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AKT2 siRNA delivery with amphiphilic-based polymeric micelles show efficacy against cancer stem cells.
Authors: Rafael D, Gener P, Andrade F, Seras-Franzoso J, Montero S, Fernández Y, Hidalgo M, Arango D, Sayós J, Florindo HF, Abasolo I, Schwartz S, Videira M Abstract Development of RNA interference-based therapies with appropriate therapeutic window remains a challenge for advanced cancers. Because cancer stem cells (CSC) are responsible of sustaining the metastatic spread of the disease to distal organs and the progressive gain of resistance of advanced cancers, new anticancer therapies should be validated specifically for this subpopulation of cells. A new amphihilic-based gene delivery system that ...
Source: Drug Delivery - April 20, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

The mechanism of lauric acid-modified protein nanocapsules escape from intercellular trafficking vesicles and its implication for drug delivery.
In conclusion, the protein nanocapsules modified with LA could enhance the protein nanocapsules escape from intercellular trafficking vesicles, and protect the protein from degradation by the lysosomes. PMID: 29667445 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - April 20, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Intra-articular injection of kartogenin-conjugated polyurethane nanoparticles attenuates the progression of osteoarthritis.
In conclusion, IA injection of PN-KGN is a better potential strategy to treat OA, with long-time cartilage protection and less IA injections. PMID: 29667446 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - April 20, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Retro-inverso follicle-stimulating hormone peptide-mediated polyethylenimine complexes for targeted ovarian cancer gene therapy.
CONCLUSIONS: D-FP21-PEG-PEI/plasmid DNA is a safe and efficient gene delivery vehicle for ovarian cancer targeted therapy. PMID: 29667478 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - April 20, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Cell penetrating peptides: a comparative transport analysis for 474 sequence motifs.
Authors: Ramaker K, Henkel M, Krause T, Röckendorf N, Frey A Abstract Delivering reagents into cells is a key demand in molecular medicine. The vehicle of choice is often cell penetrating peptides (CPPs), which can ferry conjugated cargo across membranes. Although numerous peptides have been shown to promote such uptake events, there has been no comprehensive comparison of individual performance under standardized conditions. We have devised a method to rapidly analyze the ability of a multitude of CPP conjugates to carry a model cargo into HeLa cells. Sequence information for 474 CPPs was collected from liter...
Source: Drug Delivery - April 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Preparation of poly-l-lysine-based nanoparticles with pH-sensitive release of curcumin for targeted imaging and therapy of liver cancer in vitro and in vivo.
Authors: Yang DH, Kim HJ, Park K, Kim JK, Chun HJ Abstract Poly-l-lysine (PLL) nanoparticle (NP) system was prepared for the controlled release of curcumin (CUR) by pH stimuli, and its theranostic efficacy on cancer was compared to that of CUR solution in vitro and in vivo. Deoxycholic acid (DOCA), methoxy polyethylene glycol (MPEG) and cyanine 5.5 (cy5.5) were conjugated to the amine group of PLL through condensation reaction (PLL-DOCA-MPEG-cy5.5), followed by encapsulation of CUR by dialysis method (PLL-DOCA-MPEG-cy5.5/CUR NPs). The composition, morphology and size distribution of PLL-DOCA-MPEG-cy5.5 NPs were cha...
Source: Drug Delivery - April 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Fabrication of a drug delivery system that enhances antifungal drug corneal penetration.
Authors: Li J, Li Z, Liang Z, Han L, Feng H, He S, Zhang J Abstract Fungal keratitis (FK) remains a severe eye disease, and effective therapies are limited by drug shortages and critical ocular barriers. Despite the high antifungal potency and broad spectrum of econazole, its strong irritant and insolubility in water hinder its ocular application. We designed and fabricated a new drug delivery system based on a polymeric vector for the ocular antifungal application of econazole. This novel system integrates the advantages of its constituent units and exhibits superior comprehensive performance. Using the new system...
Source: Drug Delivery - April 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Estrogen-functionalized liposomes grafted with glutathione-responsive sheddable chotooligosaccharides for the therapy of osteosarcoma.
Authors: Yin X, Feng S, Chi Y, Liu J, Sun K, Guo C, Wu Z Abstract An estrogen (ES)-functionalized cationic liposomal system was developed and exploited for targeted delivery to osteosarcoma. Natural biocompatible chotooligosaccharides (COS, MW2-5 KDa) were covalently tethered to the liposomal surface through a disulfate bond (-SS-) to confer reduction-responsive COS detachment, whereas estrogen was grafted via polyethylene glycol (PEG 2 K) chain to achieve estrogen receptor-targeting. The liposomal carriers were prepared by the ethanol injection method and fluorescent anticancer drug doxorubicin (DOX)...
