Novel triptorelin acetate-loaded microspheres prepared by a liquid/oil/oil method with high encapsulation efficiency and low initial burst release

2019 ◽  
Vol 54 ◽  
pp. 101390 ◽  
Author(s):  
Liqing Chen ◽  
Atef Mohammed Qasem Ahmed ◽  
Yibin Deng ◽  
Dingyun Cao ◽  
Huanhuan Du ◽  
...  
Keyword(s):  
Encapsulation Efficiency ◽  
Burst Release ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Triptorelin Acetate

In vitro drug release and antibacterial activity evaluation of silk fibroin coated vancomycin hydrochloride loaded poly (lactic-co-glycolic acid) (PLGA) sustained release microspheres

2022 ◽  
pp. 088532822110640
Author(s):  
Shengtang Li ◽  
Xuewen Shi ◽  
Bo Xu ◽  
Jian Wang ◽  
Peng Li ◽  
...  
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Burst Release ◽  
Plga Microspheres ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Initial Burst Release

Currently, the treatment of osteomyelitis poses a great challenge to clinical orthopedics. The use of biodegradable materials combined with antibiotics provides a completely new option for the treatment of osteomyelitis. In this study, vancomycin hydrochloride (VANCO) loaded poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by a double emulsion solvent evaporation method, and the in vitro drug release behaviors of the drug loaded microspheres were explored after coating with different concentrations of silk fibroin (SF). Drug loading, encapsulation efficiency, Scanning electron microscopy, particle size analysis, Fourier transform infrared spectroscopy, hydrophilicity, in vitro drug release, and in vitro antibacterial activity were evaluated. The results showed that the drug loading of vancomycin loaded PLGA microspheres was (24.11 ±1.72)%, and the encapsulation efficiency was (48.21 ±3.44)%. The in vitro drug release indicated that the drug loaded microspheres showed an obvious initial burst release, and the drug loaded microspheres coated with SF could alleviate the initial burst release in varying degrees. It also can reduce the amount of cumulative drug release, and the effect of microspheres coated with 0.1% concentration of SF is the best. The time of in vitro drug release in different groups of drug loaded microspheres can be up to 28 days. The microspheres coated with (0.1%SF) or without (0%SF) SF showed a cumulative release of (82.50±3.51)% and (67.70±3.81)%,respectively. Therefore, the surface coating with SF of vancomycin loaded microspheres can alleviate the initial burst release, reduce the cumulative drug release, potentially prolong the drug action time, and improve the anti-infection effect.

scholarly journals Biodegradable Nanoparticles-Loaded PLGA Microcapsule for the Enhanced Encapsulation Efficiency and Controlled Release of Hydrophilic Drug

2021 ◽  
Vol 22 (6) ◽  
pp. 2792
Author(s):  
Suji Ryu ◽  
Seungyeop Park ◽  
Ha Yeon Lee ◽  
Hyungjun Lee ◽  
Cheong-Weon Cho ◽  
...  
Keyword(s):  
Controlled Release ◽  
Side Effects ◽  
Sustained Release ◽  
Encapsulation Efficiency ◽  
Release Profile ◽  
Burst Release ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Chitosan Coating ◽  
Hydrophilic Drug

Recently, nano- and micro-particulate systems have been widely utilized to deliver pharmaceutical compounds to achieve enhanced therapeutic effects and reduced side effects. Poly (DL-lactide-co-glycolide) (PLGA), as one of the biodegradable polyesters, has been widely used to fabricate particulate systems because of advantages including controlled and sustained release, biodegradability, and biocompatibility. However, PLGA is known for low encapsulation efficiency (%) and insufficient controlled release of water-soluble drugs. It would result in fluctuation in the plasma levels and unexpected side effects of drugs. Therefore, the purpose of this work was to develop microcapsules loaded with alginate-coated chitosan that can increase the encapsulation efficiency of the hydrophilic drug while exhibiting a controlled and sustained release profile with reduced initial burst release. The encapsulation of nanoparticles in PLGA microcapsules was done by the emulsion solvent evaporation method. The encapsulation of nanoparticles in PLGA microcapsules was confirmed by scanning electron microscopy and confocal microscopy. The release profile of hydrophilic drugs can further be altered by the chitosan coating. The chitosan coating onto alginate exhibited a less initial burst release and sustained release of the hydrophilic drug. In addition, the encapsulation of alginate nanoparticles and alginate nanoparticles coated with chitosan in PLGA microcapsules was shown to enhance the encapsulation efficiency of a hydrophilic drug. Based on the results, this delivery system could be a promising platform for the high encapsulation efficiency and sustained release with reduced initial burst release of the hydrophilic drug.

