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Development of pH sensitive polymeric nanoparticles of erythromycin stearate

CONTEXT: Bioavailability of conventional tablet of erythromycin stearate is low as it is unstable at acidic pH and also shows a low dissolution rate. OBJECTIVE: It was proposed to protect it from the acidic condition of the stomach along with an increase in dissolution rate by formulating pH sensiti...

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Autores principales: Bhadra, Sulekha, Prajapati, Atin B., Bhadra, Dipankar
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Medknow Publications & Media Pvt Ltd 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4832904/
https://www.ncbi.nlm.nih.gov/pubmed/27134466
http://dx.doi.org/10.4103/0975-7406.171691
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author Bhadra, Sulekha
Prajapati, Atin B.
Bhadra, Dipankar
author_facet Bhadra, Sulekha
Prajapati, Atin B.
Bhadra, Dipankar
author_sort Bhadra, Sulekha
collection PubMed
description CONTEXT: Bioavailability of conventional tablet of erythromycin stearate is low as it is unstable at acidic pH and also shows a low dissolution rate. OBJECTIVE: It was proposed to protect it from the acidic condition of the stomach along with an increase in dissolution rate by formulating pH sensitive nanoparticles. MATERIALS AND METHODS: The nanoparticles were prepared by the solvent evaporation technique using different quantities of Eudragit L100-55 and polyvinyl alcohol (PVA). Size reduction was achieved by high speed homogenization technique using Digital Ultra Turrax homogenizer. The formulation was optimized using 3(2) factorial design, keeping drug polymer ratio and surfactant concentration as independent variables. Particle size, entrapment efficiency, and drug-release (DR) were studied as dependent variables. RESULTS: Optimized batch containing 1:0.3 erythromycin stearate: Eudragit L100-55 ratio and 1.0% PVA showed 8.24 ± 0.71% DR in pH 1.2 in 1-h and 90.38 ± 5.97% in pH 5.5 and pH 6.8 within 2-h, respectively. DISCUSSION: The optimized batch exhibited lower release in acidic pH and faster release in higher pH compared to the marketed preparation. CONCLUSION: Thus the present study concludes that pH sensitive nanoparticles of erythromycin stearate increases the dissolution of the drug in intestinal pH and also protect it from acidic pH, which may help in improving the bioavailability of erythromycin.
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spelling pubmed-48329042016-04-29 Development of pH sensitive polymeric nanoparticles of erythromycin stearate Bhadra, Sulekha Prajapati, Atin B. Bhadra, Dipankar J Pharm Bioallied Sci Original Article CONTEXT: Bioavailability of conventional tablet of erythromycin stearate is low as it is unstable at acidic pH and also shows a low dissolution rate. OBJECTIVE: It was proposed to protect it from the acidic condition of the stomach along with an increase in dissolution rate by formulating pH sensitive nanoparticles. MATERIALS AND METHODS: The nanoparticles were prepared by the solvent evaporation technique using different quantities of Eudragit L100-55 and polyvinyl alcohol (PVA). Size reduction was achieved by high speed homogenization technique using Digital Ultra Turrax homogenizer. The formulation was optimized using 3(2) factorial design, keeping drug polymer ratio and surfactant concentration as independent variables. Particle size, entrapment efficiency, and drug-release (DR) were studied as dependent variables. RESULTS: Optimized batch containing 1:0.3 erythromycin stearate: Eudragit L100-55 ratio and 1.0% PVA showed 8.24 ± 0.71% DR in pH 1.2 in 1-h and 90.38 ± 5.97% in pH 5.5 and pH 6.8 within 2-h, respectively. DISCUSSION: The optimized batch exhibited lower release in acidic pH and faster release in higher pH compared to the marketed preparation. CONCLUSION: Thus the present study concludes that pH sensitive nanoparticles of erythromycin stearate increases the dissolution of the drug in intestinal pH and also protect it from acidic pH, which may help in improving the bioavailability of erythromycin. Medknow Publications & Media Pvt Ltd 2016 /pmc/articles/PMC4832904/ /pubmed/27134466 http://dx.doi.org/10.4103/0975-7406.171691 Text en Copyright: © Journal of Pharmacy and Bioallied Sciences 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 Article
Bhadra, Sulekha
Prajapati, Atin B.
Bhadra, Dipankar
Development of pH sensitive polymeric nanoparticles of erythromycin stearate
title Development of pH sensitive polymeric nanoparticles of erythromycin stearate
title_full Development of pH sensitive polymeric nanoparticles of erythromycin stearate
title_fullStr Development of pH sensitive polymeric nanoparticles of erythromycin stearate
title_full_unstemmed Development of pH sensitive polymeric nanoparticles of erythromycin stearate
title_short Development of pH sensitive polymeric nanoparticles of erythromycin stearate
title_sort development of ph sensitive polymeric nanoparticles of erythromycin stearate
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4832904/
https://www.ncbi.nlm.nih.gov/pubmed/27134466
http://dx.doi.org/10.4103/0975-7406.171691
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