Current Drug Delivery (Curr Drug Deliv)

Publisher: Bentham Science Publishers

Journal description

The aim of Current Drug Delivery is to publish peer-reviewed articles, short communications, short and in-depth reviews in the rapidly developing field of drug delivery. Modern drug research aims to build in delivery properties of a drug at the design phase, however in many cases this ideal cannot be met and the development of delivery systems becomes as important as the development as the drugs themselves. The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance. The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.

Current impact factor: 1.48

Impact Factor Rankings

2016 Impact Factor Available summer 2017
2014 / 2015 Impact Factor 1.478
2013 Impact Factor 2.248

Additional details

5-year impact 0.00
Cited half-life 6.20
Immediacy index 0.19
Eigenfactor 0.00
Article influence 0.00
Website Current Drug Delivery website
Other titles Current drug delivery (Online)
ISSN 1875-5704
OCLC 60333013
Material type Document, Periodical, Internet resource
Document type Internet Resource, Computer File, Journal / Magazine / Newspaper

Publisher details

Bentham Science Publishers

  • Pre-print
    • Author can archive a pre-print version
  • Post-print
    • Author cannot archive a post-print version
  • Restrictions
    • 12 months embargo
  • Conditions
    • Author's pre-print on author's personal website, institutional repository and open access repository
    • Author's post-print on author's personal website, institutional repository, open access repository, PubMed Central and arXiv
    • Non-Commercial
    • Published source must be acknowledged
    • Must link to journal homepage with DOI
    • Publisher's version/PDF cannot be used
  • Classification
    yellow

