Enhancement of curcumin antitumor efficacy and further photothermal ablation of tumor growth by single-walled carbon nanotubes delivery system in vivo.
In conclusion, curcumin delivery with functionalized SWCNT is a promising strategy to enhance anticancer activity in vivo by enhancing cell uptake and blood concentration, changing physicochemical properties of curcumin and combining phototherapeutic with chemotherapeutic effects. PMID: 31578087 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - October 5, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Novel multifunctional triple folic acid, biotin and CD44 targeting pH-sensitive nano-actiniaes for breast cancer combinational therapy.
In this study, novel multifunctional folic acid, biotin, and CD44 receptors targeted and pH-sensitive "nano-actiniaes" were fabricated with icariin (ICA) and curcumin (Cur) as loaded model drugs for breast cancer therapy. The newly synthesized polymer oligomeric hyaluronic acid-hydrazone bond-folic acid-biotin (Bio-oHA-Hyd-FA) was characterized by 1H NMR spectrogram (proton nuclear magnetic resonance). The obtained drug carrier Bio-oHA-Hyd-FA self-assembled into nanomicelles, named as "nano-actiniaes", in aqueous media with hydrodynamic diameter of 162.7 ± 5 nm. The size, sur...
Source: Drug Delivery - October 3, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A novel dendrimer-based complex co-modified with cyclic RGD hexapeptide and penetratin for noninvasive targeting and penetration of the ocular posterior segment.
In this study, we show that PAMAM-PEG (reaction molar ratio 1:32) has a relatively high grafting efficiency and low cytotoxicity. The particle size was within the range of 15-20 nm after modification with RGD and PEN. Cellular uptake of RGD-modified NCs involved significant affinity toward integrin αvβ3, which validated the targeting of neovasculature. An in vitro permeation study indicated that modification with PEN significantly improved penetration of the NCs (1.5 times higher). In vivo ocular distribution studies showed that, the NCs (modified with PEN or co-modified with RGD and PEN) were highly dist...
Source: Drug Delivery - October 3, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Fabrication and characterization of solid lipid nano-formulation of astraxanthin against DMBA-induced breast cancer via Nrf-2-Keap1 and NF-kB and mTOR/Maf-1/PTEN pathway.
Authors: Sun T, Gao J, Han D, Shi H, Liu X Abstract In the current experimental study, we scrutinized the chemoprotective effect of astraxanthin against the 7,12-dimethylbenz(a)anthracene (DMBA)-induced breast cancer via Nrf-2-Keap1 and NF-kB and mTOR/Maf-1/PTEN pathway. The double emulsion solvent displacement method was used for the preparation of astraxanthin solid lipid nanoparticles (SLN). SLNs were appraised for entrapment, potential, size, drug-release performance, and gastric stability. DMBA (8 mg/kg) was used for the induction of breast cancer. Tumor weight, body weight, and tumor incidence were est...
Source: Drug Delivery - September 28, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Delivery of antisense oligonucleotide using polyethylenimine-based lipid nanoparticle modified with cell penetrating peptide.
Authors: Yang S, Wang D, Sun Y, Zheng B Abstract Efficient and stable delivery system of antisense oligonucleotide (ASO) is important and urgently needed. Here, an ASO delivery system, Lp-PPRP, which contains a cationic polymer based on PEI (branched, 25 kDa), named PEI-PC and a palmitic acid modified R8 (R8-PA) was prepared to deliver a kind of ASO, LOR-2501. The characteristics of the nanoparticles and the cellular uptake of LOR-2501 in HeLa cells and A549 cells were studied. Lp-PPRP showed suitable particle size and zeta potential to combine with LOR-2501; the particle size and zeta potential of Lp-PPRP/L...
Source: Drug Delivery - September 25, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment.
The objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q2) and hexagonal (H2) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, small-angle X-ray scattering, and rheological measurements. Moreover, the release behaviors and permeation results of PN from the gels were estimated using in vitro studies. Finally, the anti-glaucoma effect of LC gels was evaluated by in vivo animal experiments. The inner structure of the gels was Pn3m-type Q2 and H2 phase, and bo...
Source: Drug Delivery - September 25, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Evaluation of therapeutic effect of targeting nanobubbles conjugated with NET-1 siRNA by shear wave elastography: an in vivo study of hepatocellular carcinoma bearing mice model.
