Abstract：
:The paper describes sterically stabilized lipid nanocapsules (LNC) and multilamellar liposomes (MLV) coated using a new amphiphilic conjugate of PEG(2000) with a 2-alkyl-lipoamino acid (LAA). A complement activation assay (CH50) and uptake experiments by THP-1 macrophage cells were used to assess in vitro the effectiveness of the PEG-LAA derivative of modifying the surface behavior of nanocarriers. Administered to rats or Swiss mice, respectively, the PEG(2000)-LAA-modified LNC and MLV showed plasma half-lives longer than the corresponding naked carriers. To assess the ability of nanocarriers to specifically reach tumor sites, paclitaxel (PTX)-loaded LNC and MLV were administered subcutaneously to rats implanted with a 9L glioma. Animals treated with saline or naked LNC and MLV underwent a quick expansion of tumor mass, up to a volume of 2000 mm(3) 25 days after the injection of tumor cells. On the contrary, treatment with a PEG-LAA modified LNC carrier reduced the growth of the tumor volume, which did not exceed 1000 mm(3) by day 25. Analogous positive results were obtained with the liposomal systems. The experimental findings confirmed that these new PEG-LAA conjugates allow to obtain sterically stable nanocarriers that behave effectively and in a comparable or even better way than the (phospho)lipid PEG derivatives commercially available.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Basile L,Passirani C,Huynh NT,Béjaud J,Benoit JP,Puglisi G,Pignatello Rdoi
10.1016/j.ijpharm.2012.01.038subject
Has Abstractpub_date
2012-04-15 00:00:00pages
231-238issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(12)00092-0journal_volume
426pub_type
杂志文章abstract：:Naltrexone hydrochloride (NTX) is a promising treatment for corneal disorders linked to diabetes mellitus (diabetic keratopathy). However, NTX has a major stability problem due to autoxidation, which is likely to hinder its formulation as eye drops for treatment of diabetic keratopathy. In this study, in-house develop...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.05.011
更新日期：2012-08-20 00:00:00
abstract：:To introduce better antibiotics for the treatment of some infectious diseases in sheep and to expand the range of antibiotics available for veterinary medicine, pharmacokinetics of two antibiotics marbofloxacin (MBX) and trovafloxacin (TVX) were investigated in sheep after intramuscular injection. Variable and irregul...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.01.046
更新日期：2015-03-15 00:00:00
abstract：:The aim of this study was to prepare spherical agglomerates of lactose and to evaluate their physicochemical properties, flow properties, particle friability and compaction properties, and to compare them to commercially available types of lactose for direct compression (spray-dried, granulated and anhydrous β-lactose...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.11.040
更新日期：2017-01-10 00:00:00
abstract：:A polymeric prodrug of cisplatin (CP) with simple chemical structure was synthesized based on pullulan and its therapeutic effects on human hepatocellular carcinoma (HCC) were studied in vitro and in vivo. Briefly, CP was linked to pullulan monosuccinate (SUPA) via coordination bond to form prodrug of CP-SUPA with the...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.02.027
更新日期：2015-04-10 00:00:00
abstract：:Moisture-sensitive pseudo-polymorphs with different stabilities were characterized, and their polymorphisms were monitored in the process of tableting and film coating by near-infrared (NIR) spectroscopy. In this study, we proved that we could successfully maintain the crystal form ratio in the tablet by controlling t...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2008.10.010
更新日期：2009-02-23 00:00:00
abstract：:This investigation is a contribution to standardization in in vitro drug penetration measurements using excised human skin and to statistical treatment of the observations. The wide variations observed in measurements of drug accumulation in and drug permeation through the stratum corneum are caused not only by analyt...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00558-5
更新日期：2000-11-19 00:00:00
abstract：:To enhance oral bioavailability of matrine, a dedicated and newly emerging drug system called self-nanoemulsifying drug delivery system (SNEDDSs) was developed. Phospholipid complex (MPC) was prepared using solvent-evaporation method to improve the liposolubility of matrine. Solubilization test, infrared spectroscopy ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.11.026
更新日期：2010-02-15 00:00:00
