Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2018 Apr 20;86(2):16.
doi: 10.3390/scipharm86020016.

Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier

Behzad Sharif Makhmal Zadeh  1 , Hassan Niro  2 , Fakher Rahim  3 , Golbarg Esfahani  4
Affiliations

Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier

Behzad Sharif Makhmal Zadeh et al. Sci Pharm. .

Abstract

One drawback of traditional forms of medical ocular dosage is drug dilution by tear; moreover, drugs are rapidly drained away from pre-corneal cavity by tear flow and lacrimo-nasal drainage. Prolonging contact time with different strategies and mucoadhesive vehicles will help to continuously deliver drugs to the eyes. For this study, we prepared and evaluated the effects of a nanostructure lipid carrier (NLC) on propranolol hydrochloride as a hydrophilic drug model for rabbit corneal permeation. Propranolol hydrochloride NLC was prepared using cold homogenization. The lipid was melted, then the drug and surfactant were dispersed and stirred into the melted lipid. This fused lipid phase was scattered in aqueous solution containing the cosurfactant at 4 °C and then homogenized. We evaluated particle size, drug loading, drug release, and NLC permeability through rabbit cornea as well as the formula’s effect on the cornea. Our results show that drug loading efficiency depended on the surfactant/lipid ratio (S/L) and the percentages of liquid lipid and Transcutol (Gattefosse, Saint-Priest, France) (as solubilizer). Drug release data were evaluated with the Higuchi model and a significant correlation was shown between the S/L ratio and the amount of drug released after 4 and 48 h. NLC formulations improved propranolol hydrochloride permeation. We conclude that the effect of the NLC formulations was due to mucoadhesive and film forming properties.

Keywords: drug delivery; nanostructured lipid carrier; ocular; permeability; propranolol hydrochloride.

PubMed Disclaimer

Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Propranolol hydrochloride release profile using different formulations.
Figure 2
Figure 2
Scanning Electron Microscopy SEM imaging for lipid nanoparticles containing propranolol hydrochloride.
Figure 3
Figure 3
Permeated propranolol across cornea during a 5 h period (mean ± SD, n = 5).
Figure 4
Figure 4
Thermograms: (Top) cornea in buffer solution; (Middle) cornea in contact with NLC formulation; (Bottom) NLC formulation.
Figure 4
Figure 4
Thermograms: (Top) cornea in buffer solution; (Middle) cornea in contact with NLC formulation; (Bottom) NLC formulation.
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

See all "Cited by" articles

References

    1. Mitra A.K. Ophthalmic Drug Delivery Systems. Volume 130. Taylor & Francis Inc; New York, NY USA: 2003. pp. 178–197.
    1. Macha S., Hughes P., Mitra A. Drugs and the Pharmaceutical Sciences. Volume 130. CRC Press; Boca Raton, FL, USA: 2003. Overview of ocular drug delivery; pp. 1–12.
    1. Pijls R.T., Sonderkamp T., Daube G.W., Krebber R., Hanssen H.H., Nuijts R.M., Koole L.H. Studies on a new device for drug delivery to the eye. Eur. J. Pharm. Biopharm. 2005;59:283–288. doi: 10.1016/j.ejpb.2004.08.011. - DOI - PubMed
    1. Sánchez-López E., Espina M., Doktorovova S., Souto E., García M. Lipid nanoparticles (SLN, NLC): Overcoming the anatomical and physiological barriers of the eye–part i–barriers and determining factors in ocular delivery. Eur. J. Pharm. Biopharm. 2017;110:70–75. doi: 10.1016/j.ejpb.2016.10.009. - DOI - PubMed
    1. Gaudana R., Jwala J., Boddu S.H., Mitra A.K. Recent perspectives in ocular drug delivery. Pharm. Res. 2009;26:1197. doi: 10.1007/s11095-008-9694-0. - DOI - PMC - PubMed

LinkOut - more resources