Development and evaluation of isradipine via rutin-loaded coated solid–lipid nanoparticles

Abstract

The objective was to develop a stable and non-compliance coated solid–lipid nanoparticles (coated SLN) using polymer (Eudragit L100) and lipoid (glycerol monostearate: soya lecithin) for partial dose reduction of isradipine [ISR; 2.5 mg by combination of bioenhancing agent (rutin; Ru) in equivalent ratio]. The physicochemical characterizations were performed by FT-IR and DSC of elected model drug (ISR), drug mixer with Ru/polymer and coated SLN with Ru (ONbp); the resulted distinctive peaks demonstrated that no chemical interaction and incompatibility found between them. The plasma samples of formulation (ONbp) were analyzed by liquid chromatography (HPLC) using UV-spectrometer. Data were integrated and analyzed with the help of a computer-designed program “Kinetica Software” (Thermo Scientific Kinetica, PK/PD Analysis, version 5.0, Philadelphia, PA). The pharmacokinetic study showed 3.2- to 4.7-folds enhancement in oral bioavailability of coated SLN of ISR with Ru (ONbp) when compared to a coated formulation of ISR without Ru (ONps) and conventional drug suspension. In vivo studies were revealed significantly at greater extent in (drug stability and solubility) oral absorption, which has shown potential entrapment efficiency (97.85% ± 1.02%) to improve biological activity against hypertension. Hence, nano-system of ISR against hypertension is achieved with consequent dose reduction with enhanced systemic bioavailability.