Abstract:
PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG-PLA micelles, was prepared using the thin-film hydration method and evaluated in vitro. The preparation process was optimized with a central composite design (CCD). Micelles were characterized by size, transmission electron microscopy, loading capacity, and critical micelle concentration (CMC). The cytotoxicity of CUR-mPEG-PLA micelles was investigated against murine melanoma cells, B16F10 and human breast cancer cells, MDA-MB-231. RESULTS:The average size of the CUR-mPEG-PLA micelles was 110 ± 5 nm with polydispersity index in the range of 0.15-0.31, and the encapsulating efficiency for CUR was 91.89 ± 1.2, and 11.06 ± 0.8% for drug-loading. Sustained release of CUR from micelles was observed with 9.73% CUR release from micelles compared to 64.24% release of free curcumin in first 6 h under sink condition. The CUR-mPEG-PLA was efficiently taken up by the cancer cells, B16F10 and MDA-MB-231. Following 24 h incubation, CUR-mPEG-PLA induced higher cytotoxicity compared to free CUR in MDA-MB-231 cell lines indicating exposure of higher dose of free CUR to cells lead to up-regulation of drug efflux mechanisms leading to decreased cell death in case of free CUR administration. CONCLUSION:Our results indicate that the proposed micellar system has the potential to serve as an efficient carrier for CUR by effectively solubilizing, stabilizing and delivering the drug in a controlled manner to the cancer cells.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Kumari P,Swami MO,Nadipalli SK,Myneni S,Ghosh B,Biswas Sdoi
10.1007/s11095-015-1830-zsubject
Has Abstractpub_date
2016-04-01 00:00:00pages
826-41issue
4eissn
0724-8741issn
1573-904Xpii
10.1007/s11095-015-1830-zjournal_volume
33pub_type
杂志文章abstract::The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016292232513
更新日期:1995-03-01 00:00:00
abstract:PURPOSE:To examine the effect of particle size and morphology on aerosol dispersion using jet-milled and spray-dried mannitol particles in narrow size distributions within the respirable range. METHODS:Particle size and morphology were examined by laser diffraction and scanning electron microscopy, respectively. Aeros...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000033007.27278.60
更新日期:2004-07-01 00:00:00
abstract:PURPOSE:Effects of polyvinylpyrrolidone (PVP) molecular weight on the solid-state intermolecular interactions among probucol/PVP/sodium dodecyl sulfate (SDS) ternary ground mixtures (GM) and the formation of nanoparticles were investigated by solid-state NMR spectroscopy. MATERIALS AND METHODS:Ternary GMs of probucol ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9089-z
更新日期:2006-11-01 00:00:00
abstract::Colonic absorption of recombinant human insulin-like growth factor I (rhIGF-I) was measured in vitro using both rat and minipig colon. The permeability coefficients were 8.03 +/- 1.03 and 4.75 +/- 0.43 x 10(-8) cm sec-1 in the rat and minipig, respectively. The steady-state flux in rat colon was linearly related to th...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018999106684
更新日期:1994-02-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016295907266
更新日期:1995-12-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章,随机对照试验
doi:10.1007/s11095-005-2493-y
更新日期:2005-04-01 00:00:00
abstract:PURPOSE:An ex vivo intact toe model was developed to assess two different applicator designs for iontophoretic delivery of terbinafine into the nail only or the nail and surrounding skin. METHODS:Iontophoretic permeation studies were carried out on intact cadaver toes using nail-only and nail/skin applicators with a c...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-9934-y
更新日期:2009-09-01 00:00:00
abstract:PURPOSE:Permeation studies, with near infrared (NIR) light and anti-aggregation antibody formulation, were used to investigate the in vitro permeation of bevacizumab, ranibizumab and aflibercept through human sclera. METHODS:A vertical, spherical Franz cell diffusion apparatus was used for this scleral tissue permeati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2392-7
更新日期:2018-03-29 00:00:00
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journal_title:Pharmaceutical research
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doi:10.1023/A:1016381215385
更新日期:1985-11-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:1999-05-01 00:00:00
abstract:PURPOSE:The aim of this study was to test the ability of paclitaxel-loaded poly(butylcyanoacrylate) (PBCA) nanoparticles to overcome multidrug resistance (MDR) in human ovarian resistant cells (A2780/T) and investigate its possible mechanism. METHODS:We prepared paclitaxel-loaded PBCA nanoparticles by interfacial poly...