Publications in this journal

  • [Show abstract] [Hide abstract]
    ABSTRACT: In this piece of work, we have reconnoiteredthe significance of the PEGylated anticancer loaded drug onto poloxamer based thermo responsive injectable hydrogel to understand the role of delivery system. To accomplish the objective, firstly it was necessary to improve the solubility of the melphalan, achieved by PEGylation of the drug with two grades of linear methoxy poly ethylene glycol (M-PEG), viz. M-PEG 2000 and 5000 Da to form a PEGylated melphalan conjugate (MLPEG). In our previous study, we have found that the prepared conjugates were efficiently enhanced the solubility of the melphalan and significantly reduced the hemolytic effect due to the presence of the PEG chains. Thus, in the present work, the prepared conjugates (MLPEG 5000 and 2000) were loaded to the thermo sensitive Poloxamer 407 (P407) gel to produce an injectable hydrogel (MPX). To underline the reduction of the initial burst of the drug at the site of action, one of the hydrogels was prepared in the presence of the NaCl salt. This in turn, tightened the PEO chains and remarkably reduced the drug's initial burst from the delivery system as only 43 % of drug was released during 2 hours from MPX-CG hydrogel. Moreover, a lower diffusion coefficient (D) was noticed for MPX-CG gel as compared with MPX-7.4 gel. To confirm the depot formation, prepared hydrogels were administered to Wistar rats via subcutaneous and intramuscular routes. Thus, P407 based injectable hydrogel could play an important role for the delivery of a low dose-alkylating agent with reduced host cytotoxicity.
    No preview · Article · Feb 2016 · Current Drug Delivery
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    ABSTRACT: The oral bioavailability of Raloxifene hydrochloride, an FDA approved selective estrogen receptor modulator, is severely limited due to its poor aqueous solubility and extensive first pass metabolism. Present work focuses on the development of ethosomal hydrogel for transdermal delivery of RaloxifeneHCl as an alternate way to solve aforementioned problem. The physical breaching of stratum corneum, the principal barrier, by microneedle treatment was also employed to potentiate its transdermal permeation. The influence of lipid and ethanol concentration on vesicle size and entrapment efficiency was extensively investigated using response surface methodology based on central composite design. The software based optimization was done and validated using check point analysis. The optimized ethosomal batch possessed 403 nm size and 74.25 % drug entrapment. The zeta potential and in vitrodrug release of optimized batch were found favorable for transdermal permeation. The ex vivo skin permeation study revealed a transdermal flux of 4.621 μg/cm2/h through the intact pig ear skin. The permeation was further enhanced through the microporated skin (transdermal flux, 6.194 μg/cm2/h) with a 3.87 fold rise when compared to drug permeation from plain solution applied over intact skin (transdermal flux, 1.6 μg/cm2/h). Histopathological skin sections showed the non-irritant nature of the ethosomal hydrogel and microneedle treatment. The formulation was found stable under both refrigeration and room temperature conditions for 6 weeks. In a nutshell, the developed system was found efficient, safe and stable and seems promising for transdermal use.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: The goal of this study was to prepare and evaluate intravenous sustained release stealth nanoparticles encapsulating LMWH usingpoly(lactide-co-glycolide) (PLGA) and different grades of PEG (poly ethylene glycols). The nanoparticles were prepared using w/o/w solvent evaporation technique. Prepared nanoparticles were evaluated for various in vitro and in vivo parameters and stability. Scanning electron microscopy (SEM) and Transmission electron microscopy (TEM) studies confirmed the formation of smooth spherical particles. FTIR study reveals successful coating of PEG on the nanoparticles. DSC and XRD results demonstrated that drug changed its physical form in the formulation. The encapsulation efficiency was 63-74%. In vitro drug release was 57-75% for 48 hrs. Macrophage uptake of LMWH with Pegylated nanoparticles was less compared to conventional PLGA nanoparticles. In vivo drug release was sustained for 48hrs; Optimized formulation exhibited good enhancement in pharmacokinetic parameters when compared to free drug solution. In vivo sustained release was also demonstrated with antithrombotic activity as well aPTT activity. Optimized formulation demonstrated significant stability, excellent antithrombotic activity in venous thrombosis rat model, improved aPTT levels when compared to free drug solution.