Source: Drug Delivery - April 15, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Pharmacokinetic evaluation of quetiapine fumarate controlled release hybrid hydrogel: a healthier treatment of schizophrenia.
Authors: Akhlaq M, Maryam F, Elaissari A, Ullah H, Adeel M, Hussain A, Ramzan M, Ullah O, Zeeshan Danish M, Iftikhar S, Aziz N Abstract The current study aimed to rationally develop and characterize pH-sensitive controlled release hydrogels by graft polymerization of gelatin (Gel) and hydroxypropyl methyl cellulose (HPMC) in the presence of glutaraldehyde (GA) using quetiapine fumarate for the treatment of schizophrenia. The prepared hydrogels discs were subjected to various physicochemical studies including: swelling, diffusion, porosity, sol-gel analysis, Fourier transform infrared spectroscopy, differential scan...
Source: Drug Delivery - April 15, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Cefquinome-loaded microsphere formulations against Klebsiella pneumonia infection during experimental infections.
Authors: Qu S, Dai C, Zhu J, Zhao L, Li Y, Hao Z Abstract The aim of this study was to prepare cefquinome-loaded polylactic acid microspheres and to evaluate their in vitro and in vivo characteristics and pharmacodynamics for the therapy of pneumonia in a rat model. Microspheres were prepared using a 0.7 mm two-fluid nozzle spray drier in one step resulting in spherical and smooth microspheres of uniform size (9.8 ± 3.6 μm). The encapsulation efficiency and drug loading of cefquinome were 91.6 ± 2.6% and 18.7 ± 1.2%, respectively. In vi...
Source: Drug Delivery - April 15, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Improving the topical ocular pharmacokinetics of lyophilized cyclosporine A-loaded micelles: formulation, in vitro and in vivo studies.
Authors: Yu Y, Chen D, Li Y, Yang W, Tu J, Shen Y Abstract Dry eye syndrome (DES) is one of the most common disorders of the eye for which combined treatment includes modification of the ocular environment and pathogenic therapies. Cyclosporine A (CsA), a immunosuppressive agent, has been demonstrated to be effective for the treatment of DES but is limited clinically by its low ocular bioavailability due to poor water solubility. In this paper, methoxy poly (ethylene glycol)-poly (lactide) polymer (mPEG-PLA) micelles were investigated as alternative vehicles for the solubilization and delivery of CsA to the eye. Th...
Source: Drug Delivery - April 12, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Folate-targeting annonaceous acetogenins nanosuspensions: significantly enhanced antitumor efficacy in HeLa tumor-bearing mice.
In this study, folic acid (FA) modified annonaceous acetogenins nanosuspensions (FA-PEG-ACGs-NSps) had been successfully prepared using DSPE-PEG-FA and soybean lecithin (SPC) as stabilizers. The resultant FA-PEG-ACGs-NSps had a mean particle size of 119.7 nm, a zeta potential of -23.0 mV and a high drug payload of 49.68%. The obtained ACGs-NSps had a good stability in various physiological media, and showed sustained drug release. Compared to common ACGs nanoparticles (PEG-ACGs-NSps), FA-PEG-ACGs-NSps showed significantly enhanced in vitro cytotoxicity against folate receptor-positive HeLa cell lines (IC50, 0...
Source: Drug Delivery - April 3, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Modified mixed nanomicelles with collagen peptides enhanced oral absorption of Cucurbitacin B: preparation and evaluation.
Authors: Tang L, Fu L, Zhu Z, Yang Y, Sun B, Shan W, Zhang Z Abstract Polymer nanoparticles modified with collagen peptides (CPs) are an attractive strategy for the oral delivery of active ingredients from Chinese medicine. Thus, in the present study, collagen cationic CPs were simply separated using ion-exchange resin from bovine CPs, to modify mixed nanomicelles (MMs) on the surface to improve the oral bioavailability of Cucurbitacin B (CuB). The physicochemical property of micelles was characterized, which confirmed the successful modification of the nanomicelles. CPs-modified nanomicelles in vitro were found to...
Source: Drug Delivery - April 3, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Peri-tumor administration of 5-fluorouracil sol-gel using a hollow microneedle for treatment of gastric cancer.
