Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients

Katayoun Derakhshandeh1, Marzieh Soheili1, Simin Dadashzadeh2, Reza Saghiri31Department of Pharmaceutics, Faculty of Pharmacy, University of Medical Science, Kermanshah 67145-1673, Iran; 2Department of Pharmaceutics, Faculty of Pharmacy, Shaheed Beheshti University of Medical Science, Tehran, Iran;...

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Autores principales:	Katayoun Derakhshandeh, Marzieh Soheili, Simin Dadashzadeh, et al
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2010
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/7fff09ba467c4b4e8a679ab72888bb33
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spelling	oai:doaj.org-article:7fff09ba467c4b4e8a679ab72888bb332021-12-02T01:07:54ZPreparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients1176-91141178-2013https://doaj.org/article/7fff09ba467c4b4e8a679ab72888bb332010-07-01T00:00:00Zhttp://www.dovepress.com/preparation-and-in-vitro-characterization-of-9-nitrocamptothecin-loade-a4752https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Katayoun Derakhshandeh1, Marzieh Soheili1, Simin Dadashzadeh2, Reza Saghiri31Department of Pharmaceutics, Faculty of Pharmacy, University of Medical Science, Kermanshah 67145-1673, Iran; 2Department of Pharmaceutics, Faculty of Pharmacy, Shaheed Beheshti University of Medical Science, Tehran, Iran; 3Deptartment of Biochemistry, Pasteur Institute, Tehran, IranAbstract: The purpose in this study was to investigate poly(ethylene glycol)-modified poly (d,l-lactide-co-glycolide) nanoparticles (PLGA-PEG-NPs) loading 9-nitrocamptothecin (9-NC) as a potent anticancer drug. 9-NC is an analog of the natural plant alkaloid camptothecin that has shown high antitumor activity and is currently in the end stage of clinical trial. Unfortunately, at physiological pH, these potent agents undergo a rapid and reversible hydrolysis with the loss of antitumor activity. Previous researchers have shown that the encapsulation of this drug in PLGA nanoparticles could increase its stability and release profile. In this research we investigated PLGA-PEG nanoparticles and their effect on in vitro characteristics of this labile drug. 9-NC-PLGA-PEG nanoparticles with particle size within the range of 148.5 &plusmn; 30 nm were prepared by a nanoprecipitation method. The influence of four different independent variables (amount of polymer, percent of emulsifier, internal phase volume, and external phase volume) on nanoparticle drug-loading was studied. Differential scanning calorimetry and X-ray diffractometry were also evaluated for physical characterizing. The results of optimized formulation showed a narrow size distribution, suitable zeta potential (+1.84), and a drug loading of more than 45%. The in vitro drug release from PLGA-PEG NPs showed a sustained release pattern of up to 120 hours and comparing with PLGA-NPs had a significant decrease in initial burst effect. These experimental results indicate that PLGA-PEG-NPs (versus PLGA-NPs) have a better physicochemical characterization and can be developed as a drug carrier in order to treat different malignancies.Keywords: long circulating nanoparticle, 9-nitrocamptothecin, in vitro characterization Katayoun DerakhshandehMarzieh SoheiliSimin Dadashzadehet alDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2010, Iss default, Pp 463-471 (2010)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Katayoun Derakhshandeh Marzieh Soheili Simin Dadashzadeh et al Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients
description	Katayoun Derakhshandeh1, Marzieh Soheili1, Simin Dadashzadeh2, Reza Saghiri31Department of Pharmaceutics, Faculty of Pharmacy, University of Medical Science, Kermanshah 67145-1673, Iran; 2Department of Pharmaceutics, Faculty of Pharmacy, Shaheed Beheshti University of Medical Science, Tehran, Iran; 3Deptartment of Biochemistry, Pasteur Institute, Tehran, IranAbstract: The purpose in this study was to investigate poly(ethylene glycol)-modified poly (d,l-lactide-co-glycolide) nanoparticles (PLGA-PEG-NPs) loading 9-nitrocamptothecin (9-NC) as a potent anticancer drug. 9-NC is an analog of the natural plant alkaloid camptothecin that has shown high antitumor activity and is currently in the end stage of clinical trial. Unfortunately, at physiological pH, these potent agents undergo a rapid and reversible hydrolysis with the loss of antitumor activity. Previous researchers have shown that the encapsulation of this drug in PLGA nanoparticles could increase its stability and release profile. In this research we investigated PLGA-PEG nanoparticles and their effect on in vitro characteristics of this labile drug. 9-NC-PLGA-PEG nanoparticles with particle size within the range of 148.5 &plusmn; 30 nm were prepared by a nanoprecipitation method. The influence of four different independent variables (amount of polymer, percent of emulsifier, internal phase volume, and external phase volume) on nanoparticle drug-loading was studied. Differential scanning calorimetry and X-ray diffractometry were also evaluated for physical characterizing. The results of optimized formulation showed a narrow size distribution, suitable zeta potential (+1.84), and a drug loading of more than 45%. The in vitro drug release from PLGA-PEG NPs showed a sustained release pattern of up to 120 hours and comparing with PLGA-NPs had a significant decrease in initial burst effect. These experimental results indicate that PLGA-PEG-NPs (versus PLGA-NPs) have a better physicochemical characterization and can be developed as a drug carrier in order to treat different malignancies.Keywords: long circulating nanoparticle, 9-nitrocamptothecin, in vitro characterization
format	article
author	Katayoun Derakhshandeh Marzieh Soheili Simin Dadashzadeh et al
author_facet	Katayoun Derakhshandeh Marzieh Soheili Simin Dadashzadeh et al
author_sort	Katayoun Derakhshandeh
title	Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients
title_short	Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients
title_full	Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients
title_fullStr	Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients
title_full_unstemmed	Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients
title_sort	preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients
publisher	Dove Medical Press
publishDate	2010
url	https://doaj.org/article/7fff09ba467c4b4e8a679ab72888bb33
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Preparation and in vitro characterization of 9-nitrocamptothecin-loaded long circulating nanoparticles for delivery in cancer patients

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