This study aimed at investigating the tumor stiffness of hepatocellular carcinoma (HCC) bearing mice model in vivo to evaluate the therapeutic efficacy of targeting nanobubbles (TNBS) conjugated with NET-1 siRNA (NET-1 siRNA-TNBS). Also tested whether shear wave elastography (SWE) could demonstrate the pathological tumor changes and used to monitor therapeutic efficacy as a noninvasive method. The HCC bearing mice model was established by injecting human HCC cell line (HepG2). The mice were then divided into three groups randomly, and were treated with TNBS conjugated with NET-1 siRNA, TNBS conjugated with negative control...
Source: Drug Delivery - September 25, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Albumin-bioinspired iridium oxide nanoplatform with high photothermal conversion efficiency for synergistic chemo-photothermal of osteosarcoma.
Authors: Gu W, Zhang T, Gao J, Wang Y, Li D, Zhao Z, Jiang B, Dong Z, Liu H Abstract Protein-based nanocarriers with inherent biocompatibility have been widely served as building blocks to construct versatile therapeutic nanoplatforms. Herein, bovine serum albumin-iridium oxide nanoparticles (denoted BSA-IrO2 NPs) are successfully synthesized via one-step biomineralization approach. The BSA-IrO2 NPs exhibits uniform size (40 nm), superb biocompatibility and high drug loading capacity for doxorubicin (27.4 wt%). Under near-infrared (NIR) laser irradiation, the as-prepared BSA-IrO2 NPs exhibited high ph...
Source: Drug Delivery - September 20, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Numerical modeling of high-intensity focused ultrasound-mediated intraperitoneal delivery of thermosensitive liposomal doxorubicin for cancer chemotherapy.
Authors: Rezaeian M, Sedaghatkish A, Soltani M Abstract Although intraperitoneal chemotherapy (IPC) has been suggested as a promising method for the management of peritoneal dissemination (PD) of ovarian or colorectal cancers, the actual clinical use of this method has been restricted due to such problems as poor drug penetration into the tumor and high side effects. It is, therefore, necessary to develop new strategies to improve the efficacy of this approach. In the present work, a new strategy is proposed based on intraperitoneal (IP) injection of thermosensitive liposomal doxorubicin (TSL-Dox) with triggered re...
Source: Drug Delivery - September 20, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Electrochemical generation of microbubbles by carbon nanotube interdigital electrodes to increase the permeability and material uptakes of cancer cells.
In this study, we have proposed a new method of microbubble (MB) generation by local electrolysis of the medium. An integrated interdigital array of three-electrode system was designed and patterned on a nickel-coated quartz substrate and then, a short DC electrical pulse was applied that consequently resulted in distributed generation of microbubbles at the periphery of the electrodes. Growth of the carbon nanotube (CNT) nanostructures on the surface of the electrodes approximately increased the number of generated microbubbles up to 7-fold and decreased their average size from ∼20 µm for bare to ∼7&t...
Source: Drug Delivery - September 20, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Enhanced macrophage delivery to the colon using magnetic lipoplexes with a magnetic field.
Authors: Kono Y, Gogatsubo S, Ohba T, Fujita T Abstract Magnetically guided cell delivery systems would be valuable to achieve effective macrophage-based cell therapy for colonic inflammatory diseases. In the current study, we developed a method for the efficient and simultaneous introduction of superparamagnetic iron oxide nanoparticles (SPIONs) and plasmid DNA (pDNA) into RAW264 murine macrophage-like cells using SPION-incorporated cationic liposome/pDNA complexes (magnetic lipoplexes). SPIONs and pDNA were introduced for magnetization and functionalization of the macrophages, respectively. We also evaluated the ...
Source: Drug Delivery - September 20, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Biomaterial-engineered intra-articular drug delivery systems for osteoarthritis therapy.
Authors: Kou L, Xiao S, Sun R, Bao S, Yao Q, Chen R Abstract Osteoarthritis (OA) is a progressive and degenerative disease, which is no longer confined to the elderly. So far, current treatments are limited to symptom relief, and no valid OA disease-modifying drugs are available. Additionally, OA relative joint is challenging for drug delivery, since the drugs experience rapid clearance in joint, showing a poor bioavailability. Existing therapeutic drugs, like non-steroidal anti-inflammatory drugs (NSAIDs) and corticosteroids, are not conducive for long-term use due to adverse effects. Though supplementations, incl...
