Optimization of rifampicin encapsulation in PLGA polymeric reservoirs

Castañeda-Fernandez, Carolina; Chávez-Santos, Rosa María; Silva-Miranda, Mayra; Espitia-Pinzón, Clara; Martínez, Roberto; Kozina, Anna

doi:10.1016/j.ijpharm.2022.121844

Cited by 2 publications

(3 citation statements)

References 51 publications

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“…It can also undergo autoxidation, turning into rifampicin quinone. Therefore, it is necessary to administer high doses (approximately 10 mg/kg of the patient’s weight) for the drug to reach its desired therapeutic efficacy, causing the appearance of potentially toxic side effects, such as hepatitis, anorexia, skin eruptions, and renal failure [ 6 , 7 , 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

Montmorillonite–Rifampicin Nanohybrid for pH-Responsive Release of the Tuberculostatic

et al. 2023

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The present work describes the development of a hybrid and pH-responsive system for rifampicin using the clay mineral ‘montmorillonite’ as a nanocarrier. The influence of operational variables on the drug incorporation process was evaluated using 24 factorial designs. Under optimized conditions, the experiment allowed an incorporated drug dose equivalent to 98.60 ± 1.21 mg/g. Hybrid systems were characterized by different characterization techniques (FTIR, XRD, TGA, DSC, and SEM) to elucidate the mechanism of interaction between the compounds used. Through in vitro release studies, it was possible to verify the efficacy of the pH-dependent system obtained, with approximately 70% of the drug released after sixteen hours in simulated intestinal fluid. The adjustment of the experimental release data to the theoretical model of Higuchi and Korsmeyer–Peppas indicated that the release of rifampicin occurs in a prolonged form from montmorillonite. Elucidation of the interactions between the drug and this raw clay reinforces its viability as a novel carrier to develop an anti-TB/clay hybrid system with good physical and chemical stability.

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Section: Introductionmentioning

confidence: 99%

Montmorillonite–Rifampicin Nanohybrid for pH-Responsive Release of the Tuberculostatic

et al. 2023

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“…However, the use of rifampicin is limited due to several drawbacks, including its low bioavailability, which demands the administration of large doses throughout treatment. This prolonged administration can lead to significant side effects, such as skin, liver, and hypersensitivity reactions. , …”

Section: Introductionmentioning

confidence: 99%

“…This prolonged administration can lead to significant side effects, such as skin, liver, and hypersensitivity reactions. 21 , 22 …”

Section: Introductionmentioning

confidence: 99%

Enhancing Therapeutic Efficacy against Brucella canis Infection in a Murine Model Using Rifampicin-Loaded PLGA Nanoparticles

Hernández-Giottonini,

Arellano-Reynoso,

Rodríguez-Córdova

et al. 2023

ACS Omega

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The in vivo efficacy of rifampicin encapsulated in poly(lactic- co -glycolic acid) (PLGA) nanoparticles was evaluated for the treatment of BALB/c mice experimentally infected with Brucella canis . The PLGA nanoparticles loaded with rifampicin (RNP) were prepared using the single emulsification-solvent evaporation technique, resulting in nanoparticles with a hydrodynamic diameter of 138 ± 6 nm. The zeta potential and polydispersity index values indicated that the system was relatively stable with a narrow size distribution. The release of rifampicin from the nanoparticles was studied in phosphate buffer at pH 7.4 and 37 °C. The release profile showed an initial burst phase, followed by a slower release stage attributed to nanoparticle degradation and relaxation, which continued for approximately 30 days until complete drug release. A combined model of rifampicin release, accounting for both the initial burst and the degradation–relaxation of the nanoparticles, effectively described the experimental data. The efficacy of RNP was studied in vivo ; infected mice were treated with free rifampicin at concentrations of 2 mg per kilogram of mice per day (C1) and 4 mg per kilogram of mice per day (C2), as well as equivalent doses of RNP. Administration of four doses of the nanoparticles significantly reduced the B. canis load in the spleen of infected BALB/c mice. RNP demonstrated superior effectiveness compared to the free drug in the spleen, achieving reductions of 85.4 and 49.4%, respectively, when using C1 and 93.3 and 61.8%, respectively, when using C2. These results highlight the improved efficacy of the antibiotic when delivered through nanoparticles in experimentally infected mice. Therefore, the RNP holds promise as a potential alternative for the treatment of B. canis .

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Optimization of rifampicin encapsulation in PLGA polymeric reservoirs

Cited by 2 publications

References 51 publications

Montmorillonite–Rifampicin Nanohybrid for pH-Responsive Release of the Tuberculostatic

Montmorillonite–Rifampicin Nanohybrid for pH-Responsive Release of the Tuberculostatic

Enhancing Therapeutic Efficacy against Brucella canis Infection in a Murine Model Using Rifampicin-Loaded PLGA Nanoparticles

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