Chitosan based polymer-lipid hybrid nanoparticles for oral delivery of enoxaparin

Dong, Wei; Wang, Xiuhua; Liu, Chang; Zhang, Xiao; Zhang, Xin; Chen, Xianzhi; Kou, Yongqiang; Mao, Shirui

doi:10.1016/j.ijpharm.2018.05.076

Cited by 65 publications

(27 citation statements)

References 34 publications

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“…Herein, a preparation of the hybrid form of lipid-polymer nanoparticles provides better structural integrity for nanocarriers [24]. Similar results have been reported in a previous study, where the bioavailability of enoxaparin-loaded L-P-NPs was 4.5-fold higher than an enoxaparin solution [25]. However, there are no significant changes in the half-life, elimination rate constant and mean resident time between these two formulations.…”

Section: Pharmacokinetic Studiessupporting

confidence: 86%

“…DFL-loaded L-P-NPs were prepared by single-emulsion-solvent evaporation technique [25]. Briefly, DFL (10 mg) was dissolved in 2 mL of prepared lipid (stearic acid) solution in ethyl acetate, and this lipid solution was further emulsified with 10 mL of chitosan solution (1 mg/mL) in 1% w/v acetic acid solution containing pluronic 127 surfactant (50 mg) under probe sonication (Ultrasonic processor, gx-130, Berlin, Germany) for 3 min at 60% voltage efficiency at a temperature of 25 • C ( Table 1).…”

Section: Preparation Of Lipid-polymer Hybrid Nanoparticlesmentioning

confidence: 99%

“…Due to its unique characteristics, such as nontoxicity, biocompatibility and biodegradability, as well as its favorable muco-adhesiveness and bio-membrane permeability, chitosan-coated solid-lipid nanoparticles have also been recently reported to effectively promote the in vivo absorption of poorly soluble drugs [19,23]. Recently, lipid-chitosan hybrid nanoparticles (LIPOMER nanoparticles) have been used for the oral delivery of some poorly soluble drugs [19,24,25]. In addition, the role of lipid-polymer hybrid nanoparticles in encapsulating antibiotics, e.g., chitosan-coated lipid nanoparticles loaded with rifampicin, have been evaluated for the better management of tuberculosis [26,27].…”

Section: Introductionmentioning

confidence: 99%

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Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

et al. 2020

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Delafloxacin (DFL) is a novel potent and broad-spectrum fluoroquinolone group of antibiotics effective against both Gram-positive and negative aerobic and anaerobic bacteria. In this study, DFL-loaded stearic acid (lipid) chitosan (polymer) hybrid nanoparticles (L-P-NPs) have been developed by single-emulsion-solvent evaporation technique. The mean particle size and polydispersity index (PDI) of optimized DFL-loaded L-P-NPs (F1-F3) were measured in the range of 299–368 nm and 0.215–0.269, respectively. The drug encapsulation efficiency (EE%) and loading capacity (LC%) of DFL-loaded L-P-NPs (F1-F3) were measured in the range of 64.9–80.4% and 1.7–3.8%, respectively. A sustained release of DFL was observed from optimized DFL-loaded L-P-NPs (F3). Minimum inhibitory concentration (MIC) values of the DFL-loaded L-P-NPs (F3) appeared typically to be four-fold lower than those of delafloxacin in the case of Gram-positive strains and was 2-4-fold more potent than those of delafloxacin against Gram-negative strains. The pharmacokinetic study in rats confirmed that the bioavailability (both rate and extent of absorption) of DFL-loaded L-P-NPs was significantly higher (2.3-fold) than the delafloxacin normal suspension. These results concluded that the newly optimized DFL-loaded L-P-NPs were more potent against both Gram-positive and negative strains of bacteria and highly bioavailable in comparison to delafloxacin normal suspension.

