Porous silicon based intravitreal platform for dual-drug loading and controlled release towards synergistic therapy.
This study demonstrates the use of porous silicon (pSi) particles sequentially loaded with daunorubicin (DNR) and dexamethasone (DEX) to create a synergistic intravitreally injectable dual-drug delivery system. DEX targets chronic inflammation while DNR inhibits excessive cell proliferation as well as suppresses hypoxia-inducible factor 1 to reduce scarring. This pSi-based delivery system releases therapeutic concentrations of DNR for 100 days and DEX for over 165 days after a single dose. This intravitreal dual-drug delivery system is also well tolerated after injection into the rabbit eye model, attested by...
Source: Drug Delivery - July 13, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Stabilized tetraether lipids based particles guided prophyrins photodynamic therapy.
In this study, ultrastable tetraether lipids (TELs) based liposomes were developed. PpIX molecules were identified to reside physically in the monolayer; thereby the inherent π-π stacking that leads to aggregation of PpIX in aqueous milieu was dramatically improved. TEL29.9 mol% and TEL62mol% based liposomes revealed PpIX sustained release diffusion pattern from spherical particles as confirmed by converged fitting to Baker & Lonsdale model. Stability in presence of human serum albumins, a key element for PDT accomplishment was emphasized. The epitome candidates were selected for vascular photodynamic (vPD...
Source: Drug Delivery - July 13, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

The paradigm shift for drug delivery systems for oral and maxillofacial implants.
Authors: Pokrowiecki R Abstract Along with the development of nanotechnological strategies for biomaterials associated with the prevention of infections, a myriad of clinically unproven techniques have been described to date. In this work, the aim was to perform a critical analysis of the literature available concerning antibacterial biomaterials for oral implantology and to provide a practical derivation for such a purpose. As anti-adhesive strategies may affect osseointegration, they should no longer be recommended for inclusion in this class of biomaterials, despite promising results in biomedical engineering fo...
Source: Drug Delivery - July 5, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Advanced physical techniques for gene delivery based on membrane perforation.
Authors: Du X, Wang J, Zhou Q, Zhang L, Wang S, Zhang Z, Yao C Abstract Gene delivery as a promising and valid tool has been used for treating many serious diseases that conventional drug therapies cannot cure. Due to the advancement of physical technology and nanotechnology, advanced physical gene delivery methods such as electroporation, magnetoporation, sonoporation and optoporation have been extensively developed and are receiving increasing attention, which have the advantages of briefness and nontoxicity. This review introduces the technique detail of membrane perforation, with a brief discussion for future d...
Source: Drug Delivery - July 5, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Localized co-delivery of collagenase and trastuzumab by thermosensitive hydrogels for enhanced antitumor efficacy in human breast xenograft.
Authors: Pan A, Wang Z, Chen B, Dai W, Zhang H, He B, Wang X, Wang Y, Zhang Q Abstract Modulation of the collagen-rich extracellular matrix (ECM) in solid tumors by the treatment with collagenase has been proved effective in enhancement of the interstitial transport and antitumor efficacy of antibodies. We, therefore, developed a PLGA-PEG-PLGA polymer-based thermosensitive hydrogel, which incorporated a HER2-targeted monoclonal antibody trastuzumab and collagenase (Col/Tra/Gel) for peritumoral administration. HER2-positvie BT474 tumor-bearing mice were selected as a model. The Col/Tra/Gel showed the continuous and ...
Source: Drug Delivery - June 28, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Anti-GPC3 antibody-modified sorafenib-loaded nanoparticles significantly inhibited HepG2 hepatocellular carcinoma.
Authors: Tang X, Chen L, Li A, Cai S, Zhang Y, Liu X, Jiang Z, Liu X, Liang Y, Ma D Abstract Sorafenib (SFB) has improved the treatment of hepatocellular carcinoma (HCC) and has fewer severe side effects than other agents used for that purpose. However, due to a lack of tumor-specific targeting, the concentration of the drug in tumor tissue cannot be permanently maintained at a level that inhibits tumor growth. To overcome this problem, we developed a novel SFB-loaded polymer nanoparticle (NP). The NP (a TPGS-b-PCL copolymer that was synthesized from ε-caprolactone and d-α-tocopheryl polyethylene glyc...
