Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier

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...

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Main Authors: Behzad Sharif Makhmal Zadeh, Hassan Niro, Fakher Rahim, Golbarg Esfahani
Format: Article
Language:English
Published: MDPI AG 2018-04-01
Series:Scientia Pharmaceutica
Subjects:
Online Access:http://www.mdpi.com/2218-0532/86/2/16
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author Behzad Sharif Makhmal Zadeh
Hassan Niro
Fakher Rahim
Golbarg Esfahani
author_facet Behzad Sharif Makhmal Zadeh
Hassan Niro
Fakher Rahim
Golbarg Esfahani
author_sort Behzad Sharif Makhmal Zadeh
collection DOAJ
description 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.
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spelling doaj.art-c4e06bf0459240ac95b95b71d1bcb3e32022-12-22T01:57:49ZengMDPI AGScientia Pharmaceutica2218-05322018-04-018621610.3390/scipharm86020016scipharm86020016Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid CarrierBehzad Sharif Makhmal Zadeh0Hassan Niro1Fakher Rahim2Golbarg Esfahani3Nanotechnology Research Center, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, 6135715794 Ahvaz, IranDepartment of Pharmaceutics, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, 6135715794 Ahvaz, IranResearch Center of Thalassemia & Hemoglobinopathy, Ahvaz Jundishapur University of Medical Ciences, 6135715794 Ahvaz, IranDepartment of Pharmaceutics, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, 6135715794 Ahvaz, IranOne 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.http://www.mdpi.com/2218-0532/86/2/16oculardrug deliverypermeabilitypropranolol hydrochloridenanostructured lipid carrier
spellingShingle Behzad Sharif Makhmal Zadeh
Hassan Niro
Fakher Rahim
Golbarg Esfahani
Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier
Scientia Pharmaceutica
ocular
drug delivery
permeability
propranolol hydrochloride
nanostructured lipid carrier
title Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier
title_full Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier
title_fullStr Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier
title_full_unstemmed Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier
title_short Ocular Delivery System for Propranolol Hydrochloride Based on Nanostructured Lipid Carrier
title_sort ocular delivery system for propranolol hydrochloride based on nanostructured lipid carrier
topic ocular
drug delivery
permeability
propranolol hydrochloride
nanostructured lipid carrier
url http://www.mdpi.com/2218-0532/86/2/16
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AT hassanniro oculardeliverysystemforpropranololhydrochloridebasedonnanostructuredlipidcarrier
AT fakherrahim oculardeliverysystemforpropranololhydrochloridebasedonnanostructuredlipidcarrier
AT golbargesfahani oculardeliverysystemforpropranololhydrochloridebasedonnanostructuredlipidcarrier