Source: Drug Delivery - September 18, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Pharmacokinetics and drug delivery systems for puerarin, a bioactive flavone from traditional Chinese medicine.
Authors: Zhang L Abstract Pueraria lobata (Willd.) Ohwi is a medicinal and edible homologous plant with a long history in China. Puerarin, the main component isolated from the root of Pueraria lobata, possesses a wide range of pharmacological properties. Daidzein and glucuronides are the main metabolites of puerarin and are excreted in the urine and feces. As active substrates of P-gp, multidrug resistance-associated protein and multiple metabolic enzymes, the pharmacokinetics of puerarin can be influenced by different pathological conditions and drug-drug interactions. Due to the poor water-solubility and liposolu...
Source: Drug Delivery - September 18, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

SYL3C aptamer-anchored microemulsion co-loading β-elemene and PTX enhances the treatment of colorectal cancer.
SYL3C aptamer-anchored microemulsion co-loading β-elemene and PTX enhances the treatment of colorectal cancer. Drug Deliv. 2019 Dec;26(1):886-897 Authors: Zhou X, Cao C, Li N, Yuan S Abstract The aim of this study is to construct a SYL3C aptamer-anchored microemulsion based on β-elemene and PTX (SYL3C/EP-MEs) for enhancement on colorectal cancer therapy. Such microemulsion is consist of encapsulated drugs (β-elemene and PTX), tumor targeting ligand (3'-end thiolated SYL3C aptamer), thiol conjugated site (maleimide-modified PEGylated 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine, mal-DOPE...
Source: Drug Delivery - September 18, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Design and optimization of crocetin loaded PLGA nanoparticles against diabetic nephropathy via suppression of inflammatory biomarkers: a formulation approach to preclinical study.
Authors: Yang X Abstract Diabetic nephropathy (DN) is a serious complication of diabetes mellitus whose expand process is linked with the fibrosis, renal hypertrophy and inflammation. The current study was to formulate and optimize the nano-formulation of crocetin (CT-PLGA-NPs) against Streptozotocin-induced renal nephropathy in rats. Double emulsion evaporation technique was used for the preparation of CT-PLGA-NPs. CT-PLGA-NPs were scrutinized for polydispersity index, size, gastric stability, entrapment, drug-loading capacity and in-vitro drug release and in vivo preclinical study. Single intraperitoneal injectio...
Source: Drug Delivery - September 18, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Correction.
Authors: PMID: 31500472 [PubMed - as supplied by publisher] (Source: Drug Delivery)
Source: Drug Delivery - September 11, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Dehydration affects drug transport over nasal mucosa.
Authors: Ali A, Wahlgren M, Rembratt-Svensson B, Daftani A, Falkman P, Wollmer P, Engblom J Abstract Formulations for nasal drug delivery often rely on water sorption to adhere to the mucosa, which also causes a higher water gradient over the tissue and subsequent dehydration. The primary aim of this study was therefore to evaluate mucosal response to dehydration and resolve the hypothesis that mucoadhesion achieved through water sorption could also be a constraint for drug absorption via the nasal route. The effect of altering water activity of the vehicle on Xylometazoline HCl and 51Cr-EDTA uptake was studied sep...
Source: Drug Delivery - August 15, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Intraocular administration of tetramethylpyrazine hydrochloride to rats: a direct delivery pathway for brain targeting?
Authors: Mao D, Li F, Ma Q, Dai M, Zhang H, Bai L, He N Abstract The purpose of this study was to compare the pharmacokinetic profile of tetramethylpyrazine hydrochloride (TMPH) in rat plasma and tissues following intravenous (iv), intragastric (ig) and intraocular (io) administration. After io, ig and iv administration of a single dose at 10 mg/kg, tissue and plasma samples drawn from the femoral artery were collected at timed intervals. The concentration of TMPH in the samples was analyzed using high-performance liquid chromatography (HPLC). The area under the concentration-time curve (AUC) and the drug ta...
