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 targeting. PEGylated liposomes decorated with folic acid have been investigated for several anticancer agents not only to extend plasma half-life but also for tumor targeting via folic acid receptors which overexpressed on tumor cell surface. OBJECTIVE:Therefore, the objective of the present study was to prepare GEM-loaded folic acid tagged liposomes to improve the pharmacokinetics and tumor distribution of GEM. METHODS:The blank folate-targeted liposomes composed of HSPC/DSPE-mPEG2000/DSPE-mPEG-Folic acid were prepared first by thin film hydration technique. GEM was then loaded into liposomes by remote loading technique. The optimized liposomal formulations were evaluated in vitro for GEM release using dialysis technique, HeLa cell uptake using FACS technique, and cytotoxicity using MTT dye reduction assay. The comparative in vivo pharmacokinetic and biodistribution characteristics of radiolabeled (99mTc-labeled) plain GEM solution, and all liposomal formulations (conventional:CLs; stealth: SLs; folate targeted: FTLs) were evaluated in mice model. RESULTS:GEM-loaded FTLs showed sustained release profile, efficient uptake by HeLa cells and greater cytotoxicity. Further, FTLs displayed significantly improved pharmacokinetics, and biodistribution profile of loaded GEM. CONCLUSION:In conclusion, the developed GEM-loaded folic acid receptor-targeted liposomal formulation could be a promising and potential alternative formulation for further development.
journal_name
Curr Drug Delivjournal_title
Current drug deliveryauthors
Unnam S,Panduragaiah VM,Sidramappa MA,Muddana Eswara BRdoi
10.2174/1567201815666181024112252subject
Has Abstractpub_date
2019-01-01 00:00:00pages
111-122issue
2eissn
1567-2018issn
1875-5704pii
CDD-EPUB-93932journal_volume
16pub_type
杂志文章abstract::Camptothecins are a family of alkaloids originally extracted from the Chinese tree Camptotheca acuminata, Nyssaceae, exhibiting a strong activity against colorectal cancer (CRC). CRC is a common malignancy worlwide. Despite significant developments in the treatment of this disease, it still causes considerable morbidi...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720112800234558
更新日期:2012-03-01 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::Biphenyl Dimethyl Dicarboxylate (BDD) is insoluble in aqueous solution and the bioavailability after oral administration is low. Self-nanoemulsifying drug delivery system (SNEDDS) containing BDD has been successfully prepared using carefully selected ingredients which are less affected by pH and ionic strength changes...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720108784911695
更新日期:2008-07-01 00:00:00
abstract:OBJECTIVES:A ceftiofur hydrochloride long-acting oily suspension with no irritation was prepared by testing and optimizing the types and amounts of organic solvents, suspending agents, and surfactants.
Methods: Its properties, stability, injection site irritation, in vitro release, and pharmacokinetics in pigs were...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201817666200903165119
更新日期:2020-09-03 00:00:00
abstract::Selective targeting of ligand-targeted liposomes containing anticancer drugs or therapeutic genes to cell surface receptors expressed on cancer cells is a recognized strategy for improving the therapeutic effectiveness of conventional chemotherapeutics or gene therapeutics. Some recent advances in the field of ligand-...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720105774370159
更新日期:2005-10-01 00:00:00
abstract::The stratum corneum (SC) is a primary rate limiting barrier to permeation of drug molecules through the skin. Small molecular weight lipophilic drugs that are effective at low doses can be effectively delivered by passive transdermal delivery. The SC does not permit passage of polar/hydrophilic and macromolecules. Pas...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720110791011765
更新日期:2010-04-01 00:00:00
abstract:BACKGROUND:Hesperetin (HSP) is a low water-soluble flavanone aglycone with low bioavailability. OBJECTIVES:This study aimed at enhancing the hepatoprotective effects of HSP by a combinatory technique based on solid dispersions of co-crystals of HSP. METHODS:Co-crystals were prepared using citric acid, tartaric acid, ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180730141556
更新日期:2018-01-01 00:00:00
abstract::The mucosal administration of vaccines is an area currently receiving a high level of interest due to potential advantages offered by this technique. These advantages include the ability to administer vaccines without need for needles, thus improving patient compliance with vaccination schedules, and the capacity to i...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201043334588
更新日期:2004-10-01 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:BACKGROUND:The purpose of this study was to investigate Quality by Design (QbD) principle for the preparation of hydrogel products to prove both practicability and utility of executing QbD concept to hydrogel based controlled release systems. Product and process understanding will help in decreasing the variability of ...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201812666150817122506
更新日期:2016-01-01 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::Gene therapy has the potential to treat both acquired and inherited genetic diseases. Generally, two types of gene delivery vectors are used - viral vectors and non-viral vectors. Non-viral gene delivery systems have attracted significant interest (e.g. 115 gene therapies approved for clinical trials in 2018; clinical...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201816666190529072914
更新日期:2019-01-01 00:00:00
