In vivo evaluation of an oral self-emulsifying drug delivery system (SEDDS) for exenatide

Menzel, Claudia; Holzeisen, Thomas; Laffleur, Flavia; Zaichik, Sergey; Abdulkarim, Muthanna; Gumbleton, Mark; Bernkop‐Schnürch, Andreas

doi:10.1016/j.jconrel.2018.03.018

Cited by 94 publications

(53 citation statements)

References 29 publications

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“…In the present study, the physiological buffered saline was not suitable for the dissolution experiment, simply because astaxanthin was not at all soluble in such media. As reported, the ethanol was used as media to study the diffusion of astaxanthin from polyethylene active packaging film into a fatty food simulant, and it obtained good released results . Consequently, the 50% ethanol in physiological buffered saline was selected as dissolution media in this study.…”

Section: Resultsmentioning

confidence: 99%

Development of a Solid Self‐Emulsification Delivery System for the Oral Delivery of Astaxanthin

Mao

Sun

Tian

et al. 2019

Euro J Lipid Sci & Tech

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In the present study, a solid self‐emulsification delivery system (S‐SEDS) is developed to improve the bioavailability of astaxanthin (ASX). The pseudo ternary phase diagram method is used to screen the optimum composition of liquid self‐emulsification delivery system (SEDS). This liquid system is converted into solid state using the solid absorbent carrier by simple physical mixing. Through the analysis of powder flowability and adsorption capacity, silicon dioxide and anhydrous calcium hydrogen phosphate are selected as solid carriers of the liquid self‐emulsification system. Results of Fourier transform infrared spectroscopy (FTIR) and X‐ray diffraction (XRD) indicate that astaxanthin is encapsulated in these solid carriers. In the in vitro dissolution study, sustained release of astaxanthin from two different ASX‐SEDS (prepared with silicon dioxide and anhydrous calcium hydrogen phosphate) is obtained and the cumulative release is correspondingly 51.06 ± 0.98 and 49.97 ± 0.87% within 2 h. A delayed pattern of absorbed ASX‐SEDS is observed in the study with anhydrous calcium hydrogen phosphate compared to the counterpart with silicon dioxide, which is consistent with the result from the in vitro digestion study. Antioxidant study shows that astaxanthin can be encapsulated in S‐SEDS without the loss of antioxidant activity. Consequently, S‐SEDS can be a promising vehicle in food industry. Practical Applications: Traditionally, liquid‐based delivery systems are prepared using liquid components, which have some disadvantages, such as, complex production process, low active ingredient loading, narrow application range, and lacking of effective evaluation methods. The present study adopts physical adsorption, a gentle and simple process, to prepare the solid self‐emulsifying system. This system combines the advantages of liquid‐based systems and solid dosage forms, which can improve the solubility of poorly solubility active ingredient in intestinal environments, and the high solubility of active ingredient is favor to its absorption. In the present work, the active ingredients solubilization capability of solid formulations is evaluated by in vitro dissolution and digestion studies. It can be seen that over 40% of astaxanthin are released from solid self‐emulsifying systems in 120 min. After the process of digestion, the bioaccessibility reaches 10%. The results of in vitro dissolution and digestion show that after solid adsorption, astaxanthin exhibits delayed release patterns. All the studies demonstrate that solid self‐emulsifying system is an appropriate strategy to improve the bioavailability of astaxanthin. The pseudo ternary phase diagram method is used to screen the optimum composition of liquid self‐emulsification delivery system. Then, this liquid system is converted into solid state using the solid absorbent carrier by simple physical mixing.

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Section: Resultsmentioning

confidence: 99%

Development of a Solid Self‐Emulsification Delivery System for the Oral Delivery of Astaxanthin

Mao

Sun

Tian

et al. 2019

Euro J Lipid Sci & Tech

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“…3.1. 13 C NMR and FT-IR of mPEG-Rg3-BSA NPs. The mPEG-Rg3 powder was obtained by freeze drying, and the water solubility of Rg3 was 1 mg/mL after being conjugated with mPEG-SA, and the yield was 48.5%.…”

Section: Resultsmentioning

confidence: 99%

“…The mPEG-Rg3 was obtained by freeze drying. Then, the structure of mPEG-Rg3 was confirmed by 13 C NMR (Japan Electron Optics Laboratory Co. Ltd., Japan) and FT-IR (Brook Spectrometer Co. Ltd., USA).…”

