Abstract：
:Targeting of drug delivery systems (DDSs) to specific intracellular organelles (i.e., subcellular targeting) has been investigated in numerous publications, but targeting efficiency of these systems is seldom reported. We searched scientific publications in the subcellular DDS targeting field and analyzed targeting efficiency and major formulation parameters that affect it. We identified 77 scientific publications that matched the search criteria. In the majority of these studies nanoparticle-based DDSs were applied, while liposomes, quantum dots and conjugates were used less frequently. The nucleus was the most common intracellular target, followed by mitochondrion, endoplasmic reticulum and Golgi apparatus. In 65% of the publications, DDSs surface was decorated with specific targeting residues, but the efficiency of this surface decoration was not analyzed in predominant majority of the studies. Moreover, only 23% of the analyzed publications contained quantitative data on DDSs subcellular targeting efficiency, while the majority of publications reported qualitative results only. From the analysis of publications in the subcellular targeting field, it appears that insufficient efforts are devoted to quantitative analysis of the major formulation parameters and of the DDSs' intracellular fate. Based on these findings, we provide recommendations for future studies in the field of organelle-specific drug delivery and targeting.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Maity AR,Stepensky Ddoi
10.1016/j.ijpharm.2015.10.053subject
Has Abstractpub_date
2015-12-30 00:00:00pages
268-74issue
2eissn
0378-5173issn
1873-3476pii
S0378-5173(15)30321-5journal_volume
496pub_type
杂志文章,评审abstract：:Insulin replacement therapy is integral to the management of type 1 diabetes, which is characterised by absolute insulin deficiency. Optimal glycaemic control, as assessed by glycated haemoglobin, and avoidance of hyper- and hypoglycaemic excursions have been shown to prevent diabetes-related complications. Insulin pu...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2017.12.022
更新日期：2018-06-15 00:00:00
abstract：:Hydrotalcite (HT), also known as a layered double hydroxide (LDH) compound, has been widely used in past years in the formulation of drugs due to its specific properties including good biocompatibility, null toxicity, high chemical stability and pH-dependent solubility which aid in drug controlled release. In this wor...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.04.048
更新日期：2016-06-15 00:00:00
abstract：:Topical preparations of capsaicin, the major pungent ingredient of hot pepper, are being used for management of pain and inflammatory disorders. Purpose of this study was to use nanoemulsion as an effective topical drug carrier for in vivo delivery of capsaicin. An oil-in-water nanoemulsion containing capsaicin was pr...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2019.01.043
更新日期：2019-03-25 00:00:00
abstract：:The PEGylated liposomal (PEG-LP) Doxorubicin, PEG-LP (DOX), with a diameter of around 100nm, accumulates in tumors via the enhanced permeability and retention (EPR) effect, and is used clinically for the treatment of several types of cancer. However, there are a number of tumor types that are resistant to DOX. We repo...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.05.047
更新日期：2016-07-25 00:00:00
abstract：:HN-1, a 12-amino acid peptide, has been reported to possess strong capabilities for targeting and penetrating head and neck squamous cell carcinoma. Here, we designed a simple but effective nanoparticle system for the delivery of doxorubicin (DOX) targeting oral squamous cell carcinoma (OSCC) through the mediation of ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.04.027
更新日期：2017-06-15 00:00:00
abstract：:The purpose of this study was to develop a nanosuspension of a poorly soluble drug by nanomilling process using wet media milling to achieve superior in vitro dissolution and high in vivo exposure in pharmacokinetic studies. A promising nanosuspension was developed with Vitamin E TPGS based formulation with particle s...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2011.02.051
更新日期：2011-05-16 00:00:00
abstract：:The aim of this work was to investigate chitosomes, i.e. liposomes coated by a polyelectrolyte complex between chitosan (CH) and xantan gum (XG), as potential delivery system for oral administration of the protein C-phycocyanin. To this purpose several CH-XG-microcomplexes were prepared in aqueous lactic acid at diffe...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2010.03.038
更新日期：2010-06-15 00:00:00