Source: Drug Delivery - August 15, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Hyaluronic acid-functionalized bilosomes for targeted delivery of tripterine to inflamed area with enhancive therapy on arthritis.
This study was intended to develop hyaluronic acid (HA)-functionalized bilosomes for targeted delivery of tripterine (Tri), an antiphlogistic phytomedicine, to the inflamed joint via ligand-receptor interaction. Tri-loaded bilosomes (Tri-BLs) with cationic lipid (DOTAP) were prepared by a thin film hydration method followed by HA coating to form HA@Tri-BLs. HA@Tri-BLs were then characterized by particle size (PS), entrapment efficiency (EE), and structural morphology. The in vitro drug release, hemocompatibility test and cellular uptake were performed to examine the formulation performances of HA@Tri-BLs. The in vivo pharm...
Source: Drug Delivery - August 9, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Effects of rosiglitazone/PHBV drug delivery system on postoperative fibrosis in rabbit glaucoma filtration surgery model.
Authors: Zhang F, Liu K, Pan Z, Cao M, Zhou D, Liu H, Huang Y, Duan X Abstract The aim of this study is to investigate the effects and toxicities of poly(3-hydroxybutyric acid-co-3-hydroxyvaleric acid) (PHBV)-loading rosiglitazone on preventing scar formation after glaucoma filtration surgery (GFS) in the rabbit model. Rosiglitazone/PHBV drug delivery system was prepared via electrospinning. Release behavior of RSG/PHBV membrane was evaluated by high-performance liquid chromatography. The different concentration membranes were implanted under the conjunctiva of the rabbit's eyes (RSG/PHBV groups). Also, MMC-soaked ...
Source: Drug Delivery - August 9, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Co-delivery of Bmi1 small interfering RNA with ursolic acid by folate receptor-targeted cationic liposomes enhances anti-tumor activity of ursolic acid in vitro and in vivo.
Authors: Li W, Yan R, Liu Y, He C, Zhang X, Lu Y, Khan MW, Xu C, Yang T, Xiang G Abstract Overexpression of Bmi1 gene is an important feature of cancer stem cell in various human tumors. Therefore, Bmi1 gene can be a potential target for small interfering RNA (siRNA) mediated cancer therapy. Ursolic acid (UA) as a natural product plays a pivotal role in anti-tumor field, although its performance is limited by low bioavailability and poor hydrophilicity. A folate receptor-targeted cationic liposome system was designed for the purpose of investigating the relationship between Bmil siRNA and UA. The folate receptor-ta...
Source: Drug Delivery - August 2, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Effect of tissue permeability and drug diffusion anisotropy on convection-enhanced delivery.
Authors: Zhan W, Rodriguez Y Baena F, Dini D Abstract Although convection-enhanced delivery (CED) can successfully facilitate a bypass of the blood brain barrier, its treatment efficacy remains highly limited in clinic. This can be partially attributed to the brain anisotropic characteristics that lead to the difficulties in controlling the drug spatial distribution. Here, the responses of six different drugs to the tissue anisotropy are examined through a parametric study performed using a multiphysics model, which considers interstitial fluid flow, tissue deformation and interlinked drug transport processes in CE...
Source: Drug Delivery - August 1, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Sorafenib-loaded hydroxyethyl starch-TG100-115 micelles for the treatment of liver cancer based on synergistic treatment.
Authors: Li G, Zhao L Abstract Tumor microenvironment is closely related to the occurrence and development of liver cancer. Tumor-associated macrophages (TAMs) are an important part of tumor microenvironment promoting tumor deterioration and metastasis by inhibiting immune cells. Previous studies showed that PI3Kγ inhibitor could reverse the phenotype of TAMs, relieve immunosuppression and sensitize chemotherapy drugs, suggesting that the combination of PI3Kγ inhibitor and chemotherapeutics is likely to bring new breakthroughs in the treatment of liver cancer. Based on it, this paper builds HES-TG100-11...
Source: Drug Delivery - August 1, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Lipid-chitosan hybrid nanoparticles for controlled delivery of cisplatin.