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Section: Pharmacokinetic Studiessupporting

confidence: 86%

Section: Preparation Of Lipid-polymer Hybrid Nanoparticlesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

et al. 2020

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“…Also, co-loading of drugs with different physicochemical properties became possible. In other words, the polymeric core functions to encapsulate either water or oil-soluble drugs and to provide robust structures, whereas the external lipid coat offers the following advantages; (i) acts as a biocompatible shield, (ii) a template for surface modifications, (iii) a barrier preventing the fast leakage of water-soluble drugs (iv) possesses favourable stability in serum (longer circulation times) and (v) good cellular accumulation and targeting ability [33,[56][57][58][59][60][61]. In another study, it was observed that the incorporation of phospholipid into polymeric NPs could significantly enhance their intracellular accumulation [62].…”

Section: Alternative Coatingsmentioning

confidence: 99%

Limitations of Pegylated Nanocarriers: Unfavourable Physicochemical Properties, Biodistribution Patterns and Cellular and Subcellular Fates

Sebak

2018

Int J App Pharm

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Assuming that polyethylene glycol (PEG)-conjugated or PEGylated nanocarriers always offer outstanding physicochemical properties and pharmacokinetics profiles when compared to non-PEGylated ones, is not always accurate. For example, drug-loaded PEGylated nanocarriers for the treatment of cancer will not magically escape the reticuloendothelial system (RES) sequestration and clearance, benefit from the enhanced permeability and retention (EPR) effect of the tumor leaky vasculature and preferentially accumulate in the target tissue or cells. This is too good to be true. In this review, several drawbacks of PEGylation will be discussed; for example, how PEGylation can give rise to unfavourable physicochemical characteristics (e. g. particle size and release patterns) and post in vivo administration limitations of the formulated nanocarriers (e. g. limited evasion of RES uptake, development of hypersensitivity reactions, reduced intracellular accumulation and interference with the subcellular processing of nanocarriers necessary to produce the intended pharmacological effect).This review aims at providing better understanding of the pros and cons of PEGylation, encouraging the use of PEGylation with caution, avoiding the assumption that PEGylation will provide all advantages needed to deliver nanocarriers to the target tissue and looking for alternatives to optimize nanocarriers’ utilization especially in the delivery of chemotherapeutic agents for the treatment of different types of cancer. This review comprises a summary of some of the reported literature between 2013 and 2018 using different search engines; PubMed, Science Direct and Google Scholar, and the keywords listed below.

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“…It was found that all tested fatty glycerides modified-nanoparticles could improve oral bioavailability of LMWH, and short-chain fatty acid performed better absorption enhancement. In recent study [55] , this group also studied the influence of fatty glycerides amount on hydrophobicity of nanoparticles and oral absorption of LMWH. The results showed that all tested amount of fatty glycerides could not only enhance the hydrophobicity of nanoparticles, but also improve oral absorption of LMWH.…”

Section: Strategies For Oral Delivery Of Heparinsmentioning

confidence: 99%

Advanced delivery strategies facilitating oral absorption of heparins

Fang

Tang

2020

Asian Journal of Pharmaceutical Sciences

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Heparins show great anticoagulant effect with few side effects, and are administered by subcutaneous or intravenous route in clinics. To improve patient compliance, oral administration is an alternative route. Nonetheless, oral administration of heparins still faces enormous challenges due to the multiple obstacles. This review briefly analyzes a series of barriers ranging from poorly physicochemical properties of heparins, to harsh biological barriers including gastrointestinal degradation and pre-systemic metabolism. Moreover, several approaches have been developed to overcome these obstacles, such as improving stability of heparins in the gastrointestinal tract, enhancing the intestinal epithelia permeability and facilitating lymphatic delivery of heparins. Overall, this review aims to provide insights concerning advanced delivery strategies facilitating oral absorption of heparins.

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Chitosan based polymer-lipid hybrid nanoparticles for oral delivery of enoxaparin

Cited by 65 publications

References 34 publications

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

Development of Lipomer Nanoparticles for the Enhancement of Drug Release, Anti-Microbial Activity and Bioavailability of Delafloxacin

Limitations of Pegylated Nanocarriers: Unfavourable Physicochemical Properties, Biodistribution Patterns and Cellular and Subcellular Fates

Advanced delivery strategies facilitating oral absorption of heparins

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