Abstract:
:Formulations of ultra-deformable liposomes containing bleomycin (Bleosome) have previously been described and proposed for topical treatment of skin cancer [Lau, K.G., Chopra, S., Maitani, Y., 2003. Entrapment of bleomycin in ultra-deformable liposomes. S. T. P. Pharm. Sci. 13, 237-239]. In this study, the stability of various Bleosome formulations was characterised and a purification process was established to isolate Bleosome for testing on cultures of either human cutaneous keratinocytes (NEB-1) immortalised by human papilloma virus (HPV)-type 16, or a spontaneously immortalised human squamous cell carcinoma (SCC) from a primary tumour. Bleosome facilitated entrapment of high concentrations of active bleomycin and samples purified by gel-filtration chromatography remained stable during 7 days of storage at 4 degrees C or at room temperature. Serially-diluted samples of this purified, high-strength product, 'high dose' were applied onto keratinocyte cell cultures to elucidate Bleosome LD50 profiles. In vitro data revealed that the LD50 of bleomycin encapsulated in Bleosome was approximately three-fold higher than free bleomycin solution for SCC cells, and nearly 30 times higher for NEB-1 cells. However, Bleosome containing 30 microg/ml of active bleomycin killed more than twice as many SCC cells than NEB-1 cells. At that concentration, the potency of liposomal bleomycin on causing cell death of SCC cells was found to be similar to that of free bleomycin solution. This effect was not seen on NEB-1 cells. It seems that SCC cells were particularly susceptible to Bleosome containing high levels of bleomycin. Results from these experiments promote the development of a novel product for the topical treatment of skin cancer.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Lau KG,Hattori Y,Chopra S,O'Toole EA,Storey A,Nagai T,Maitani Ydoi
10.1016/j.ijpharm.2005.04.019keywords:
subject
Has Abstractpub_date
2005-08-26 00:00:00pages
4-12issue
1-2eissn
0378-5173issn
1873-3476pii
S0378-5173(05)00285-1journal_volume
300pub_type
杂志文章abstract::The objectives of this study were to determine the oral bioavailability of cefuroxime (C) and to evaluate the pharmacokinetic model that best describes the plasma concentration behaviour following single intravenous (IV), intraperitoneal (IP) and oral single doses. The same dose of C was administered by IV, IP and ora...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00420-8
更新日期:2000-07-20 00:00:00
abstract::Current efforts on inflammatory bowel diseases (IBD) treatment are focused on strategies for localised drug delivery at the intestinal mucosa. Despite the potential of curcumin (CC) for IBD treatment, its low solubility and stability limit its application. Thus, the design of nanocarriers that focus CC delivery at the...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119533
更新日期:2020-08-30 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::In this study, polyethylene glycol (PEG) conjugated melanin nanoparticles (MNPs) were prepared (PEG-MNPs). A model chemotherapy drug, doxorubicin (DOX), was loaded into the PEG-MNPs with varied concentrations (0.125, 0.250, 0.500 mg/mL). TEM images showed that, DOX-PEG-MNPs are spherical-shaped and 15 ± 2.2 nm in diam...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118613
更新日期:2019-10-30 00:00:00
abstract::Raman spectroscopy may be implemented through a microscope to provide fine scale axial and lateral chemical maps. The molecular structure of many drugs makes Raman spectroscopy particularly well suited to the investigation of pharmaceutical systems. Chemometric methods currently used to assess bulk Raman spectroscopic...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2010.12.030
更新日期:2011-09-30 00:00:00