In this study, cisplatin-loaded lipid-chitosan hybrid nanoparticles were formulated by the single step ionic gelation method based on ionic interaction of positively charged chitosan and negatively charged lipid. Formulations with various chitosan to lipid ratios were investigated to obtain the optimal particle size, encapsulation efficiency, and controlled release pattern. Transmission electron microscope and dynamic light scattering analysis demonstrated a size range of 181-245 nm and a zeta potential range of 20-30 mV. The stability of the formulation was demonstrated by thermal studies. Cytotoxicity and c...
Source: Drug Delivery - August 1, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Ganoderic acid loaded nano-lipidic carriers improvise treatment of hepatocellular carcinoma.
Authors: Rahman M, Al-Ghamdi SA, Alharbi KS, Beg S, Sharma K, Anwar F, Al-Abbasi FA, Kumar V Abstract This work evaluates nano-lipid carrier of ganoderic acid (GA) and molecular docking on various cancer signaling pathways, an attempt to improve the hepatic condition associated with hepatic carcinoma (HCC) induced by diethyl-nitrosamine (DEN) in Wistar rats. Molecular docking mechanism of GA was performed through binding simulation analysis for various cancer signaling pathway, viz., Bcl-2, Pl3K, NF-κB, Akt/PKB, and Stat-3. Double emulsion solvent displacement method was implied for preparation of GA-loaded n...
Source: Drug Delivery - August 1, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Transferrin-targeting redox hyperbranched poly(amido amine)-functionalized graphene oxide for sensitized chemotherapy combined with gene therapy to nasopharyngeal carcinoma.
Authors: Liu T, Li J, Wu X, Zhang S, Lu Z, Li G, Li J, Chen S Abstract A drug and gene co-delivery system with chemotherapeutic sensibilization was prepared and used for nasopharyngeal carcinoma therapy. For this purpose, the graphene oxide (GO) was conjugated with the redox hyperbranched poly(amido amine) (HPAA) and then the targeting molecule, transferrin (Tf), was also conjugated. The obtained Tf-HPAA-GO could co-deliver docetaxel (DOC) and MMP-9 shRNA plasmid (pMMP-9) effectively and showed the targeting effect to HNE-1 cells. The co-delivery system showed the effective drug and gene delivery ability with high ...
Source: Drug Delivery - July 26, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Zinc oxide end-capped Fe3O4@mSiO2 core-shell nanocarriers as targeted and responsive drug delivery system for chemo-/ions synergistic therapeutics.
Authors: Liu M, Sun X, Liao Z, Li Y, Qi X, Qian Y, Fenniri H, Zhao P, Shen J Abstract Multifunctional core-shell nanocarriers based on zinc oxide (ZnO)-gated magnetic mesoporous silica nanoparticles (MMSN) were prepared for cancer treatment through magnetic targeting and pH-triggered controlled drug release. Under an external magnetic field, the MMSN could actively deliver chemotherapeutic agent, daunomycin (DNM), to the targeted sites. At neutral aqueous, the functionalized MMSN could stably accommodate the DNM molecules since the mesopores were capped by the ZnO gatekeepers. In contrast, at the acid intercellular...
Source: Drug Delivery - July 26, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

A novel nanoparticle drug delivery system based on PEGylated hemoglobin for cancer therapy.
In this study, we successfully synthesized PEG-Hb nanoparticles loading with PTX based on previously well-established acid-denatured method. PEG-Hb-PTX NPs showed enhanced cellular uptake and great cellular inhibition ability in vitro. Moreover, our animal study showed that PEGylated NPs greatly accumulated in tumor tissues and exhibited excellent anticancer activity in vivo. We found that PEG-Hb-PTX NPs possess a better in vivo antitumor effect than the commercially available Taxol® formulation. We believe that PEG-Hb has great potential as an efficient drug delivery system for further clinic study. PMID: 31293178...
Source: Drug Delivery - July 13, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development and characteristics of novel sonosensitive liposomes for vincristine bitartrate.
Authors: Lin W, Ma X, Zhou C, Yang H, Yang Y, Xie X, Yang C, Han C Abstract The aim of drug delivery is to increase therapeutic efficacy. Externally triggered drug delivery systems enable site-specific and time-controlled drug release. To achieve this goal, our strategy was based on ultrasound-triggered release of an anticancer agent from sonosensitive liposomes (SL). To realize the ultrasound-triggered drug release, a lipophilic sonosensitizer, hematoporphyrin monomethyl ether (HMME) was incorporated into the lipid bilayer of liposomes. Once irradiated by the ultrasound in tumor tissues, the sonodynamic effect gen...