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pub_type: 杂志文章
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更新日期:2011-04-01 00:00:00
abstract:PURPOSE:Design of intravaginal rings (IVRs) for delivery of antiretrovirals is often guided by in vitro release under sink conditions, based on the assumption that in vivo release will follow a similar release profile. METHODS:We conducted a dose-ranging study in the female reproductive tract of pigtail macaques using...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2224-1
更新日期:2017-10-01 00:00:00
abstract::Recently a new in vivo approach in man, using a regional intestinal perfusion technique, has been developed. The perfusion tube consists of a multichannel tube with two inflatable balloons, which are placed 10 cm apart. The tube is introduced orally and the time required for insertion and positioning of the tube is ap...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015888813741
更新日期:1992-10-01 00:00:00
abstract::Various derivatives of the C-terminal amide group in N-protected amino acid and peptide amides were synthesized to assess their suitability as prodrug forms with the aim of protecting the amide or peptide bond against cleavage by alpha-chymotrypsin. Whereas N-acetylation, N-hydroxymethylation, and N-phthalidylation di...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015854718903
更新日期:1991-12-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9371-8
更新日期:2008-04-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1026147620304
更新日期:2003-10-01 00:00:00
abstract:PURPOSE:To better understand the nature of drug-excipient interactions we have studied the phase behavior of amorphous binary and ternary mixtures of citric acid, indomethacin and PVP, as model systems. METHODS:We have prepared amorphous mixtures by co-melting or coprecipitation from solvents, and have measured glass ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011983606606
更新日期:1998-08-01 00:00:00
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journal_title:Pharmaceutical research
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doi:10.1023/a:1018938722768
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journal_title:Pharmaceutical research
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更新日期:2005-10-01 00:00:00
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更新日期:2004-10-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:1987-04-01 00:00:00
abstract::The crystal growth kinetics of theophylline monohydrate from aqueous buffered supersaturated solutions were investigated at 10, 20, 30, and 40 degrees C. Crystallization experiments were carried out isothermally at pH 6. During growth the crystal count and size distributions were monitored in situ. The growth rate was...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015817109932
更新日期:1991-05-01 00:00:00
abstract::Four lipophilic, low molecular weight drugs solubilized in phosphatidylcholine-bile salt mixed micelles were injected s.c. into the hind legs of sheep and their cumulative recoveries in lymph draining from the site of application were determined. Surprisingly, the cumulative recoveries (percentage of dose) varied betw...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015807913934
更新日期:1991-10-01 00:00:00
abstract::The influence of varying protein and fat content in milk of New Zealand White rabbits on the milk-to-plasma drug concentration (M/P) ratio of diazepam was studied. At various time points after littering, a bolus dose (1.5 mg/kg) followed by a 26-hr infusion (1.8 mg/h) of diazepam was administered to freely moving rabb...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:1992-10-01 00:00:00
abstract:PURPOSE:Novel therapeutics are greatly needed that target specific pathological receptors and pathways involved in Neuropathic Pain (NP). Extending our previous work published in this Journal on Group I metabotropic glutamate receptor (mGluR) modulators, we now investigate the therapeutic potential of niclosamide in mo...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2027-9
更新日期:2016-12-01 00:00:00
abstract:PURPOSE:The use of "Trojan Horse" nanocarriers for antibiotics to enhance the activity of antibiotics against susceptible and resistant bacteria is investigated. METHODS:Antibiotic carriers (CD-MAN and CD-GLU) are prepared from β-cyclodextrin grafted with sugar molecules (D-mannose and D-glucose, respectively) via azi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1861-0
更新日期:2016-05-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2002-12-01 00:00:00