Abstract:
:Alternative formulations of paclitaxel were developed in order to improve its aqueous solubility, and characterized in vitro. A methacrylic acid based nanoconjugate of paclitaxel was synthesized by a simple esterification reaction with molecular weight of 1657 Da. The in vitro hydrolysis study on the prodrug of paclitaxel in presence of rat plasma has shown that the ester bond was quite stable (less than 1% of paclitaxel was liberated from prodrug in 24 h). This water-soluble prodrug was encapsulated into polyethylene glycol coated liposomes optimized with saturated lipids, to overcome the physical instability associated with paclitaxel. Under in vitro testing, prodrug liposomes seem very impressive with release of only 45% of payload in 180 h. Further, chemical as well as physical stability studies have shown that liposomes were stable without any signs of crystallization of paclitaxel. In addition, paclitaxel was covalently coupled to poloxamer via methacrylic acid linker to obtain a micelle forming conjugate. Evidence for self-assembly of this conjugate into micelles was provided by fluorescence spectroscopy, light scattering and differential scanning calorimetry techniques. Micellization of the conjugate was thermodynamically favored and the core of resulting micelles exhibited higher microviscosities (than poloxamer micelles). Release studies using dialysis technique along with high performance liquid chromatography revealed that paclitaxel is liberated from micelle in the form of methacrylic acid oligomer based prodrug in a gradual manner. These preliminary studies provided indication on the performance and feasibility of testing these carrier systems as a safer alternative to the Cremophor EL based paclitaxel formulation.
journal_name
Curr Drug Delivjournal_title
Current drug deliveryauthors
Dhanikula AB,Panchagnula Rdoi
10.2174/1567201052772861keywords:
subject
Has Abstractpub_date
2005-01-01 00:00:00pages
75-91issue
1eissn
1567-2018issn
1875-5704journal_volume
2pub_type
杂志文章abstract:BACKGROUND:The management of TB is difficult due to the resistance developed by Mycobacterium tuberculosis against anti-tubercular drugs causes the new challenges for treating and managing the disease. OBJECTIVE:The objective of the study was to combat multiple drug resistance (MDR) exhibited by mycobacterium species ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160502124811
更新日期:2016-01-01 00:00:00
abstract::A palpable need for the optimization of therapeutic agents, due to challenges tackled by them such as poor pharmacokinetics and chemoresistance, has steered the journey towards novel interdisciplinary scientific field for emergence of nanostructure materials as a carrier for targeted delivery of therapeutic agents. Am...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201812666141229104304
更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:PnPP-19 is a 19-amino-acid synthetic peptide previously described as a novel drug for the treatment of erectile dysfunction. OBJECTIVE:The aim of this work was to evaluate the physicochemical properties of cationic transfersomes containing PnPP-19 and the skin permeation of free PnPP-19 and PnPP-19-loaded t...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180108170206
更新日期:2018-01-01 00:00:00
abstract::Fast-dissolving drug delivery systems have been developed as an alternative to conventional dosage form as an oral means of drug delivery in case of chronic conditions. Now a day's fast dissolving films are preferred over conventional tablets and capsules for masking the taste of bitter drugs to increase the patient c...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720111795768022
更新日期:2011-07-01 00:00:00
abstract:AIM:The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. BACKGROUND:Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been rep...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200902150646
更新日期:2020-09-02 00:00:00
abstract::The placenta has traditionally been considered as a highly permeable organ for a large variety of substances with diverse molecular structures that are readily able to cross it from the maternal blood to reach the foetus. This has recommended limiting the use of drugs during pregnancy as far as possible. However, our ...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201043334731
更新日期:2004-07-01 00:00:00
abstract::Polar lipids and various surfactants exhibit rich phase behavior depending on the composition of the lipids and the physicochemical conditions. Lamellar (L(alpha)), hexagonal (Inverted [H(II)]) and normal or inverted cubic (bicontinuous or micellar) structures are some of the most common lyotropic liquid crystalline p...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720110790396526
更新日期:2010-01-01 00:00:00