abstract：:The pharmacokinetics of NS-49, a newly developed phenethylamine class alpha(1A)-adrenoceptor agonist, was investigated in rats, rabbits, and dogs given intravenous and oral doses that have little effect on the renal blood flow rate (approximating the range of clinical doses). A three-compartment open model adequately ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00184-2
更新日期：1999-09-20 00:00:00
abstract：:The presence of large amounts of reactive oxygen species (ROS) leads to oxidative stress that can damage cell membranes, lead to DNA breakage and cause inactivation of free radical scavenger enzymes, eventually resulting in skin damage. Quercetin is a natural flavonoid that has been shown to have the highest anti-radi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.12.013
更新日期：2013-01-30 00:00:00
abstract：:The application of nanoparticles (NPs) as radio-sensitizers and carriers has opened up a new horizon to overcome the limitations of chemo and radiotherapy. In this study, bovine serum albumin-coated Bi2S3 NPs (Bi2S3@BSA NPs) were synthesized and evaluated in terms of their ability to be used as a radio-sensitizer and ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119320
更新日期：2020-05-30 00:00:00
abstract：:Multilayered coated liposomes were prepared using the layer-by-layer (LbL) technique in an effort to improve their stability in biological media. The formulation strategy was based on the alternate deposition of two biocompatible and biodegradable polyelectrolytes - poly(L-lysine) (PLL) and poly(L-glutamic acid) (PGA)...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119568
更新日期：2020-08-30 00:00:00
abstract：:The ionization and transport properties of lidocaine hydrochloride (LidHCl) in aqueous propylene glycol (PG) containing 20% PG by weight was studied by means of electrical precision conductometry. For drug concentrations exceeding about 1.7 mM a slight formation of LidH(+)Cl(-) ion-pairs is indicated; ion-pair associa...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00400-2
更新日期：2000-05-15 00:00:00
abstract：:Cationic polyphosphoesters (PPEs) with different side-chain charge groups were designed and synthesized as biodegradable gene carriers. Poly(N-methyl-2-aminoethyl propylene phosphate) (PPE-MEA), with a secondary amino group (-CH(2)CH(2)NHCH3) side chain released DNA in several hours at N/P (amino group of polymer to p...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2003.07.006
更新日期：2003-10-20 00:00:00
abstract：:Glioblastoma (GBM) is a difficult-to-treat cancer, likely attributed to the blood brain barrier and drug resistance. Nose-to-brain drug delivery is a direct and non-invasive pathway for brain targeting with low systemic toxicity. Disulfiram (DSF) has shown its effectiveness against GBM, especially with copper ion (Cu)...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2021.120250
更新日期：2021-01-21 00:00:00
abstract：:Liposomes modified using cationic and hydrophilic nonionic polymers are 2 popular carriers for improving oral drug absorption. Cationic polymer-modified liposomes can adhere to the intestinal wall mucus (mucoadhesive type), while liposomes modified using hydrophilic nonionic polymers can penetrate across the mucus bar...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.04.002
更新日期：2013-06-05 00:00:00
abstract：:The particle size of peptide DNA condensates were studied after freeze-drying and rehydration as a function of sugar excipient, concentration, pH, DNA concentration, and peptide condensing agent. In the absence of an excipient, freeze-dried 50 microg/ml AlkCWK(18) (iodoacetic acid alkylated Cys-Typ-Lys(18)) DNA conden...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00435-x
更新日期：2000-08-10 00:00:00
abstract：:The model anti-inflammatory drug prednisolone (PS) was retained in chitosan (CS) gel beads, which were prepared in a 10% aqueous amino acid solution (pH 9.0). Sustained release of PS from the CS gel beads was observed. Carrageenan solution was injected into air pouches (AP), which were prepared subcutaneously on the d...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2003.11.036
更新日期：2004-03-19 00:00:00
abstract：:In this paper, a fast forming nano-composite hydrogel was developed for potential application in ocular drug delivery. The optical transmission (OT) as well as rheological properties of nano-composite hydrogel was characterized. The developed nano-composite hydrogel given a high diclofenac micelles loading and provide...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.03.024
更新日期：2013-05-01 00:00:00
abstract：:A drug carrier of colloidal lipid particles with improved payloads and enhanced storage stability was investigated. Based on the experiences with hard fats nanoparticles, a new type of solid lipid nanoparticles (SLN) has been developed by incorporating triglyceride containing oils in the solid core of said particle. T...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(00)00378-1
