Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

Heba F SalemFaculty of Pharmacy, Beni-Suef University, Beni-Suef, EgyptAbstract: The production of an intramuscular (IM) injection of natural progesterone would provide a safer solution than using semi synthetic progesterone. However, disadvantages such as low solubility and a short half life preven...

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Autor principal:	Heba F Salem
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2010
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/659bc889a56947cb9987da5a8734a16c
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spelling	oai:doaj.org-article:659bc889a56947cb9987da5a8734a16c2021-12-02T02:10:26ZSustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats1176-91141178-2013https://doaj.org/article/659bc889a56947cb9987da5a8734a16c2010-11-01T00:00:00Zhttp://www.dovepress.com/sustained-release-progesterone-nanosuspension-following-intramuscular--a5622https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Heba F SalemFaculty of Pharmacy, Beni-Suef University, Beni-Suef, EgyptAbstract: The production of an intramuscular (IM) injection of natural progesterone would provide a safer solution than using semi synthetic progesterone. However, disadvantages such as low solubility and a short half life prevent the use of natural progesterone. In this study, we formulated a sustained release form of natural progesterone to be given as IM injection. A progesterone nanosuspension (PNS) was first developed and then dispersed in a thermosensitive gel matrix. The selected nanoparticles showed an average particle size of 267 nm and a zeta potential approaching-41 mV. The in vitro release profile of PNS from the F127 plus methyl cellulose gel followed zero order kinetics and correlated linearly with the weight percentage of gel dissolved, demonstrating that the overall rate of release of PNS is controlled by dissolution of the pluronic F127/methyl cellulose (MC) gel (r2 &gt; 0.99). The pharmacokinetic parameters of the PNS (6 mg/mL) in pluronic F127/MC gel were evaluated in comparison with the control progesterone suspension. After the administration of PNS in F127/MC gel into the rats, a maximum serum concentration of 22.1 &plusmn; 1.9 ng/mL was reached at a Tmax of 4.05 &plusmn; 0.1 h. The terminal half life was 12.7 &plusmn; 0.8 h. The area under the curve AUC0-&infin; of the injected formula was 452.75 &plusmn; 42.8 ng&bull;h/mL and the total mean residence time was 18.57 &plusmn; 1.44 h. The PNS in gel was significantly different from the control in rate and extent at P &lt; 0.001. The natural progesterone which was nanosized and formulated in a thermosensitive gel significantly sustained the action of natural progesterone so that it could be injected every 36 h instead of every day. Moreover, this formula is expected to provide a much safer choice than the use of semi-synthetic progesterone.Keywords: progesterone, nanosuspension, thermosensitive gel, ovariectomized female rats Heba F SalemDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2010, Iss default, Pp 943-954 (2010)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Heba F Salem Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats
description	Heba F SalemFaculty of Pharmacy, Beni-Suef University, Beni-Suef, EgyptAbstract: The production of an intramuscular (IM) injection of natural progesterone would provide a safer solution than using semi synthetic progesterone. However, disadvantages such as low solubility and a short half life prevent the use of natural progesterone. In this study, we formulated a sustained release form of natural progesterone to be given as IM injection. A progesterone nanosuspension (PNS) was first developed and then dispersed in a thermosensitive gel matrix. The selected nanoparticles showed an average particle size of 267 nm and a zeta potential approaching-41 mV. The in vitro release profile of PNS from the F127 plus methyl cellulose gel followed zero order kinetics and correlated linearly with the weight percentage of gel dissolved, demonstrating that the overall rate of release of PNS is controlled by dissolution of the pluronic F127/methyl cellulose (MC) gel (r2 &gt; 0.99). The pharmacokinetic parameters of the PNS (6 mg/mL) in pluronic F127/MC gel were evaluated in comparison with the control progesterone suspension. After the administration of PNS in F127/MC gel into the rats, a maximum serum concentration of 22.1 &plusmn; 1.9 ng/mL was reached at a Tmax of 4.05 &plusmn; 0.1 h. The terminal half life was 12.7 &plusmn; 0.8 h. The area under the curve AUC0-&infin; of the injected formula was 452.75 &plusmn; 42.8 ng&bull;h/mL and the total mean residence time was 18.57 &plusmn; 1.44 h. The PNS in gel was significantly different from the control in rate and extent at P &lt; 0.001. The natural progesterone which was nanosized and formulated in a thermosensitive gel significantly sustained the action of natural progesterone so that it could be injected every 36 h instead of every day. Moreover, this formula is expected to provide a much safer choice than the use of semi-synthetic progesterone.Keywords: progesterone, nanosuspension, thermosensitive gel, ovariectomized female rats
format	article
author	Heba F Salem
author_facet	Heba F Salem
author_sort	Heba F Salem
title	Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats
title_short	Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats
title_full	Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats
title_fullStr	Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats
title_full_unstemmed	Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats
title_sort	sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats
publisher	Dove Medical Press
publishDate	2010
url	https://doaj.org/article/659bc889a56947cb9987da5a8734a16c
work_keys_str_mv	AT hebafsalem sustainedreleaseprogesteronenanosuspensionfollowingintramuscularinjectioninovariectomizedrats
_version_	1718402652061040640

Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats

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