Tailoring of Antihypertensive Drug-Loaded Nanoparticles: In Vitro, Toxicity, and Bioavailability Assessment

Autor: Mhetre, Raksha Laxman, Hol, Vishal Bhanudas, Chanshetty, Rahul, Dhole, Shashikant N.
Zdroj: BioNanoScience; 20210101, Issue: Preprints p1-13, 13p
Abstrakt: Telmisartan is an antihypertensive drug with low solubility and poor bioavailability. The goal of this study was to fabricate and characterize telmisartan nanoparticles to improve the dissolution and bioavailability of telmisartan. This study aims to tailor nanoparticles of telmisartan for the solubility and bioavailability enhancement by cost-effective technique. Telmisartan nanoparticles were prepared by antisolvent precipitation-ultrasonication technology using stabilizers and surfactants. The combination of hydroxypropyl methylcellulose-sodium dodecyl sulfate along with ultrasonication for 20 min was found to be effective for the stabilization of telmisartan nanoparticles. Stable nanoparticles of 52 nm particle size were obtained. Differential scanning calorimetry and powder X-ray diffraction studies confirmed that the crystallinity of the drug was reduced in the nanoparticles. Saturation solubility and dissolution were increased due to the reduction in particle size and the amorphous nature of the drug in the formulated nanoparticles. An acute oral toxicity study of telmisartan nanoparticles was performed and concluded that nanoparticles of telmisartan at selected doses are not toxic and do not show mortality at the administered dose. Significant values of pharmacokinetic parameters—maximum plasma concentration and area under curve—have indicated better absorption of drug in the form of nanoparticles. The value of half-life of telmisartan nanoparticles (12.73 ± 0.59 h) was decreased compared to drug (26.86 ± 2.0 h), which concluded the increased oral absorption of telmisartan nanoparticles. All these findings reinforce the fact that the formulation of telmisartan nanoparticles is a new approach for solubility and bioavailability enhancement of telmisartan.
Databáze: Supplemental Index
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