Characterization of biodegradable chitosan microspheres containing vancomycin and treatment of experimental osteomyelitis caused by methicillin-resistant Staphylococcus aureus with prepared microspheres

Cevher, Erdal; Orhan, Zafer; Mülazımoğlu, Lütfiye; Şensoy, Demet; Alper, Murat; Yildiz, Ayca; Özsoy, Yıldız

doi:10.1016/j.ijpharm.2006.03.014

Cited by 133 publications

(81 citation statements)

References 68 publications

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“…However, many of these compounds are associated with anaphylaxis, cytotoxicity or low efficiency [5,13]. These limiting aspects prompt the use of true antibiotics such as vancomycin, tobramycin, cefalozin, teicoplanin, carbenicillin, amoxicillin, penicillin, ampicillin and gentamicin [3,[34][35][36][37], through two different strategies: substance-releasing coating and substance covalent immobilization. The release strategy offers the potential for extended activity, but has to date failed to achieve delivery of a sustained and effective dosage over a relatively prolonged period of time.…”

Section: Antimicrobial Coatingsmentioning

confidence: 99%

“…Thus, stable immobilization of AMPs onto a biomaterial could be the pathway to overcome these difficulties [72]. Covalent immobilization of AMP can increase their long-term stability while decreasing their toxicity, as compared to incorporation approaches on leach-or releasebased systems [11,35,36,69,[72][73][74][75]. Furthermore, the proper orientation of the peptide may result in enhanced activity [34].…”

Section: Covalent Immobilization Of An Antimicrobial Peptidementioning

confidence: 99%

“…polyamide resins, PEG-modified polystyrene resins, cellulose), as done in Refs. [28,35,39] or [46] (Table 1). To this end, standard solid-phase peptide synthesis (SPPS) methods may be used, such as the wellestablished Fmoc/ t Bu strategy [79].…”

Section: Solid Supports and Chemical Coupling Strategiesmentioning

confidence: 99%

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Covalent immobilization of antimicrobial peptides (AMPs) onto biomaterial surfaces

et al. 2011

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a b s t r a c tBacterial adhesion to biomaterials remains a major problem in the medical devices field. Antimicrobial peptides (AMPs) are well-known components of the innate immune system that can be applied to overcome biofilm-associated infections. Their relevance has been increasing as a practical alternative to conventional antibiotics, which are declining in effectiveness. The recent interest focused on these peptides can be explained by a group of special features, including a wide spectrum of activity, high efficacy at very low concentrations, target specificity, anti-endotoxin activity, synergistic action with classical antibiotics, and low propensity for developing resistance. Therefore, the development of an antimicrobial coating with such properties would be worthwhile. The immobilization of AMPs onto a biomaterial surface has further advantages as it also helps to circumvent AMPs' potential limitations, such as short half-life and cytotoxicity associated with higher concentrations of soluble peptides. The studies discussed in the current review report on the impact of covalent immobilization of AMPs onto surfaces through different chemical coupling strategies, length of spacers, and peptide orientation and concentration. The overall results suggest that immobilized AMPs may be effective in the prevention of biofilm formation by reduction of microorganism survival post-contact with the coated biomaterial. Minimal cytotoxicity and longterm stability profiles were obtained by optimizing immobilization parameters, indicating a promising potential for the use of immobilized AMPs in clinical applications. On the other hand, the effects of tethering on mechanisms of action of AMPs have not yet been fully elucidated. Therefore, further studies are recommended to explore the real potential of immobilized AMPs in health applications as antimicrobial coatings of medical devices.

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Section: Antimicrobial Coatingsmentioning

confidence: 99%

Section: Covalent Immobilization Of An Antimicrobial Peptidementioning

confidence: 99%

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Covalent immobilization of antimicrobial peptides (AMPs) onto biomaterial surfaces

et al. 2011

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“…These factors emphasize the need to develop methods to enhance delivery of vancomycin to bone in the treatment of osteomyelitis. One way to accomplish this is to employ local antibiotic delivery, which while useful suffers from inherent limitations, not the least being the ability to gain direct access to the infection site (8)(9)(10)(11)(12)(13)(14)(15)(16). Thus, one of the major challenges to improve therapeutic outcomes for osteomyelitis patients is to develop methods for the systemic deliv-ery of vancomycin, and potentially other antibiotics, in sufficient concentrations to achieve the desired therapeutic effect.…”

