Continuous microchannel precipitation to enhance the solubility of telmisartan with poloxamer 407 using Box-Behnken design approach

2019 
Abstract Poloxamer 407 encapsulated Telmisartan (TEL) nanoparticles were prepared by continuous microchannel precipitation methodology to enhance Telmisartan's solubility and bioavailability. For this purpose, quality by design (QbD) approach was applied using Box-Behnken design (BBD). A three level, three factors BBD was employed to investigate the individual and interactive effect of polymer: drug ratio ( X 1 ), solvent flowrate ( X 2 ), and length of microchannel ( X 3 ) on desired responses. Encapsulation efficiency ( Y 1 ) and Drug release ( Y 2 ) in 20 min were the selected responses. The prepared nanoparticles were characterized by FESEM, TEM, FTIR, PSA, and XRD. An average particle size of 204.3 nm with 0.09 PDI was obtained for TEL loaded polymeric nanoparticles. Fast dissolving tablets for all the batches were prepared for in-vitro drug release analysis. A 4-fold enhancement in TEL solubility was observed compared to pure TEL. An absence of chemical interaction between TEL, polymer, and excipients were confirmed using FTIR which concludes the compatibility of excipients used. Optimized TEL formulation showed 77.72% drug release (% DR) in 20 min with 80.19% encapsulation efficiency (% EE).
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