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.

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 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

scholarly journals Fabrication of tri-layered electrospun polycaprolactone mats with improved sustained drug release profile

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
S. Manjunath Kamath ◽  
K. Sridhar ◽  
D. Jaison ◽  
V. Gopinath ◽  
B. K. Mohamed Ibrahim ◽  
...  
Keyword(s):  
Burst Release ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Electron Microscopic ◽  
Initial Burst ◽  
Cumulative Release ◽  
Scanning Electron Microscopic ◽  
Magnetic Resonance Spectroscopic Analysis ◽  
Ibuprofen Release

Abstract Modulation of initial burst and long term release from electrospun fibrous mats can be achieved by sandwiching the drug loaded mats between hydrophobic layers of fibrous polycaprolactone (PCL). Ibuprofen (IBU) loaded PCL fibrous mats (12% PCL-IBU) were sandwiched between fibrous polycaprolactone layers during the process of electrospinning, by varying the polymer concentrations (10% (w/v), 12% (w/v)) and volume of coat (1 ml, 2 ml) in flanking layers. Consequently, 12% PCL-IBU (without sandwich layer) showed burst release of 66.43% on day 1 and cumulative release (%) of 86.08% at the end of 62 days. Whereas, sandwich groups, especially 12% PCLSW-1 & 2 (sandwich layers—1 ml and 2 ml of 12% PCL) showed controlled initial burst and cumulative (%) release compared to 12% PCL-IBU. Moreover, crystallinity (%) and hydrophobicity of the sandwich models imparted control on ibuprofen release from fibrous mats. Further, assay for cytotoxicity and scanning electron microscopic images of cell seeded mats after 5 days showed the mats were not cytotoxic. Nuclear Magnetic Resonance spectroscopic analysis revealed weak interaction between ibuprofen and PCL in nanofibers which favors the release of ibuprofen. These data imply that concentration and volume of coat in flanking layer imparts tighter control on initial burst and long term release of ibuprofen.

scholarly journals Preparation and in vitro characterization of gellan based floating beads of acetohydroxamic acid for eradication of H. pylori

2007 ◽  
Vol 57 (4) ◽  
pp. 413-427 ◽  
Author(s):  
Parauvathanahalli Rajinikanth ◽  
Brahmeshwar mishra
Keyword(s):  
Drug Release ◽  
Encapsulation Efficiency ◽  
Diffusion Mechanism ◽  
Oral Dosage ◽  
Acetohydroxamic Acid ◽  
Burst Release ◽  
Sustained Drug Release ◽  
H Pylori

Preparation andin vitrocharacterization of gellan based floating beads of acetohydroxamic acid for eradication ofH. pyloriGellan based floating beads of acetohydroxamic acid (AHA) were prepared by the ionotropic gellation method to achieve controlled and sustained drug release for treatment ofHelicobacter pyloriinfection. The prepared beads were evaluated for diameter, surface morphology and encapsulation efficiency. Formulation parameters like concentrations of gellan, chitosan, calcium carbonate and the drug influenced thein vitrodrug release characteristics of beads. Drug and polymer interaction studies were carried out using differential scanning calorimetry. Chitosan coating increased encapsulation efficiency of the beads and reduced the initial burst release of the drug from the beads. Kinetic treatment of the drug release data revealed a matrix diffusion mechanism. Prepared floating beads showed good antimicrobial activity (in vitro H. pyloriculture) as potent urease inhibitors. In conclusion, an oral dosage form of floating gellan beads containing AHA may form a useful stomach site specific drug delivery system for the treatment ofH. pyloriinfection.

Development of Biodegradable Injectable In situ Forming Implants for Sustained Release of Lornoxicam

2018 ◽  
Vol 16 (1) ◽  
pp. 66-78 ◽  
Author(s):  
Ruby Christian ◽  
Vaishali Thakkar ◽  
Tushar Patel ◽  
Mukesh Gohel ◽  
Lalji Baldaniya ◽  
...  
Keyword(s):  
Plasma Concentration ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Maximum Plasma ◽  
Sustained Drug Release ◽  
Drug Entrapment Efficiency ◽  
Ft Ir

Objective: The focus of this study was to develop in situ injectable implants of Lornoxicam which could provide sustained drug release. Methods: Biodegradable in situ injectable implants were prepared by polymer precipitation method using polylactide-co-glycolide (PLGA). An optimized formulation was obtained on the basis of drug entrapment efficiency, gelling behavior and in vitro drug release. The compatibility of the formulation ingredients were tested by Fourier transform infrared (FT-IR) spectroscopy, and differential scanning colorimetry (DSC). SEM study was performed to characterize in vivo behavior of in situ implant. Pharmacokinetic study and in vivo gelling study of the optimized formulation were performed on Sprague-Dawley rats. Stability testing of optimized formulation was also performed. Results: The drug entrapment efficiency increased and burst release decreased with an increase in the polymer concentration. Sustained drug release was obtained up to five days. SEM photomicrographs indicated uniform gel formation. Chemical interaction between the components of the formulation was not observed by FT-IR and DSC study. Pharmacokinetic studies of the optimized formulation revealed that the maximum plasma concentration (Cmax), time to achieve Cmax (Tmax) and area under plasma concentration curve (AUC) were significantly higher than the marketed intramuscular injection of lornoxicam. Stability study of optimized batch showed no change in physical and chemical characteristics. Conclusion: Lornoxicam can be successfully formulated as in situ injectable implant that provides long-term management of inflammatory disorders with improved patient compliance.

Development and Evaluation of Guaifenesin Bilayer Tablet

2010 ◽  
Vol 3 (3) ◽  
pp. 1122-1128 ◽  
Author(s):  
Vijaya Kumar B ◽  
Prasad G ◽  
Ganesh B ◽  
Swathi C ◽  
Rashmi A ◽  
...  
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Drug Content ◽  
Bilayer Tablet

The objective of the present research was to develop a Bilayer tablet of guaifenesin (GBT) using superdisintegrant MCC and sodium starch glycolate for the fast release layer and metalose 90 SH and carbopol 934 for the sustaining layer. The guaifenesin SR granules of different formulation were evaluated for bulk density, tapped density, angle of repose, Carr’s index and Hausners ratio and results were found to be 0.460 ± 0.12 to 0.515 ± 0.03 gm/cm3 , 0.550 ±0.03 to 0.590 ±0.04 gm/cm3 , 19 ±0.01 to 26 ± 0.23, 13.72 ± 0.03 to 19.56 ± 0.04 & 1.137 to 1.196, respectively. The prepared bilayer tablets were evaluated for weight variation, hardness, friability, drug content and in vitro drug release. In vitro dissolution studies were carried out in a USP 24 apparatus I. The formulations gave an initial burst effect to provide the loading dose of the drug followed by sustained release for 12 h from the sustaining layer of matrix embedded tablets. In vitro dissolution kinetics followed the Higuchi model via a non-Fickian diffusion controlled release mechanism after the initial burst release. Stability studies conducted for optimized formulation did not show any change in physical appearance, drug content, matrix integrity and in vitro drug release. The results of the present study clearly indicated that GBT was a stable dosage form and a promising potential of the guaifenesin bilayer system as an alternative to the conventional dosage forms

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