Abstract：
:The vitamin E analogue, α-tocopherol succinate (α-TOS), has a broad anti-tumor effect. α-TOS can induce cancer cells apoptosis and suppress tumor growth by targeting mitochondria. Low bioavailability of α-TOS is the major problem encountered with formulation development. In our study, α-TOS nanoemulsion (α-TOS-NE) was demonstrated as a new drug delivery system of α-TOS to increase the bioavailability. MTT-based cytotoxicity assay and mitochondrial membrane potential (ΔY) were performed on human breast cancer cell lines MCF-7 and human oral epithelial cancer cell lines KB to evaluate in vitro anticancer efficacy of α-TOS-NE. In comparison with free α-TOS, α-TOS-NE exhibited a stronger cytotoxicity and decreased ΔΨ. Pharmacokinetic profiles of I.V. α-TOS-NE group, I.P. α-TOS-NE group, and I.P. free α-TOS group (7% DMSO/93% PEG) were drawn. First of all, nanoemultion (NE) enables the I.V. injection of α-TOS, make it possible to be an I.V. preparation. Second, compare to the I.P. free α-TOS group, I.P. α-TOS-NE group had a higher bioavailability. Thus, NE improved the strong anti-cancer efficacy of α-TOS while increasing its in vivo bioavailability in rats. In conclusion, our laboratory-made NE was a safe drug delivery system for clinical trials and could be a promising formulation for α-TOS by I.V administration.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Gao Y,Qi X,Zheng Y,Ji H,Wu L,Zheng N,Tang Jdoi
10.1016/j.ijpharm.2016.10.026subject
Has Abstractpub_date
2016-12-30 00:00:00pages
506-514issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(16)30960-7journal_volume
515pub_type
杂志文章abstract：:Prostaglandin E(1) (PGE1) shows various pharmacological activities including anti-inflammation. However, the rapid metabolization and inactivation of the intravenously administered PGE1 during the first passage through the lungs result in significant non-compliance in clinical trials which greatly limits its applicati...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.12.019
更新日期：2010-03-15 00:00:00
abstract：:Antimicrobial resistance (AMR) has become a global health problem. Bacteria are able to adapt to different environments, with the presence or absence of a host, forming colonies and biofilms. In fact, biofilm formation confers chemical protection to the microbial cells, thus making most of the conventional antibiotics...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2020.119478
更新日期：2020-07-30 00:00:00
abstract：:Piroxicam crystallises into two polytypes, α1 and α2, with crystal structures that contain identical molecular layers but differ in the way that these layers are stacked. In spite of having close structural similarity, the polytypes have significantly different powder tabletting behaviour: α2 forms only weak tablets a...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.03.040
更新日期：2018-05-30 00:00:00
abstract：:The implementation of a blend monitoring and control method based on a process analytical technology such as near infrared spectroscopy requires the selection and optimization of numerous criteria that will affect the monitoring outputs and expected blend end-point. Using a five component formulation, the present arti...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.06.061
更新日期：2014-10-01 00:00:00
abstract：:Transferosomes, also known as transfersomes, are ultradeformable vesicles for transdermal applications consisting of a lipid bilayer with phospholipids and an edge activator and an ethanol/aqueous core. Depending on the lipophilicity of the active substance, it can be encapsulated within the core or amongst the lipid ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2019.118817
更新日期：2020-01-05 00:00:00
abstract：:Superparamagnetic iron oxide nanoparticles (SPIO-NPs) have traditionally been used as MRI contrast agent for disease imaging via passive targeting. However, there has been an increasing interest in the development of SPIO-NPs to cellular-specific targeting for imaging and drug delivery currently. The objective of our ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.10.038
更新日期：2011-02-14 00:00:00
abstract：:Monoclonal antibodies are routinely used as tools in immunotherapies against solid tumors. However, administration of monoclonal antibodies may cause undesired side effects due to their accumulation in non-targeted organs. Nanoliposomes of less than 200 nm can target antibodies to tumors by enhanced permeation and ret...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.08.048
更新日期：2015-11-10 00:00:00