Source: Drug Delivery - July 13, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Brain-targeted intranasal delivery of dopamine with borneol and lactoferrin co-modified nanoparticles for treating Parkinson's disease.
This study was designed to formulate borneol and lactoferrin co-modified nanoparticles (Lf-BNPs) encapsulated dopamine as a novel drug delivery system to achieve maximum therapeutic efficacy and reduce side effects for PD. Dopamine Lf-BNPs were prepared using the double emulsion solvent evaporation method and evaluated for physicochemical and pharmaceutical properties. In vitro cytotoxicity studies indicated that treatment with dopamine Lf-BNPs has relatively low cytotoxicity in SH-SY5Y and 16HBE cells. Qualitative and quantitative cellular uptake experiments indicated that Lf modification of NPs increased cellular uptake ...
Source: Drug Delivery - July 12, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development of synthetic high-density lipoprotein-based ApoA-I mimetic peptide-loaded docetaxel as a drug delivery nanocarrier for breast cancer chemotherapy.
In this study, a synthetic high-density lipoprotein (sHDL), peptide-based nanocarrier loaded with docetaxel (DTX) was constructed, against breast cancer. The thermodynamic and molecular dynamic analyses were conducted to examine the stability of nanoparticles synthesized from mimetic peptide 5 A and various types of phospholipids. Furthermore, the cellular uptake and in vivo fluorescence imaging analysis experiments, with scavenger receptor B-I (SR-BI) were carried out to examine the tumor-targeting ability of sHDL. The nanoparticles were investigated for their pharmacodynamic and cytotoxic effects to show their eff...
Source: Drug Delivery - July 12, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Synergistic effects of a cremophor EL drug delivery system and its U0126 cargo in an ex vivo model.
Authors: Christensen ST, Grell AS, Johansson SE, Andersson CM, Edvinsson L, Haanes KA Abstract Neuroprotection has proven clinically unsuccessful in subarachnoid hemorrhage. We believe that this is because the major component in the early damage pathway, the vascular wall, has not been given the necessary focus. U0126 is a potent inhibitor of vascular phenotypical changes, exemplified by functional endothelin B (ETB) receptor upregulation. The current study aimed to determine the optimal dose of U0126 ex vivo and test the toxicology of this dose in vivo. To find the optimal dose and test a suitable in vivo delivery...
Source: Drug Delivery - July 6, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

In-vitro and in-vivo respiratory deposition of a developed metered dose inhaler formulation of an anti-migraine drug.
Authors: Abdou EM, Kandil SM, Morsi A, Sleem MW Abstract Enhancement of zolmitriptan bioavailability through development of micronized zolmitriptan pressurized metered dose inhaler (MDI) as an alternative to its traditional drug delivery systems. A reversed phase HPLC method for zolmitriptan determination was developed and evaluated. Micronized zolmitriptan MDI formulations were prepared using two different propellants. The prepared formulations were evaluated for mean shot weight, drug content, and leakage rate in addition to in-vitro deposition using next generation impactor where mass median aerodynamic diameter...
Source: Drug Delivery - July 6, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Preparation and in vitro and in vivo evaluations of 10-hydroxycamptothecin liposomes modified with stearyl glycyrrhetinate.
Authors: Zhou T, Tang X, Zhang W, Feng J, Wu W Abstract 10-Hydroxycamptothecin (HCPT) liposomes surface modified with stearyl glycyrrhetinate (SG) were prepared by the film dispersion method. Characterization of the liposomes, including drug release in vitro, pharmacokinetics and tissue distribution, was done. HCPT in plasma and tissues was determined by high-performance liquid chromatography (HPLC). Compared with the conventional HCPT-liposomes and commercially available hydroxycamptothecin injection (HCPT Inject), pharmacokinetic parameters indicated that SG-HCPT-liposomes had better bioavailability. Regarding ti...
Source: Drug Delivery - July 5, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Synergistic photothermal/photodynamic suppression of prostatic carcinoma by targeted biodegradable MnO2 nanosheets.