abstract：:In this work calcium stearate (CaSt) multi-particulates loaded with codeine phosphate (COP) were developed in an attempt to provide extended release (ER) combined with alcohol dose dumping (ADD) resistance. The pellets were prepared via wet/extrusion spheronization and ER characteristics were obtained after fluid bed ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.05.049
更新日期：2016-07-25 00:00:00
abstract：:Liquid dosage forms, generally based on aqueous solutions, take an important role in drug administration. The approaches to a theoretical description of solvent and solubility properties have not yet proved completely satisfying. In this work, the Debye equation, which describes well polar and nonpolar molecules in an...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/s0378-5173(01)00771-2
更新日期：2001-08-28 00:00:00
abstract：:The thermal properties of two polymorphs (A and C) of a Merck development compound were studied using high-speed differential scanning calorimetry (Hyper-DSC). The utility of this novel technique as a fast analytical tool for studying the polymorphic behaviour of metastable polymorphs has previously been demonstrated ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.08.015
更新日期：2008-02-28 00:00:00
abstract：:The absorption mechanisms of drugs play an important role on development and various application of drugs. However, the present methods of absorption mechanisms are not perfect enough. Hence, exploring a novel method to accurately predict the absorption mechanisms is necessary. In this study, we developed an Ussing mo...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2020.119170
更新日期：2020-04-15 00:00:00
abstract：:This study reports on the immunogenicity assessment of a novel chimeric peptide vaccine including Tax, gp21, gp46, and gag immunodominant epitopes of human T-cell lymphotropic virus type 1 (HTLV-1) to induce immunity against HTLV-1 after subcutaneous (SC) or intranasal administration in a mice model. Additionally, to ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.07.069
更新日期：2018-10-05 00:00:00
abstract：:In vitro and in vivo investigations were conducted to develop a suitable formulation for early toxicology and clinical studies of ((R)-7-(3,4-dichlorophenyl)-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(4-fluorophenyl)pyrrolidin-1-yl)methanone (Compound A), a nonionizable and poorly water-soluble compound...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2012.04.075
更新日期：2012-08-20 00:00:00
abstract：:In this study, a temperature and ROS-responsive drug delivery system ROSP@MSN based on mesoporous silica nanoparticles has been designed and synthesized by taking advantage of 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzyl acrylate modified polymers (ROSP) as "nano-valve", which can respond selectively to cance...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.11.025
更新日期：2018-01-30 00:00:00
abstract：:In this short note we report on the shelf-life stability of pDERMATT (plasmid DNA encoding recombinant MART-1 and tetanus toxin fragment-c) 2mg lyophilized powder for reconstitution for intradermal administration, used in an in-house, investigator-initiated clinical phase I study. pDERMATT was stored at 25°C/60% relat...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2013.06.010
更新日期：2013-09-10 00:00:00
abstract：:The objective of this study was to develop a novel fenofibric acid-loaded controlled release pellet showing enhanced, or equivalent to, bioavailability compared with two commercially available products containing fenofibrate or choline fenofibrate. The effect of solubilizing agents on drug solubility and the impact of...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.05.059
更新日期：2015-07-25 00:00:00
abstract：:Here we explore the opportunity to design and then produce tailored release of therapeutic drugs from microcapsules. By use of "building blocks," formed from well characterized microcapsule populations, an inverse design algorithm has been developed that provides an optimal (in a least squares sense) combination of bu...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2009.09.010
更新日期：2010-01-04 00:00:00
abstract：:Ciclopirox olamine (CPO) metal complexes have been prepared and characterized using elemental analysis, infra red (IR), melting point and differential scanning calorimetry (DSC). Spectroscopic titration using molar ratio method indicated the occurrence of 1:1 complexes for CPO with almost all the examined metals. Phys...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2004.11.009
更新日期：2005-01-31 00:00:00
