Mucoadhesive chitosan-coated solid lipid nanoparticles for better management of tuberculosis

Vieira, Alexandre C.C.; Chaves, Luíse L.; Pinheiro, Sara; Pinto, Soraia; Pinheiro, Marina; Lima, Sofia A. Costa; Ferreira, Domingos; Sarmento, Bruno

doi:10.1016/j.ijpharm.2017.11.071

Cited by 120 publications

(59 citation statements)

References 33 publications

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“…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]. Therefore, the aim of this study was the development and optimization of novel DFL-loaded stearic acid (lipid) chitosan (polymer) hybrid nanoparticles (L-P-NPs) and their in-vitro/in vivo characterizations.…”

Section: Introductionmentioning

confidence: 99%

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: Introductionmentioning

confidence: 99%

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

et al. 2020

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“…Moreover, NPs coated with chitosan have been reported in the literature to enhance stability and drug loading, controlling the drug release and maximizing the efficacy. Chitosan-coated poly (lactic-co-glycolic acid) NPs, magnetic NPs coated with chitosan, chitosan-coated cobalt ferrite NPs, chitosan-coated solid lipid NPs and chitosan-coated liposomes are common examples [5,8,14,17,21,24,42].…”

Section: Introductionmentioning

confidence: 99%

Development of rosuvastatin flexible lipid-based nanoparticles: promising nanocarriers for improving intestinal cells cytotoxicity

Ahmed

2020

BMC Pharmacol Toxicol

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Background: Rosuvastatin (RSV) is a poorly water-soluble drug that has an absolute oral bioavailability of only 20%. The aim of this work was to prepare a positively charged chitosan coated flexible lipid-based vesicles (chitosomes) and compare their characteristics to the corresponding negatively charged flexible liposomal nanoparticles (NPs) in order to develop new RSV nanocarrier systems. Methods: Three formulation factors affecting the development of chitosomes nano-formulation were optimized for their effects on the particles size, entrapment efficiency (EE) and zeta potential. The optimized flexible chitosomes and their corresponding liposomal NPs were characterized for morphology, in vitro release, flexibility and intestinal cell viability. The half maximum inhibitory concentrations (IC50) for both formulations were calculated.Results: The drug to lipid molar ratio, edge activator percent and the chitosan concentration were significantly affecting the characteristics of NPs. The optimized chitosomes nano-formulation exhibited larger size, higher EE and greater zeta potential value when compared to the corresponding liposomal NPs. Both formulations showed a spherical shape nanostructure with a marked outer shell for the chitosomes nano-formulation. Chitosomes illustrated an extended drug release profile when compared with the corresponding liposomal NPs and the prepared drug suspension. Flexibility of both vesicles was confirmed with superiority of liposomal NPs over chitosomes. RSV loaded chitosomes nano-formulation exhibited lower IC50 values and higher therapeutic window while liposomal NPs were compatible with the intestinal cells. Conclusions: RSV loaded chitosomes nano-formulation could be considered as a promising nanocarrier system with a marked cytotoxic activity while, RSV loaded liposomal NPs are suitable nanocarrier to improve RSV activity in treatment of cardiovascular disorders.

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“…The particle size, PDI, ZP, EE% and DL% were also different from each other, mainly because the materials and methods used to prepare these formulations were different. Compared with these studies, [37][38][39][40][41] the NPs presented in our study may have a relatively smaller particle size, lower PDI and higher ZP and %EE, which may be ascribed to the combined method used in the present study and the inherent property of RPT. Esmaeili et al 42 fabricated PLGA NPs loaded with rifampicin using the combined method of homogenisation and solvent evaporation.…”

Section: Physicochemical Characterisationmentioning

confidence: 56%

<p>Development of Rifapentine-Loaded PLGA-Based Nanoparticles: In vitro Characterisation and in vivo Study in Mice</p>

Liang¹,

Xiang²,

Li³

et al. 2020

IJN

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Background: Tuberculosis (TB) is a leading cause of death amongst infectious diseases. The poor response to antitubercular agents necessitates the long-term use of high drug doses, resulting in low patient compliance, which is the main reason for chemotherapy failure and contributes to the development of multidrug-resistant TB. Patient non-compliance has been a major obstacle in the successful management of TB. The aim of this work was to develop and characterise rifapentine (RPT)-loaded PLGA-based nanoparticles (NPs) for reducing dosing frequency. Methods: RPT-loaded PLGA and PLGA-PEG NPs were prepared using premix membrane homogenisation combined with solvent evaporation method. The resulting NPs were characterised in terms of physicochemical characteristics, toxicity, cellular uptake and antitubercular activity. NPs were further evaluated for pharmacokinetic and biodistribution studies in mice. Results: The resulting NPs showed suitable and safe physicochemical characteristics and could be taken up by macrophages. RPT-loaded NPs were more effective against Mycobacterium tuberculosis than free RPT. In vivo studies revealed that NPs could improve pharmacokinetic parameters, particularly for RPT/PLGA-PEG NPs. Moreover, both formulations had no toxicity to the organs of mice and could reduce hepatotoxicity. Conclusion: The application of PLGA-based NPs as sustained-release delivery vehicles for RPT could prolong drug release, modify pharmacokinetics, increase antitubercular activity and diminish toxicity, thereby allowing low dosage and frequency.

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Mucoadhesive chitosan-coated solid lipid nanoparticles for better management of tuberculosis

Cited by 120 publications

References 33 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

Development of rosuvastatin flexible lipid-based nanoparticles: promising nanocarriers for improving intestinal cells cytotoxicity

<p>Development of Rifapentine-Loaded PLGA-Based Nanoparticles: In vitro Characterisation and in vivo Study in Mice</p>

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