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Chylomicron mimicking nanocolloidal carriers of rosuvastatin calcium for lymphatic drug targeting and management of hyperlipidemia

Beg, Sarwar, Alam, Mohammad Naushad, Ahmad, Farhan Jalees, Singh, Bhupinder
Colloids and surfaces 2019 v.177 pp. 541-549
absorption, biopharmaceuticals, calcium, cell lines, cytotoxicity, emulsifying, hyperlipidemia, intestines, particle size, permeability, pharmacodynamics, pharmacokinetics, phospholipids, zeta potential
The present work entails development of novel phospholipid-based self-nanoemulsifying systems (SNES) of rosuvastatin calcium for improving the oral biopharmaceutical performance via intestinal lymphatic pathways. The phospholipid complex-loaded SNES exhibited emulsification time of 142 s, particle size of 182.5 nm, polydispersity index of 0.35, zeta potential of −22.5 mV and complete in vitro drug release within 3 h. Cell line study on Caco-2 indicated absence of cytotoxicity and excellent cellular uptake of PL-SNES vis-à-vis plain SNES. Permeability study revealed >85% enhancement in the permeation, while intestinal perfusion study showed 2.9 and 3.5-fold increase in the permeation and absorption of the drug from the optimized PL-SNES over the pure drug suspension. Nearly 2.2 and 7.2-folds improvement in AUC0-t and Cmax, and 0.33-fold reduction in the Tmax of drug was observed for PL-SNES vis-à-vis the pure drug suspension during pharmacokinetic study. Moreover, PL-SNES also showed superior antihyperlipidemic activity over the pure drug suspension during pharmacodynamic study. Overall, the developed nanoformulation yielded significant improvement in the oral deliverability of the explored drug candidate.