Source: Drug Delivery - June 21, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Hyaluronic acid/doxorubicin nanoassembly-releasing microspheres for the transarterial chemoembolization of a liver tumor.
Authors: Lee SY, Choi JW, Lee JY, Kim DD, Kim HC, Cho HJ Abstract Doxorubicin (DOX)-loaded, hyaluronic acid-ceramide (HACE) nanoassembly-releasing poly(lactic-co-glycolic acid) (PLGA) microspheres (MSs) were developed for transarterial chemoembolization (TACE) therapy of liver cancer. DOX/HACE MSs with a mean diameter of 27 μm and a spherical shape were prepared based on the modified emulsification method. Their in vitro biodegradability in artificial biological fluids was observed. A more sustained drug release pattern was observed from DOX/HACE MS than from DOX MS at pH 7.4. The cellular internalization...
Source: Drug Delivery - June 19, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Ultrahigh verapamil-loaded controlled release polymeric beads using superamphiphobic substrate: D-optimal statistical design, in vitro and in vivo performance.
Authors: Yousry C, Amin MM, Elshafeey AH, El Gazayerly ON Abstract Controlled-release multiparticulate systems of hydrophilic drugs usually suffer from poor encapsulation and rapid-release rate. In the present study, ultra-high loaded controlled release polymeric beads containing verapamil hydrochloride (VP) as hydrophilic model drug were efficiently prepared using superamphiphobic substrates aiming to improve patient compliance by reducing dosing frequency. Superamphiphobic substrates were fabricated using clean aluminum sheets etched with ammonia solution and were treated with 1.5% (w/v) perfluorodecyltriethoxysi...
Source: Drug Delivery - June 16, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Improved lymphatic targeting: effect and mechanism of synthetic borneol on lymph node uptake of 7-ethyl-10-hydroxycamptothecin nanoliposomes following subcutaneous administration.
In conclusion, the present study may provide a basic study for improving lymphatic-targeting ability of SN-38-Lips by the S-BO regulation, and to be the helpful guidance for further study in lymphatic targeting of delivery system. PMID: 29902927 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - June 16, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A nanoparticle-based approach to improve the outcome of cancer active immunotherapy with lipopolysaccharides.
This study sought to develop a simple nanoparticle-based approach to enhance the efficiency and tolerability of lipopolysaccharide (LPS), a potent ligand of Toll-like Receptor 4 (TLR4), for immunotherapy in cancer. Despite holding promise within this context, the strong pro-inflammatory properties of LPS also account for its low tolerability given localized and systemic side effects, which restrict the administrable dosage. Herein, we investigated the effect of LPS decoration as a surface-active molecule on a polymeric matrix upon its efficiency and tolerability. The LPS-decorated nanoparticles (LPS-NP) were about 150&thin...
Source: Drug Delivery - June 16, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Selective delivery of PLXDC1 small interfering RNA to endothelial cells for anti-angiogenesis tumor therapy using CD44-targeted chitosan nanoparticles for epithelial ovarian cancer.
This study aimed to improve targeted delivery and enhance therapeutic efficacy for tumor anti-angiogenesis. The HA-CH-NP/siRNA was 200 ± 10 nm in size with a zeta potential of 26.4 mV. The loading efficiency of siRNA to the HA-CH-NP/siRNA was up to 60%. The selective binding of HA-CH-NP/siRNA to CD44-positive tumor endothelial cells increased by 2.1-fold compared with that of the CD44 nontargeted CH-NP/siRNA. PLXDC1 silencing by the HA-CH-NP/siRNA significantly inhibited tumor growth in A2780 tumor-bearing mice compared with that in the control group (p 
Source: Drug Delivery - June 14, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Dipeptide-modified nanoparticles to facilitate oral docetaxel delivery: new insights into PepT1-mediated targeting strategy.