abstract::The research presented in this paper discusses the potential of iontophoresis facilitated transdermal delivery of glycine. Iontophoresis has been widely investigated as a noninvasive transdermal drug delivery system. Iontophoresis is the use of a low electric current to carry ionized as well as unionized drug molecule...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720109787846207
更新日期:2009-04-01 00:00:00
abstract:BACKGROUND:Nasal delivery of 20 (R) -ginsenoside Rg3 (Rg3) has a short-lived anti-fatigue effect owing to rapid clearance by nasal cilia. Thus, in order to extend the residence time of Rg3 in the nasal cavity, a new drug delivery system is needed. METHODS:Chitosan microspheres loaded with Rg3 were prepared using a mul...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201814666161109121151
更新日期:2017-09-06 00:00:00
abstract:PURPOSE:To develop and evaluate the suitability of lecithin organogels containing aceclofenac for topical application and compare its In vitro and In vivo effects with conventionally used hydrogels. METHODS:The components and their concentration necessary for organogels formation were evaluated using phase diagram. So...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720109787048320
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:Bupivacaine is the most used local anesthetic in surgical procedures, producing prolonged anesthesia. The major limiting factor for the clinical use of bupivacaine comes from its systemic toxicity. Nanostructured lipid carriers (NLC) are vehicles for sustained drug delivery that are able to minimize the toxi...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201814666170726101113
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Cystic Fibrosis (CF) is a genetic disease which affects the patient's lungs, pancreas, liver, kidney and intestine and lacks sulfatase enzyme, leading to mucopolysaccharidosis. Colistin sulfate acts by interacting with phospholipids of bacterial cell membranes. Sulfatase enzyme reduces the high levels of sul...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200122160110
更新日期:2020-01-01 00:00:00
abstract:OBJECTIVES:This study aimed to develop and evaluate chitosan (CTS) solid dispersion particulate matrix (SDPM) for sustained oral delivery of ketorolac tromethamine (KT). METHODS:SDPM formulations were prepared by freeze drying method and characterized for their effectiveness and biological activities via in vitro and ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201812666151012114006
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Transdermal route of delivery of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) has several advantages over other routes like reduced adverse effects, less systemic absorption, and avoidance of first-pass effect and degradation in the gastrointestinal tract (GIT). Transdermal route is also beneficial for dru...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201815666180605114131
更新日期:2018-01-01 00:00:00
abstract::The present study performed by preparation and evaluation of floating tablets of Acyclovir as model drug for prolongation of gastric residence time. Floating effervescent tablets were formulated by various materials like hydroxypropyl methylcellulose K 4M, K 15M, psyllium husk, swelling agent as crospovidone and micro...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720109789941678
更新日期:2009-10-01 00:00:00
abstract:AIM:This study aimed to investigate the influence of the preparation process and composition on the microstructure of the O/W primary emulsions and the corresponding impact on the formation of oil-in-water-in-oil (O/W/O) multiple emulsions. OBJECTIVES:Multiple emulsions were prepared by a two-step emulsification metho...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201818666210101114517
更新日期:2020-12-31 00:00:00
abstract::The aim of this work is to study liposomes as carriers of nutrients and therapeutic agents in aquaculture with Venerupis decussatus and Venerupis pullastra larvae. Multilamellar (MLVs) and large unilamellar (LUVs) vesicles were prepared from a commercial mixture of soy phosphatidylcholine, rich in unsaturated and poly...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201043479957
更新日期:2004-04-01 00:00:00
abstract::Since its discovery in 1796 by Edward Jenner, vaccines have been an integral aspect of therapeutics, combating a number of infectious diseases with remarkable success. In recent years, due to rapid advances in proteomics, genomics, biotechnology and immunology and the plethora of knowledge amassed in related fields, i...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720106776359249
更新日期:2006-04-01 00:00:00
abstract::Since the discovery of Helicobacter pylori (H. pylori) in the early 1980s, its eradication has been one of the most important global challenges in gastroenterology. Various circumstances make the treatment with antimicrobials particularly difficult. One problem has been that antibiotics commonly used were designed for...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201811666140327145049