Authors: Jung YS, Koo DH, Yang JY, Lee HY, Park JH, Park JH Abstract The aim of this study was to investigate the effectiveness of treating gastric cancer by injecting a pluronic F-127 sol-gel formulation of 5-fluorouracil (5-FU) into normal tissue surrounding the tumor using a hollow microneedle. The MTS tetrazolium assay was performed to assess the cytotoxicity of 5-FU after application to gastric cancer cells at different concentrations for 1, 5 and 10 h. Gastric cancer cells were inoculated subcutaneously into 30 male nude mice (CrjBALB/c-nu/nu mice, male); the inoculated mouse were divided into three gr...
Source: Drug Delivery - April 3, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Puerarin-loaded PEG-PE micelles with enhanced anti-apoptotic effect and better pharmacokinetic profile.
Authors: Li W, Wu J, Zhang J, Wang J, Xiang D, Luo S, Li J, Liu X Abstract Puerarin (PUE) is the most abundant isoflavonoid in kudzu root. It is widely used as a therapeutic agent for the treatment of cardiovascular diseases. However, the short elimination half-life, poor-bioavailability, and acute intravascular hemolysis of PUE are the main obstacles to its widespread clinical applications. Whereas PEG-PE micelles possess the ability to release medicine slowly, enhance the cellular uptake of drugs and improve their biocompatibility. Therefore, it was aim to fabricate puerarin-loaded PEG-PE (PUE@PEG-PE) micelles to...
Source: Drug Delivery - March 30, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Uncovering the regional localization of inhaled salmeterol retention in the lung.
Authors: Bäckström E, Hamm G, Nilsson A, Fihn BM, Strittmatter N, Andrén P, Goodwin RJA, Fridén M Abstract Treatment of respiratory disease with a drug delivered via inhalation is generally held as being beneficial as it provides direct access to the lung target site with a minimum systemic exposure. There is however only limited information of the regional localization of drug retention following inhalation. The aim of this study was to investigate the regional and histological localization of salmeterol retention in the lungs after inhalation and to compare it to systemic administration. L...
Source: Drug Delivery - March 30, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Magnetically assisted intraperitoneal drug delivery for cancer chemotherapy.
Authors: Shamsi M, Sedaghatkish A, Dejam M, Saghafian M, Mohammadi M, Sanati-Nezhad A Abstract Intraperitoneal (IP) chemotherapy has revived hopes during the past few years for the management of peritoneal disseminations of digestive and gynecological cancers. Nevertheless, a poor drug penetration is one key drawback of IP chemotherapy since peritoneal neoplasms are notoriously resistant to drug penetration. Recent preclinical studies have focused on targeting the aberrant tumor microenvironment to improve intratumoral drug transport. However, tumor stroma targeting therapies have limited therapeutic windows and sh...
Source: Drug Delivery - March 30, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Bioresponsive albumin-conjugated paclitaxel prodrugs for cancer therapy.
Authors: Yang J, Lv Q, Wei W, Yang Z, Dong J, Zhang R, Kan Q, He Z, Xu Y Abstract The efficacy of traditional chemotherapy often suffers from rapid clearance and off-target toxicity. Drug delivery systems and controlled release are applied to improve the therapeutic efficiencies of small-molecule drugs. In this work, two novel oxidative/reductive (Ox/Re) -sensitive and one non-sensitive Paclitaxel (PTX) prodrugs were synthesized with a maleimide group, which rapidly conjugates with albumin in vivo. Albumin serves as a good vehicle to deliver more prodrug to tumors due to the enhanced permeation and retention (EPR) ...
Source: Drug Delivery - March 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Fabrication of novel elastosomes for boosting the transdermal delivery of diacerein: statistical optimization, ex-vivo permeation, in-vivo skin deposition and pharmacokinetic assessment compared to oral formulation.
Authors: Aziz DE, Abdelbary AA, Elassasy AI Abstract Diacerein (DCN) is a hydrophobic osteoarthritis (OA) drug with short half-life and low oral bioavailability. Furthermore, DCN oral administration is associated with diarrhea which represents obstacle against its oral use. Hence, this article aimed at developing elastosomes (edge activator (EA)-based vesicular nanocarriers) as a novel transdermal system for delivering DCN efficiently and avoiding its oral problems. For achieving this goal, elastosomes were prepared according to 41.21 full factorial design using different EAs in varying amounts. The prepared formul...
Source: Drug Delivery - March 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Application of hyaluronic acid as carriers in drug delivery.