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: The present study discloses the preparation of core shell nanoparticles, with gold nanoparticles (AuNPs) as the core and nevirapine (NVP) loaded in glycerylmonostearate (GMS) as the shell by 'Double Emulsion Solvent Evaporation' technique. Glycerylmonostearate-nevirapine-gold nanoparticles (GMS-NVP-AuNPs) revealed high entrapment efficiency (> 70 %) and high loading (~ 40 %), average particle size < 250 nm and zeta potential -35.9 mv ± 1.41 and exhibited sustained release with good stability.Surfaceplasmon resonance indicated shell formation while SEM coupled EDAX confirmed the presence of Au in the core shell nanoparticles. TEM confirmed formation of spherical core shell nanoparticles. GMS-NVP-AuNPs revealed low hemolysis (< 10 %) and good serum stability up to 6 h.GMS-NVP-AuNPs exhibited rapid, high and sustained accumulation in the possible HIV reservoir organs, including the major organs of liver, spleen, lymph nodes, thymus and also remote locations of brain, ovary and bone marrow. High cell viability and enhanced uptake in PBMC's and TZM-bl cells was observed. While uptake in PBMC's proposed monocytes/macrophages enabled brain delivery. High uptake in TZM-bl cells was associated with superior anti-HIV activity. An important finding is the synergistic activity exhibited by the core shell GMS-NVP-AuNPs. So the superior anti-HIV activity in-vitro coupled with extensive localization of the nanoparticles in possible HIV reservoirs suggests great promise of the core shell GMS-NVP-AuNPs for improved therapy of HIV.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: Oral administration of medication is the first option when patient compliance is considered. However, many barriers face oral absorption of drugs that limit bioavailability in about 90% of therapeutic agents. Utilization of nanoparticulate drug delivery systems is a major strategy for increasing oral absorption. They can improve oral bioavailability through mechanisms such as protection of the drug in the GI tract, increasing cellular contact and residence time of the drug, protection of the drug from pre-systemic metabolism and efflux and increasing diffusion across the mucosal and epithelial layers. Liposomes are biocompatible carriers employed to improve oral bioavailability of drugs and in addition to the general advantages of nanocarriers for oral delivery, they offer benefits derived from their lipidic bilayer structure. They can better adhere to biomembranes, form mixed-micelle structures with bile salts to increase the solubility of poorly-soluble drugs and are suitable candidates for lymphatic uptake. They have been successful in improving oral bioavailability of a variety of compounds including peptide and proteins, hydrophilic and lipophilic drugs. Stability under GI conditions is the main concern for oral liposomes, however, promising approaches have been suggested to increase the stability of oral liposomes. These include: using appropriate lipid compositions, polymer coating, addition of stabilizing lipids to liposomal structures, preparation of double liposomes and proliposomes and some other innovative methods. The present review focuses on the role of liposomes in improving oral absorption of drugs, the problems encountered, and the types of liposomes designed to overcome these issues. Barriers to oral delivery will be discussed and examples of bioavailability enhancement upon encapsulation in various types of liposomes investigated.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: Recent studies have focused on the potential use of metal-based complexes for the treatment of cancer. However, there are some limitations of metal-based ligands for the treatment of cancer due to their toxic effects. In the present study, a novel bimetallic Cu(II) complex, [Cu2(µ-(C6H5)2CHCOO)3(bipy)2)](ClO4), has firstly been synthesized and characterized by FT-IR, and X-ray crystallography. Furthermore, Cu(II) complex-loaded solid lipid nanoparticles (SLNs) were initially prepared by hot homogenization method to overcome their toxic effects. After characterization, comparative cytotoxic and apoptotic activities of the complex and Cu(II) complex-SLNs on human breast cancer cells (MCF-7) and human umbilical vein endothelial cells (HUVEC) were determined.Cu(II) complex demonstrated considerable in vitro cytotoxic effects on MCF-7 (p<0.05) and induced apoptotic cell death (88.02 ± 3.95%) of MCF-7 cells. But, the complex has also toxic effects (69.5%) on HUVEC control cells. For this purpose, Cu(II) complex-loaded solid lipid nanoparticles (SLN) were firstly produced, with a distrubution range of 190±1.45 nm to 350±1.72 nm and zeta potentials of -27.4±1.98 mV and -18.2±1.07 mV, respectively. The scanning electron microscopy (SEM) images of SLNs were also obtained. In vitro studies have shown that Cu(II) complex-SLNs help in reducing the side effect of Cu(II) complex (29.9%) on HUVEC control cells. Therefore, metal based complex might potentially be used for cancer treatment through nanoparticle based drug delivery systems.