abstract::Benzoyl peroxide as a monotherapeutic and in combination with adapalene is a cornerstone of current acne therapy, but its unfavourable side effect profile reduces the therapeutic value of this compound. The incorporation into an adapalene-loaded microparticulate lipid matrix, which - via the principle of targeted eros...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2019.118792
更新日期:2019-12-15 00:00:00
abstract::In the present study, a novel synthesis technique based on the flow focusing (FF) technology is investigated for the preparation of green fluorescent protein (GFP)-loaded poly(D,L-lactide-co-glycolide) (PLGA) microparticles. To our knowledge, this novel technique has never been applied to the formulation of proteins i...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2009.07.017
更新日期:2009-10-01 00:00:00
abstract::Low density porous carriers are widely used in the pharmaceutical applications. Response surface methodology, using 3(2) factorial design was used to study drug adsorption on and its release patterns from microporous polypropylene (Accurel MP 1000) in the absence of additives. Ibuprofen, as model drug, was adsorbed on...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.09.013
更新日期:2007-02-22 00:00:00
abstract::A relatively high molecular weight of 4-arm star PELA was obtained by ring-opening polymerization of l-lactic acid O-carboxyanhydride with 4-arm-PEG in the presence of DMAP as an initiator. The results via(1)H NMR and (13)C NMR show that the end of the star PELA chain is a hydroxyl group and the central core is a PEG ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.05.074
更新日期:2015-08-01 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::Indolicidin (IL), an antimicrobial peptide, was investigated as a vehicle to promote oligodeoxynucleotides (ODNs) delivery. To increase charge density, IL was dimerized by adding a cysteine to its C or N terminus, which was denoted as ILC or CIL, respectively. In contrast to IL, cytotoxicity of ILC and CIL was signifi...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.12.082
更新日期:2019-03-10 00:00:00
abstract::Ball Milling technique has been used to prepare for the first time Vitis Vinifera extract-silica nanocomposites (VV-SiO2 NCs), which combine the pharmacological effects of the extract with the effectiveness of silica as drug delivery system and active component in the treatment of wound healing. Different contents (1....
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2018.08.057
更新日期:2018-11-15 00:00:00
abstract::Comparison of single and multiple dose pharmacokinetics between patches and conventional tablets of Huperzine A (Hup-A) was performed in beagle dogs to evaluate the patches' controlled drug release characteristics in vivo, a newly developed transdermal system for treatment of Alzheimer disease. Results showed that tra...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2008.01.007
更新日期:2008-05-22 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::Establishing a method to evaluate the reliability of an optimal solution is an exciting challenge for the nonlinear response surface method. We reported previously that the bootstrap (BS) resampling technique and Kohonen's self-organizing map are promising tools for meeting this challenge. To understand the usefulness...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.06.013
更新日期:2010-08-30 00:00:00
abstract::The objective was to quantify drug loss due to cold flow (CF) in marketed estradiol transdermal drug delivery systems (TDDS), and study its influence on the in vitro flux and drug transfer across contacting skin. TDDS samples (products-A and B) were induced with CF at 25 and 32°C/60% RH by applying 1-kg force for 72h....
