+ Site Statistics
References:
52,654,530
Abstracts:
29,560,856
PMIDs:
28,072,755
+ Search Articles
+ Subscribe to Site Feeds
Most Shared
PDF Full Text
+ PDF Full Text
Request PDF Full Text
+ Follow Us
Follow on Facebook
Follow on Twitter
Follow on LinkedIn
+ Translate
+ Recently Requested

Enhanced cellular uptake by "pharmaceutically oriented devices" of new simplified analogs of Linezolid with antimicrobial activity



Enhanced cellular uptake by "pharmaceutically oriented devices" of new simplified analogs of Linezolid with antimicrobial activity



International Journal of Pharmaceutics 461(1-2): 163-170



The aim of the present study was to enhance cellular uptake of simplified analogs of Linezolid by their incorporation into suitable delivery devices in order to improve the antimicrobial activity of these novel synthesized oxazolidin-2-one derivatives. The oxazolidin-2-one derivatives were synthesized by developing a rather simple one-pot reaction starting from oxiranylmethanol and several primary amines. Three delivery devices were prepared by following different synthetic approaches, such as single-step free radical grafting, precipitation polymerization and nano-emulsion. Finally, the antimicrobial activity of the novel synthesized compounds, without any vehicle and after their incorporation into the delivery devices, was evaluated against Escherichia coli and Saccharomyces cerevisiae by performing time-kill analyses. The synthesized oxazolidinones exhibited modest antimicrobial activity against E. coli and S. cerevisiae (MIC 16 μg/mL). A good activity was, instead, highlighted after their incorporation into the prepared delivery devices (lecithin-based nano-emulsion, poly(N-vinyl-pyrrolidone)-methacrylic acid grafted copolymer and spherical polymeric nanoparticles) (MIC≤4 μg/mL). The incorporation into suitable vehicles, indeed, reduced by 4 times the normal MICs of the newly synthesized oxazolilidin-2-ones and represents an effective strategy to overcome cellular penetration constraints.

(PDF emailed within 0-6 h: $19.90)

Accession: 052982688

Download citation: RISBibTeXText

PMID: 24296047

DOI: 10.1016/j.ijpharm.2013.11.048


Related references

Antimicrobial activity of human α-defensin 5 and its linear analogs: N-terminal fatty acylation results in enhanced antimicrobial activity of the linear analogs. Peptides 71: 128-140, 2016

Enhanced cellular uptake and cytotoxic effect of doxorubicin entrapped in new analogs of low density lipoproteins, the SMBV. Proceedings of the American Association for Cancer Research Annual Meeting 34(0): 365, 1993

Cellular uptake of apidaecin 1b and related analogs in Gram-negative bacteria reveals novel antibacterial mechanism for proline-rich antimicrobial peptides. Protein and Peptide Letters 21(4): 391-398, 2014

Cellular uptake and anti hiv activity of oligonucleotides and their analogs. Erickson, R P And J G Izant (Ed ) Raven Press Series on Molecular And Cellular Biology, Vol 1 Gene Regulation: Biology Of Antisense Rna And Dna Xix+364p Raven Press: New York, New York, Usa Illus 273-283, 1992

Dendrimer-encapsulated camptothecins: increased solubility, cellular uptake, and cellular retention affords enhanced anticancer activity in vitro. Cancer Research 66(24): 11913-11921, 2006

Novel synthetic, salt-resistant analogs of human beta-defensins 1 and 3 endowed with enhanced antimicrobial activity. Antimicrobial Agents and ChemoTherapy 54(6): 2312-2322, 2010

Novel C-4'' modified azithromycin analogs with remarkably enhanced activity against erythromycin-resistant Streptococcus pneumoniae: the synthesis and antimicrobial evaluation. European Journal of Medicinal Chemistry 46(10): 5196-5205, 2012

Cellular uptake of transportan 10 and its analogs in live cells: Selectivity and structure-activity relationship studies. Peptides 32(9): 1934-1941, 2012

Cellular uptake of transportan 1 and its analogs in live cells selectivity and structure-activity relationship studies. 2011

Structure-activity relationships of the antimicrobial peptide gramicidin S and its analogs: aqueous solubility, self-association, conformation, antimicrobial activity and interaction with model lipid membranes. Biochimica et Biophysica Acta 1838(5): 1420-1429, 2014

Multicentre assessment of linezolid antimicrobial activity and spectrum in Europe: report from the Zyvox antimicrobial potency study (ZAPS-Europe). Clinical Microbiology and Infection 8(12): 791-800, 2003

Cationic lipids enhanced cellular uptake and activity of bcl-2 antisence oligodeoxynucleotide G3139 in HL-60 cells. Acta Pharmacologica Sinica 22(11): 1007-1012, 2001

Polyethylene glycol-complexed cationic liposome for enhanced cellular uptake and anticancer activity. International Journal of Pharmaceutics 382(1-2): 254-261, 2010

Esterification of Ginsenoside Rh2 Enhanced Its Cellular Uptake and Antitumor Activity in Human HepG2 Cells. Journal of Agricultural and Food Chemistry 64(1): 253-261, 2016

Enhanced cellular uptake and gene silencing activity of siRNA molecules mediated by chitosan-derivative nanocomplexes. International Journal of Pharmaceutics 473(1-2): 579-590, 2015