Authors: Huang G, Huang H Abstract Hyaluronic acid has good biocompatibility, biodegradability, and nonimmunogenicity. In addition, it has the ability to recognize specific receptors that are overexpressed on the surface of tumor cells, and cancer drugs can be targeted to the tumor cells to better kill them. Therefore, hyaluronic acid has attracted much attention as drug delivery vehicle. Herein, the application of hyaluronic acid as carrier in drug delivery was analyzed and summarized in detail. It showed that hyaluronic acid would have broad prospects for drug delivery. PMID: 29536778 [PubMed - in process] (S...
Source: Drug Delivery - March 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development of redox-responsive theranostic nanoparticles for near-infrared fluorescence imaging-guided photodynamic/chemotherapy of tumor.
Authors: Yang X, Shi X, Ji J, Zhai G Abstract The development of imaging-guided smart drug delivery systems for combinational photodynamic/chemotherapy of the tumor has become highly demanded in oncology. Herein, redox-responsive theranostic polymeric nanoparticles (NPs) were fabricated innovatively using low molecular weight heparin (LWMH) as the backbone. Chlorin e6 (Ce6) and alpha-tocopherol succinate (TOS) were conjugated to LMWH via cystamine as the redox-sensitive linker, forming amphiphilic Ce6-LMWH-TOS (CHT) polymer, which could self-assemble into NPs in water and encapsulate paclitaxel (PTX) inside the inn...
Source: Drug Delivery - March 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Transcriptional control of the MUC16 promoter facilitates follicle-stimulating hormone peptide-conjugated shRNA nanoparticle-mediated inhibition of ovarian carcinoma in vivo.
Authors: Zhang MX, Hong SS, Cai QQ, Zhang M, Chen J, Zhang XY, Xu CJ Abstract Ovarian cancer is the leading cause of cancer death among gynecological malignancies. The high mortality rate has not been significantly reduced despite advances in surgery and chemotherapy. Gene therapy shows therapeutic potential, but several key issues must be resolved before clinical application. To minimize toxicity in noncancerous tissues, tumor-specific ligands are conjugated to vectors to increase the selectivity of drug delivery. The expression pattern of follicle-stimulating hormone (FSH) receptor in normal and cancer tissues pr...
Source: Drug Delivery - March 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Nasal delivery of H5N1 avian influenza vaccine formulated with GenJet ™ or in vivo-jetPEI® induces enhanced serological, cellular and protective immune responses.
In this study, we formulated H5N1 influenza vaccines with GenJet™ or in vivo-jetPEI®, and showed that these formulations significantly enhanced the immunogenicity of H5N1 vaccines and conferred protective immunity in a mouse model. Detailed analyses of adaptive immune responses revealed that both formulations induced mixed TH1/TH2 antigen-specific CD4 T-cell responses, antigen-specific cytotoxic CD8 T-cell and memory B-cell responses. Our findings suggest that cationic polymers merit future development as potential adjuvants for mucosal delivery of poorly immunogenic vaccines. PMID: 29542358 [PubMed - in proc...
Source: Drug Delivery - March 17, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Cell penetrating peptides functionalized gambogic acid-nanostructured lipid carrier for cancer treatment.
In conclusion, RGERPPR has a potential as an effective carrier in targeting drug delivery of anticancer agents. PMID: 29528244 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - March 14, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

An α-tocopheryl succinate enzyme-based nanoassembly for cancer imaging and therapy.
An α-tocopheryl succinate enzyme-based nanoassembly for cancer imaging and therapy. Drug Deliv. 2018 Nov;25(1):738-749 Authors: Lee SY, Cho HJ Abstract Nanoassembly (NA) based on a D-α-tocopherol succinate (αTS) conjugated lysozyme (Lys) (Lys-αTS) was fabricated for tumor-selective delivery of curcumin (CUR) for breast cancer therapy. Lys and αTS were used as a biocompatible enzyme and a hydrophobic residue, respectively, for the preparation of nanocarriers in this study. Compared with CUR-loaded cross-linked Lys (c-Lys/CUR) NA, Lys-αTS/CUR NA exhibited a smaller hyd...
Source: Drug Delivery - March 10, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Targeted delivery of hyaluronic acid-coated solid lipid nanoparticles for rheumatoid arthritis therapy.