Authors: Du Y, Tian C, Wang M, Huang D, Wei W, Liu Y, Li L, Sun B, Kou L, Kan Q, Liu K, Luo C, Sun J, He Z Abstract Oligopeptide transporter 1 (PepT1) has been a striking prodrug-designing target. However, the underlying mechanism of PepT1 as a target to facilitate the oral absorption of nanoparticles (NPs) remains unclear. Herein, we modify Poly (lactic-co-glycolic acid) (PLGA) NPs with the conjugates of dipeptides (L-valine-valine, L-valine-phenylalanine) and polyoxyethylene (PEG Mw: 1000, 2000) stearate to facilitate oral delivery of docetaxel (DTX) to investigate the oral absorption mechanism and regulatory eff...
Source: Drug Delivery - June 14, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Improved delivery of natural alkaloids into lung cancer through woody oil-based emulsive nanosystems.
In this study, woody oil-based emulsive nanosystems efficiently deliver poorly soluble natural alkaloids. PMID: 29890855 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - June 14, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Controlled release of celecoxib inhibits inflammation, bone cysts and osteophyte formation in a preclinical model of osteoarthritis.
Authors: Tellegen AR, Rudnik-Jansen I, Pouran B, de Visser HM, Weinans HH, Thomas RE, Kik MJL, Grinwis GCM, Thies JC, Woike N, Mihov G, Emans PJ, Meij BP, Creemers LB, Tryfonidou MA Abstract Major hallmarks of osteoarthritis (OA) are cartilage degeneration, inflammation and osteophyte formation. COX-2 inhibitors counteract inflammation-related pain, but their prolonged oral use entails the risk for side effects. Local and prolonged administration in biocompatible and degradable drug delivery biomaterials could offer an efficient and safe treatment for the long-term management of OA symptoms. Therefore, we evaluated...
Source: Drug Delivery - June 14, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Novel in situ gelling vaginal sponges of sildenafil citrate-based cubosomes for uterine targeting.
Authors: Aboud HM, Hassan AH, Ali AA, Abdel-Razik AH Abstract Sildenafil citrate (SIL), a type 5-specific phosphodiesterase inhibitor, demonstrates valuable results in the management of infertility in women; however, the absence of vaginal dosage form in addition to the associated oral adverse effects minimize its clinical performance. The present study is concerned with SIL uterine targeting following intravaginal administration via optimization of cubosomal in situ gelling sponges (CIS). An emulsification method was employed for preparation of cubosomal dispersions incorporating glyceryl monooleate as a lipid pha...
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Sustained ocular delivery of Dorzolamide-HCl via proniosomal gel formulation: in-vitro characterization, statistical optimization, and in-vivo pharmacodynamic evaluation in rabbits.
Authors: Fouda NH, Abdelrehim RT, Hegazy DA, Habib BA Abstract Glaucoma is the second cause of blindness worldwide. Frequent administration of traditional topical dosage forms may lead to patient incompliance and failure of treatment. Our study aims to formulate proniosomal gel formulations that sustain the release of the water-soluble anti-glaucoma drug Dorzolamide-HCl (Dorz). Proniosomal gel formulations were prepared using coacervation phase separation method according to a 52 full factorial design. The effects of Cholesterol and surfactant (Span 40) amounts (independent variables) on the percentage entrapment e...
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Temporary suppression the sequestrated function of host macrophages for better nanoparticles tumor delivery.
In conclusion, the encouraging results from this study inspire the generation of a rational strategy to focus on microenvironmental priming for modulation of innate immunity and to improve delivery efficiency of nanoparticles. PMID: 29869519 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Multivesicular liposomes for sustained release of bevacizumab in treating laser-induced choroidal neovascularization.
