Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics

Qunyou Tan,1,* Rong Jiang,3,* Meiling Xu,2,4,* Guodong Liu,5,* Songlin Li,1 Jingqing Zhang21Department of Thoracic Surgery, Institute of Surgery Research, Daping Hospital, Third Military Medical University, 2Medicine Engineering Research Center, Chongqing Medical University, 3Stem Cells and Tissue E...

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Autores principales:	Tan Q, Jiang R, Xu M, Liu G, Li S, Zhang J
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/1a60d169ff7e4618bba737daef06d9d5
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spelling	oai:doaj.org-article:1a60d169ff7e4618bba737daef06d9d52021-12-02T02:07:00ZNanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics1176-91141178-2013https://doaj.org/article/1a60d169ff7e4618bba737daef06d9d52013-02-01T00:00:00Zhttp://www.dovepress.com/nanosized-sustained-release-pyridostigmine-bromide-microcapsules-proce-a12259https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Qunyou Tan,1,* Rong Jiang,3,* Meiling Xu,2,4,* Guodong Liu,5,* Songlin Li,1 Jingqing Zhang21Department of Thoracic Surgery, Institute of Surgery Research, Daping Hospital, Third Military Medical University, 2Medicine Engineering Research Center, Chongqing Medical University, 3Stem Cells and Tissue Engineering Research, Chongqing Medical University, 4Department of Pharmacy, Chongqing Emergency Medical Center, 5Eighth Department, Institute of Surgery Research, Daping Hospital, Third Military Medical University, Chongqing, People&rsquo;s Republic of China*These authors contributed equally to this workBackground: Pyridostigmine bromide (3-[[(dimethylamino)-carbonyl]oxy]-1-methylpyridinium bromide), a reversible inhibitor of cholinesterase, is given orally in tablet form, and a treatment schedule of multiple daily doses is recommended for adult patients. Nanotechnology was used in this study to develop an alternative sustained-release delivery system for pyridostigmine, a synthetic drug with high solubility and poor oral bioavailability, hence a Class III drug according to the Biopharmaceutics Classification System. Novel nanosized pyridostigmine-poly(lactic acid) microcapsules (PPNMCs) were expected to have a longer duration of action than free pyridostigmine and previously reported sustained-release formulations of pyridostigmine.Methods: The PPNMCs were prepared using a double emulsion-solvent evaporation method to achieve sustained-release characteristics for pyridostigmine. The preparation process for the PPNMCs was optimized by single-factor experiments. The size distribution, zeta potential, and sustained-release behavior were evaluated in different types of release medium.Results: The optimal volume ratio of inner phase to external phase, poly(lactic acid) concentration, polyvinyl alcohol concentration, and amount of pyridostigmine were 1:10, 6%, 3% and 40 mg, respectively. The negatively charged PPNMCs had an average particle size of 937.9 nm. Compared with free pyridostigmine, PPNMCs showed an initial burst release and a subsequent very slow release in vitro. The release profiles for the PPNMCs in four different types of dissolution medium were fitted to the Ritger-Peppas and Weibull models. The similarity between pairs of dissolution profiles for the PPNMCs in different types of medium was statistically significant, and the difference between the release curves for PPNMCs and free pyridostigmine was also statistically significant.Conclusion: PPNMCs prepared by the optimized protocol described here were in the nanometer range and had good uniformity, with significantly slower pyridostigmine release than from free pyridostigmine. This novel sustained-release delivery nanosystem for pyridostigmine might alleviate the need to identify new acetylcholinesterase inhibitors.Keywords: nanosized microcapsules, process optimization, characteristics, sustained-release, pyridostigmine bromideTan QJiang RXu MLiu GLi SZhang JDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 737-745 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Tan Q Jiang R Xu M Liu G Li S Zhang J Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics
description	Qunyou Tan,1,* Rong Jiang,3,* Meiling Xu,2,4,* Guodong Liu,5,* Songlin Li,1 Jingqing Zhang21Department of Thoracic Surgery, Institute of Surgery Research, Daping Hospital, Third Military Medical University, 2Medicine Engineering Research Center, Chongqing Medical University, 3Stem Cells and Tissue Engineering Research, Chongqing Medical University, 4Department of Pharmacy, Chongqing Emergency Medical Center, 5Eighth Department, Institute of Surgery Research, Daping Hospital, Third Military Medical University, Chongqing, People&rsquo;s Republic of China*These authors contributed equally to this workBackground: Pyridostigmine bromide (3-[[(dimethylamino)-carbonyl]oxy]-1-methylpyridinium bromide), a reversible inhibitor of cholinesterase, is given orally in tablet form, and a treatment schedule of multiple daily doses is recommended for adult patients. Nanotechnology was used in this study to develop an alternative sustained-release delivery system for pyridostigmine, a synthetic drug with high solubility and poor oral bioavailability, hence a Class III drug according to the Biopharmaceutics Classification System. Novel nanosized pyridostigmine-poly(lactic acid) microcapsules (PPNMCs) were expected to have a longer duration of action than free pyridostigmine and previously reported sustained-release formulations of pyridostigmine.Methods: The PPNMCs were prepared using a double emulsion-solvent evaporation method to achieve sustained-release characteristics for pyridostigmine. The preparation process for the PPNMCs was optimized by single-factor experiments. The size distribution, zeta potential, and sustained-release behavior were evaluated in different types of release medium.Results: The optimal volume ratio of inner phase to external phase, poly(lactic acid) concentration, polyvinyl alcohol concentration, and amount of pyridostigmine were 1:10, 6%, 3% and 40 mg, respectively. The negatively charged PPNMCs had an average particle size of 937.9 nm. Compared with free pyridostigmine, PPNMCs showed an initial burst release and a subsequent very slow release in vitro. The release profiles for the PPNMCs in four different types of dissolution medium were fitted to the Ritger-Peppas and Weibull models. The similarity between pairs of dissolution profiles for the PPNMCs in different types of medium was statistically significant, and the difference between the release curves for PPNMCs and free pyridostigmine was also statistically significant.Conclusion: PPNMCs prepared by the optimized protocol described here were in the nanometer range and had good uniformity, with significantly slower pyridostigmine release than from free pyridostigmine. This novel sustained-release delivery nanosystem for pyridostigmine might alleviate the need to identify new acetylcholinesterase inhibitors.Keywords: nanosized microcapsules, process optimization, characteristics, sustained-release, pyridostigmine bromide
format	article
author	Tan Q Jiang R Xu M Liu G Li S Zhang J
author_facet	Tan Q Jiang R Xu M Liu G Li S Zhang J
author_sort	Tan Q
title	Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics
title_short	Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics
title_full	Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics
title_fullStr	Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics
title_full_unstemmed	Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics
title_sort	nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/1a60d169ff7e4618bba737daef06d9d5
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Nanosized sustained-release pyridostigmine bromide microcapsules: process optimization and evaluation of characteristics

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