Authors: Zhou M, Hou J, Zhong Z, Hao N, Lin Y, Li C Abstract Rheumatoid arthritis (RA) is a chronic, systemic inflammatory disease. Long-term, high-dose glucocorticoid therapy can be used to treat the disease, but the fact that the drug distributes systemically can give rise to severe adverse effects. Here we develop a targeted system for treating RA in which the glucocorticoid prednisolone (PD) is encapsulated within solid lipid nanoparticles (SLNs) coated with hyaluronic acid (HA), giving rise to HA-SLNs/PD. HA binds to hyaluronic receptor CD44, which is over-expressed on the surface of synovial lymphocytes, macr...
Source: Drug Delivery - March 10, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Combined sustained release of BMP2 and MMP10 accelerates bone formation and mineralization of calvaria critical size defect in mice.
Authors: Reyes R, Rodríguez JA, Orbe J, Arnau MR, Évora C, Delgado A Abstract The effect of dual delivery of bone morphogenetic protein-2 (BMP-2) and matrix metalloproteinase 10 (MMP10) on bone regeneration was investigated in a murine model of calvarial critical-size defect, hypothesizing that it would result in an enhanced bone formation. Critical-size calvarial defects (4 mm diameter) were created in mice and PLGA microspheres preloaded with either BMP-2, MMP10 or a microsphere combination of both were transplanted into defect sites at different doses. Empty microspheres were used as the neg...
Source: Drug Delivery - March 10, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Eph A10-modified pH-sensitive liposomes loaded with novel triphenylphosphine-docetaxel conjugate possess hierarchical targetability and sufficient antitumor effect both in vitro and in vivo.
Authors: Zhang J, Yang C, Pan S, Shi M, Li J, Hu H, Qiao M, Chen D, Zhao X Abstract Mitochondrial-targeting therapy was considered to be a promising approach for the efficient treatment of cancer while positive charge induced nonspecific cytotoxicity severely limits its application. To overcome this drawback, a novel mitochondria targeted conjugate triphenylphosphine-docetaxel (TD) has been synthesized successfully and incorporated it into liposomes (EPSLP/TD), which possessed excellent pH-sensitive characteristic, EphA 10 mediated active targetability as well as mitochondria-targeting capability. EPSLP/TD was char...
Source: Drug Delivery - March 9, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

On-target and direct modulation of alloreactive T cells by a nanoparticle carrying MHC alloantigen, regulatory molecules and CD47 in a murine model of alloskin transplantation.
Authors: Shahzad KA, Wan X, Zhang L, Pei W, Zhang A, Younis M, Wang W, Shen C Abstract Biomimetic nanoparticles have been reported as immune modulators in autoimmune diseases and allograft rejections by numerous researchers. However, most of the therapeutics carrying antigens, toxins or cytokines underlay the mechanism of antigen presentation by cellular uptake of NPs through pinocytosis and phagocytosis. Few researches focus on the direct and antigen-specific modulation on T cells by NPs and combined use of multiple regulatory molecules. Here, polylactic-co-glycolic acid nanoparticles (PLGA-NPs) were fabricated as...
Source: Drug Delivery - March 7, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Multifunctional nanoemulsions for intraductal delivery as a new platform for local treatment of breast cancer.
In this study, a cationic bioadhesive nanoemulsion was developed for intraductal administration of C6 ceramide, a sphingolipid that mediates apoptotic and non-apoptotic cell death. Bioadhesive properties were obtained by surface modification with chitosan. The optimized nanoemulsion displayed size of 46.3 nm and positive charge, properties that were not affected by ceramide encapsulation (0.4%, w/w). C6 ceramide concentration necessary to reduce MCF-7 cells viability to 50% (EC50) decreased by 4.5-fold with its nanoencapsulation compared to its solution; a further decrease (2.6-fold) was observed when tributyrin (a ...
Source: Drug Delivery - March 4, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Water-soluble substituted chitosan derivatives as technology platform for inhalation delivery of siRNA.
Authors: Capel V, Vllasaliu D, Watts P, Clarke PA, Luxton D, Grabowska AM, Mantovani G, Stolnik S Abstract Despite research efforts full potential of siRNA-based therapeutics has not yet been fully realized due to a need for suitable, effective delivery formulations. Here, we examine a potential of a new class of water-soluble chitosans as siRNA platform for pulmonary delivery. The system is based on piperazine-substituted chitosans, a material designed to integrate established, safe application of chitosan for mucosal administration with novel properties: the piperazine-substituted chitosans are freely water-solub...
Source: Drug Delivery - March 3, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Regression of prostate tumors after intravenous administration of lactoferrin-bearing polypropylenimine dendriplexes encoding TNF- α, TRAIL, and interleukin-12.