In this study, Bev-MVLs with high encapsulation efficiency were prepared by double emulsification technique, and antibody activity was determined. The results revealed that 10% of human serum albumin (HSA) could preserve the activity of bevacizumab. In vitro release of Bev-MVLs appeared to be in a more sustained manner, the underlying mechanisms of Bev-MVLs indicated that bevacizumab was released from MVLs through diffusion and erosion. Results of sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) demonstrated that bevacizumab could retain its structural integrity after being released from MVLs in vitro. ...
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

SPECT/CT imaging of chemotherapy-induced tumor apoptosis using 99mTc-labeled dendrimer-entrapped gold nanoparticles.
In this study, we report the synthesis, characterization, and utilization of radionuclide technetium-99m (99mTc)-labeled dendrimer-entrapped gold nanoparticles (Au DENPs) for targeted SPECT/CT imaging of chemotherapy-induced tumor apoptosis. Generation five poly(amidoamine) (PAMAM) dendrimers (G5.NH2) were sequentially conjugated with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), polyethylene glycol (PEG) modified duramycin, PEG monomethyl ether, and fluorescein isothiocyanate (FI) to form the multifunctional dendrimers, which were then utilized as templates to entrap gold nanoparticles. Followed by acet...
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Ratiometric delivery of two therapeutic candidates with inherently dissimilar physicochemical property through pH-sensitive core-shell nanoparticles targeting the heterogeneous tumor cells of glioma.
Authors: Xu HL, Fan ZL, ZhuGe DL, Tong MQ, Shen BX, Lin MT, Zhu QY, Jin BH, Sohawon Y, Yao Q, Zhao YZ Abstract Currently, combination drug therapy is one of the most effective approaches to glioma treatment. However, due to the inherent dissimilar pharmacokinetics of individual drugs and blood brain barriers, it was difficult for the concomitant drugs to simultaneously be delivered to glioma in an optimal dose ratio manner. Herein, a cationic micellar core (Cur-M) was first prepared from d-α-tocopherol-grafted-ε-polylysine polymer to encapsulate the hydrophobic curcumin, followed by dopamine-modified-...
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Nanoparticle drug delivery systems: an excellent carrier for tumor peptide vaccines.
Authors: Wang J, Hu X, Xiang D Abstract In the past 40 years, the nanoparticle drug delivery system for tumor peptide vaccines has been widely studied which also reached a splendid result. Nanomaterial can enhance the targeting of vaccines, help vaccines enter the cells and trigger immune response by themselves. They also help in increasing cellular uptake, improving permeability and efficacy. Currently, several categories of nanopreparation, such as liposome, polymeric micelle, polymeric nanoparticle, gold nanoparticle and so on, are proved that they are appropriate for peptide vaccines. This review we discus...
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development of a docetaxel micellar formulation using poly(ethylene glycol)-polylactide-poly(ethylene glycol) (PEG-PLA-PEG) with successful reconstitution for tumor targeted drug delivery.
Authors: Sim T, Kim JE, Hoang NH, Kang JK, Lim C, Kim DS, Lee ES, Youn YS, Choi HG, Han HK, Weon KY, Oh KT Abstract Docetaxel (DTX)-loaded polymeric micelles (DTBM) were formulated using the triblock copolymer, poly(ethylene glycol)-polylactide-poly(ethylene glycol) (PEG-PLA-PEG), to comprehensively study their pharmaceutical application as anticancer nanomedicine. DTBM showed a stable formulation of anticancer nanomedicine that could be reconstituted after lyophilization (DTBM-R) in the presence of PEG 2000 and D-mannitol (Man) as surfactant and protectant, respectively. DTBM-R showed a particle size less than 150...
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Cancer-targeted design of bioresponsive prodrug with enhanced cellular uptake to achieve precise cancer therapy.
