Effects of Pluronic F127-PEG multi-gel-core on the release profile and pharmacodynamics of Exenatide loaded in PLGA microspheres

Wang, Puxiu; Wang, Qian; Ren, Tianyang; Gong, Haoyu; Gou, Jingxin; Zhang, Yu; Cai, Cuifang; Tang, Xing

doi:10.1016/j.colsurfb.2016.08.032

Cited by 22 publications

(11 citation statements)

References 60 publications

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“…In summary, the structural integrity and chemical stability of GOS were maintained during 50 days of incubation, making it suitable for the Poloxamer hydrogel PLGA microsphere delivery system. Good chemical stability of GOS, fine compatibility of GOS and PLGA, and the protection of Poloxamer hydrogel contribute to the desirable structural integrity during the release.…”

Section: Resultsmentioning

confidence: 99%

“…Poloxamer has been applied as a hydrogel at the concentration of 15–50% (w/w); with a progressive increase in temperature, Poloxamer micelles rearrange into cubic structure and then into a hexagonal configuration, promoting the gelation process, making Poloxamer hydrogel thermoreversible and thermosensitive. The three-dimensional network structure of Poloxamer hydrogel could not only avoid the harm of hostile environment such as organic solvent or violent shearing during preparation processes but also protect the biological activity and stability of the hydrophilic drug and control the release rate of microsphere during release period. − F 68 (Poloxamer 188, M w 7680–9510 Da) and F 127 (Poloxamer 407, M w 9840–14 600 Da) are employed as hydrogels, among which F 68 enhances the bioadhesive force and has a higher gelation temperature than that of F 127 . By introducing Poloxamer hydrogel system into the PLGA microsphere, the viscosity of the inner phase is increased, preventing its leakage significantly; thus, the drug-loading capacity and encapsulation efficiency are increased, while burst release is decreased .…”

Section: Introductionmentioning

confidence: 99%

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Goserelin Acetate Loaded Poloxamer Hydrogel in PLGA Microspheres: Core–Shell Di-Depot Intramuscular Sustained Release Delivery System

Pan

Zhang

et al. 2019

Mol. Pharmaceutics

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This study aimed to prepare and optimize goserelin acetate (GOS) loaded hydrogel poly(D,L-lactic acid-coglycolic acid) (PLGA) microsphere that is suitable for long-acting clinical treatment, investigate its structure, and regulate the initial release manner. Here, the PLGA microsphere containing Poloxamer hydrogel loaded with ∼15% (w/w) GOS was prepared by double-emulsion−solvent evaporation method and evaluated in terms of microscopic structure, physicochemical properties, and release manner in vitro and in vivo. Raman volume imaging and scanning electron microscopy studies revealed a core−shell Di-Depot structure of the microsphere, in which multi-GOS-loaded hydrogel depots were distributed in the core region. Under the interaction of hydrogel and PLGA depots, high encapsulation efficiency (94.16%) and low burst release (less than 2%) were achieved, along with the accompanying prolonged administration interval (49 days); an enhanced relative bioavailability 9.36-fold higher than that of Zoladex implant was also observed. Also, by addition of 1−5% acetic acid, the lag time was shortened to 6 days. The strategy for regulating the initial release provides new insights for manipulating the release behavior of the PLGA microspheres. The desirable property of the Poloxamer hydrogel PLGA microsphere indicated its promising application in controlled release drug delivery system.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Goserelin Acetate Loaded Poloxamer Hydrogel in PLGA Microspheres: Core–Shell Di-Depot Intramuscular Sustained Release Delivery System

Pan

Zhang

et al. 2019

Mol. Pharmaceutics

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“…However, as the incubation progressed, polymer degradation accelerated, which was mainly attributed to an autocatalytic effect on PLGA . Polymer erosion produced a water-soluble acid oligomer by ester bond cleavage. , With increasing the incubation time, acidity accumulated inside the matrix and the microclimate pH steeply decreased . The acidic microclimate pH in turn accelerated polymer degradation, causing a rapid decrease on the T g of microspheres .…”

Section: Resultsmentioning

confidence: 99%

Long-Acting Release Microspheres Containing Novel GLP-1 Analog as an Antidiabetic System