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: Gemcitabine (GEM) is a highly hydrophil anticancer drug which extensively used in the clinic for the treatment of a range of solid tumors, including pancreatic and lung cancers. We have designed a drug delivery system based on single-walled carbon nanotubes (SWCNTs) for the anticancer drug GEM, which has limitations under biological conditions, by using polyethylene glycol (PEG) to obtain nano conjugates with high loading capacity, controlled drug release and effective cytotoxicity. Raw SWCNTs were functionalized through carboxylation, acylation, PEGylation and finally GEM conjugation via a cleavable ester bond. Different characterization techniques such as Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance spectrometer (NMR) and differential scanning calorimetry analysis (DSC) were performed to confirm the successful functionalization. Next, the influence of molecular weight (MW) of PEG on the drug loading capacity, drug release and cytotoxicity was studied. Experimental results showed that the drug loading capacity was dependent on the MW of PEG, but the drug release was independent. Also, the results revealed that the nanoconjugates with lower PEG MW caused higher cytotoxicity in A549 and MIA PaCa-2 cancer cells. Our studies indicated which of PEG MWs could be useful for this drug delivery system.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: In this study, fluorescein labeled SLN and NLC formulations were prepared for improving the dermal distribution of the hydrophilic active ingredients and for enhancing the skin penetration. To determine skin distribution of the lipid nanoparticles ex-vivo penetration/permeation experiments were performed using full thickness rat skin by means of Franz diffusion cells. Studies on the localization of fluorescence labeled nanoparticles were performed by confocal laser scanning microscopy (CLSM). Cellular uptake studies were performed on human keratinocyte cell line (HaCaT) and visualized by fluorescence microscope. Both tissue and cell uptake were also quantitatively determined by means of fluorimetric method in the skin extract or cell extract. Both imaging and quantification studies suggest that the dermal localization of the lipid nanoparticles depends on their dimensions and particle size distribution. The CLSM images clearly show that the Tripalmitin based lipid nanoparticles have higher accumulation in the skin. It is possible to overcome the stratum corneum barrier function with T-NLC05 coded lipid nanoparticle formulation. Additionally cellular uptake of this NLC formulation is time dependent.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: To assess in vivo behavior through in vitro method, the dissolution test is mostly used, both for quality control (QC) and for development purpose. In view of the fact that a dissolution test can hardly achieve two goals at the same time, the design of dissolution testing generally varies along with the development stage of drug products and therefore the selection of dissolution media may change with the goals of the dissolution test. To serve the QC purpose, a dissolution medium is designed to provide a sink condition; for development purpose, the dissolution medium is required to simulate the physiological conditions in the gastrointestinal tract as far as possible. In this review, we intended to provide an initial introduction to the various dissolution media applied for QC and formulation development purposes for poorly water soluble drugs. We focused on these methods like addition of cosolvents, surfactants and utilization of biphasic media, applied to provide sink conditions which are difficult to achieved by simple aqueous buffers for lipophilic drugs, and introduced the development of physiologically relevant media for human and animals like dog and rat in respect to of the choice of buffers, bile salts, lipids and so on. In addition, we further discussed the influence of biorelevant dissolution media on the modification of drug Biopharmaceutical Classification System (BCS) classification, especially for BCS class II drugs with low solubility and high permeability, whose solubility is relatively sensitive to the presence of bile salts and lipids.