scholarly journals Drug Delivery Applications of Core-Sheath Nanofibers Prepared by Coaxial Electrospinning: A Review

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 305 ◽  
Author(s):  
Bishweshwar Pant ◽  
Mira Park ◽  
Soo-Jin Park
Keyword(s):  
Drug Delivery ◽  
Electrospun Nanofibers ◽  
Coaxial Electrospinning ◽  
Burst Release ◽  
High Porosity ◽  
Nanofiber Membrane ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Small Pore ◽  
Drug Delivery Applications

Electrospinning has emerged as one of the potential techniques for producing nanofibers. The use of electrospun nanofibers in drug delivery has increased rapidly over recent years due to their valuable properties, which include a large surface area, high porosity, small pore size, superior mechanical properties, and ease of surface modification. A drug loaded nanofiber membrane can be prepared via electrospinning using a model drug and polymer solution; however, the release of the drug from the nanofiber membrane in a safe and controlled way is challenging as a result of the initial burst release. Employing a core-sheath design provides a promising solution for controlling the initial burst release. Numerous studies have reported on the preparation of core-sheath nanofibers by coaxial electrospinning for drug delivery applications. This paper summarizes the physical phenomena, the effects of various parameters in coaxial electrospinning, and the usefulness of core-sheath nanofibers in drug delivery. Furthermore, this report also highlights the future challenges involved in utilizing core-sheath nanofibers for drug delivery applications.

scholarly journals PLGA Microspheres of hGH of Preserved Native State Prepared Using a Self-Regulated Process

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 683
Author(s):  
Jebun Nessa Diana ◽  
Ying Tao ◽  
Qiran Du ◽  
Meng Wang ◽  
Chinta Uday Kumar ◽  
...  
Keyword(s):  
Osmotic Pressure ◽  
Recombinant Human Growth Hormone ◽  
Human Growth ◽  
High Dose ◽  
Burst Release ◽  
Polymeric Microspheres ◽  
Aqueous Emulsion ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Physical Chemical

The challenges of formulating recombinant human growth hormone (rhGH) into sustained-release polymeric microspheres include two mutual causal factors, protein denaturing by the formulation process and severe initial burst release related with relative high dose. The stabilizers to protect the proteins must not evoke osmotic pressure inside the microspheres, and the contact of the protein with the interface between water and organic solution of the polymer must be minimized. To meet these criteria, rhGH was pre-formulated into polysaccharide particles via an aqueous–aqueous emulsion in the present study, followed by encapsulating the particles into microspheres through a self-regulated process to minimize the contact of the protein with the water–oil interface. Polysaccharides as the protein stabilizer did not evoke osmotic pressure as small sugar stabilizers, the cause of severe initial burst release. Reduced initial burst enabled reduced protein loading to 9% (from 22% of the once commercialized Nutropin depot), which in turn reduced the dosage form index from 80 to 8.7 and eased the initial burst. A series of physical chemical characterizations as well as biologic and pharmacokinetic assays confirmed that the present method is practically feasible for preparing microspheres of proteins.

scholarly journals Effect of Self-healing Encapsulation on the Initial Burst Release from PLGA Microspheres Containing a Long-Acting Prostacyclin Agonist, ONO-1301

