1 Analog Designed for Oral Delivery

et al. 2019

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Purpose To design and stabilize Liraglutide loaded poly (lactic-co-glycolic acid) nanoparticles (PLGA NPs) proper for oral administration. Methods PLGA NPs were prepared by means of double emulsion solvent evaporation method and optimized by applying 7-factor 2-level Plackett-Burman screening design. Results Spherical shaped NPs with homogeneous distribution, 188.95 nm particle size and 51.81% encapsulation efficiency were obtained. Liraglutide was successfully entrapped in the NPs while maintaining its native amorphous nature, and its structural integrity as well. Conclusion Lira-PLGA NPs with the required Critical Quality Attributes (CQAs) were successfully designed by implementing a 7-factor 8-run Plackett Burman design into the extended Quality by Design (QbD) model, to elucidate the effect of formulation and process variables on the particle size, size-distribution, encapsulation efficiency and surface charge. As the developed nanoparticles maintained the native structure of the active pharmaceutical ingredient (API), they are promising compositions for the further development for the oral delivery of Lira. Graphical Abstract Electronic supplementary material The online version of this article (10.1007/s11095-019-2620-9) contains supplementary material, which is available to authorized users.

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Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Synthesis and Statistical Optimization of Poly (Lactic-Co-Glycolic Acid) Nanoparticles Encapsulating GLP1 Analog Designed for Oral Delivery

et al. 2019

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“…[13d] Benefiting from the high drug loading to peptides and proteins, the codelivery of GLP‐1 and DPP4 enzyme inhibitor for diabetes therapy by oral administration was achieved. [4g,177] Before the encapsulation by HPMCAS, the GLP‐1 was loaded into the PSi nanoparticles, whose surface was sequentially modified with chitosan and CPP. Due to the pH‐responsive properties of the HPMCAS polymer, all the payloads released in responsive to the pH condition of the release medium (Figure b).…”

Section: Emerging Technologies For Engineering Psi‐based Compositesmentioning

confidence: 99%

Tailoring Porous Silicon for Biomedical Applications: From Drug Delivery to Cancer Immunotherapy

et al. 2018

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In the past two decades, porous silicon (PSi) has attracted increasing attention for its potential biomedical applications. With its controllable geometry, tunable nanoporous structure, large pore volume/high specific surface area, and versatile surface chemistry, PSi shows significant advantages over conventional drug carriers. Here, an overview of recent progress in the use of PSi in drug delivery and cancer immunotherapy is presented. First, an overview of the fabrication of PSi with various geometric structures is provided, with particular focus on how the unique geometry of PSi facilitates its biomedical applications, especially for drug delivery. Second, surface chemistry and modification of PSi are discussed in relation to the strengthening of its performance in drug delivery and bioimaging. Emerging technologies for engineering PSi-based composites are then summarized. Emerging PSi advances in the context of cancer immunotherapy are also highlighted. Overall, very promising research results encourage further exploration of PSi for biomedical applications, particularly in drug delivery and cancer immunotherapy, and future translation of PSi into clinical applications.

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“…Serum and livers were frozen in liquid nitrogen instantly and stored at -80℃ for biochemical analysis, and aliquots of the livers were fixed for histological examination. The experiments were performed with the approval of the Animal Care and Use Committee of the Harbin Medical University of China according to the institutional guidelines for the use and care of laboratory animals [31].…”

Section: Methodsmentioning

confidence: 99%

Glucagon-Like Peptide-1 Modulates Cholesterol Homeostasis by Suppressing the miR-19b-Induced Downregulation of ABCA1

Yao¹,

Li²,

Wang³

et al. 2018

Cell Physiol Biochem

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Background/Aims: Abnormal regulation of cholesterol homeostasis is associated with type 2 diabetes mellitus (T2DM) and multiple other diseases. Glucagon-like peptide-1 (GLP-1) has unique effects on modulating hepatic lipid metabolism. However, the mechanism behind these is largely unknown. The aim of this study was to investigate the effects of GLP-1 on cholesterol-induced lipotoxicity in hepatocytes and examine the underlying mechanisms. Methods: Cell viability was determined by CCK-8. Caspase-3 detection was used to assess the effects of GLP-1 on cholesterol-induced apoptosis. TNF-α and IL-6 as the inflammatory markers were measured by ELISA. The alterations of miR-19b and ATP-binding cassette transporter A1 (ABCA1) resulting from high-fat diet/cholesterol incubation or GLP-1 were detected by real-time PCR and western blot. Results: GLP-1 markedly up-regulated the expression of ABCA1 protein, but didn’t affect peroxisome proliferator-activated receptor α (PPAR-α) protein. The miR-19b levels were significantly down-regulated in GLP-1-treated groups. The inhibition and overexpression of miR-19b were established to explore the effects of a GLP-1-mediated alteration in miR-19b. Cholesterol transport assays revealed that treatment with GLP-1 alone or together with miR-19b inhibitor significantly enhanced ABCA1-dependent cholesterol efflux, resulting in reduced total cholesterol. Further, histological examination was used to detect lipid accumulation. Cholesterol significantly attenuated cell viability, promoted hepatic cell apoptosis, and facilitated lipid accumulation, and these effects could be reversed by GLP-1. Conclusion: GLP-1 may affect cholesterol homeostasis by regulating the expression of miR-19b and ABCA1.

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In vivo dual-delivery of glucagon like peptide-1 (GLP-1) and dipeptidyl peptidase-4 (DPP4) inhibitor through composites prepared by microfluidics for diabetes therapy

Abstract: Nanoparticles are promising carrier systems for the oral delivery of proteins, a challenge in the pharmaceutical field.

Cited by 64 publications

References 51 publications

Synthesis and Statistical Optimization of Poly (Lactic-Co-Glycolic Acid) Nanoparticles Encapsulating GLP1 Analog Designed for Oral Delivery

Synthesis and Statistical Optimization of Poly (Lactic-Co-Glycolic Acid) Nanoparticles Encapsulating GLP1 Analog Designed for Oral Delivery

Tailoring Porous Silicon for Biomedical Applications: From Drug Delivery to Cancer Immunotherapy

Glucagon-Like Peptide-1 Modulates Cholesterol Homeostasis by Suppressing the miR-19b-Induced Downregulation of ABCA1

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