abstract：:Once introduced into physiological environment, nanoparticles (NPs) are immediately coated with proteins, resulting in formation of what is known as protein corona. The formation of protein corona can be affected by many factors. Likewise, the addition of protein corona can alter the physicochemical properties and bio...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2018.10.011
更新日期：2018-12-01 00:00:00
abstract：:The melting point of lidocaine was significantly lowered when mixed with thymol and/or aqueous ethanol. Mixtures of lidocaine and thymol at ratios within the range of 30:70-70:30 (w:w) became homogeneous oils at 25 degrees C. In a pH 9.2 carbonate buffer containing 25% ethanol, lidocaine (5%, w:w) also liquefied at 25...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00689-5
更新日期：2001-07-03 00:00:00
abstract：:A novel dual drug-tailed betaine conjugate amphiphile has been firstly synthesized in which the polar headgroup is derived from glycine betaine and the hydrophobic tails are chlorambucil molecules. The newly prepared conjugate undergoes self-assembly to form stable liposome-like nanocapsules as an effective carrier wi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.08.006
更新日期：2015-09-30 00:00:00
abstract：:Amphipathic asymmetric dendrimers have been investigated for use in delivery of genes into cells, with the objective of optimising transfection efficiency and maintaining cell viability. We have synthesised amphipathic asymmetric dendrimers by solid phase methods. The ability of two of these to transfect BHK cells in ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00534-2
更新日期：2000-11-04 00:00:00
abstract：:Water-soluble calixarenes are promising macrocyclic compounds which have found numerous applications in chemistry and biology. However, these compounds have been less studied in regard to their behavior in aqueous solutions and mechanisms of drug solubilization. The present work is devoted to the evaluation of the sol...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.09.011
更新日期：2010-12-15 00:00:00
abstract：:Anti-neuroexcitation peptide (ANEP) is a promising candidate for the treatment of neuroexcitation-associated diseases. N-Trimethyl chitosan (TMC) with different degrees of quaternization was synthesized, characterized and evaluated as a brain-targeting delivery vehicle for ANEP. ANEP-loaded TMC nanoparticles were prep...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.11.002
更新日期：2010-02-15 00:00:00
abstract：:Surface functionalisation of polymeric electrospun scaffolds with therapeutic biomolecules is often explored in regenerative medicine and tissue engineering. However, the bioconjugation method must be carefully selected to prevent partial or full loss of activity of the biomolecule following chemical manipulation. Per...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2021.120231
更新日期：2021-01-20 00:00:00
abstract：:In this study, the active components of grape pomaces were first extracted by maceration in ethanol and propylene glycol, then in extra virgin olive oil. The main components of the hydrophilic extractive solutions were flavonoids, while monounsaturated fatty acids were the most abundant constituents of the extractive ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.03.037
更新日期：2017-05-15 00:00:00
abstract：:The aims of this study were to develop novel liposome formulations for tranexamic acid (TA) from various lipid compositions [neutral (hydrogenated soya phosphatidylcholine and cholesterol), positive (stearylamine) or negative (dicetyl phosphate) charged lipid], and to investigate the effects of concentrations of TA (5...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00980-2
更新日期：2002-03-20 00:00:00
abstract：:Optical surface roughness of starch acetate compacts was investigated by specular reflection of a laser beam as a function of angle of incidence. The intensity data was fitted using the model of Gaussian and Lorentzian curves to solve numerical values for optical surface roughness which was observed to be order of 1 m...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00077-0
更新日期：1999-05-25 00:00:00
abstract：:A range of 17 ternary formulations of itraconazole (ITZ), HPMCP and Soluplus have been manufactured using spray drying. These amorphous solid dispersions (ASDs) were very stable against crystallisation and ITZ was found to be amorphous in all formulations after one year at 40°C/75% RH. A number of solid state analytic...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.01.043
更新日期：2017-03-15 00:00:00
abstract：:This paper presents in situ time-resolved drug mass fraction measurements in pressurised metered dose inhaler (PMDI) sprays, using a novel combination of synchrotron X-ray fluorescence and scattering. Equivalent suspension and solution formulations of ipratropium bromide in HFA-134a propellant were considered. Measure...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.05.067