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: Coenzyme Q10, a natural yellow benzoquinone, is a vitamin-like substance commonly found in blood and inner mitochondrial and cellular membranes. It is natural antioxidant principle which plays an essential role in maintaining several biochemical pathways of body. It has exhibited many pharmacological activities in chronic heart failure, cardio faciocutaneous syndrome, diabetes mellitus, carcinomas, autoimmune disease, cataract, asthma, periodontal disease and thyroid disorders. Moreover, it has demonstrated efficacy as nutritional supplement, in addition to its relevance in cosmetics. Coenzyme Q10 is a potent molecule but its high molecular weight and low aqueous solubility hamper its use as therapeutic agent. Therefore, various novel drug delivery systems has been explored and developed to overcome these limitations. In this review, we summarize the recent works on design and development of novel drug delivery systems for CoQ10,which include liposomes, polymeric nanoparticles, polymeric micelles, solid lipid nanoparticles, nanostructured lipid carriers, self-emulsifying drug delivery systems, nanoemulsions, solid and aqueous dispersions. Further, an account of pharmaceutical studies has also been given. The successful application of this molecule in medicine, cosmetic and nutraceuticals points the way for its future development.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: Novel drug delivery system aims at spatial and temporal drug delivery leading to enhanced safety, efficacy, cost effective and patient compliant therapy. Recently, research has been focused on combining various novel methods with techniques to mimic the natural phenomenon of bio-recognition in order to develop a biocompatible and intelligent drug delivery system. One such step taken towards this direction is molecular imprinting which deals with imprinting of a template over a polymer to form molecularly imprinted polymer (MIP). Development of these polymers has opened up an array of applications like molecular trap, chromatographic separation, sensitive mass balance, drug delivery etc. MIP possesses certain inherent characteristic which makes them superior over other novel drug delivery systems and help to modulate the release of drug. Although enormous research has been done about application of MIP in drug delivery, its development is still in infancy. This paper presents the recent advances in molecular imprinting for drug delivery and a few recent techniques to develop MIP.
    No preview · Article · Jan 2016 · Current Drug Delivery
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    ABSTRACT: Development of drug resistance to anticancer drugs is an important challenge for cancer treatment. Recent studies focus on co-delivery of anticancer drugs and siRNA to overcome this challenge. Mesoporous silica nanoparticles (MSNs) are one of the promising nanoparticles that enable the delivery of drugs and siRNA simultaneously. MSNs coated with copolymer that able for co-delivery of drug and siRNA were prepared and characterized. In the present study, MSNs functionalized with polyethylenimine-polyethylene glycol (PEI-PEG) copolymer were prepared. MSNs were characterized using dynamic light scattering (DLS), Transmission Electron Microscopy (TEM) and elemental analysis. Nanoparticles were loaded with epirubicin hydrochloride (EPI) and anti B-cell lymphoma 2 (BCL-2) siRNA. The in vitro cytotoxicity and in vivo efficacy of different formulations were evaluated. Mean size of MSNs was ranged from 98 to 247 nm. EPI release from MSNs was pH-dependent. MSNs loaded with EPI and siRNA showed better in vitro cytotoxicity with 1 μg/mL EPI and 50-400 ng/mL siRNA, besides MSNs loaded with 9 mg/kg EPI and 1.2 mg/kg siRNA resulted in improved in vivo effects compared with EPI or MSNs containing EPI or siRNA alone. The results of in vitro and in vivo studies indicated the synergistic effect of EPI and anti BCL-2 siRNA. This formulation could be a promising nanoparticle for co-delivery of drug and siRNA in cancer cells.
    No preview · Article · Dec 2015 · Current Drug Delivery
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    ABSTRACT: Aim of the present study wasdevelopment and characterization of ligand anchored pH sensitive liposomes (PSL) as dry powder inhaler for thetargeted delivery of drugs in the target site i.e. lungs. Ligand anchored PSL (TPSL)was prepared by thin film hydrationfor the combined delivery of Isoniazid (INH) and Ciprofloxacin HCl (CIP HCl) using 4-aminophenyl-ɑ-D mannopyranoside (Man) as surface functionalized ligand. It was observed that size of the ligand anchored liposomes (TPSL) were slightly more than the non-ligand anchored liposomes (PSL). Drug release was studied at different pH for 24 hrs and it was observed that liposomes exhibited slow release at alkaline pH (58-64%) as compared to macrophage pH(81-87%) where it increased dramatically due to the destabilization of pH sensitive liposome (PSL). In vitro cellular uptake study showed that much higher concentration was achieved in the alveolar macrophage using ligand anchored liposomes as compared to its counterpart. In vivo study showed that maximum drug accumulation was achieved in the lung by delivering drug using ligand anchored PSL (approximately 12-13 %) as compared to conventional PSL (approximately 4-5 %). Thus, it was concluded that ligand anchored pH sensitive liposome is one of the promising system for the targeted drug therapy in pulmonary tuberculosis.
    No preview · Article · Dec 2015 · Current Drug Delivery
