Development of enteric submicron particle formulation of papain for oral delivery

Manu Sharma1, Vinay Sharma2, Amulya K Panda3, Dipak K Majumdar41Department of Pharmacy, Banasthali Vidhyapith, Banasthali, India; 2Department of Bioscience and Biotechnology, Banasthali Vidhyapith, Banasthali, India; 3National Institute of Immunology, Aruna Asaf Ali Marg, New Delhi, India; 4Departme...

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Autores principales:	Sharma M, Sharma V, Panda AK, Majumdar DK
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2011
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/ce3d90015d7d47fb88cfee6eee7938a4
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spelling	oai:doaj.org-article:ce3d90015d7d47fb88cfee6eee7938a42021-12-02T07:37:55ZDevelopment of enteric submicron particle formulation of papain for oral delivery1176-91141178-2013https://doaj.org/article/ce3d90015d7d47fb88cfee6eee7938a42011-09-01T00:00:00Zhttp://www.dovepress.com/development-of-enteric-submicron-particle-formulation-of-papain-for-or-a8349https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Manu Sharma1, Vinay Sharma2, Amulya K Panda3, Dipak K Majumdar41Department of Pharmacy, Banasthali Vidhyapith, Banasthali, India; 2Department of Bioscience and Biotechnology, Banasthali Vidhyapith, Banasthali, India; 3National Institute of Immunology, Aruna Asaf Ali Marg, New Delhi, India; 4Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, University of Delhi, New Delhi, IndiaBackground: Particulate systems have received increasing attention for oral delivery of biomolecules. The objective of the present study was to prepare submicron particulate formulations of papain for pH-dependent site-specific release using pH-sensitive polymers.Methods: Enteric submicron particle formulations of papain were prepared by w/o/w emulsion solvent evaporation using hydroxypropyl methylcellulose phthalate (HPMCP), Eudragit L100, and Eudragit S100, to avoid gastric inactivation of papain.Results: Smaller internal and external aqueous phase volumes provided maximum encapsulation efficiency (75.58%&ndash;82.35%), the smallest particle size (665.6&ndash;692.4 nm), and 25%&ndash;30% loss of enzyme activity. Release studies in 0.1 N HCl confirmed the gastroresistance of the formulations. The anionic submicron particles aggregated in 0.1 N HCl (ie, gastric pH 1.2) due to protonation of carboxylic groups in the enteric polymer. Aggregates &lt; 500 &micro;m size would not impede gastric emptying. However, at pH &gt; 5.0 (duodenal pH), the submicron particles showed deaggregation due to restoration of surface charge. HPMCP submicron particles facilitated almost complete release of papain within 30 minutes at pH 6.0, while Eudragit L100 and Eudragit S100 particles released 88.82% and 53.00% of papain at pH 6.8 and pH 7.4, respectively, according to the Korsmeyer&ndash;Peppas equation. Sodium dodecyl sulfate polyacrylamide gel electrophoresis and fluorescence spectroscopy confirmed that the structural integrity of the enzyme was maintained during encapsulation. Fourier transform infrared spectroscopy revealed entrapment of the enzyme, with powder x-ray diffraction and differential scanning calorimetry indicating an amorphous character, and scanning electron microscopy showing that the submicron particles had a spherical shape.Conclusion: In simulated gastrointestinal pH conditions, the HPMCP, Eudragit L100, and Eudragit S100 submicron particles showed good digestion of paneer and milk protein, and could serve as potential carriers for oral enzyme delivery. Stability studies indicated that formulations with approximately 6% overage would ensure a two-year shelf-life at room temperature.Keywords: papain, hydroxypropyl methylcellulose phthalate, Eudragit L100, Eudragit S100, zeta potentialSharma MSharma VPanda AKMajumdar DKDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2011, Iss default, Pp 2097-2111 (2011)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Sharma M Sharma V Panda AK Majumdar DK Development of enteric submicron particle formulation of papain for oral delivery
description	Manu Sharma1, Vinay Sharma2, Amulya K Panda3, Dipak K Majumdar41Department of Pharmacy, Banasthali Vidhyapith, Banasthali, India; 2Department of Bioscience and Biotechnology, Banasthali Vidhyapith, Banasthali, India; 3National Institute of Immunology, Aruna Asaf Ali Marg, New Delhi, India; 4Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, University of Delhi, New Delhi, IndiaBackground: Particulate systems have received increasing attention for oral delivery of biomolecules. The objective of the present study was to prepare submicron particulate formulations of papain for pH-dependent site-specific release using pH-sensitive polymers.Methods: Enteric submicron particle formulations of papain were prepared by w/o/w emulsion solvent evaporation using hydroxypropyl methylcellulose phthalate (HPMCP), Eudragit L100, and Eudragit S100, to avoid gastric inactivation of papain.Results: Smaller internal and external aqueous phase volumes provided maximum encapsulation efficiency (75.58%&ndash;82.35%), the smallest particle size (665.6&ndash;692.4 nm), and 25%&ndash;30% loss of enzyme activity. Release studies in 0.1 N HCl confirmed the gastroresistance of the formulations. The anionic submicron particles aggregated in 0.1 N HCl (ie, gastric pH 1.2) due to protonation of carboxylic groups in the enteric polymer. Aggregates &lt; 500 &micro;m size would not impede gastric emptying. However, at pH &gt; 5.0 (duodenal pH), the submicron particles showed deaggregation due to restoration of surface charge. HPMCP submicron particles facilitated almost complete release of papain within 30 minutes at pH 6.0, while Eudragit L100 and Eudragit S100 particles released 88.82% and 53.00% of papain at pH 6.8 and pH 7.4, respectively, according to the Korsmeyer&ndash;Peppas equation. Sodium dodecyl sulfate polyacrylamide gel electrophoresis and fluorescence spectroscopy confirmed that the structural integrity of the enzyme was maintained during encapsulation. Fourier transform infrared spectroscopy revealed entrapment of the enzyme, with powder x-ray diffraction and differential scanning calorimetry indicating an amorphous character, and scanning electron microscopy showing that the submicron particles had a spherical shape.Conclusion: In simulated gastrointestinal pH conditions, the HPMCP, Eudragit L100, and Eudragit S100 submicron particles showed good digestion of paneer and milk protein, and could serve as potential carriers for oral enzyme delivery. Stability studies indicated that formulations with approximately 6% overage would ensure a two-year shelf-life at room temperature.Keywords: papain, hydroxypropyl methylcellulose phthalate, Eudragit L100, Eudragit S100, zeta potential
format	article
author	Sharma M Sharma V Panda AK Majumdar DK
author_facet	Sharma M Sharma V Panda AK Majumdar DK
author_sort	Sharma M
title	Development of enteric submicron particle formulation of papain for oral delivery
title_short	Development of enteric submicron particle formulation of papain for oral delivery
title_full	Development of enteric submicron particle formulation of papain for oral delivery
title_fullStr	Development of enteric submicron particle formulation of papain for oral delivery
title_full_unstemmed	Development of enteric submicron particle formulation of papain for oral delivery
title_sort	development of enteric submicron particle formulation of papain for oral delivery
publisher	Dove Medical Press
publishDate	2011
url	https://doaj.org/article/ce3d90015d7d47fb88cfee6eee7938a4
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Development of enteric submicron particle formulation of papain for oral delivery

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