Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet

Abstract

ABSTRACT:The oral application of drugs is the most popular route for achieving systemic effects, nevertheless, it is limited by difficulties related to physicochemical properties of the drug. Solid lipid nanoparticles (SLNs) are appealing extensive notice because of showing increased solubility and improved oral bioavailability via different mechanisms. The aim of the study is to compare and peruse the in-situ permeation of nebivolol (NBV) loaded SLN and its commercial tablet formulation used for the treatment of hypertension. For this aim Single-Pass Intestinal Perfusion (SPIP) method was used for in-situ permeation studies. NBV loaded SLNs were prepared and modified with polyethylene glycol (PEG). In order to prepare SLNs by homogenization technique, compritol, lecithin and poloxamer were chosen. Particle sizes of blank and loaded SLN were 213.4±17.5 and 264.1±18.8 nm, respectively with polydispersity index values of approximately 0.3 for each. NBV loading resulted in positive electrical charge on SLNs. The encapsulation efficiency was 98.04±0.2 %. Permeability coefficient values were tripled when NBV was incorporated in SLNs and doubled when pure NBV was given separately with a blank SLN. PEG modified SLN can be used to enhance oral absorption of NBV, and SLNs alone can be used as permeation enhancer in oral drug delivery..

A newly developed and fully validated HPLC method for simultenous determination of in-situ single pass intestinal permeability of domperidone, metoprolol tartarate and phenol red

“…For the in-situ SPIP research, the experimental approach was carried out in accordance with the previously published studies that had been previously described [22,[25][26][27][28][29]. Ketamine-xylazine mixtures (90 and 10 mg/kg, respectively) were used to anesthetize the rats, which were administered intraperitoneally to ensure complete anesthesia.…”