更新日期：2019-07-20 00:00:00
abstract：:Exposure of a drug to irradiation can influence the stability of the formulation, leading to changes in the physicochemical properties of the product. The influence of excipients of frequently used stabilizers is often difficult to predict and, therefore, stability testing of the final preparation is important. The se...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/s0378-5173(01)00746-3
更新日期：2001-08-28 00:00:00
abstract：:Ran is a small ras-related GTPase and is highly expressed in aggressive breast carcinoma. Overexpression induces malignant transformation and drives metastatic growth. We have designed a novel series of anti-Ran-GTPase peptides, which prevents Ran hydrolysis and activation, and although they display effectiveness in s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.02.006
更新日期：2017-04-15 00:00:00
abstract：:Fibrous films have attracted considerable attention in the field of drug delivery and wound dressings owing to their porous structure and highly aligned fiber orientation. However, current fabrication methods such as electrospinning have certain limitations, including high voltage requirement and conductivity dependen...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.02.005
更新日期：2019-04-05 00:00:00
abstract：:To increase colonoscopy capability to discriminate benign from malignant polyps, we suggest combining two imaging approaches based on targeted polymeric platforms. Water-soluble cationized polyacrylamide (CPAA) was tagged with the near infrared (NIR) dye IR-783-S-Ph-COOH to form Flu-CPAA. The recognition peptide VRPMP...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.11.066
更新日期：2015-01-30 00:00:00
abstract：:N-Acetyl-l-cysteine (NAC) commonly used as an antidote in acetaminophen poisoning has shown promise in the treatment of neurological disorders such as cerebral palsy (CP). However, NAC suffers from drawbacks such as poor oral bioavailability and suboptimal blood-brain-barrier (BBB) permeability limiting its clinical s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.04.040
更新日期：2018-07-10 00:00:00
abstract：:To prolong the precorneal resident time and improve ocular bioavailability of the drug, Pluronic F127-g-poly(acrylic acid) copolymers were studied as in situ gelling vehicle for ophthalmic drug delivery system. The rheological properties and in vitro drug release of Pluronic-g-PAA copolymer gels were investigated. The...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.09.005
更新日期：2008-02-28 00:00:00
abstract：:Integrin alpha(5)beta(1) is expressed on several types of cancer cells, including colon cancer, and plays an important role in tumor growth and metastasis. The ability to target the integrin alpha(5)beta(1) using an appropriate drug delivery nano-vector can significantly help in inhibiting tumor growth, reducing tumor...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.09.016
更新日期：2009-01-21 00:00:00
abstract：:The present study deals with controlled drug delivery from hydrocolloid tablets by polymer particle erosion. The influence of excipients and formulation factors on the dissolution behaviour of the methyl hydroxyethyl cellulose (MHEC)-tablets is investigated. Linear drug release with low susceptibility to hydrodynamic ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00596-8
更新日期：2001-04-17 00:00:00
abstract：:The purpose of this investigation was to evaluate the performance of poly (amidoamine) (PAMAM) dendrimers, with three different surface groups, to be used as drug carriers. Drug-dendrimers complexes were investigated for solubility studies, dissolution studies, in vitro drug release studies, and for stability studies....
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.12.002
更新日期：2011-02-28 00:00:00
abstract：:Emulsion technology has been utilized extensively in the pharmaceutical industry. This article presents a comprehensive review of the literature on an important subcategory of emulsions, microemulsions. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10-100nm diameter, that form s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2017.05.005
更新日期：2017-06-30 00:00:00
abstract：:There is a realisation that small quantities of amorphous material can have a significant impact on the properties of crystalline solids. Consequently there is a growing interest in quantifying the amount of amorphous material that is present in "crystalline powders". Success has been reported when using isothermal mi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00527-5
更新日期：2000-10-10 00:00:00
