Document Detail


Duloxetine HCl lipid nanoparticles: preparation, characterization, and dosage form design.
MedLine Citation:
PMID:  22167415     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Solid lipid nanoparticles (SLNs) of duloxetine hydrochloride (DLX) were prepared to circumvent the problems of DLX, which include acid labile nature, high first-pass metabolism, and high-dosing frequency. The DLX-SLNs were prepared by using two different techniques, viz. solvent diffusion method and ultrasound dispersion method, and evaluated for particle size, zeta potential, entrapment efficiency, physical characteristics, and chemical stability. Best results were obtained when SLNs were prepared by ultrasound dispersion method using glyceryl mono stearate as solid lipid and DLX in ratio of 1:20 and mixture of polysorbate 80 and poloxamer 188 as surfactant in concentration of 3%. The mean particle size of formulation and entrapment efficiency was 91.7 nm and 87%, respectively, and had excellent stability in acidic medium. Differential scanning calorimetry and X-ray diffraction data showed complete amorphization of DLX in lipid. In vitro drug release from SLNs was observed for 48 h and was in accordance with Higuchi kinetics. In vivo antidepressant activity was evaluated in mice by forced swim test. DLX-SLNs showed significant enhancement in antidepressant activity at 24 h when administered orally in comparison to drug solution. These results confirm the potential of SLNs in enhancing chemical stability and improving the efficacy of DLX via oral route. The SLN dispersion was converted into solid granules by adsorbing on colloidal silicon dioxide and characterized for particle size after redispersion, morphology, and flow properties. Results indicated that nanoparticles were successfully adsorbed on the carrier and released SLNs when dispersed in water.
Authors:
Ketan Patel; Sameer Padhye; Mangal Nagarsenker
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't     Date:  2011-12-14
Journal Detail:
Title:  AAPS PharmSciTech     Volume:  13     ISSN:  1530-9932     ISO Abbreviation:  AAPS PharmSciTech     Publication Date:  2012 Mar 
Date Detail:
Created Date:  2012-02-21     Completed Date:  2012-10-30     Revised Date:  2013-06-27    
Medline Journal Info:
Nlm Unique ID:  100960111     Medline TA:  AAPS PharmSciTech     Country:  United States    
Other Details:
Languages:  eng     Pagination:  125-33     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz, Mumbai, India.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antidepressive Agents / administration & dosage,  chemical synthesis*
Depression / drug therapy
Dosage Forms
Drug Design*
Lipids
Male
Mice
Nanoparticles / administration & dosage,  chemistry*
Particle Size
Thiophenes / administration & dosage,  chemical synthesis*
X-Ray Diffraction
Chemical
Reg. No./Substance:
0/Antidepressive Agents; 0/Dosage Forms; 0/Lipids; 0/Thiophenes; O5TNM5N07U/duloxetine
Comments/Corrections

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