abstract:OBJECTIVE:A new tumor targeted polymer-coated gold/graphene hybrid has been developed for achieving simultaneously thermoablation and chemoterapy of folate receptor-positive cancer cells. METHODS:The gold/graphene hybrid was prepared by depositing gold nanospheres onto graphene oxide and coating it with an inulin-fola...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666160520113804
更新日期:2017-01-01 00:00:00
abstract::Gelrite is an ion-activated polymer prepared by partial acetylation of gellan gum, an exogeneous polysaccharide present in Pseudomonas elodea. Its unique cation-dependent gelling property at 33 degrees C has been exploited for the formulation of in situ gelling hydrogels for ophthalmic and oral drug delivery. Gelrite ...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720108783954905
更新日期:2008-04-01 00:00:00
abstract::A number of Polycyclic Aromatic Hydrocarbons (PAHs) have been shown to be toxicants, and induce carcinogenic and immunotoxic effects. Since PAHs are often present in low concentrations and it may be difficult to determine them in complex matrices, it is therefore essential to use powerful analytical tools to separate ...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/1567201811310010014
更新日期:2013-02-01 00:00:00
abstract::Phase-sensitive in situ gel forming controlled release formulations of cyclosporine were prepared using poly (lactide-co-glycolide) and a solvent system consisting of various proportions of benzyl benzoate and benzyl alcohol. Uniformity of content of cyclosporine in the formulation and in vitro release samples was det...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720109789941669
更新日期:2009-10-01 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:BACKGROUND:Drug design and discovery studies still remain of great importance in the search for more convenient chemotherapeutic to avoid the drug resistance, systemic toxicity or the longterm side effects. OBJECTIVE:A series of mononuclear gold (III) and platinum (II) complexes based on 4-dihydroxyboryl- DL-phenylala...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180727145724
更新日期:2018-01-01 00:00:00
abstract::The most common feature for antigen-delivery systems is their particulate nature. Together with a certain depot effect, it is the particulate nature that primarily dictates whether the antigen-delivery system will be successful in inducing a certain type and strength of immune response. In this article, we will summar...
journal_title:Current drug delivery
pub_type: 杂志文章,评审
doi:10.2174/156720106778559029
更新日期:2006-10-01 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::The aim of this study was to design a silica-supported solid dispersion of lacidipine (LCDP) to enhance the dissolution rate and oral absorption using supercritical CO2 (scCO2) as a solvent. The formulation was characterized using differential scanning calorimetry, powder X-ray diffraction, scanning electron microscop...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666151203233232
更新日期:2016-01-01 00:00:00
abstract::The objective of present investigation was the characterization of chitosan films after in vivo implantation. Chitosan films were prepared at three dose loadings of paclitaxel by classical casting method. They were implanted subcutaneously in Swiss mice in the neck region and were removed at 7, 15, 21 and 30 days post...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720106777731028
更新日期:2006-07-01 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::Relief of chronic pain is an important clinical problem requiring special care and approaches. The present study was designed for the construction of a controlled release system for local application of analgesics (hydromorphone (HM), morphine (M), and codeine (C)) and a local anesthetic, bupivacaine (BP). An interpen...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201043480081
更新日期:2004-01-01 00:00:00
abstract::Metformin (MTF) improves hyperglycemia primarily by suppressing glucose production by the liver. The objective of our investigation was to evaluate nanoemulsion as a promising carrier for MTF for sustained hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion, which finally improved biopharmace...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/156720181102140411160817
更新日期:2014-01-01 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:BACKGROUND:One of the major abundant proteins in the nucleous is nucleolin that overexpressed on the cytoplasmic membrane of malignant and endothelial cells and makes it as a promising condidate for targeted drug delivery. OBJECTIVES:In this study, doxorubicin (Dox) as a chemotherapy drug was entrapped into the Poly l...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201815666180724104451
更新日期:2018-01-01 00:00:00
abstract::The development of oral insulin using the eligen technology represents a significant advance in insulin administration which is expected to improve the quality of life of diabetic patients. As clinical studies progress, a great deal of interest has focused on the process by which this technology enables insulin absorp...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201053586001
更新日期:2005-04-01 00:00:00
abstract::The objective of the present research is to prepare stable nano suspensions of Valsartan (VAL) with high solubility and dissolution. VAL is an orally administered anti-hypertensive drug with lower bio-availability of 25%, this is attributed to its lower aqueous solubility (0.082 mg/ml). VAL nano suspensions were prepa...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201812666150724094358
更新日期:2016-01-01 00:00:00
abstract::The low bioavailability and consequently the poor therapeutic response of traditional ophthalmic formulations is caused by reduced pre-corneal residence time of the formulation in contact with the ocular surface. The use of colloidal carrier systems, namely lipid nanoparticles in combination with in situ gelling polym...
journal_title:Current drug delivery
pub_type: 杂志文章
doi:10.2174/1567201813666151111143434
更新日期:2016-01-01 00:00:00