In this study, we presented a smart targeted delivery system (Biotin-ss-CPT) that consists of cancer-targeted moiety (biotin), a cleavable disulfide linker (S-S bond) and the active drug CPT. Biotin-ss-CPT was found to exhibit potent effects on the migration of cancer cells and induced apoptosis by induction of ROS-mediated mitochondrial dysfunction and perturbation of GSH/GPXs system, as well as activation of caspases. In vivo tumor suppression investigation including toxicity evaluation and pathology analysis, accompanied by MR images showed that Biotin-ss-CPT can be recognized specifically and selectively and taken up p...
Source: Drug Delivery - June 6, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

l-Peptide functionalized dual-responsive nanoparticles for controlled paclitaxel release and enhanced apoptosis in breast cancer cells.
Authors: Niu S, Bremner DH, Wu J, Wu J, Wang H, Li H, Qian Q, Zheng H, Zhu L Abstract Nanoparticles and macromolecular carriers have been widely used to increase the efficacy of chemotherapeutics, largely through passive accumulation provided by their enhanced permeability and retention effect. However, the therapeutic efficacy of nanoscale anticancer drug delivery systems is severely truncated by their low tumor-targetability and inefficient drug release at the target site. Here, the design and development of novel l-peptide functionalized dual-responsive nanoparticles (l-CS-g-PNIPAM-PTX) for active targeting and ...
Source: Drug Delivery - June 4, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Biomimetic carbon monoxide delivery based on hemoglobin vesicles ameliorates acute pancreatitis in mice via the regulation of macrophage and neutrophil activity.
In this study, we examined the issue of whether CO targeting macrophages using a nanotechnology-based CO donor, namely CO-bound hemoglobin vesicles (CO-HbV), modulates their polarization and show therapeutic effects against inflammatory disorders. The results showed that the CO-HbV treatment polarized a macrophage cell line toward an M2-like phenotype. Furthermore, in an in vivo study using acute pancreatitis model mice as a model of an inflammatory disease, a CO-HbV treatment also tended to polarize macrophages toward an M2-like phenotype and inhibited neutrophil infiltration in the pancreas, resulting in a significant in...
Source: Drug Delivery - June 4, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Hyaluronic acid modified MPEG-b-PAE block copolymer aqueous micelles for efficient ophthalmic drug delivery of hydrophobic genistein.
Authors: Li C, Chen R, Xu M, Qiao J, Yan L, Guo XD Abstract The ophthalmic drug delivery is a challenge in the clinical treatment of ocular diseases. The traditional drug administration usually shows apparent limitations, such as the low bioavailability from the reason of low penetration of the cornea and the short survival time of drug in the eyes. To overcome these shortcomings, we propose an amphiphilic polymer micelle modified with hyaluronic acid (HA) for high efficient ophthalmic delivery of genistein, a widely used hydrophobic drug for treatment of ocular angiogenesis. The MPEG-b-PAE copolymer was synthesize...
Source: Drug Delivery - June 4, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Delivering CRISPR: a review of the challenges and approaches.
Authors: Lino CA, Harper JC, Carney JP, Timlin JA Abstract Gene therapy has long held promise to correct a variety of human diseases and defects. Discovery of the Clustered Regularly-Interspaced Short Palindromic Repeats (CRISPR), the mechanism of the CRISPR-based prokaryotic adaptive immune system (CRISPR-associated system, Cas), and its repurposing into a potent gene editing tool has revolutionized the field of molecular biology and generated excitement for new and improved gene therapies. Additionally, the simplicity and flexibility of the CRISPR/Cas9 site-specific nuclease system has led to its widespread use i...
Source: Drug Delivery - May 30, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Gastroretentive raft liquid delivery system as a new approach to release extension for carrier-mediated drug.
Authors: Abouelatta SM, Aboelwafa AA, El-Gazayerly ON Abstract Gabapentin (GBP), an antiepileptic and anti-neuropathic agent, suffers from short half-life (5-7 h), has narrow absorption window, and is absorbed via carrier-mediated mechanism resulting in frequent dosing, poor compliance, and poor bioavailability (
Source: Drug Delivery - May 26, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Folate receptor-targeted mixed polysialic acid micelles for combating rheumatoid arthritis: in vitro and in vivo evaluation.