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    ABSTRACT: Liposomes can serve as promising carriers for targeting delivery and controlled release of anti-cancer drugs. Doxorubicin-loaded liposomes have achieved enhanced efficacy in some solid tumors due to EPR effect with prolonged circulation and reduced toxicity. In this study the effects of liposomal structure have been investigated on the loading efficiency and controlled release behavior. Liposomes with various compositions were prepared through a thin film hydration method, and extruded to large unilamellar vesicles (LUVs) with mean particle size (Z ave~ 100 nm) by high-pressure extrusion technique. Then, doxorubicin was loaded into liposomes using remote active loading strategy. The loading efficiency and drug release behavior were evaluated using various parameters such as medium pH, liposome compositions and cholesterol concentrations. Liposomes prepared with different compositions showed high levels of drug encapsulation. Drug loading efficiencies (>90%) achieved with high final drug/lipid ratio (0.18-0.2). Faster release was observed at pH 5.5 when compared to pH 7.4 for all formulations. The fastest release rate was observed for unsaturated lipid (<48hr) and the slowest release rate was observed for saturated lipids with high phase transition temperature such as 1, 2- distearoylphosphatidylcholine (DSPC) and hydrogenated soy phosphatidylcholine (HSPC) (10-18 days). The sustained release was observed for liposomal formulations containing cholesterol. In conclusion, we have demonstrated that drug release rate could be controlled by manipulating the composition of liposomal structures.
    No preview · Article · Dec 2015 · Current Drug Delivery
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    ABSTRACT: Drug delivery through liposomes offers several advantages, but still challenging to the researchers for the use of liposomes as carriers in drug delivery due to their poor physical stability, unpredictable drug encapsulation and systemic availability of the loaded drug. The present investigation was planned with an objective to prepare and evaluate Rifampicin loaded liposomes by using response surface methodology of statistical 32 factorial design and further to formulate them into pastilles for deliver through buccal route thereby to enhance systemic absorption. Rifampicin liposomes were prepared by using different ratios of soya lecithin and cholesterol by solvent Injection method. Main effects and interaction terms of the formulation variables were evaluated quantitatively using a mathematical statistical model approach showing that both independent variables have significant (P value < 0.05) effects on particle size (P value: 0.0273), percentage entrapment efficiency (P value: 0.0096), percentage drug release through dialysis membrane (P value: 0.0047) and percentage drug release through porcine buccal membrane (P value: 0.0019). The statistical factorial design of liposomal formulations fulfilled all the requirements of the target set and exhibited suitable values for the selected test parameters. Pastilles were prepared for liposomes using glycerol gelatin base and were found to be soft, smooth, uniform drug content and drug release was completed.
    No preview · Article · Dec 2015 · Current Drug Delivery
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    ABSTRACT: Insects-borne diseases constitute a public health concern. Since there is no vaccine or curative treatment for many of these diseases, individual protection is the main approaches to prevent them. Nowadays, the search for replacing synthetic molecules for insect repellents from natural sources, such as essential oils, is increasing. However, most of them present low efficiency compared to synthetic repellents. Therefore, decreasing skin permeation of synthetic repellents or yet, increasing effectiveness of natural repellents are challenges that must be overcame during the development of novel insect repellent formulations. In this context, polymer-based formulations allow entrapping active ingredients and provide release control. Encapsulation into polymeric micro/nanocapsules, cyclodextrins, polymeric micelles or hydrogels constitutes an approach to modify physicochemical properties of encapsulated molecules. Such techniques, applied in topical formulations, fabrics modification for personal protection, or food packaging have proved to be more effective in increasing repellency time and also in reducing drug dermal absorption, improving safety profiles of these products. In this work, the main synthetic and natural insect repellents are described as well as their polymeric carrier systems and their potential applications.
    No preview · Article · Dec 2015 · Current Drug Delivery