更新日期：2000-04-20 00:00:00
abstract：:Enhancing transdermal delivery of insulin using chemical penetration enhancers (CPEs) has several advantages over other non-traditional methods; however, lack of suitable predictive models, make experimentation the only alternative for discovering new CPEs. To address this limitation, a quantitative structure-property...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.12.028
更新日期：2010-03-30 00:00:00
abstract：:The objectives of this study were to describe the pharmacokinetics and tissue distribution of superparamagnetic iron oxide nanoparticle (SPIO) stabilized with alginate (SPIO-alginate), and investigate its potential in detecting liver cancers as a newly developed magnetic resonance (MR) contrast agent. Pharmacokinetics...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.11.036
更新日期：2008-04-16 00:00:00
abstract：:Autophagy is a lysosomal degradation pathway that acts as a cytoprotective mechanism causing treatment resistance in various cancer cells. Recent studies showed that hydroxychloroquine can inhibit the latter step of autophagy and therefore enhance the anti-glioma efficiency of ZD6474, a tyrosine kinase inhibitor. Howe...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.09.007
更新日期：2018-01-30 00:00:00
abstract：:Cyclosporin A (CyA) is a lipophilic, cyclic polypeptide drug with anti-inflammatory properties. It is used in topical treatment of dry eyes and is now commercially available in oil based surfactant containing eye drops. Surfactants can irritate the eye surface causing burning, itching and irritation of the conjunctiva...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.07.040
更新日期：2015-09-30 00:00:00
abstract：:A hybrid silica-liposome nanocapsule system containing insulin has been developed and the encapsulation, protection and release properties are evaluated. The formulation strategy is based on using insulin-loaded 1,2-dipalmitoyl-sn-glycero-3-phosphocholine and cholesterol liposomes as a template for the deposition of i...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.03.061
更新日期：2010-06-15 00:00:00
abstract：:A centrifuge method has been applied to the assessment of water retention in pharmaceutical powders. Five drug models and microcrystalline cellulose (MCC) were each mixed with different amounts of water and centrifuged at different speeds. The amount of water retained by the wet mass was evaluated by drying the powder...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(99)00201-x
更新日期：1999-10-15 00:00:00
abstract：:Dermal administration of different macromolecules, such as nucleic acids, remains a real challenge because of the difficulty of crossing the main skin barrier, the stratum corneum (SC). To overcome this barrier, the use of deformable lipid-based nanovectors were developed to increase topical penetration through the SC...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.118793
更新日期：2019-12-15 00:00:00
abstract：:Mathematical models for the release of drug from both non-degradable and degradable slab matrices in which the initial drug loading is greater than the solubility are presented in this paper. Taking the anomalous diffusions in the drug release processes into account, the fractional calculus is introduced to model the ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2010.12.009
更新日期：2011-10-10 00:00:00
abstract：:Oral absorption of lopinavir (LPV) is limited due to P-glycoprotein (P-gp) and multidrug resistance-associated protein2 (MRP2) mediated efflux by intestinal epithelial cells. Moreover, LPV is extensively metabolized by CYP3A4 enzymes. In the present study, dipeptide prodrug approach was employed to circumvent efflux p...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.09.035
更新日期：2014-12-10 00:00:00
abstract：:The aim of this study was to investigate the potential of solid dispersion to improve the dissolution rate and bioavailability of osthole (Ost), a coumarin derivative with various pharmacological activities but with poor aqueous solubility. In present studies, the Ost solid dispersions were prepared with various polym...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2014.02.040
更新日期：2014-04-25 00:00:00
abstract：:Different types of Carbopols are frequently applied excipients of various dosage forms. Depending on the supramolecular structure, their water sorption behaviour could significantly differ. The purpose of the present study was to track the supramolecular changes of two types of Carbopol polymers (Carbopol 71G and Ultr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.06.028
更新日期：2011-09-15 00:00:00