2017 ◽  
Vol 65 (7) ◽  
pp. 653-659 ◽  
Author(s):  
Mai Hazekawa ◽  
Honami Kojima ◽  
Tamami Haraguchi ◽  
Miyako Yoshida ◽  
Takahiro Uchida
Keyword(s):  
Burst Release ◽  
Self Healing ◽  
Plga Microspheres ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Long Acting

Novel Electrospun Bicomponent Scaffolds for Bone Tissue Engineering: Fabrication, Characterization and Sustained Release of Growth Factor

2012 ◽  
Vol 1418 ◽  
Author(s):  
Chong Wang ◽  
Min Wang ◽  
Xiao-Yan Yuan
Keyword(s):  
Tissue Engineering ◽  
Bone Tissue Engineering ◽  
Bone Tissue ◽  
Biological Tissues ◽  
Osteoblastic Cell ◽  
Burst Release ◽  
Electrospinning Technique ◽  
Initial Burst ◽  
Initial Burst Release

ABSTRACTElectrospinning is a versatile technique for fabricating three-dimensional (3D) nanofibrous scaffolds and the scaffolds have been found to elicit desirable cellular behavior for tissue regeneration because the nanofibrous structures mimic the nanofibrous extracellular matrix (ECM) of biological tissues. From the material point of view, the ECM of bone is a nanofibrous nanocomposite consisting of an organic matrix (mainly collagen) and inorganic bone apatite nanoparticles. Therefore, for bone tissue engineering scaffolds, it is natural to construct nanofibrous nanocomposites having a biodegradable polymer matrix and nanosized bioactive bioceramics. Our previous studies demonstrated: (1) electrospun nanocomposite fiber loaded with calcium phosphate (Ca-P) were osteoconductive and could promote osteoblastic cell proliferation and differentiation better than pure polymer fibers; (2) The controlled release of recombinant human bone morphogenetic protein (rhBMP-2) from scaffolds provided the scaffolds with desired osteoinductivity. In the current investigation, novel bicomponent scaffolds for bone tissue engineering were produced using our established dual-source dual-power electrospinning technique to achieve both osteoconductivity and osteoinductivity. In the bicomponent scaffolds, one fibrous component was electrospun Ca-P/PLGA nanocomposite fibers and the other component was emulsion electrospun PDLLA nanofibers incorporated with rhBMP-2. Through electrospinning optimization, both fibers were evenly distributed in bicomponent scaffolds. The mass ratio of rhBMP-2/PDLLA fibers to Ca-P/PLGA fibers in bicomponent scaffolds could be controlled using multiple syringes. The structure and morphology of mono- and bicomponent scaffolds were examined. The in vitro release of rhBMP-2 from mono- and bicomponent scaffolds showed different release amount but similar release profile, exhibiting an initial burst release. Blending PDLLA with polyethylene glycol (PEG) could reduce the initial burst release of rhBMP-2.

Core-shell poly(d,l-lactide-co-glycolide)/poly(ethyl 2-cyanoacrylate) microparticles with doxorubicin to reduce initial burst release

2009 ◽  
Vol 17 (12) ◽  
pp. 1010-1014 ◽  
Author(s):  
Sang-Hyuk Lee ◽  
Hyon-Ho Baek ◽  
Jung Hyun Kim ◽  
Sung-Wook Choi
Keyword(s):  
Core Shell ◽  
Burst Release ◽  
Initial Burst ◽  
Initial Burst Release

The immobilization of antibiotic-loaded polymeric coatings on osteoarticular Ti implants for the prevention of bone infections

2017 ◽  
Vol 5 (11) ◽  
pp. 2337-2346 ◽  
Author(s):  
Dan Li ◽  
Pengfei Lv ◽  
Linfeng Fan ◽  
Yaoyi Huang ◽  
Fei Yang ◽  
...  
Keyword(s):  
Drug Release ◽  
Release Time ◽  
Burst Release ◽  
Polymeric Coatings ◽  
Sustained Drug Release ◽  
Initial Burst ◽  
Initial Burst Release ◽  
Bone Infections

Polymeric multilayers covalently fixed to Ti surfaces could offer a sustained drug release with no initial burst release and extend the drug release time.

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