CONCLUSION: FA-PSA-CC micelles demonstrated significant advantages in terms of the suppression of inflammation and the treatment of inflammatory arthritis. These reliable and stable micelles possess a high potential to be transferred for clinical use. PMID: 29790372 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - May 25, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Hybrid liposomes showing enhanced accumulation in tumors as theranostic agents in the orthotopic graft model mouse of colorectal cancer.
This study aimed to elucidate the therapeutic effects and ability of HLs to detect (diagnosis) cancer in an orthotopic graft mouse model of colorectal cancer with HCT116 cells for the use of HLs as theranostic agents. In the absence of a chemotherapeutic drug, HLs exhibited therapeutic effects by inhibiting the growth of HCT116 colorectal cancer cells in vitro, possibly through an increase in apoptosis. Intravenously administered HLs also caused a remarkable reduction in the relative cecum weight in an orthotopic graft mouse model of colorectal cancer. A decrease in tumor size in the cecal sections was confirmed by histolo...
Source: Drug Delivery - May 25, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Plateau hypoxia attenuates the metabolic activity of intestinal flora to enhance the bioavailability of nifedipine.
Authors: Zhang J, Chen Y, Sun Y, Wang R, Zhang J, Jia Z Abstract Nifedipine is completely absorbed by the gastrointestinal tract and its pharmacokinetics and metabolism may be influenced by microorganisms. If gut microbes are involved in the metabolism of nifedipine, plateau hypoxia may regulate the bioavailability and the therapeutic effect of nifedipine by altering the metabolic activity of the gut microbiota. We herein demonstrated for the first time that gut flora is involved in the metabolism of nifedipine by in vitro experiments. In addition, based on the results of 16S rRNA analysis of feces in rats after ac...
Source: Drug Delivery - May 25, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Neutrophil-mediated delivery of pixantrone-loaded liposomes decorated with poly(sialic acid)-octadecylamine conjugate for lung cancer treatment.
Authors: Luo X, Hu L, Zheng H, Liu M, Liu X, Li C, Qiu Q, Zhao Z, Cheng X, Lai C, Su Y, Deng Y, Song Y Abstract Poly(sialic acid) (PSA) is a natural hydrophilic biodegradable and non-immunogenic biopolymer, receptors for its monomer are expressed on peripheral blood neutrophils (PBNs), which plays important roles in the progression and invasion of tumors. A poly(sialic acid)-octadecylamine conjugate (PSA-ODA) was synthesized and then anchor it on the surface of liposomal pixantrone (Pix-PSL), to achieve an improved anticancer effect. The liposomes were prepared using a remote loading method via a pH gradient, and t...
Source: Drug Delivery - May 25, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Liver-targeted delivery of insulin-loaded nanoparticles via enterohepatic circulation of bile acids.
In this study, we developed innovative nanoparticles for oral and liver-targeted delivery of insulin by using enterohepatic circulation of bile acids. The nanoparticles were produced from cholic acid and quaternary ammonium modified chitosan derivative and hydroxypropyl methylcellulose phthalate (HPMCP). The nanoparticles had a diameter of 239 nm, an insulin loading efficiency of 90.9%, and a loading capacity of 18.2%. Cell culture studies revealed that the cholic acid groups effectively enhanced the transport of the nanoparticles through Caco-2 cell monolayer and greatly increased the absorption of the nanoparticle...
Source: Drug Delivery - May 25, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Licorice root extract and magnesium isoglycyrrhizinate protect against triptolide-induced hepatotoxicity via up-regulation of the Nrf2 pathway.
Authors: Tan QY, Hu Q, Zhu SN, Jia LL, Xiao J, Su HZ, Huang SY, Zhang J, Jin J Abstract Triptolide, the predominant biologically active component of the Chinese herb Tripterygium wilfordii Hook f., possesses numerous pharmacological activities, including anti-inflammatory, anti-fertility, anti-neoplastic, and immunosuppressive effects. However, toxicity and severe adverse effects, particularly hepatotoxicity, limit the clinical application of triptolide. Licorice root extract contains various bioactive compounds and is potent hepatoprotective. Magnesium isoglycyrrhizinate, a magnesium salt of the 18α-glycyrrh...
