Enhanced oral bioavailability of insulin using PLGA nanoparticles co-modified with cell-penetrating peptides and Engrailed secretion peptide (Sec)

Zhu, Siqi; Chen, Shuangxi; Gao, Yuan; Guo, Feng; Li, Fengying; Xie, Baogang; Zhou, Jianuan; Zhong, Hongshan

doi:10.3109/10717544.2015.1043472

Cited by 53 publications

(32 citation statements)

References 48 publications

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“…Comparing to other routes, and for chronic treatment schedules, oral administration offers comfort and improves patient’s compliance. Recent studies have demonstrated the added-value of loading drugs in PLGA NPs to enhance their oral bioavailability [ 13 , 14 ]. PEG surfacing PLGA NPs have enhanced mucus permeating properties, therefore contributing to increase the drug’s bioavailability after oral administration [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization

et al. 2018

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BackgroundMemantine, drug approved for moderate to severe Alzheimer’s disease, has not shown to be fully effective. In order to solve this issue, polylactic-co-glycolic (PLGA) nanoparticles could be a suitable solution to increase drug’s action on the target site as well as decrease adverse effects. For these reason, Memantine was loaded in biodegradable PLGA nanoparticles, produced by double emulsion method and surface-coated with polyethylene glycol. MEM–PEG–PLGA nanoparticles (NPs) were aimed to target the blood–brain barrier (BBB) upon oral administration for the treatment of Alzheimer’s disease.ResultsThe production parameters were optimized by design of experiments. MEM–PEG–PLGA NPs showed a mean particle size below 200 nm (152.6 ± 0.5 nm), monomodal size distribution (polydispersity index, PI < 0.1) and negative surface charge (− 22.4 mV). Physicochemical characterization of NPs confirmed that the crystalline drug was dispersed inside the PLGA matrix. MEM–PEG–PLGA NPs were found to be non-cytotoxic on brain cell lines (bEnd.3 and astrocytes). Memantine followed a slower release profile from the NPs against the free drug solution, allowing to reduce drug administration frequency in vivo. Nanoparticles were able to cross BBB both in vitro and in vivo. Behavioral tests carried out on transgenic APPswe/PS1dE9 mice demonstrated to enhance the benefit of decreasing memory impairment when using MEM–PEG–PLGA NPs in comparison to the free drug solution. Histological studies confirmed that MEM–PEG–PLGA NPs reduced β-amyloid plaques and the associated inflammation characteristic of Alzheimer’s disease.ConclusionsMemantine NPs were suitable for Alzheimer’s disease and more effective than the free drug.Electronic supplementary materialThe online version of this article (10.1186/s12951-018-0356-z) contains supplementary material, which is available to authorized users.

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Section: Introductionmentioning

confidence: 99%

Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization

et al. 2018

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“…A considerable amount of research on topics such as liposomes, micelles, and solid lipid nanoparticles have been reported to improve drug solubility (Gao et al., 2012 ; Tapeinos et al., 2017 ; Zhang et al., 2017 ). Currently, the carrier that has been reported to potentially promote drug transport across the membrane mainly includes plant lectins, membrane fusion proteins, and cell-penetrating peptides (CPPs) (Mora et al., 2016 ; Zheng et al., 2016 ; Zhu et al., 2016 ). Among them, CPPs, a series of short peptides, were found to be supremely effective in enhancing penetration through biological membranes for different cargos, such as micelles, liposomes, and solid lipid nanoparticles (Jiang et al., 2012 ; Ramsey & Flynn, 2015 ).…”

Section: Introductionmentioning

confidence: 99%

Modified mixed nanomicelles with collagen peptides enhanced oral absorption of Cucurbitacin B: preparation and evaluation

Tang

Zhu

et al. 2018

Drug Delivery

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Polymer nanoparticles modified with collagen peptides (CPs) are an attractive strategy for the oral delivery of active ingredients from Chinese medicine. Thus, in the present study, collagen cationic CPs were simply separated using ion-exchange resin from bovine CPs, to modify mixed nanomicelles (MMs) on the surface to improve the oral bioavailability of Cucurbitacin B (CuB). The physicochemical property of micelles was characterized, which confirmed the successful modification of the nanomicelles. CPs-modified nanomicelles in vitro were found to significantly increase cellular uptake and transportation. Compared to unmodified micelles, the quantity of CPs-modified micelles internalized by Caco-2 cells were 3.74 times greater and the cumulative transportation flux (AP-BL) was 2.81 times greater. The membrane transportation process of CuB-MMs-CPs was found to be associated with energy consumption and clathrin- and caveolin-mediated endocytosis. In vivo studies performed on rats indicated that in comparison to CuB and CuB-MMs, the relative bioavailability of CuB-MMs-CPs increased by 3.43 times and 2.14 times, respectively. In addition, the tumor inhibition caused by CuB-MMs-CPs was increased significantly. Therefore, the nanomicelles co-modified with isolated CPs could act as attractive carriers for oral delivery of CuB.

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“…It is recognized that oral delivery of peptide has been a great continuous challenge due to its poor stability in the GI tract and low permeability through the intestinal epithelium membrane [40,41,42]. Numerous promising strategies have been utilized to circumvent these obstacles [43], including enzyme inhibitors [44] and solid lipid NPs [45] to protect these drugs from enzymatic degradation.…”

Section: Discussionmentioning

confidence: 99%

Enhanced and Extended Anti-Hypertensive Effect of VP5 Nanoparticles

Takata

Zhao

et al. 2016

IJMS

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Hypertension has become a significant global public health concern and is also one of the most common risk factors of cardiovascular disease. Recent studies have shown the promising result of peptides inhibiting angiotensin converting enzyme (ACE) in lowering the blood pressure in both animal models and humans. However, the oral bioavailability and continuous antihypertensive effectiveness require further optimization. Novel nanoparticle-based drug delivery systems are helpful to overcome these barriers. Therefore, a poly-(lactic-co-glycolic) acid nanoparticle (PLGANPs) oral delivery system, of the antihypertensive small peptides Val-Leu-Pro-Val-Pro (VLPVP, VP5) model, was developed in this study and its antihypertensive effect was investigated in spontaneously hypertensive rats (SHRs) for the first time. The obtained VP5 nanoparticles (VP5-NPs) showed a small particle size of 223.7 ± 2.3 nm and high entrapment efficiency (EE%) of 87.37% ± 0.92%. Transmission electronic microscopy (TEM) analysis showed that the nanoparticles were spherical and homogeneous. The optimal preparation of VP5-NPs exhibited sustained release of VP5 in vitro and a 96 h long-term antihypertensive effect with enhanced efficacy in vivo. This study illustrated that PLGANPs might be an optimal formulation for oral delivery of antihypertensive small peptides and VP5-NPs might be worthy of further development and use as a potential therapeutic strategy for hypertension in the future.

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Enhanced oral bioavailability of insulin using PLGA nanoparticles co-modified with cell-penetrating peptides and Engrailed secretion peptide (Sec)

Cited by 53 publications

References 48 publications

Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization

Memantine loaded PLGA PEGylated nanoparticles for Alzheimer’s disease: in vitro and in vivo characterization

Modified mixed nanomicelles with collagen peptides enhanced oral absorption of Cucurbitacin B: preparation and evaluation

Enhanced and Extended Anti-Hypertensive Effect of VP5 Nanoparticles

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