Section: Synthesis Of Mpeg-rg3mentioning

confidence: 99%

“…They are designed to deliver poorly water-soluble drugs and improve the pharmacological and therapeutic properties of drugs administered parenterally. Moreover, the hydrophilicity of nanoparticles provides excellent water solubility and superior biocompatibility, because they effectively protect the activity of drugs, achieve slow and controlled release, and avoid reticuloendothelial system (RES) phagocytosis [12][13][14]. Thus far, many types of nanocarriers have been invented by researchers, such as lipid-or polymer-based nanoparticles, nanofibres, and biodegradable carrier systems [15][16][17].…”

Section: Introductionmentioning

confidence: 99%

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PEGylation of Ginsenoside Rg3-Entrapped Bovine Serum Albumin Nanoparticles: Preparation, Characterization, and In Vitro Biological Studies

Zhang

Hui

et al. 2019

Journal of Nanomaterials

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Ginsenoside Rg3 (Rg3) is one of three triterpene saponins from red ginseng. It has important structural functions and pharmacological properties. However, due to its poor solubility, low bioavailability, and short half-life in blood circulation, its clinical application was unsuccessful for the treatment of a variety of cancers. In order to overcome this limitation, this study prepared mPEGylation-Rg3 bovine serum albumin nanoparticles (mPEG-Rg3-BSA NPs). The characteristics of the NPs, such as drug entrapment efficiency, drug loading efficiency, surface morphology, thermal stability, and cytotoxicity in vitro, were investigated. The results showed that the appropriate particle size of the obtained NPs was 149.5 nm, the water solubility and stability were better than free Rg3, and the drug entrapment efficiency and drug loading efficiency were 76.56% and 17.65%, respectively. Moreover, the cytotoxicity assays of the mPEG-Rg3-BSA NPs and free Rg3 revealed that the mPEG-Rg3-BSA NPs have greater anticancer effects in HepG2 cells and A549 cells. However, the cytotoxic effect of free Rg3 was higher than the mPEG-Rg3-BSA NPs in L929 cells. The results indicated that using the mPEGylation method and selecting BSA as a carrier to form the nanodrug carrier system were effective for improving the properties of Rg3.

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“…Nanoparticles self‐assembled from biomacromolecules have been widely used as a drug delivery system (DDS) to deliver and control the release of small‐molecule antitumor drugs . With thermal‐, pH‐, and redox‐responsive units, nanoparticles can specifically deliver drugs to tumor cells/tissues and enhance the concentration of the drugs in the tumor zone .…”

Section: Introductionmentioning

confidence: 99%

pH‐Triggered Conformational Change of Antp‐Based Drug Delivery Platform for Tumor Treatment with Combined Photothermal Therapy and Chemotherapy

Liang

Zhang

Wang

et al. 2019

Adv Healthcare Materials

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Poor cellular uptake and low therapeutic efficacy of small‐molecule antitumor drugs limit the application of drug delivery systems (DDSs) in cancer therapy. A conformational change of the Antp mimetic peptide (AMP) in tumor microenvironments can greatly increase the cellular uptake as well as control drug release from a DDS. In this study, AMP‐based nanoparticles (AMP‐NPs) conjugated with tyroserleutide (YSL), an immunologically therapeutic tripeptide, are designed to encapsulate doxorubicin (Dox) and indocyanine green (ICG) to improve cellular uptake and cancer therapeutic efficacy by combining chemotherapy with photothermal therapy. In vitro studies verify that AMP‐NPs can control the release of Dox and YSL at different pH values. Cell experiments show that AMP‐NPs can promote the cellular uptake of Dox, and YSL can promote hepatocarcinoma cell (H22) apoptosis through downregulating Bcl‐2 and cyclin D1 expression. In a mouse xenograft model using H22 cells, tumors are ablated when Dox‐ and ICG‐loaded AMP‐NPs are injected with the combination of hyperthermia effect induced by near‐infrared (NIR) laser irradiation and chemotherapy from Dox and YSL. The pH‐, photothermal‐, and glutathione‐responsive AMP‐NPs with a conformational transition strategy can be utilized to synergistically enhance the cancer therapeutic efficacy with few side effects upon NIR laser irradiation.

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In vivo evaluation of an oral self-emulsifying drug delivery system (SEDDS) for exenatide

Abstract: According to these results, hydrophobic ion pairing in combination with SEDDS represents a promising tool for oral peptide delivery.

Cited by 94 publications

References 29 publications

Development of a Solid Self‐Emulsification Delivery System for the Oral Delivery of Astaxanthin

Development of a Solid Self‐Emulsification Delivery System for the Oral Delivery of Astaxanthin

PEGylation of Ginsenoside Rg3-Entrapped Bovine Serum Albumin Nanoparticles: Preparation, Characterization, and In Vitro Biological Studies

pH‐Triggered Conformational Change of Antp‐Based Drug Delivery Platform for Tumor Treatment with Combined Photothermal Therapy and Chemotherapy

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