In this study, we demonstrated that the intravenous administration of Lf-bearing DAB dendriplexes encoding TNFα resulted in the complete suppression of 70% of PC-3 and 50% of DU145 tumors over one month. Treatment with DAB-Lf dendriplex encoding TRAIL led to tumor suppression of 40% of PC-3 tumors and 20% of DU145 tumors. The treatment was well tolerated by the animals. Lf-bearing generation 3-polypropylenimine dendrimer is therefore a highly promising delivery system for non-viral gene therapy of prostate cancer. PMID: 29493296 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - March 3, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Multiseed liposomal drug delivery system using micelle gradient as driving force to improve amphiphilic drug retention and its anti-tumor efficacy.
In conclusion, ASL-ML prepared by active loading method can effectively load drug into micelles with expected structure and improve drug retention. PMID: 29493300 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - March 3, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Antitumor efficacy of liposome-encapsulated NVP-BEZ 235 in combination with irreversible electroporation.
Authors: Tian L, Qiao Y, Lee P, Wang L, Chang A, Ravi S, Rogers TA, Lu L, Singhana B, Zhao J, Melancon MP Abstract Irreversible electroporation (IRE) is an emerging minimally invasive tumor ablation technique that delivers short pulses of strong electric fields and kills cancer cells by disrupting their cell membranes with the electric pulses. However, clinical studies report that more than 10% of local tumor recurrences occur at the original ablated site. NVP BEZ-235 (BEZ) is a dual PI3K/mTOR inhibitor that has substantial anticancer effects. However, the clinical trials of BEZ was not satisfactory because of its ...
Source: Drug Delivery - February 28, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Chitosan-based liposomal thermogels for the controlled delivery of pingyangmycin: design, optimization and in vitro and in vivo studies.
Authors: Zhang L, Chen F, Zheng J, Wang H, Qin X, Pan W Abstract Pingyangmycin (PYM) has been applied clinically for many years to treat vascular malformations (VM) in China. The major limitation of PYM injections is quick diffusion from the injection site, which increases side effects, especially the possibility of pulmonary injury. In this paper, chitosan/glycerophosphate disodium (CS/GP) thermogels containing liposomes for sustained and localized PYM delivery were prepared and optimized by a three-level three-factorial Box-Behnken experimental design to evaluate the effects of different variables (the PYM concen...
Source: Drug Delivery - February 28, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Follicle-stimulating hormone peptide-conjugated nanoparticles for targeted shRNA delivery lead to effective gro- α silencing and antitumor activity against ovarian cancer.
In conclusion, gro-α shRNA-loaded nanoparticles conjugated with FSH peptides overcame the drawbacks of the in vivo application of RNAi therapeutics and polymer-based nanocarriers and showed safe antitumor efficacy. Our study might contribute to the application of FSHR-based targeted therapy and imaging in cancer. PMID: 29461120 [PubMed - as supplied by publisher] (Source: Drug Delivery)
Source: Drug Delivery - February 22, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Synchronous delivery of oxygen and photosensitizer for alleviation of hypoxia tumor microenvironment and dramatically enhanced photodynamic therapy.
Authors: Guo X, Qu J, Zhu C, Li W, Luo L, Yang J, Yin X, Li Q, Du Y, Chen D, Qiu Y, Lou Y, You J Abstract Photosensitizer, proper laser irradiation, and oxygen are essential components for effective photodynamic therapy (PDT) in clinical cancer therapy. However, native hypoxic tumoral microenvironment is a major barrier hindering photodynamic reactions in vivo. Thus, we have prepared biocompatible liposomes by loading complexes of oxygen-carrier (hemoglobin, Hb) and photosensitizer (indocyanine green, ICG) for enhanced PDT against hypoxic tumor. Ideal oxygen donor Hb, which is an oxygen-carried protein in red blood...
Source: Drug Delivery - February 22, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

New model of proliferative vitreoretinopathy in rabbit for drug delivery and pharmacodynamic studies.
Authors: Moon SW, Sun Y, Warther D, Huffman K, Freeman WR, Sailor MJ, Cheng L Abstract Blinding retinal diseases become more epidemic as the population ages. These diseases, such as diabetic retinopathy and macular edema, are of chronic nature and require protracted drug presence at the disease site. A sustained intravitreal porous silicon delivery system with dexamethasone (pSiO2-COO-DEX) was evaluated in a new rabbit model of proliferative vitreoretinopathy (PVR) in a real treatment design. In contrast to the pretreatment design model, pSiO2-COO-DEX was intravitreally injected into the eyes with active inflammati...
