Analysis of the molecular association of rifampicin with hydroxypropyl-²-cyclodextrin

Ferreira, Denise Alves; Ferreira, Antônio Gilberto; Vizzotto, Lucinéia; Neto, Alberto Federman; Oliveira, Anselmo Gomes de

doi:10.1590/s1516-93322004000100008

Cited by 11 publications

(7 citation statements)

References 27 publications

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“…However, only a 2-fold solubilization extent was apparent with β-CD when a common solvent technique was employed. As opposed to the findings by Ferreira et al [36], herein no solubility improvement of RIF was found with HPβCD. On the other hand, all the complexes improved the thermal stability of the drug.…”

Section: Cyclodextrinscontrasting

confidence: 99%

“…Several works reported on the complexation of RIF by means of different CD molecules, though results regarding the efficiency of this approach are ambiguous. Ferreira and collaborators prepared inclusion complexes of RIF with HPβCD [36]. The aqueous solubility of the drug increased linearly with the concentration of the CD, with the CD/RIF ratio in the complex being 1:1.…”

Section: Cyclodextrinsmentioning

confidence: 99%

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Nanotechnology: A focus on Treatment of Tuberculosis.

Kumar¹,

Kumar²,

Kumar³

et al. 2011

Int J Drug Del

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Despite the fact that we live in an era of advanced technology and innovation, infectious diseases, like Tuberculosis (TB), continue to be one of the greatest health challenges worldwide. The main drawbacks of conventional TB treatment are the development of multiple drug resistance, resulting in high dose requirements and subsequent intolerable toxicity. Therefore there is a need of a new system have been receiving special attention with the aim of minimizing the side effects of drug therapy, such as poor bioavailability and the selectivity of drugs. Nanoparticle-based drug delivery systems have considerable potential for treatment of TB. The important technological advantages of nanoparticles used as drug carriers are high stability, high carrier capacity, feasibility of incorporation of both hydrophilic and hydrophobic substances, and feasibility of variable routes of administration, including oral application and inhalation. Nanoparticles can also be designed to allow controlled (sustained) drug release from the matrix. These properties of nanoparticles enable improvement of drug bioavailability and reduction of the dosing frequency, and may resolve the problem of nonadherence to prescribed therapy, which is one of the major obstacles in the control of TB epidemics. In this review, we discuss the challenges with the current treatment of the disease and shed light on the remarkable potential of nanotechnology to provide more effective treatment and prevention for TB.

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Section: Cyclodextrinscontrasting

confidence: 99%

Section: Cyclodextrinsmentioning

confidence: 99%

Nanotechnology: A focus on Treatment of Tuberculosis.

Kumar¹,

Kumar²,

Kumar³

et al. 2011

Int J Drug Del

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show abstract

“…Ferreira et al, prepared inclusion complexes of RIF with hydroxyl propyl β cyclodextrin (HPβCD) [103]. The complexation increased aqueous solubility of the drug linearly to the concentration of the CD used.…”

Section: Cyclodextrin Inclusion Complexesmentioning

confidence: 99%

Present status of nanoparticle research for treatment of Tuberculosis

2011

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-Nanotechnology has offered enormous improvement in field of therapeutics by means of designing of drug delivery systems and opened the possibility of controlling infections at the molecular level. Nanocarriers can cross biological barriers and are able to target cellular reservoirs of Mycobacterium tuberculosis (M. tuberculosis). Nanoparticle-based systems have significant potential for treatment and prevention of tuberculosis (TB). A variety of nanocarriers have been widely evaluated as potential drug delivery systems for various administration routes. Targeting the drugs to certain physiological sites such as the lymph nodes has emerged as a promising strategy in treating TB with improved drug bioavailability and reduction of the dosing frequency. Nanotechnology based rational targeting may improve therapeutic success by limiting adverse drug effects and requiring less frequent administration regimes, ultimately resulting in more patients compliance and thus attain higher adherence levels. The development of nanoparticle based aerosol vaccine is undergoing which could serve as new platform for immunization. Present article compiles the general physiological aspects of the infection along with new research uptades on nanocarriers used in prevention of tuberculosis. _______________________________________________________________________________________

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“…With regard to modified HP-βCD and γCD cyclodextrins, the data obtained allowed us to suspect that the piperazine side chain of RIF is preferably enclosed into HP-βCD hydrophobic cavity, whereas for HP-γCD the complex shows the bulkiest region of RIF molecule is preferably enclosed into cyclodextrin cavity. In fact, the results indicate that the most stable complex (due to less energy value) has the RIF complexed with HP-βCD through the piperazine tail enclosed into the hydrophobic cavity of HP-βCD and the bulky region of the molecule in the surface cavity of cyclodextrin [16,19,31]. The data regarding HP-γCD shows that the preferred poses have the bulky fragment of RIF placed in the inner cavity.…”

Section: Molecular Modeling Studiesmentioning

confidence: 98%

Inclusion Complexes of Rifampicin with Native and Derivatized Cyclodextrins: In Silico Modeling, Formulation, and Characterization

et al. 2021

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Inclusion complexation of rifampicin (RIF) with several types of cyclodextrins (βCD, hydroxypropyl-βCD, γCD, hydroxypropyl-γCD) in aqueous solutions at different pH values was investigated to assess the interactions between RIF and cyclodextrins (CDs). Molecular modeling was performed to determine the possible interactions between RIF and CDs at several pH values. The inclusion complexes were characterized by differential scanning calorimetry, Fourier transform infrared spectroscopy, powder X-ray diffractometry, and scanning electron microscopy. Moreover, this study evaluated the dissolution profile and antibacterial activity of the formed complexes. Phase solubility analysis suggested the formation of RIF-CD affirmed 1:1 stoichiometry at all pH values (except RIF-βCD at pH 4.0 and both βCD and γCD at pH 9.0). The inclusion complexation of RIF with CD successfully increased the percentage of RIF released in in vitro studies. The inclusion complexes of RIF exhibited more than 60% of RIF released in 2 h which was significantly higher (p < 0.05) than release of pure RIF, which was only less than 10%. Antibacterial activity of RIF-CD complexes (measured by the minimum inhibitory concentration of RIF against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus) was lower for both RIF-βCD and RIF-HPγCD at pH 7.0 to pure RIF suspension. In conclusion, this work reports that both βCD and γCD can be used to enhance the solubility of RIF and thus, improve the effectivity of RIF by decreasing the required daily dose of RIF for the treatment of bacterial infections.

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Analysis of the molecular association of rifampicin with hydroxypropyl-²-cyclodextrin

Cited by 11 publications

References 27 publications

Nanotechnology: A focus on Treatment of Tuberculosis.

Nanotechnology: A focus on Treatment of Tuberculosis.

Present status of nanoparticle research for treatment of Tuberculosis

Inclusion Complexes of Rifampicin with Native and Derivatized Cyclodextrins: In Silico Modeling, Formulation, and Characterization

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