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Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine

BACKGROUND: The aim of the present study was to formulate and optimize the self-emulsifying drug delivery systems (SEDDS) of nevirapine (NVP) by use of 2(2) factorial designs to enhance the oral absorption of NVP by improving its solubility, dissolution rate, and diffusion profile. SEDDS are the iso...

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Autores principales: Chintalapudi, Ramprasad, Murthy, T. E. G. K., Lakshmi, K. Rajya, Manohar, G. Ganesh
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4675002/
https://www.ncbi.nlm.nih.gov/pubmed/26682191
http://dx.doi.org/10.4103/2230-973X.167676
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author Chintalapudi, Ramprasad
Murthy, T. E. G. K.
Lakshmi, K. Rajya
Manohar, G. Ganesh
author_facet Chintalapudi, Ramprasad
Murthy, T. E. G. K.
Lakshmi, K. Rajya
Manohar, G. Ganesh
author_sort Chintalapudi, Ramprasad
collection PubMed
description BACKGROUND: The aim of the present study was to formulate and optimize the self-emulsifying drug delivery systems (SEDDS) of nevirapine (NVP) by use of 2(2) factorial designs to enhance the oral absorption of NVP by improving its solubility, dissolution rate, and diffusion profile. SEDDS are the isotropic mixtures of oil, surfactant, co-surfactant and drug that form oil in water microemulsion when introduced into the aqueous phase under gentle agitation. MATERIALS AND METHODS: Solubility of NVP in different oils, surfactants, and co-surfactants was determined for the screening of excipients. Pseudo-ternary phase diagrams were constructed by the aqueous titration method, and formulations were developed based on the optimum excipient combinations with the help of data obtained through the maximum micro emulsion region containing combinations of oil, surfactant, and co-surfactant. The formulations of SEDDS were optimized by 2(2) factorial designs. RESULTS: The optimum formulation of SEDDS contains 32.5% oleic acid, 44.16% tween 20, and 11.9% polyethylene glycol 600 as oil, surfactant, and co-surfactant respectively. The SEDDS was evaluated for the following drug content, self-emulsification time, rheological properties, zeta potential, in vitro diffusion studies, thermodynamic stability studies, and in vitro dissolution studies. An increase in dissolution was achieved by SEDDS compared to pure form of NVP. CONCLUSION: Overall, this study suggests that the dissolution and oral bioavailability of NVP could be improved by SEDDS technology.
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spelling pubmed-46750022015-12-17 Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine Chintalapudi, Ramprasad Murthy, T. E. G. K. Lakshmi, K. Rajya Manohar, G. Ganesh Int J Pharm Investig Original Research Article BACKGROUND: The aim of the present study was to formulate and optimize the self-emulsifying drug delivery systems (SEDDS) of nevirapine (NVP) by use of 2(2) factorial designs to enhance the oral absorption of NVP by improving its solubility, dissolution rate, and diffusion profile. SEDDS are the isotropic mixtures of oil, surfactant, co-surfactant and drug that form oil in water microemulsion when introduced into the aqueous phase under gentle agitation. MATERIALS AND METHODS: Solubility of NVP in different oils, surfactants, and co-surfactants was determined for the screening of excipients. Pseudo-ternary phase diagrams were constructed by the aqueous titration method, and formulations were developed based on the optimum excipient combinations with the help of data obtained through the maximum micro emulsion region containing combinations of oil, surfactant, and co-surfactant. The formulations of SEDDS were optimized by 2(2) factorial designs. RESULTS: The optimum formulation of SEDDS contains 32.5% oleic acid, 44.16% tween 20, and 11.9% polyethylene glycol 600 as oil, surfactant, and co-surfactant respectively. The SEDDS was evaluated for the following drug content, self-emulsification time, rheological properties, zeta potential, in vitro diffusion studies, thermodynamic stability studies, and in vitro dissolution studies. An increase in dissolution was achieved by SEDDS compared to pure form of NVP. CONCLUSION: Overall, this study suggests that the dissolution and oral bioavailability of NVP could be improved by SEDDS technology. Medknow Publications & Media Pvt Ltd 2015 /pmc/articles/PMC4675002/ /pubmed/26682191 http://dx.doi.org/10.4103/2230-973X.167676 Text en Copyright: © 2015 International Journal of Pharmaceutical Investigation http://creativecommons.org/licenses/by-nc-sa/3.0 This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms.
spellingShingle Original Research Article
Chintalapudi, Ramprasad
Murthy, T. E. G. K.
Lakshmi, K. Rajya
Manohar, G. Ganesh
Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine
title Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine
title_full Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine
title_fullStr Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine
title_full_unstemmed Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine
title_short Formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine
title_sort formulation, optimization, and evaluation of self-emulsifying drug delivery systems of nevirapine
topic Original Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4675002/
https://www.ncbi.nlm.nih.gov/pubmed/26682191
http://dx.doi.org/10.4103/2230-973X.167676
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