Source: Drug Delivery - February 22, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Novel application of pluronic lecithin organogels (PLOs) for local delivery of synergistic combination of docetaxel and cisplatin to improve therapeutic efficacy against ovarian cancer.
In this study, using Capryol-90 (C90) with the addition of lecithin as the oil phase was developed to carry DTX, which was then incorporated into a PLO-containing CIS to formulate a dual-drug injectable PLO for local delivery. An optimal PLO composite, P13L0.15O1.5, composed of PF127:lecithin:C90 at a 13:0.15:1.5 weight ratio was obtained. The sol-gel transition temperature of P13L0.15O1.5 was found to be 33 °C. Tumor inhibition studies illustrated that DTX/CIS-loaded P13L0.15O1.5 could efficiently suppress tumor growth by both intratumoral and peritumoral injections in SKOV-3 xenograft mouse model. Pharmacokine...
Source: Drug Delivery - February 22, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Designed construction of tween 60@2 β-CD self-assembly vesicles as drug delivery carrier for cancer chemotherapy.
We report a simple strategy to prepare Tween 60@2β-CD self-assembly vesicles in aqueous solution as a new drug delivery carrier for cancer chemotherapy. The spherical shape of vesicles was confirmed by transmission electron microscopy (TEM) and mean particle sizes were about 33.7 nm, as measured by dynamic light scattering, micro-IR results indicated that the self-assembly vesicles was driven by hydrogen bonding. Hydrophilic doxorubicin (DOX) was successfully loaded into the self-assembly vesicles with drug loading content of 7.85% and loading efficiency of 42%. In addition, an in vitro cytotoxicity study and c...
Source: Drug Delivery - February 22, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Surface modification of doxorubicin-loaded nanoparticles based on polydopamine with pH-sensitive property for tumor targeting therapy.
Authors: Bi D, Zhao L, Yu R, Li H, Guo Y, Wang X, Han M Abstract One major challenge of current surface modification of nanoparticles is the demand for chemical reactive polymeric layers, such modification is always complicated, inefficient, and may lead the polymer lose the ability to encapsulate drug. To overcome this limitation, we adopted a pH-sensitive platform using polydopamine (PDA) as a way of functionalizing nanoparticles (NPs) surfaces. All this method needed to be just a brief incubation in weak alkaline solution of dopamine, which was simple and applicable to a variety of polymer carriers regardless of...
Source: Drug Delivery - February 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Control release of mitochondria-targeted antioxidant by injectable self-assembling peptide hydrogel ameliorated persistent mitochondrial dysfunction and inflammation after acute kidney injury.
This study aims to develop an SAP-based carrier to slow release MT for enhancing its long-term therapeutic potency on AKI. The KLD with aspartic acid (KLDD) was designed. The microstructure and in vitro release of MT was assayed. The protective role of MT-loaded SAP (SAP-MT) hydrogel on renal mitochondrial injury, tubular apoptosis, and inflammation was evaluated in mice at five days after ischemia-reperfusion injury (IRI). Our results showed that KLDD could self-assemble into cross-linked nanofiber hydrogel and it had lower release rate than free MT and KLD hydrogel. Compared to IRI and free MT mice, SAP-MT mice exerted r...
Source: Drug Delivery - February 18, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Effect of finasteride particle size reduction on its pharmacokinetic, tissue distribution and cellular permeation.
Authors: Ahmed TA, Al-Abd AM Abstract Finasteride (FSD), a specific competitive inhibitor of the steroid type-II 5α-reductase enzyme, is used in treatment of benign prostate hyperplasia (BPH) and male pattern baldness. The drug is of limited solubility that affect its dissolution and bioavailability. The aim was to study the effect of FSD particle size reduction on the pharmacokinetic, tissue distribution and cellular permeation. An optimized drug micro- and nano-particles were developed, characterized, administered to group of rats, and systemic pharmacokinetic and tissue distribution within target and not-t...
Source: Drug Delivery - February 18, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Pulmonary delivery of influenza vaccine formulations in cotton rats: site of deposition plays a minor role in the protective efficacy against clinical isolate of H1N1pdm virus.
In conclusion, immune responses induced by liquid formulation were significantly higher than responses induced by powder formulation, but the overall protective efficacy of both formulations was comparable. Thus, pulmonary immunization is capable of inducing protective immunity and the site of antigen deposition seems to be of minor relevance in inducing protection. PMID: 29451040 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - February 18, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Transferrin and octaarginine modified dual-functional liposomes with improved cancer cell targeting and enhanced intracellular delivery for the treatment of ovarian cancer.