Source: Drug Delivery - May 25, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Preparation of a mesoporous silica-based nano-vehicle for dual DOX/CPT pH-triggered delivery.
Authors: Llinàs MC, Martínez-Edo G, Cascante A, Porcar I, Borrós S, Sánchez-García D Abstract A dual doxorubicin/camptothecin (DOX/CPT) pH-triggered drug delivery mesoporous silica nanoparticle (MSN)-based nano-vehicle has been prepared. In this drug-delivery system (DDS), CPT is loaded inside the pores of the MSNs, while DOX is covalently attached to the surface of an aldehyde-functionalized MSN through a dihydrazide-polyethylene glycol chain. Thus, DOX and the linker act as pH-sensitive gatekeeper. The system is versatile and easy to assemble, not requiring the chemical modifica...
Source: Drug Delivery - May 23, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Inhalation delivery of topotecan is superior to intravenous exposure for suppressing lung cancer in a preclinical model.
Authors: Kuehl PJ, Grimes MJ, Dubose D, Burke M, Revelli DA, Gigliotti AP, Belinsky SA, Tessema M Abstract Intravenous (IV) topotecan is approved for the treatment of various malignancies including lung cancer but its clinical use is greatly undermined by severe hematopoietic toxicity. We hypothesized that inhalation delivery of topotecan would increase local exposure and efficacy against lung cancer while reducing systemic exposure and toxicity. These hypotheses were tested in a preclinical setting using a novel inhalable formulation of topotecan against the standard IV dose. Respirable dry-powder of topotecan was...
Source: Drug Delivery - May 23, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A novel phenolic propanediamine moiety-based lung-targeting therapy for asthma.
Authors: Li J, Yang Y, Wan D, Peng Y, Zhang J Abstract Asthma is one of the most prevalent chronic inflammatory diseases of lung. Current asthma therapy using inhaled corticosteroid often results in undesired treatment outcome due to poor compliance and drugs' lack of tissue specificity. N,N,N'-trimethyl-N'-(2-hydroxyl-3-methyl-5-123Iiodobenzyl)-1,3-propanediamine (HIPD), a phenolic propanediamine derivative, has been used as an imaging agent for localized pulmonary diseases. Inspired by this, N,N,N'-trimethyl-N'-(4-hydroxyl-benzyl)-1,3-propanediamine (TPD), a new HIPD analog, was proposed as a lung-targeting ligan...
Source: Drug Delivery - May 23, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Graphene oxide enhances alginate encapsulated cells viability and functionality while not affecting the foreign body response.
Authors: Ciriza J, Saenz Del Burgo L, Gurruchaga H, Borras FE, Franquesa M, Orive G, Hernández RM, Pedraz JL Abstract The combination of protein-coated graphene oxide (GO) and microencapsulation technology has moved a step forward in the challenge of improving long-term alginate encapsulated cell survival and sustainable therapeutic protein release, bringing closer its translation from bench to the clinic. Although this new approach in cell microencapsulation represents a great promise for long-term drug delivery, previous studies have been performed only with encapsulated murine C2C12 myoblasts genetically ...
Source: Drug Delivery - May 23, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Sericin nanomicelles with enhanced cellular uptake and pH-triggered release of doxorubicin reverse cancer drug resistance.
Authors: Guo W, Deng L, Yu J, Chen Z, Woo Y, Liu H, Li T, Lin T, Chen H, Zhao M, Zhang L, Li G, Hu Y Abstract Drug resistance is the major challenge facing cancer chemotherapy and nanoscale delivery systems based on natural materials, such as sericin, are a promising means of overcoming drug resistance. Yet, no attempt of introducing synthetic poly(γ-benzyl-L-glutamate) (PBLG) onto sericin polypeptide to fabricate a facile biocompatible and biodegradable micelle has been tried. Here, we prepared a polypeptide-based amphiphilic polymer containing hydrophilic sericin polypeptide backbone and PBLG side chains vi...
