Mechanistic approach for the development of ultrafine oil-water emulsions using monoglyceride and blends of medium and long chain triglycerides: enhancement of the solubility and bioavailability of Perphenazine

A kinetically stable ultra-fine oil-water (o/w) emulsion containing Perphenazine and blends of long and medium chain triglycerides was prepared. The purpose of the ultra-fine emulsion was to increase the oral bioavailability of Perphenazine. The formulations were prepared using a low energy emulsifi...

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Main Authors: Sanjula Baboota, Abdullah Gulam Mustafa, Jasjeet Kaur Sahni, Javed Ali
Format: Article
Language:English
Published: International Pharmaceutical Excipients Council 2016-11-01
Series:Journal of Excipients and Food Chemicals
Online Access:https://jefc.scholasticahq.com/article/1099-mechanistic-approach-for-the-development-of-ultrafine-oil-water-emulsions-using-monoglyceride-and-blends-of-medium-and-long-chain-triglycerides-enhan
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author Sanjula Baboota
Abdullah Gulam Mustafa
Jasjeet Kaur Sahni
Javed Ali
author_facet Sanjula Baboota
Abdullah Gulam Mustafa
Jasjeet Kaur Sahni
Javed Ali
author_sort Sanjula Baboota
collection DOAJ
description A kinetically stable ultra-fine oil-water (o/w) emulsion containing Perphenazine and blends of long and medium chain triglycerides was prepared. The purpose of the ultra-fine emulsion was to increase the oral bioavailability of Perphenazine. The formulations were prepared using a low energy emulsification phase titration method. The optimized formulations consisted of blends of linseed oil and Sefsol 218 (1:1) (oil phase), polysorbate 40 (surfactant), polyethylene glycol 400 (cosurfactant) and distilled water (dispersion medium). Characterization of viscosity, refractive index, particle size distribution, spectral transmittance and surface morphology of the formulations was performed. The release rate of Perphenazine from the formulations was quantified using the everted gut sac of rat intestinal mucosa. The ex vivo release data demonstrated that the formulated nanoemulsions increased significantly the permeation rate of Perphenazine when compared with a suspension. Following oral administration of selected nanoemulsions in Wistar rats, the AUC and Cmax of Perphenazine increased by 2.9 and 2.54-fold respectively compared with the Perphenazine suspension. The observed increase in bioavailability may be due to the increase in the dissolution rate from the molecularly dissolved drug in the oil phase and an increased rate of dispersion of the drug in the gastrointestinal (GI) tract which leads to greater absorption into the blood.
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spelling doaj.art-4d69404e6a0b478e8820f75068a4c3242024-03-20T18:01:23ZengInternational Pharmaceutical Excipients CouncilJournal of Excipients and Food Chemicals2150-26682016-11-0141Mechanistic approach for the development of ultrafine oil-water emulsions using monoglyceride and blends of medium and long chain triglycerides: enhancement of the solubility and bioavailability of PerphenazineSanjula BabootaAbdullah Gulam MustafaJasjeet Kaur SahniJaved AliA kinetically stable ultra-fine oil-water (o/w) emulsion containing Perphenazine and blends of long and medium chain triglycerides was prepared. The purpose of the ultra-fine emulsion was to increase the oral bioavailability of Perphenazine. The formulations were prepared using a low energy emulsification phase titration method. The optimized formulations consisted of blends of linseed oil and Sefsol 218 (1:1) (oil phase), polysorbate 40 (surfactant), polyethylene glycol 400 (cosurfactant) and distilled water (dispersion medium). Characterization of viscosity, refractive index, particle size distribution, spectral transmittance and surface morphology of the formulations was performed. The release rate of Perphenazine from the formulations was quantified using the everted gut sac of rat intestinal mucosa. The ex vivo release data demonstrated that the formulated nanoemulsions increased significantly the permeation rate of Perphenazine when compared with a suspension. Following oral administration of selected nanoemulsions in Wistar rats, the AUC and Cmax of Perphenazine increased by 2.9 and 2.54-fold respectively compared with the Perphenazine suspension. The observed increase in bioavailability may be due to the increase in the dissolution rate from the molecularly dissolved drug in the oil phase and an increased rate of dispersion of the drug in the gastrointestinal (GI) tract which leads to greater absorption into the blood.https://jefc.scholasticahq.com/article/1099-mechanistic-approach-for-the-development-of-ultrafine-oil-water-emulsions-using-monoglyceride-and-blends-of-medium-and-long-chain-triglycerides-enhan
spellingShingle Sanjula Baboota
Abdullah Gulam Mustafa
Jasjeet Kaur Sahni
Javed Ali
Mechanistic approach for the development of ultrafine oil-water emulsions using monoglyceride and blends of medium and long chain triglycerides: enhancement of the solubility and bioavailability of Perphenazine
Journal of Excipients and Food Chemicals
title Mechanistic approach for the development of ultrafine oil-water emulsions using monoglyceride and blends of medium and long chain triglycerides: enhancement of the solubility and bioavailability of Perphenazine
title_full Mechanistic approach for the development of ultrafine oil-water emulsions using monoglyceride and blends of medium and long chain triglycerides: enhancement of the solubility and bioavailability of Perphenazine
title_fullStr Mechanistic approach for the development of ultrafine oil-water emulsions using monoglyceride and blends of medium and long chain triglycerides: enhancement of the solubility and bioavailability of Perphenazine
title_full_unstemmed Mechanistic approach for the development of ultrafine oil-water emulsions using monoglyceride and blends of medium and long chain triglycerides: enhancement of the solubility and bioavailability of Perphenazine
title_short Mechanistic approach for the development of ultrafine oil-water emulsions using monoglyceride and blends of medium and long chain triglycerides: enhancement of the solubility and bioavailability of Perphenazine
title_sort mechanistic approach for the development of ultrafine oil water emulsions using monoglyceride and blends of medium and long chain triglycerides enhancement of the solubility and bioavailability of perphenazine
url https://jefc.scholasticahq.com/article/1099-mechanistic-approach-for-the-development-of-ultrafine-oil-water-emulsions-using-monoglyceride-and-blends-of-medium-and-long-chain-triglycerides-enhan
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