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.10.013
更新日期:2014-12-30 00:00:00
abstract::Niacinamide-containing moisturisers are known be efficacious in alleviating dry skin conditions and improving stratum corneum (SC) barrier function. However, the mechanisms of action of niacinamide at the molecular level in the SC are still not well understood. Previously, we have reported the development of novel met...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.ijpharm.2012.11.043
更新日期:2013-01-30 00:00:00
abstract::Calcium phosphate nanoparticles present a unique class of non-viral vectors, which can serve as efficient and alternative DNA carriers for targeted delivery of genes. In this study we report the design and synthesis of ultra-low size, highly monodispersed DNA doped calcium phosphate nanoparticles of size around 80 nm ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(02)00452-0
更新日期:2003-01-02 00:00:00
abstract::The blending process is a key step in the production of dry powder inhaler formulations, but only little is known about the influence of process parameters. This is especially true for high shear blending of ternary formulations. For this reason, this study aims to investigate the influence of high shear mixing proces...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2017.10.033
更新日期:2017-12-20 00:00:00
abstract::Electrospun nanofibers are being utilized for a wide range of healthcare applications. A plethora of natural and synthetic polymers are exploited for their ability to be electrospun and replace the complex habitat provided by the extracellular matrix for the cells. The fabrication of nanofibers can be tuned to act as ...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章,评审
doi:10.1016/j.ijpharm.2017.03.013
更新日期:2017-05-15 00:00:00
abstract::Poor mechanical properties of crystalline drug particles require wet granulation technique for tablet production which is uneconomical, laborious, and tedious. The present investigation was aimed to improve flow and mechanical properties of racecadotril (RCD), a poorly water soluble antidiarrheal agent, by a crystallo...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2013.04.073
更新日期:2013-08-16 00:00:00
abstract::As a new oral drug delivery system for colon targeting, enteric coated timed-release press-coated tablets (ETP tablets) were developed by coating enteric polymer on timed-release press-coated tablets composed of an outer shell of hydroxypropylcellulose and core tablet containing diltiazem hydrochloride (DIL) as a mode...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(00)00454-3
更新日期:2000-08-25 00:00:00
abstract::The purpose of this study was to develop solid dispersions of fenretinide(4HPR), incorporate them into poly(lactic-co-glycolic)(PLGA) millicylindrical implants, and evaluate the resulting implants in vitro and in vivo for future applications in oral cancer chemoprevention. Due to the extreme hydrophobicity of 4HPR, 4H...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2020.119475
更新日期:2020-08-30 00:00:00
abstract::Dosage forms with fixed dose combinations of drugs is a frequent and advantageous mode of administration, but their production involves a number of technological problems. Numerous interactions in a homogeneous vehicle may be avoided through the use of layered tablets. The mechanical properties of these dosage forms d...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2015.10.061
更新日期:2015-12-30 00:00:00
abstract::The purpose of this study was to determine quantitatively the amorphous fraction in crystalline-amorphous powder mixtures of trehalose, in order to assess the ability of the (13)C NMR technique for quantitative amorphous characterization. The NMR method is described in detail and its accuracy is compared to that of th...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2004.05.012
更新日期:2004-08-06 00:00:00
abstract::Microemulsions show significant promise for enhancing the oral bioavailability of biopharmaceutics classification system (BCS) class II drugs, but how about class III drugs remains unclear. Here we employed metformin hydrochloride (MET) as the model drug and prepared drug-loaded water-in-oil (W/O) microemulsions selec...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2014.07.011
更新日期:2014-10-01 00:00:00
abstract::The mechanical properties of a drug tablet can affect its performance (e.g., dissolution profile and its physical robustness. An ultrasonic system for real-time in-die tablet mechanical property monitoring during compaction has been demonstrated. The reported set-up is a proof of concept compaction monitoring system w...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2012.09.014
更新日期:2013-02-14 00:00:00
abstract::The focus of present investigation was to assess the utility of non-destructive techniques in the evaluation of risperidone solid dispersions (SD) with methyl-β-cyclodextrin (MBCD) and subsequent incorporation of the SD into orally disintegrating tablets (ODT) for a faster release of risperidone. The SD was prepared b...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2010.08.025
更新日期:2010-11-15 00:00:00
abstract::The purpose of this study was to construct microemulsion-base hydrogel formulation for topical delivery of ibuprofen. Ethyl oleate (EO) was screened as the oil phase of microemulsions, due to a good solubilizing capacity of the microemulison systems and excellent skin permeation rate of ibuprofen. The pseudo-ternary p...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/j.ijpharm.2006.02.015
更新日期:2006-06-06 00:00:00
abstract::The purpose of this study was to determine the plasma concentrations of selected NSAIDs after topical gel administration and to determine the influence of the physicochemical characteristics of these drugs on transdermal absorption. Plasma concentrations of the drugs were determined using high performance liquid chrom...
journal_title:International journal of pharmaceutics
pub_type: 杂志文章
doi:10.1016/s0378-5173(99)00340-3
更新日期:2000-01-05 00:00:00