Abstract:
:The objective of this study was to develop an efficient tumor vasculature targeted liposome delivery system for combretastatin A4, a novel antivascular agent. Liposomes composed of hydrogenated soybean phosphatidylcholine (HSPC), cholesterol, distearoyl phosphoethanolamine-polyethylene-glycol-2000 conjugate (DSPE-PEG), and DSPE-PEG-maleimide were prepared by the lipid film hydration and extrusion process. Cyclic RGD (Arg-Gly-Asp) peptides with affinity for alphavbeta3-integrins expressed on tumor vascular endothelial cells were coupled to the distal end of PEG on the liposomes sterically stabilized with PEG (long circulating liposomes, LCL). The liposome delivery system was characterized in terms of size, lamellarity, ligand density, drug loading, and leakage properties. Targeting nature of the delivery system was evaluated in vitro using cultured human umbilical vein endothelial cells (HUVEC). Electron microscopic observations of the formulations revealed presence of small unilamellar liposomes of approximately 120 nm in diameter. High performance liquid chromatography determination of ligand coupling to the liposome surface indicated that more than 99% of the RGD peptides were reacted with maleimide groups on the liposome surface. Up to 3 mg/mL of stable liposomal combretastatin A4 loading was achieved with approximately 80% of this being entrapped within the liposomes. In the in vitro cell culture studies, targeted liposomes showed significantly higher binding to their target cells than nontargeted liposomes, presumably through specific interaction of the RGD with its receptors on the cell surface. It was concluded that the targeting properties of the prepared delivery system would potentially improve the therapeutic benefits of combretastatin A4 compared with nontargeted liposomes or solution dosage forms.
journal_name
AAPS PharmSciTechjournal_title
AAPS PharmSciTechauthors
Nallamothu R,Wood GC,Pattillo CB,Scott RC,Kiani MF,Moore BM,Thoma LAdoi
10.1208/pt070232subject
Has Abstractpub_date
2006-04-07 00:00:00pages
E32issue
2issn
1530-9932journal_volume
7pub_type
杂志文章abstract::The purpose of the present study was to design mucoadhesive gliadin nanoparticles (GNP) containing amoxicillin and to evaluate their effectiveness in eradicating Helicobacter pylori. GNP-bearing amoxicillin (AGNP) was prepared by desolvation method. The effect of process variables such as gliadin concentration and ini...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt050232
更新日期:2004-04-07 00:00:00
abstract::The solvent used for preparing the binder solution in wet granulation can affect the granulation end point and also impact the thermal, rheological, and flow properties of the granules. The present study investigates the effect of solvents and percentage relative humidity (RH) on the granules of microcrystalline cellu...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0424-8
更新日期:2016-08-01 00:00:00
abstract::The purpose of this study was to develop and validate a rapid, sensitive, and specific reversed-phase high-performance liquid chromatography method for the quantitative determination of native tenofovir (TNF) for various applications. Different analytical performance parameters such as linearity, precision, accuracy, ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-011-9735-6
更新日期:2012-03-01 00:00:00
abstract::Anti-vascular endothelial growth factor agents have been widely used to treat several eye diseases including age-related macular degeneration (AMD). An approach to maximize the local concentration of drug at the target site and minimize systemic exposure is to be sought. Sunitinib malate, a multiple receptor tyrosine ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1474-0
更新日期:2019-08-09 00:00:00
abstract::The process of developing an old drug for new indications is now a widely accepted strategy of shortening drug development time, reducing drug costs, and improving drug availability, especially for rare and neglected diseases. In this mini-review, we highlighted the impact of drug delivery systems in the fulfillment o...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-019-1333-z
更新日期:2019-02-15 00:00:00
abstract::Co-encapsulation of anticancer drugs paclitaxel and imatinib in nanocarriers is a promising strategy to optimize cancer treatment. Aiming to combine the cytotoxic and antiangiogenic properties of the drugs, a liposome formulation targeted to folate receptor co-encapsulating paclitaxel and imatinib was designed in this...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-017-0830-1
更新日期:2018-01-01 00:00:00
abstract::Individualized medicines for pediatrics are a useful alternative if there is no correct dosage marketed for this segment (easy to swallow, adequate volume and content, correct composition for pediatrics, good organoleptic properties, etc.). Its validation process must ensure quality testing: its content uniformity, ph...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1432-x