mentioning

confidence: 99%

Novel Bone-Targeting Agent for Enhanced Delivery of Vancomycin to Bone

Albayati

Sunkara

Schmidt-Malan

et al. 2016

Antimicrob Agents Chemother

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hWe examined the pharmacokinetic properties of vancomycin conjugated to a bone-targeting agent (BT) with high affinity for hydroxyapatite after systemic intravenous administration. The results confirm enhanced persistence of BT-vancomycin in plasma and enhanced accumulation in bone relative to vancomycin. This suggests that BT-vancomycin may be a potential carrier for the systemic targeted delivery of vancomycin in the treatment of bone infections, potentially reducing the reliance on surgical debridement to achieve the desired therapeutic outcome. Osteomyelitis is defined as any inflammatory process in bone, the most common cause of which is infection. Although many bacterial pathogens have been associated with osteomyelitis, Staphylococcus aureus is the predominant cause and the pathogen responsible for the most serious forms of bone infection (1). Given the increasing prevalence of S. aureus strains resistant to methicillin (2), vancomycin remains the most commonly used antibiotic for the treatment of these infections (3). While true vancomycin resistance is rare, S. aureus strains with reduced susceptibility are common and often arise as a consequence of the prolonged periods of vancomycin therapy required to treat bone infections (1, 4). Vancomycin acts by inhibiting bacterial cell wall biosynthesis (5, 6) and is a large hydrophilic molecule that has limited penetration into bone and therefore low bone bioavailability when administered systemically (7). These factors emphasize the need to develop methods to enhance delivery of vancomycin to bone in the treatment of osteomyelitis. One way to accomplish this is to employ local antibiotic delivery, which while useful suffers from inherent limitations, not the least being the ability to gain direct access to the infection site (8-16). Thus, one of the major challenges to improve therapeutic outcomes for osteomyelitis patients is to develop methods for the systemic deliv-

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“…AlQadi investigated this process successfully to produce microencapsulated proteinloaded CS nanoparticles as DPI formulation (Al-Qadi, Grenha, Carrión-Recio, Seijo, & Remuñán-López, 2012). However, after spray-drying, the production yield of particles is relatively low (~ 47-50%) (Sosnik & Seremeta, 2015) due to the loss of liquid droplets inside the wall of the drying chamber (Cevher et al, 2006). Besides, the ineffective separation capacity of cyclone and the insufficient forces of liquid atomization affects the formation of appropriate submicron particles, which influences the size and size distribution in the development of the pulmonary drug delivery system (Oliveira, Guimarães, Cerize, Tunussi, & Poço, 2014).…”

Section: Nanocarriers For Pulmonary Deliverymentioning

confidence: 99%

Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery

Wang¹

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Cigarette smoking has become one of the leading causes of preventable deaths all over the world, causing a serious threat to human wellbeing and a tremendous economic burden to governments. The currently available treatment options for smoking cessation are not efficient. The pulmonary delivery of drugs by methods such as dry powder inhaler (DPI) has been recognized as one of the most efficient routes of drug delivery to the targeted area. The lung delivery of nicotine in this way would be expected to mimic the effects of tobacco smoking and could significantly reduce the negative health effects of smoking that result from nicotine addiction.The aim of this study is to develop nanoparticles with controlled physicochemical properties using biodegradable polymer of chitosan (CS) loaded with nicotine salt for pulmonary delivery as DPI formulations. The outcomes of this project are expected to be a safe and effective CS-based nicotine formulation for pulmonary delivery to treat nicotine dependence. This thesis specially addresses the research questions: (1) how to develop a feasible process to manufacture the nanoparticles suitable for pulmonary drug delivery using biodegradable polymer of CS containing nicotine salt; (2) how to develop an animal model for pulmonary drug delivery from DPI formulation using a nose-only inhalation device.The current therapeutic options for treatment of smoking addiction have been reviewed, and current advancements of technology in pulmonary drug delivery are summarised. Buccal administration of drugs exhibits a low oral bioavailability, and sublingual tablets and chewing gums can be swallowed before being absorbed.Although nasal spray of nicotine is a fast way to deliver nicotine into the bloodstream, Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery iii the rate of absorption is still not as rapid as cigarette smoking. Therefore, it is proposed that delivery of nicotine with sustained drug release profile direct into the deep lung is likely to more effectively mimic the rapid effects of cigarette smoking on a physiological level, which could eliminate patient craving and allow the tapering of nicotine level over time to improve patients' compliance.Water in oil (w/o) emulsion crosslinking method has been used to fabricate nicotine hydrogen tartrate (NHT)-loaded CS nanoparticles which separate as solid microaggregates. The physicochemical properties of particles are characterized by a series of techniques. Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) shows that the prepared particles are spherical in morphology with rough surface after loading CS particles with NHT. Dynamic Light Scattering (DLS)by Zetasizer determined nanoparticle size ranging from 167.6 nm to 411 nm, while DLS by Mastersizer demonstrated that the microaggregates of these nanoparticles are in the respirable range (<5µm). The surface positive charge as measured by zeta potential tends to decrease with increase of mass ratios of NHT to CS, which is in contr...

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Characterization of biodegradable chitosan microspheres containing vancomycin and treatment of experimental osteomyelitis caused by methicillin-resistant Staphylococcus aureus with prepared microspheres

Cited by 133 publications

References 68 publications

Covalent immobilization of antimicrobial peptides (AMPs) onto biomaterial surfaces

Covalent immobilization of antimicrobial peptides (AMPs) onto biomaterial surfaces

Novel Bone-Targeting Agent for Enhanced Delivery of Vancomycin to Bone

Development of Nicotine Loaded Chitosan Nanoparticles for Lung Delivery

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