Source: Drug Delivery - May 12, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Glioma targeting peptide modified apoferritin nanocage.
In this study, we demonstrate a strategy for glioma targeting by encapsulating vincristine sulfate (VCR) into a naturally available apoferritin nanocage-based drug delivery system with the modification of GKRK peptide ligand (GKRK-APO). Apoferritin (APO), an endogenous nanosize spherical protein, can specifically bind to brain endothelial cells and glioma cells via interacting with the transferrin receptor 1 (TfR1). GKRK is a peptide ligand of heparan sulfate proteoglycan (HSPG) over-expressed on angiogenesis and glioma, presenting excellent glioma-homing property. By combining the dual-targeting delivery effect of GKRK pe...
Source: Drug Delivery - May 7, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Drug delivery systems based on biocompatible imino-chitosan hydrogels for local anticancer therapy.
Authors: Ailincai D, Tartau Mititelu L, Marin L Abstract A series of drug delivery systems were prepared by chitosan hydrogelation with citral in the presence of an antineoplastic drug: 5-fluorouracil. The dynamic covalent chemistry of the imine linkage allowed the obtaining of supramolecular tridimensional architectures in which the drug has been homogenously dispersed. Fourier-transform infrared spectroscopy (FTIR), wide-angle X-ray diffraction (WXRD) and polarized light microscopy (POM) measurements were used in order to follow the hydrogelation and drug encapsulation processes. The ability of the prepared syste...
Source: Drug Delivery - May 5, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Bispecific antibodies (anti-mPEG/anti-HER2) for active tumor targeting of docetaxel (DTX)-loaded mPEGylated nanocarriers to enhance the chemotherapeutic efficacy of HER2-overexpressing tumors.
In conclusion, the BsAbs-LsbMDDs preserved the physical properties of the LsbMDDs and actively targeted tumors with a drug cargo to enhance drug accumulation in tumors leading to greater antitumor activity against antigen-positive tumors. PMID: 29718725 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - May 3, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Preparation of psoralen polymer-lipid hybrid nanoparticles and their reversal of multidrug resistance in MCF-7/ADR cells.
In conclusion, PSO-PLN not only reverses MDR but also improves therapeutic efficiency by enhancing sustained release of PSO. PMID: 29695174 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - April 27, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development of Kupffer cell targeting type-I interferon for the treatment of hepatitis via inducing anti-inflammatory and immunomodulatory actions.
In conclusion, this proof-of-concept study demonstrates the therapeutic effectiveness and utility of Kupffer cell targeting type-I interferon against hepatitis via its anti-inflammatory and immunomodulatory actions. PMID: 29688069 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - April 26, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Localized delivery of therapeutic doxorubicin dose across the canine blood-brain barrier with hyperthermia and temperature sensitive liposomes.
This study demonstrates that localized doxorubicin delivery to the brain can be facilitated by TSL-Dox with localized hyperthermia with no significant neurological deficits. PMID: 29688083 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - April 26, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Modification of translationally controlled tumor protein-derived protein transduction domain for improved intranasal delivery of insulin.
In this study, we tested whether its efficiency could be further improved by replacing amino acids in TCTP-PTD 13 or changing the amino acids in the carrier peptides from the l- to the d-form. We assessed the pharmacokinetics of PTD-mediated transmucosal delivery of insulin in normal rats and the activity of insulin in alloxan-induced diabetic rats. The safety/toxicity profile of the carrier peptides was evaluated based on the release of lactate dehydrogenase (LDH) in nasal wash fluid, body weight changes, and several biochemical parameters. Pharmacokinetic and pharmacodynamic studies showed that the l-form of a double sub...
Source: Drug Delivery - April 26, 2018 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

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