更新日期:2019-06-03 00:00:00
abstract::Celecoxib (CXB) is a poorly aqueous solubility sulfonamide non-steroidal anti-inflammatory drug (NSAID). Hence, the formulation of CXB was selected for solubilization and bioavailability. To find out suitable formulation for microemulsion, the solubility of CXB in triacetin (oil phase), Tween 80 (surfactant), and Tran...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-016-0667-z
更新日期:2017-08-01 00:00:00
abstract::The present study was carried out with a view to enhance the dissolution of poorly water-soluble BCS-class II drug aceclofenac by co-grinding with novel porous carrier Neusilin US(2.) (amorphous microporous granules of magnesium aluminosilicate, Fuji Chemical Industry, Toyama, Japan). Neusilin US(2) has been used as a...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-009-9221-6
更新日期:2009-01-01 00:00:00
abstract::The objective of this study was to determine the influence of mechanical stresses simulating gastrointestinal contraction forces of 2.0 N (stomach) and 1.2 N (intestine) on the gel properties and drug release characteristics from sustained release swelling and eroding hydrophilic matrices during dissolution studies. T...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-014-0225-5
更新日期:2015-04-01 00:00:00
abstract::The main principles of green chemistry and engineering were extended to pharmaceutical formulations to prepare eco-friendly surfactant-free dry emulsion tablets (SFDETs) devoid of solvents or synthetic surfactants. Surfactant-free emulsions were stabilized by in situ cyclodextrins/sweet almond oil inclusion complexes ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1450-8
更新日期:2019-07-18 00:00:00
abstract::The aims of the current study were to develop and evaluate clindamycin palmitate hydrochloride (CPH) 3D-printed tablets (printlets) manufactured by selective laser sintering (SLS). Optimization of the formulation was performed by studying the effect of formulation and process factors on critical quality attributes of ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01775-0
更新日期:2020-08-13 00:00:00
abstract::Hypertension remains a significant risk factor for several cardiovascular disorders including coronary artery disease and heart failure. Despite the large armamentarium of drugs available for the management of high blood pressure, low oral availability is an ongoing challenge. Researchers are constantly developing alt...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章,评审
doi:10.1208/s12249-019-1583-9
更新日期:2020-01-06 00:00:00
abstract::A simple, reliable, highly sensitive and selective spectrofluorimetric method has been developed for determination of certain aminoglycosides namely amikacin sulfate, tobramycin, neomycin sulfate, gentamicin sulfate, kanamycin sulfate and streptomycin sulfate. The method is based on the formation of a charge transfer ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-9969-6
更新日期:2013-06-01 00:00:00
abstract::This study assessed the utility of near-infrared (NIR) spectroscopy for the real-time monitoring of content uniformity and critical quality attributes (tensile strength, Young's modulus, and relative density) of ribbed roller compacted flakes made by axially corrugated or ribbed rolls. A custom-built setup was used to...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9890-4
更新日期:2013-03-01 00:00:00
abstract::The aim of the present work was the investigation of robustness and reliability of drug release from 50 to 400 mg quetiapine extended release HPMC matrix tablets towards mechanical stresses of biorelevant intensity. The tests were performed under standard conditions (USP apparatus II) as well as under simulated gastro...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-0050-2
更新日期:2014-02-01 00:00:00
abstract::Polymeric films are safe and effective and can be used for vaginal administration of microbicide drug candidates. Dapivirine (DPV), an investigational and clinically advanced antiretroviral drug, was selected as a model compound for this study. We have previously developed and clinically tested a quick-dissolving DPV ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1442-8
更新日期:2019-06-26 00:00:00
abstract::Spheroid formation mechanisms were investigated using extrusion-spheronization (ES) and rotary processing (RP). Using ES (cross-hatch), ES (teardrop), and RP (teardrop), spheroids with similar mass median diameter (MMD) and span were produced using equivalent formulation and spheronization conditions. During spheroniz...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt0801010
更新日期:2007-02-09 00:00:00