Authors: Deshpande P, Jhaveri A, Pattni B, Biswas S, Torchilin V Abstract Off-target effects of drugs severely limit cancer therapy. Targeted nanocarriers are promising to enhance the delivery of therapeutics to tumors. Among many approaches for active tumor-targeting, arginine-rich cell penetrating peptides (AR-CPP) and ligands specific to target over-expressed receptors on cancer-cell surfaces, are popular. Earlier, we showed that the attachment of an AR-CPP octaarginine (R8) to the surface of DOXIL® (Doxorubicin encapsulated PEGylated liposomes) improved cytoplasmic and nuclear DOX delivery that enhanced the...
Source: Drug Delivery - February 14, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Correction to: Ma et  al., Controlled synthesis and size effects of multifunctional mesoporous silica nanosystem for precise cancer therapy.
Correction to: Ma et al., Controlled synthesis and size effects of multifunctional mesoporous silica nanosystem for precise cancer therapy. Drug Deliv. 2018 Feb 12;:1 Authors: PMID: 29433358 [PubMed - as supplied by publisher] (Source: Drug Delivery)
Source: Drug Delivery - February 14, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

α-Conotoxin ImI-modified polymeric micelles as potential nanocarriers for targeted docetaxel delivery to α7-nAChR overexpressed non-small cell lung cancer.
α-Conotoxin ImI-modified polymeric micelles as potential nanocarriers for targeted docetaxel delivery to α7-nAChR overexpressed non-small cell lung cancer. Drug Deliv. 2018 Nov;25(1):493-503 Authors: Mei D, Zhao L, Chen B, Zhang X, Wang X, Yu Z, Ni X, Zhang Q Abstract A micelle system modified with α-Conotoxin ImI (ImI), a potently antagonist for alpha7 nicotinic acetylcholine receptor (α7-nAChR) previously utilized for targeting breast cancer, was constructed. Its targeting efficiency and cytotoxicity against non-small cell lung cancer (NSCLC) highly expressing α7-nAChR w...
Source: Drug Delivery - February 12, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Lipid-based nanocarrier efficiently delivers highly water soluble drug across the blood-brain barrier into brain.
Authors: Dutta L, Mukherjee B, Chakraborty T, Das MK, Mondal L, Bhattacharya S, Gaonkar RH, Debnath MC Abstract Delivering highly water soluble drugs across blood-brain barrier (BBB) is a crucial challenge for the formulation scientists. A successful therapeutic intervention by developing a suitable drug delivery system may revolutionize treatment across BBB. Efforts were given here to unravel the capability of a newly developed fatty acid combination (stearic acid:oleic acid:palmitic acid = 8.08:4.13:1) (ML) as fundamental component of nanocarrier to deliver highly water soluble zidovudine (AZT) as a...
Source: Drug Delivery - February 12, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Doxorubicin conjugated with a trastuzumab epitope and an MMP-2 sensitive peptide linker for the treatment of HER2-positive breast cancer.
Authors: You Y, Xu Z, Chen Y Abstract HER2-positive breast cancer correlates with more aggressive tumor growth, a poorer prognosis and reduced overall survival. Currently, trastuzumab (Herceptin), which is an anti-HER2 antibody, is one of the key drugs. There is evidence indicating that conjugation of trastuzumab with chemotherapy drugs, such as doxorubicin (DOX), for multiple targets could be more effective. However, incomplete penetration into tumors has been noted for those conjugates. Compared to an antibody, peptides may represent an attractive alternative. For HER2, a similar potency has been observed for a 1...
Source: Drug Delivery - February 8, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Formulation and in vivo assessment of terconazole-loaded polymeric mixed micelles enriched with Cremophor EL as dual functioning mediator for augmenting physical stability and skin delivery.
Authors: Abd-Elsalam WH, El-Zahaby SA, Al-Mahallawi AM Abstract The aim of the current study was to formulate terconazole (TCZ) loaded polymeric mixed micelles (PMMs) incorporating Cremophor EL as a stabilizer and a penetration enhancer. A 23 full factorial design was performed using Design-Expert® software for the optimization of the PMMs which were formulated using Pluronic P123 and Pluronic F127 together with Cremophor EL. To confirm the role of Cremophor EL, PMMs formulation lacking Cremophor EL was prepared for the purpose of comparison. Results showed that the optimal PMMs formulation (F7, where the ratio...
Source: Drug Delivery - February 8, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research