abstract：:Composite dispersions of chitosan (CS), a positively charged polymer, and magnesium aluminum silicate (MAS), a negatively charged clay, were prepared and rheology, flocculate size and zeta potential of the CS-MAS dispersions were investigated. High and low molecular weights of CS (HCS and LCS, respectively) were used ...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2007.09.038
更新日期：2008-03-03 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：:Polyamine content, which is associated with tumor growth, can be regulated by ornithine decarboxylase (ODC) and S-adenosyl methionine decarboxylase (SAMDC), two key enzymes in polyamine biosynthesis. Here we aim to develop a pH-responsive cationic poly(agmatine) based on a polyamine analogue-agmatine that can dually f...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.04.039
更新日期：2016-06-15 00:00:00
abstract：:The objective of the present study was to synthesize and investigate the transgene expression efficacy of quaternized derivatives of aminoglycoside polymers in different cancer cell lines. A series of glycidyltrimethylammonium chloride (GTMAC) derivatives of aminoglycoside polymers (GTMAC-AM polymers), containing vary...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.04.026
更新日期：2015-07-15 00:00:00
abstract：:Polysaccharide-coated liposomes have been studied for their potential use for peptide drug delivery by the oral route because they are able to minimize the disruptive influences on peptide drugs of gastrointestinal fluids. The aim of this work was to synthesize and characterize a modified polysaccharide, O-palmitoylsc...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.06.040
更新日期：2006-11-15 00:00:00
abstract：:Curcumin (CUR) has been formulated into a host of nano-sized formulations in a bid to improve its in vivo solubility, stability and bioavailability. The aim of this study was to investigate whether the encapsulation of CUR in nanocarriers would impede its biological interactivity, specifically its potential anti-cance...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2015.08.066
更新日期：2015-11-10 00:00:00
abstract：:This study explored the transition of lamellar-type liquid crystal (LLC) to biocompatible oil-in-water nanoemulsions able to modify benznidazole (BNZ) release and target the drug to cells infected with the T. cruzi parasite. Three cosolvents (2methylpyrrolidone [NMP], polyethylene glycol [POL], and propylene glycol [P...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2018.11.041
更新日期：2019-01-30 00:00:00
abstract：:The purpose of this study is designing non-viral gene delivery vectors for transfection of the primary human retinal pigment epithelial cells (RPE). In the design process of gene delivery vectors, considering physicochemical properties of vectors alone does not seem to be enough since they interact with constituents o...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2016.12.048
更新日期：2017-02-25 00:00:00
abstract：:Pharmacopoeias prescribe tests to determine the levels of arsenic in raw materials and glass containers. In this study, glass ampoules for injectables containing individually the main components of intravenous nutrition formulations were submitted to the hydrolytic resistance test by heating at 121 degrees C for 30 mi...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2006.02.008
更新日期：2006-06-06 00:00:00
abstract：:Cell replacement therapy is a widely discussed novel concept of medical treatment. The increased knowledge in the stem cell field, particularly pluripotent stem cells, potentially provides powerful tools for this therapeutic concept. A large number of disease characterized by the loss of functional cells are potential...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/j.ijpharm.2009.03.003
更新日期：2009-11-03 00:00:00
abstract：:There has been limited research done on the downstream processing of nanosuspensions into solid oral dosage forms. This paper demonstrates the bead layering process with a layering level at 150% and 240%, as well as the selection and justification of the outer phase excipients for tabletability and disintegrating prop...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章
doi：10.1016/j.ijpharm.2017.08.107
更新日期：2017-10-30 00:00:00
abstract：:In the 1990s chitosan turned out to be a useful excipient in various pharmaceutical formulations. By modifications of the primary amino group at the 2-position of this poly(beta1-->4 D-glucosamine), the features of chitosan can even be optimised according to a given task in drug delivery systems. For peroral peptide d...
journal_title：International journal of pharmaceutics
pub_type： 杂志文章,评审
doi：10.1016/s0378-5173(99)00365-8
更新日期：2000-01-20 00:00:00
