Document Detail


Sustained-release progesterone nanosuspension following intramuscular injection in ovariectomized rats.
MedLine Citation:
PMID:  21187946     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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 > 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 ± 1.9 ng/mL was reached at a T(max) of 4.05 ± 0.1 h. The terminal half life was 12.7 ± 0.8 h. The area under the curve AUC₀₋∞ of the injected formula was 452.75 ± 42.8 ng·h/mL and the total mean residence time was 18.57 ± 1.44 h. The PNS in gel was significantly different from the control in rate and extent at P < 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.
Authors:
Heba F Salem
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Publication Detail:
Type:  Journal Article     Date:  2010-11-10
Journal Detail:
Title:  International journal of nanomedicine     Volume:  5     ISSN:  1178-2013     ISO Abbreviation:  Int J Nanomedicine     Publication Date:  2010  
Date Detail:
Created Date:  2010-12-28     Completed Date:  2011-04-18     Revised Date:  2013-07-03    
Medline Journal Info:
Nlm Unique ID:  101263847     Medline TA:  Int J Nanomedicine     Country:  New Zealand    
Other Details:
Languages:  eng     Pagination:  943-54     Citation Subset:  IM    
Affiliation:
Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt. heba_salem2004@yahoo.co.uk
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MeSH Terms
Descriptor/Qualifier:
Animals
Calorimetry, Differential Scanning
Delayed-Action Preparations
Drug Stability
Female
Gels / chemistry
Injections, Intramuscular
Microscopy, Electron, Scanning
Nanoparticles / administration & dosage*,  chemistry,  ultrastructure
Ovariectomy
Poloxamer
Progesterone / administration & dosage*,  blood,  chemistry,  pharmacokinetics
Rats
Rats, Sprague-Dawley
Rheology
Stearic Acids / chemistry
Temperature
Chemical
Reg. No./Substance:
0/Delayed-Action Preparations; 0/Gels; 0/Stearic Acids; 106392-12-5/Poloxamer; 4ELV7Z65AP/stearic acid; 57-83-0/Progesterone
Comments/Corrections

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