Distribution coefficient of rifabutin in liposome/water system as measured by different methods

Vostrikov, Vitaly V.; Селищева, А. А.; Сорокоумова, Г. М.; Shakina, Yulia N.; Швец, В. И.; Savel’ev, O. Yu.; Polshakov, Vladimir I.

doi:10.1016/j.ejpb.2007.05.014

Cited by 18 publications

(26 citation statements)

References 10 publications

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“…Since this transition occurs when the proteins and the PG lipids are "squeezed out" from the monolayer to form the multilayers [53] and at smaller pressures when in the presence of RFB, it is predictable that, in comparison to RFB2, RFB's interactions with PG and proteins are higher. According to the distribution of the charged species, predicted by MarvinView ® 5.4.1.1 software from ChemAxon, at the physiological pH RFB has a higher contribution of the positively charged species (due to the ionization of the piperidine nitrogen with a pKa 9.5) [54], possibly promoting stronger electrostatic interactions with the negatively charged phospholipids (like PG).…”

Section: Comparison Of Compression Isothermsmentioning

confidence: 99%

Interplay of mycolic acids, antimycobacterial compounds and pulmonary surfactant membrane: A biophysical approach to disease

Pinheiro

Giner‐Casares

Lúcio

et al. 2013

Biochimica et Biophysica Acta (BBA) - Biomembranes

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This work focuses on the interaction of mycolic acids (MAs) and two antimycobacterial compounds (Rifabutin and N'-acetyl-Rifabutin) at the pulmonary membrane level to convey a biophysical perspective of their role in disease. For this purpose, accurate biophysical techniques (Langmuir isotherms, Brewster angle microscopy, and polarization-modulation infrared reflection spectroscopy) and lipid model systems were used to mimic biomembranes: MAs mimic bacterial lipids of the Mycobacterium tuberculosis (MTb) membrane, whereas Curosurf® was used as the human pulmonary surfactant (PS) membrane model. The results obtained show that high quantities of MAs are responsible for significant changes on PS biophysical properties. At the dynamic inspiratory surface tension, high amounts of MAs decrease the order of the lipid monolayer, which appears to be a concentration dependent effect. These results suggest that the amount of MAs might play a critical role in the initial access of the bacteria to their targets. Both molecules also interact with the PS monolayer at the dynamic inspiratory surface. However, in the presence of higher amounts of MAs, both compounds improve the phospholipid packing and, therefore, the order of the lipid surfactant monolayer. In summary, this work discloses the putative protective effects of antimycobacterial compounds against the MAs induced biophysical impairment of PS lipid monolayers. These protective effects are most of the times overlooked, but can constitute an additional therapeutic value in the treatment of pulmonary tuberculosis (Tb) and may provide significant insights for the design of new and more efficient anti-Tb drugs based on their behavior as membrane ordering agents.

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Section: Comparison Of Compression Isothermsmentioning

confidence: 99%

Interplay of mycolic acids, antimycobacterial compounds and pulmonary surfactant membrane: A biophysical approach to disease

Pinheiro

Giner‐Casares

Lúcio

et al. 2013

Biochimica et Biophysica Acta (BBA) - Biomembranes

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“…As is known, the RB molecule contains several ionized groups with рК а in the ranges of рН 4.0-5.0, 6.5-7.5, and 9.7-11 [17]. To determine the effect of the charge of the RB molecule on the interaction in the RB-(HP-β-CD) system, we studied the dependence of the solubility of RB on рН in aqueous solutions in the absence and presence of HP-β-CD.…”

Section: Resultsmentioning

confidence: 99%

Intermolecular interactions in rifabutin—2-hydroxypropyl-β-cyclodextrin—water solutions

Anshakova

Yermolenko

Konyukhov

et al. 2015

Russ. J. Phys. Chem.

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“…Considering the results of the rheological study, no differences in the characteristics of the polymer were found comparing the two spray-dried microparticle formulations that could justify this behaviour. Therefore, one possible explanation for this effect could be that HCl remaining in the formulation after spray-drying facilitated RFB solubilisation afterwards, by providing a certain degree of protonation [32]. Another reason could be the existence of a different pattern of dispersion of RFB within the microparticle matrix in each formulation.…”

Section: Inh and Rfb Release From Chs Microparticlesmentioning

confidence: 99%

Inhalable Spray-Dried Chondroitin Sulphate Microparticles: Effect of Different Solvents on Particle Properties and Drug Activity

et al. 2020

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Spray-drying stands as one of the most used techniques to produce inhalable microparticles, but several parameters from both the process and the used materials affect the properties of the resulting microparticles. In this work, we describe the production of drug-loaded chondroitin sulphate microparticles by spray-drying, testing the effect of using different solvents during the process. Full characterisation of the polymer and of the aerodynamic properties of the obtained microparticles are provided envisaging an application in inhalable tuberculosis therapy. The spray-dried microparticles successfully associated two first-line antitubercular drugs (isoniazid and rifabutin) with satisfactory production yield (up to 85%) and drug association efficiency (60%–95%). Ethanol and HCl were tested as co-solvents to aid the solubilisation of rifabutin and microparticles produced with the former generally revealed the best features, presenting a better ability to sustainably release rifabutin. Moreover, these presented aerodynamic properties compatible with deep lung deposition, with an aerodynamic diameter around 4 μm and fine particle fraction of approximately 44%. Finally, it was further demonstrated that the antitubercular activity of the drugs remained unchanged after encapsulation independently of the used solvent.

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Distribution coefficient of rifabutin in liposome/water system as measured by different methods

Cited by 18 publications

References 10 publications

Interplay of mycolic acids, antimycobacterial compounds and pulmonary surfactant membrane: A biophysical approach to disease

Interplay of mycolic acids, antimycobacterial compounds and pulmonary surfactant membrane: A biophysical approach to disease

Intermolecular interactions in rifabutin—2-hydroxypropyl-β-cyclodextrin—water solutions

Inhalable Spray-Dried Chondroitin Sulphate Microparticles: Effect of Different Solvents on Particle Properties and Drug Activity

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