Ruan

Liu

et al. 2018

Mol. Pharmaceutics

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Glucagon-like peptide 1 (GLP-1) has recently received significant attention as an efficacious way to treat diabetes mellitus. However, the short half-life of the peptide limits its clinical application in diabetes. In our previous study, a novel GLP-1 analog (PGLP-1) with a longer half-life was synthesized and evaluated. Herein, we prepared the PGLP-1-loaded poly(d,l-lactide- co-glycolide) microspheres to achieve long-term effects on blood glucose control. The incorporation of zinc ion into the formulation can effectively decrease the initial burst release, and a uniform drug distribution was obtained, in contrast to native PGLP-1 encapsulated microspheres. We demonstrated that the solubility of the drug encapsulated in microspheres played an important role in in vitro release behavior and drug distribution inside the microspheres. The Zn-PGLP-1 microspheres had a prominent acute glucose reduction effect in the healthy mice. A hypoglycemic effect was observed in the streptozotocin (STZ) induced diabetic mice through a 6-week treatment of Zn-PGLP-1-loaded microspheres. Meanwhile, the administration of Zn-PGLP-1 microspheres led to the β-cell protection and stimulation of insulin secretion. The novel GLP-1 analog-loaded sustained microspheres may greatly improve patient compliance along with a desirable safety feature.

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“…and no viscous material inside the microspheres, water may carry a certain amount of drugs to the outer layer or surface when it is removed through holes in the microspheres. For the other two inner phases of F-2 and F-3, gelatine polymer and F127 could increase the viscidity of inner phase, so as to more tightly bind the drugs, hindering outside water from diffusing into the inner core and removing the encapsulated drug [38,39], so accordingly decreased burst release for F-2 and F-3 ( Figure 6), as well as increased drug loading and encapsulation efficiency. However, as gelatine existed as a liquid state at the release temperature of 37 C, while F127 was gel under such conditions (Figure 8), the viscidity of the inner phase for F-3 was higher, resulting in a relatively decelerating drug release in this formulation.…”

Section: Discussionmentioning

confidence: 99%

Core/shell PLGA microspheres with controllable in vivo release profile via rational core phase design

Yao

Zhang

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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Highly soluble drugs tend to release from preparations at high speeds, which make them need to be taken at frequent intervals. Additionally, some drugs need to be controlled to release in vivo at certain periods, so as to achieve therapeutic effects. Thus, the objective of this study is to design injectable microparticulate systems with controllable in vivo release profile. Biodegradable PLGA was used as the matrix material to fabricate microspheres using the traditional double emulsification-solvent evaporation method as well as improved techniques, with gel (5% gelatine or 25% F127) or LP powders as the inner phases. Their physicochemical properties were systemically investigated. Microspheres prepared by modified methods had an increase in drug loading (15.50, 16.72, 15.66%, respectively) and encapsulation efficiencies (73.46, 79.42, 74.40%, respectively) when compared with traditional methods (12.01 and 57.06%). The morphology of the particles was characterized by optical microscope (OM) and scanning electron microscopy (SEM), and the amorphous nature of the encapsulated drug was confirmed by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. To evaluate their release behaviour, the in vitro degradation, in vitro release and in vivo pharmacodynamics were subsequently studied. Traditional microspheres prepared in this study with water as the inner phase had a relatively short release period within 16 d when compared with modified microspheres with 5% gelatine as the inner phase, which resulted in a smooth release profile and appropriate plasma LP concentrations over 21 d. Thus this type of modified microspheres can be better used in drugs requiring sustained release. The other two formulations containing 25% F127 and LP micropowders presented two-stage release profiles, resulting in fluctuant plasma LP concentrations which may be suitable for drugs requiring controlled release. All the results suggested that drug release rates from the microspheres prepared by various methods were mainly controlled by either the porosity inside the microspheres or the degradation of materials, which could, therefore, lead to different release behaviours. This results indicated great potential of the PLGA microsphere formulation as an injectable depot for controllable in vivo release profile via rational core phase design. Core/shell microspheres fabricated by modified double emulsification-solvent evaporation methods, with various inner phases, to obtain high loading drugs system, as well as appropriate release behaviours. Accordingly, control in vivo release profile via rational core phase design.

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Effects of Pluronic F127-PEG multi-gel-core on the release profile and pharmacodynamics of Exenatide loaded in PLGA microspheres

Cited by 22 publications

References 60 publications

Goserelin Acetate Loaded Poloxamer Hydrogel in PLGA Microspheres: Core–Shell Di-Depot Intramuscular Sustained Release Delivery System

Goserelin Acetate Loaded Poloxamer Hydrogel in PLGA Microspheres: Core–Shell Di-Depot Intramuscular Sustained Release Delivery System

Long-Acting Release Microspheres Containing Novel GLP-1 Analog as an Antidiabetic System

Core/shell PLGA microspheres with controllable in vivo release profile via rational core phase design

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