| Duloxetine HCl lipid nanoparticles: preparation, characterization, and dosage form design. | |
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MedLine Citation:
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PMID: 22167415 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Ketan Patel; Sameer Padhye; Mangal Nagarsenker |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't Date: 2011-12-14 |
Journal Detail:
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Title: AAPS PharmSciTech Volume: 13 ISSN: 1530-9932 ISO Abbreviation: AAPS PharmSciTech Publication Date: 2012 Mar |
Date Detail:
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Created Date: 2012-02-21 Completed Date: 2012-10-30 Revised Date: 2013-02-20 |
Medline Journal Info:
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Nlm Unique ID: 100960111 Medline TA: AAPS PharmSciTech Country: United States |
Other Details:
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Languages: eng Pagination: 125-33 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutics, Bombay College of Pharmacy, Kalina, Santacruz, Mumbai, India. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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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:
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0/Antidepressive Agents; 0/Dosage Forms; 0/Lipids; 0/Thiophenes; O5TNM5N07U/duloxetine |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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