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


GÖKÇE E. H. , KAYNAK M. S. , YURDASİPER ERDEM A., Ustundag-Okur N., ŞAHİN S.

JOURNAL OF RESEARCH IN PHARMACY, cilt.22, ss.578-586, 2018 (ESCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 22 Konu: 4
  • Basım Tarihi: 2018
  • Doi Numarası: 10.12991/jrp.2018.100
  • Dergi Adı: JOURNAL OF RESEARCH IN PHARMACY
  • Sayfa Sayıları: ss.578-586

Özet

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..