更新日期:2014-01-01 00:00:00
abstract:BACKGROUND:Triple negative breast cancer (TNBC) is an aggressive disease associated with poor prognosis and lack of validated targeted therapy. Thus chemotherapy is a main adjuvant treatment for TNBC patients, but it associates with severe toxicities. For a better treatment outcome, we developed an alternative therapeu...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201814666170712122508
更新日期:2018-01-01 00:00:00
abstract:BACKGROUND:Gemcitabine (GEM) is found effective in the treatment of many solid tumors. However, its use is restricted due to its small circulation half-life, fast metabolism and low capacity for selective tumor uptake. Folate receptors (FRs) have been recognized as cellular surface markers, which can be used for cancer...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666181024112252
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Alzheimer's disease is a chronic progressive neurodegenerative disorder associated with depletion of acetylcholine. Oral treatment with tacrine hydrochloride; a reversible inhibitor of acetylcholinesterase, finds limited use in Alzheimer's disease due to frequent dosing, hepatotoxicity and extensive pre-syst...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201816666191022105036
更新日期:2019-01-01 00:00:00
abstract::Paclitaxel (taxol, 1a) and docetaxel (taxotere, 1b) have established themselves as an important class of antitumor drugs currently available to the oncologist. While the great contribution of these drugs to the management of the disease and their effect on the improvement of the patient quality of life could not be ov...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720108783331005
更新日期:2008-01-01 00:00:00
abstract::Methylene blue (MB) has been shown to slow down the progression of the Alzheimer's disease (AD) and other tauopathies; however distribution of MB into the brain is limited due its high hydrophilicity. In this study, we aimed to prepare novel hydrophobic glutathione coated PLGA nanoparticles to improve bioavailability ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201810666131113102037
更新日期:2014-01-01 00:00:00
abstract::ADMET Chemoinformatics multi-output models are useful for a parallel prediction of multiple experimental parameters related the absorption (A), distribution (D), metabolism (M), excretion (E), and toxicity (T) process of drugs, pollutants, and NPs with a single QSPR model. Here we present one state-of-art review about...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:
更新日期:2016-04-19 00:00:00
abstract:BACKGROUND:Amphotericin B eye drops are widely used in the treatment of ocular infections. However, amphotericin's toxicity leads to low patient compliance and aggravation of symptoms. This work describes the development of a microemulsion system containing amphotericin B, aiming for its use in ocular applications. ME...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1570159x14666151109110734
更新日期:2016-01-01 00:00:00
abstract::Previous studies suggested that caspofungin dose escalation against Candida species is more beneficial than currently used lower daily doses. Thus, we determined in vitro and in vivo activity of caspofungin against six wild-type C. albicans clinical isolates, the ATCC 10231 strain and an echinocandin resistant strain....
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201812666150623091336
更新日期:2016-01-01 00:00:00
abstract::There are still so-called unmet needs in the treatment of epithelial and cutaneous lesions. Mucositis, ocular lesions, chronic skin wounds represent typical examples. These pathologies do not yet afford a satisfactory treatment. In particular chronic wounds represent a major health care burden, likely to increase as t...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201811310010005
更新日期:2013-02-01 00:00:00
abstract::The aim of the present study was to formulate a combined patch containing salicylic (SA) acid and nicotinamide (NA), useful for the treatment of mild acne, and to verify their mutual effect on drug permeation and skin retention. The performance of the patch was tested in vitro in permeation experiments using pig ear s...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720110793566218
更新日期:2010-12-01 00:00:00
abstract:OBJECTIVE:An injectable long acting In-Situ Forming Gel (ISFG) of human Growth Hormone (hGH) was prepared by using triblock PCL-PEG-PCL (Mw 1500-1500-1500). Ring-Opening Polymerization (ROP) of triblock using microwave was applied. METHODS:The BCA protein assay Kit was used to determine the concentration of hGH in the...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200120120105
更新日期:2020-01-01 00:00:00