EN
Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet
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..
Keywords
References
- [1] Campbell N, Young ER, Drouin D, Legowski B, Adams MA, Farrell J, Kaczorowski J, Lewanczuk R, Lum-Kwong MM, Tobe S. A framework for discussion on how to improve prevention, management, and control of hypertension in Canada. Can J Cardiol. 2012; 28(3): 262–269.
- [2] Ahada A, Aqil M, Kohli K, Sultana Y, Mujeeb M. Enhanced transdermal delivery of an anti-hypertensive agent via nanoethosomes: Statistical optimization, characterization and pharmacokinetic assessment. Int J Pharm. 2013; 443(1–2): 26–38.
- [3] Mancia G, Fagard R, Narkiewicz K, Redon J, Zanchetti A, Bohem M, et al. ESH/ESC guidelines for the management of arterial hypertension: The task force for the management of arterial hypertension of the European Society of Hypertension (ESH) and of the European Society of Cardiology (ESC). J Hypertens. 2013; 31(7): 1281–1357.
- [4] Altoama K, Yassine Mallem M, Thorin C, Betti E, Desfontis J. Effect of nebivolol treatment during pregnancy on the genital circulation, fetal growth and postnatal development in the Wistar rat. Eur J Pharm. 2015; 758: 31–39.
- [5] Wang S, Chow M, Zuo Z. An approach for rapid development of nasal delivery of analgesics—Identification of relevant features, in vitro screening and in vivo verification. Int J Pharm. 2011; 420(1): 43–50.
- [6] Nigris F, Rienzo M, Schiano C, Fiorito C, Casamassimi A, Napoli C. Prominent cardioprotective effects of third generation beta blocker nebivolol against anthracycline-induced cardiotoxicity using the model of isolated perfused rat heart. Eur J Cancer. 2008; 44(3): 334–340.
- [7] Das S, Chaudhary A. Recent advances in lipid nanoparticle formulations with solid matrix for oral drug delivery. AAPS PharmSciTech. 2011; 12(1): 62-76.
- [8] Ranpise NS, Korabu SS, Ghodake VN. Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride. Colloids Surf B Biointerfaces. 2014; 116: 81–87.
Details
Primary Language
English
Subjects
Pharmaceutical Biotechnology, Pharmaceutical Delivery Technologies
Journal Section
Research Article
Publication Date
June 27, 2025
Submission Date
February 15, 2018
Acceptance Date
April 26, 2018
Published in Issue
Year 2018 Volume: 22 Number: 4
APA
Homan Gökçe, E., Kaynak, M. S., Yurdasiper, A., Üstündağ Okur, N., & Şahin, S. (2025). Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet. Journal of Research in Pharmacy, 22(4), 578-586. https://doi.org/10.12991/jrp.2018.100
AMA
1.Homan Gökçe E, Kaynak MS, Yurdasiper A, Üstündağ Okur N, Şahin S. Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet. J. Res. Pharm. 2025;22(4):578-586. doi:10.12991/jrp.2018.100
Chicago
Homan Gökçe, Evren, Mustafa Sinan Kaynak, Aysu Yurdasiper, Neslihan Üstündağ Okur, and Selma Şahin. 2025. “Comparison of Intestinal Permeability of Nebivolol Hydrochloride Loaded Solid Lipid Nanoparticles With Commercial Nebivolol Tablet”. Journal of Research in Pharmacy 22 (4): 578-86. https://doi.org/10.12991/jrp.2018.100.
EndNote
Homan Gökçe E, Kaynak MS, Yurdasiper A, Üstündağ Okur N, Şahin S (June 1, 2025) Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet. Journal of Research in Pharmacy 22 4 578–586.
IEEE
[1]E. Homan Gökçe, M. S. Kaynak, A. Yurdasiper, N. Üstündağ Okur, and S. Şahin, “Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet”, J. Res. Pharm., vol. 22, no. 4, pp. 578–586, June 2025, doi: 10.12991/jrp.2018.100.
ISNAD
Homan Gökçe, Evren - Kaynak, Mustafa Sinan - Yurdasiper, Aysu - Üstündağ Okur, Neslihan - Şahin, Selma. “Comparison of Intestinal Permeability of Nebivolol Hydrochloride Loaded Solid Lipid Nanoparticles With Commercial Nebivolol Tablet”. Journal of Research in Pharmacy 22/4 (June 1, 2025): 578-586. https://doi.org/10.12991/jrp.2018.100.
JAMA
1.Homan Gökçe E, Kaynak MS, Yurdasiper A, Üstündağ Okur N, Şahin S. Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet. J. Res. Pharm. 2025;22:578–586.
MLA
Homan Gökçe, Evren, et al. “Comparison of Intestinal Permeability of Nebivolol Hydrochloride Loaded Solid Lipid Nanoparticles With Commercial Nebivolol Tablet”. Journal of Research in Pharmacy, vol. 22, no. 4, June 2025, pp. 578-86, doi:10.12991/jrp.2018.100.
Vancouver
1.Evren Homan Gökçe, Mustafa Sinan Kaynak, Aysu Yurdasiper, Neslihan Üstündağ Okur, Selma Şahin. Comparison of intestinal permeability of nebivolol hydrochloride loaded solid lipid nanoparticles with commercial nebivolol tablet. J. Res. Pharm. 2025 Jun. 1;22(4):578-86. doi:10.12991/jrp.2018.100