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    ABSTRACT: Particles from Gas Saturated Solution (PGSS)is an emerging method that employs supercritical carbon dioxide(scCO2,) to produce microparticles. It is suitable for encapsulating biologically active compounds including therapeutic peptides and proteins. Poly(lactide acid) (PLA) and/or poly(lactic-co-glycolic acid) (PLGA) are the most commonly used materials in PGSS due to their good processability in scCO2. Previous studies demonstrated that the properties of the microparticles can be modulated by adding polyethylene glycol (PEG) or tri-block PEGylated copolymers. In the present work, the effect of the addition of biodegradable PEGylated di-block copolymers on the physical properties and drug release performance of microparticles prepared by the PGSS technique was evaluated. mPEG5kDa-P(L)LA and mPEG5kDa-P(L)LGA with similar molecular weights were synthesized and their behaviour when exposed to supercritical CO2 was investigated. Different microparticle formulations containing a high (81%) or low (9%) percentage of the synthesized copolymers were prepared and compared in terms of particle size distribution, morphology and yield. Drug release studies were performed using bovine serum albumin (BSA) as a model protein. PEGylated copolymers showed good processability in PGSS without significant changes to the physical properties of the microparticles. However, the addition of PEG exerted a modulating effect on the microparticle drug dissolution behaviour, increasing the rate of BSA release as a function of its content in the formulation.
    No preview · Article · Dec 2015 · Current Drug Delivery
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    ABSTRACT: Background: The aim of this study was to determine the concentrations of propranolol in periocular tissues and plasma after ocular instillation of 0.5% propranolol gel-forming solution (GFS) as compared to 0.5% propranolol non-gel-forming solution (non-GFS) for potential use in the treatment of periocular capillary hemangiomas. Methods: A GFS prepared in 1% sodium alginate or a non-GFS in phosphate-buffered saline was instilled into the eyes of rabbits. At predetermined time intervals after dosing, blood was withdrawn, rabbits were euthanized, and periocular tissues were dissected. Results: Ocular instillation of the GFS resulted in higher concentrations of propranolol in the outer layers of both the upper and lower eyelids (in the range of 9.9-36.9g/g) and maintained higher levels of propranolol in these tissues for 24 h after dosing, as compared to the ocular instillation of the non-GFS (in the range of 3.4-15.1g/g). While the concentrations of propranolol in the other periocular tissues were generally similar for GFS and non-GFS at 1 h after dosing, the concentrations of propranolol in the extraocular muscles and periocular fat were higher for GFS than those for non-GFS between 424 h after dosing. Lower level of propranolol in plasma was observed at 1 h with GFS as compared with non-GFS. Conclusion: The use of the propranolol gel-forming solution can prolong drug retention on the ocular surface and increase its distribution to the outer layers of the eyelids while decreasing systemic exposure to the drug.
    No preview · Article · Dec 2015 · Current Drug Delivery
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    ABSTRACT: Formulation of nanoparticulate DNA vaccines requires the assessment of stability and integrity of the components implicated. Stability of cationic nanoparticles made of N-trimethyl chitosan and chondroitin sulfate (TMC nanoparticles) was investigated in aqueous solution and after freeze-drying by characterization of their size, polydispersity index (PDI), and zeta potential. Furthermore, the structural integrity of plasmid DNA (pDNA) on adsorption to the nanoparticle surface was investigated. Agarose gel electrophoresis showed DNA retention when applied with the nanocarrier, suggesting that pDNA adsorption on nanoparticles took place. In circular dichroism (CD) spectra, ellipticity of pDNA decreased at 280 nm and increased at 245 nm, and the maximum wavelength shifted from 275 nm to 285 nm when nanoparticles were present. Once released from the particles, the secondary structure of the plasmid was retained in its native form. pDNA release from pDNA-TMC nanoparticles was indicated by a rise in zeta potential from initially -32 mV (pDNA adsorbed to particles) to 14 mV during one hour, and to 36 mV after 24 hours. Unloaded TMC nanoparticles remained stable in suspension for 24 hours, maintaining diameters of around 200 nm, and zeta potential values of approximately 38 mV. Freeze-drying with sucrose could ensure storage for 30 days, with minimal increase in size (291 nm) and charge (62 mV). In conclusion, TMC nanoparticles may potentially be freeze-dried in the presence of sucrose to be stored for prolonged periods of time. Furthermore, pDNA was successfully adsorbed to the cationic nanoparticles and remains intact after being released.
    No preview · Article · Dec 2015 · Current Drug Delivery