Azithromycin Cationic Non-Lecithoid Nano/Microparticles Improve Bioavailability and Targeting Efficiency

Zhong, Meng; Feng, Yulin; Liao, Hong; Hu, Xueyuan; Wan, Shengli; Zhu, Biyue; Zhang, Mi; Xiong, Hua; Zhou, Yunli; Zhang, Jingqing

doi:10.1007/s11095-014-1382-7

Cited by 29 publications

(14 citation statements)

References 41 publications

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“…They were designed to overcome the limitations of liposomes, particularly those related to phospholipid oxidation. Cationic niosome-based azithromycin delivery systems (AMCNS) were successfully developed by Zhong et al [38].…”

Section: Nanostructures For Drug Delivery By Oral Administrationmentioning

confidence: 99%

Role of nanostructures in improvising oral medicine

Ghosh

Sil

2019

Toxicology Reports

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Section: Nanostructures For Drug Delivery By Oral Administrationmentioning

confidence: 99%

Role of nanostructures in improvising oral medicine

Ghosh

Sil

2019

Toxicology Reports

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“…Different strategies and techniques were employed for this purpose such as complexation, chemical modification, solid dispersions, and the use of nanocarriers and drug delivery systems. Solid dispersions [11,15,25], nanosuspensions [26], and niosomes [27] of AZM were employed to enhance its solubility and dissolution rates.…”

Section: Introductionmentioning

confidence: 99%

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

et al. 2020

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Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1(H)), and S-SEDDs (S-F1(H)) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.

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“…However, nanotechnology shows appealing potency in traditional drug design, delivery, medical diagnostics and therapy [ 20 – 22 ]. Among the nanocarriers addressing the obstacles of low-solubility bioactive compounds, nanoemulsions may be superior over micelles, and some other nanocarriers in terms of (1) higher solubilization capacity derived from the inner oil phase besides the surfactant and cosurfactant; (2) easiness and steadiness for sterilization through membrane filtration and autoclave treatment, which is of great importance for experimental and clinical utilization; (3) spherical droplets with tiny size (usually < 100 nm), suggesting huge surface to volume ratios, a very vital property for the efficient delivery of drugs [ 23 ]; (4) favorable transparent appearance.…”

Section: Discussionmentioning

confidence: 99%

Efficient intracellular delivery makes cancer cells sensitive to nanoemulsive chemodrugs

et al. 2017

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Evodiamine has been documented to possess activities in numerous cancer cells. Our preliminary study showed that A549 cells were insensitive to evodiamine. In this paper, A549 cells are sensitive to nanoemulsive evodiamine (EVONE) through an efficient intracellular and systematic delivery. EVONE entered tumor cells by energy-dependent and mainly through clathrin-mediated endocytosis. EVONE exerted a higher cytotoxicity in a dose- and time-dependent manner. The enhanced induction of cell cycle arrest was ascribed to the down-regulation of cyclin B and cyclin dependent kinase 1, while the enhanced induction of apoptosis was due to the activation of caspase −3, −8 and −9 and the decreased B-cell lymphoma 2/ assaciated X protein ratio. Furthermore, the in vivo kinetic, bioavailability and in situ absorption characteristics of EVONE were much better than those of free evodiamine. The cancer cells insensitive to free chemodrugs became sensitive to nanoemulsive chemodrugs.

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Azithromycin Cationic Non-Lecithoid Nano/Microparticles Improve Bioavailability and Targeting Efficiency

Abstract: The development of niosome-based AM nanocarriers provides valuable tactics in antibacterial therapy and in non-lecithoid niosomal application.

Cited by 29 publications

References 41 publications

Role of nanostructures in improvising oral medicine

Role of nanostructures in improvising oral medicine

Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

Efficient intracellular delivery makes cancer cells sensitive to nanoemulsive chemodrugs

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