Nano-formulation of rifampicin with enhanced bioavailability: Development, characterization and in-vivo safety
Abstract
Rifampicin (RIF) was encapsulated into solid lipid nanoparticles (SLNs) to overcome its poor and unreliable oral bioavailability. Novel microemulsification method with high drug loading (50%) and entrapment efficiency (∼67%) was developed (Indian Patent Application 3356/DEL/2013). RIF-SLNs were characterized using TEM, AFM, DSC and XRD. Near neutral SLNs (zeta -3.5 ± 0.8), with average particle size of 130.0 ± 22.6 nm showed 70.12% release in phosphate buffer pH 6.8 in 9 days. Single oral dose (50mg/kg) pharmacokinetic studies in Wistar rats indicated 8.14 times higher (in comparison to free RIF) plasma bioavailability with sustained levels for 5 days. Pharmacodynamic parameters viz. TMIC (120 h; time for which plasma levels were above MIC of 0.2 μg/ml), AUC0-∞/MIC (1868.9h) and Cmax/MIC (75.6) for RIF-SLNs were greater than free RIF by 2.5, 8.2 and 6.6 times, respectively. Similar LD50 (1570 mg/kg) and absence (or reversal in satellite group) of adverse events in repeat dose (three doses; highest dose was up to 50 times the human therapeutic dose) toxicity studies confirmed safety of RIF-SLNs. Improved pharmacokinetic profile of RIF-SLNs can be translated to a reduced dose and dosage frequency of RIF, thus resulting in lower or no hepatotoxicity commonly associated with its use.
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Solid lipid nanoparticles have been tested in rodents to improve the bioavailability of rifampicin and the combination of rifampicin, isoniazid and pyrazinamide.
“Solid lipid nanoparticles have been tested in rodents with the goal of improving the bioavailability of rifampicin and the combination of rifampicin, isoniazid and pyrazinamide 122,123 .”
From Nanotechnology approaches for global infectious diseases (2021) · cites this paper as [122]
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References 55 · Cited by 61
- Authors
- Singh, H., Jindal, S., Singh, M., Sharma, G., & Kaur, I. P.
- Affiliations
- Panjab University (IN)
- Corresponding author
- Kaur, Indu Pal
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2015-05
- Volume
- 485
- Issue
- 1-2
- Pages
- 138-151
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W2029176085
- Cited by
- 61
- References
- 55
- Citations by year
- 2026: 1 · 2025: 6 · 2024: 6 · 2023: 7 · 2022: 7 · 2021: 12 · 2020: 10 · 2019: 5 · 2018: 2 · 2017: 1 · 2016: 3 · 2015: 1
- FWCI
- 1.29
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Department of Biotechnology, Government of India
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Keywords
- rifampicin, solid lipid nanoparticles, oral bioavailability, microemulsification, sustained drug release, pharmacokinetics, pharmacodynamics, toxicity, nanoparticle formulation
- MeSH terms
- Administration, Oral, Animals, Antibiotics, Antitubercular, Biological Availability, Calorimetry, Differential Scanning, Chemistry, Pharmaceutical, Dose-Response Relationship, Drug, Drug Carriers, Emulsions, Lethal Dose 50, Lipids, Metabolic Clearance Rate, Particle Size, Rifampin, Solubility, Technology, Pharmaceutical, Rats, Wistar, Crystallography, X-Ray, Microscopy, Atomic Force, Area Under Curve, Powder Diffraction, Microscopy, Electron, Transmission, Nanomedicine, Nanoparticles, Chemical and Drug Induced Liver Injury
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