abstract::The aim of this study was to investigate the effects of a type of hydrophobic moiety, extent of N-substitution (ES), and degree of quaternization (DQ) of chitosan (CS) on the transepithelial electrical resistance and permeability of Caco-2 cells monolayer, using fluorescein isothiocyanate dextran 4,400 (FD-4) as the m...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-010-9399-7
更新日期:2010-06-01 00:00:00
abstract::To enhance the stability of coenzyme Q10 (CoQ10), Kolliphor® HS 15 (HS15) was employed as a carrier to build up a stable CoQ10-loaded micelle delivery system. The impact of micellar compositions, the preparation condition, and the preparation method on size characteristics, the solubilization efficiency, and micellar ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0399-5
更新日期:2016-06-01 00:00:00
abstract::The present investigation was undertaken to fabricate modified transport fluconazole transdermal spray using ethyl cellulose and Eudragit RS100 as film-forming polymers. Eudragit RS100 (X(1)) and ethyl cellulose (X(2)) were selected as independent variables in 3(2) full factorial design, whereas drug transport in firs...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-009-9256-8
更新日期:2009-01-01 00:00:00
abstract::While polyethylene oxide (PEO)-based matrix tablets are frequently used as abuse-deterrent dosage forms, there is limited information available regarding how the selection of formulation components and manufacturing processes affect the resulting abuse-deterrent properties. The objective of the current study was to ev...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-019-1565-y
更新日期:2019-12-19 00:00:00
abstract::A folic acid-conjugated paclitaxel (PTX)-doxorubicin (DOX)-loaded nanostructured lipid carrier(s) (FA-PTX-DOX NLCs) were prepared by using emulsion-evaporation method and extensively characterized for particle size, polydispersity index, zeta potential, and % entrapment efficiency which were found to be 196 ± 2.5 nm, ...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1185-y
更新日期:2018-11-01 00:00:00
abstract::The objective of the present study is to investigate the effect of hydrocarbon chain length in 1,2-alkanediols on percutaneous absorption of metronidazole (MTZ). Twelve formulations (1,2-propanediol, 1,2-butanediol, 1,2-pentanediol, 1,2-hexanediol in 4% concentration, 1,2-hexanediol, and 1,2-heptanediol in 1% concentr...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-013-0066-7
更新日期:2014-04-01 00:00:00
abstract::This study examined the mechanical (hardness, compressibility, adhesiveness, and cohesiveness) and rheological (zero-rate viscosity and thixotropy) properties of polyethylene glycol (PEG) gels that contain different ratios of Carbopol 934P (CP) and polyvinylpyrrolidone K90 (PVP). Mechanical properties were examined us...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt010324
更新日期:2000-08-17 00:00:00
abstract::Two different types of derivatives of theophylline (Th-H) incorporating ethyleneoxy groups into the promoiety have been synthesized. One is a soft alkyl type where N-methyl-N-methoxyethyleneoxycarbonylaminomethyl chlorides have been used to alkylate Th-H in the 7 position. The other is in an acyl type where methoxyeth...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-012-9803-6
更新日期:2012-09-01 00:00:00
abstract::A hydroxyethylcellulose-poly(acrylic acid) (HEC-PAA) lyomatrix was developed for ganciclovir (GCV) intestine targeting to overcome its undesirable degradation in the stomach. GCV was encapsulated within the HEC-PAA lyomatrix prepared by lyophilization. Conventional tablets were also prepared with identical GCV concent...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-015-0442-6
更新日期:2016-10-01 00:00:00
abstract::Onychomycosis is considered a stubborn nail fungal infection that does not respond to conventional topical antifungal treatments. This study aimed to develop and characterize novel solid lipid nanoparticles (SLNs) formulae containing terbinafine HCl (TFH) and loaded with different nail penetration enhancers (nPEs). Th...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-020-01893-9
更新日期:2021-01-06 00:00:00
abstract::Curcumin is a naturally occurring constituent of turmeric that is a good substitute for synthetic medicines for the treatment of different diseases, due to its comparatively safer profile. However, there are certain shortcomings that limit its use as an ideal therapeutic agent. In order to overcome these drawbacks, we...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/s12249-018-1098-9
更新日期:2018-08-01 00:00:00
abstract::The purpose of this research was to compare the viscoelastic properties of several neutral and anionic polysaccharide polymers with their mucociliary transport rates (MTR) across explants of ciliated bovine tracheal tissue to identify rheologic parameters capable of predicting the extent of reduction in mucociliary tr...
journal_title:AAPS PharmSciTech
pub_type: 杂志文章
doi:10.1208/pt0802032
更新日期:2007-04-20 00:00:00