Authors: Zeng D, Wang L, Tian L, Zhao S, Zhang X, Li H Abstract The biodegradability and clearance of metal-based nanomaterials have been questioned worldwide, which have greatly limited their clinical translation. Herein, ultrathin manganese dioxide (MnO2) nanosheets with broad near-infrared (NIR) absorption and pH-dependent degradation properties were prepared. After being modified with polyethylene glycol-cyclic arginine-glycineaspartic acid tripeptide (PEG-cRGD), the MnO2 nanosheets were then used as photothermal agent and nanocarrier to encapsulate chlorin e6 (Ce6) for targeted photothermal (PTT) and photodyna...
Source: Drug Delivery - July 3, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Preparation, characterization, and pharmacodynamics of insulin-loaded fumaryl diketopiperazine microparticle dry powder inhalation.
Conclusion: To sum up, the aim was to develop a non-injection system for insulin, INS@FDKP-MPs powder inhalation with high dose, low toxicity, and good lung deposition inhalation could rapidly decrease the blood glucose level without immune stimulation, which shows remarkably potential on diabetes treatment by pulmonary delivery route. PMID: 31257946 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - July 3, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Up-regulation of MIAT aggravates the atherosclerotic damage in atherosclerosis mice through the activation of PI3K/Akt signaling pathway.
This study is performed to elucidate the role of long non-coding RNA myocardial infarction associated transcript (lncRNA MIAT) in vulnerable plaque formation in rats with atherosclerosis (AS) through the regulation of the PI3K/Akt signaling pathway. The mice model of AS was established, and the successful modeled AS mice were treated with overexpressed MIAT and silenced MIAT. The levels of blood lipids, atherosclerotic plaques (AP) formation, the lipid content, collagen content, apoptosis of aortic cells, angiogenesis as well as the expression of inflammatory factors, such as tumor necrosis factor α (TNF-α), in...
Source: Drug Delivery - June 28, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Polydopamine-tailored paclitaxel-loaded polymeric microspheres with adhered NIR-controllable gold nanoparticles for chemo-phototherapy of pancreatic cancer.
In this study, we develop adherent gold nanoparticles (GNPs) and paclitaxel (PTX)-loaded PLGA microspheres for the treatment of PC. Polydopamine (pD) was used as a linker to adhere GNPs to the surface of PLGA-Ms and characterized using TEM. Short-term cytotoxicity of GNPs-pD-PTX-PLGA-Ms with or without NIR treatment was evaluated using CCK-8 assays. ROS and western blot assay were performed to determine the intensity of ROS following the treatment of GNPs-pD-PTX-PLGA-Ms with or without NIR in Panc-1 cell line. Successful adhesion of GNPs on the microspheres was confirmed by TEM. CCK-8 assay revealed that GNPs-pD-PTX-PLGA-M...
Source: Drug Delivery - June 28, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Biophysical and chemical stability of surfactant/budesonide and the pulmonary distribution following intra-tracheal administration.
Authors: Chen CM, Chang CH, Chao CH, Wang MH, Yeh TF Abstract Intra-tracheal instillation of budesonide using surfactant as a vehicle significantly decreased the incidence of bronchopulmonary dysplasia or death in preterm infants. The formularity of surfactant supplemented with budesonide and biophysical and chemical stability of the suspension has not been well reported. The aims are to investigate the biophysical and chemical stability of two surfactant preparations, Survanta and Curosurf, supplemented with budesonide. Biophysical property of the surface tension of Survanta and Survanta/budesonide suspension and ...
Source: Drug Delivery - June 19, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Optimization of formulation for enhanced intranasal delivery of insulin with translationally controlled tumor protein-derived protein transduction domain.
This study evaluated bioavailability (BA) of various formulations of insulin intranasally delivered with protein transduction domain (PTD) derived from translationally controlled tumor protein. The therapeutic efficacy of newly formulated intranasal insulin + PTD was compared in vivo studies with normal and alloxan-induced diabetic rats, to those of free insulin and subcutaneously injected insulin. BA of insulin in two new formulations was, respectively, 60.71% and 45.81% of subcutaneously injected insulin, while the BA of free insulin was only 3.34%. Histological analysis of tissues, lactate dehydrogenase ac...
Source: Drug Delivery - June 19, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Inhibition of microRNA-183 expression resists human umbilical vascular endothelial cells injury by upregulating expression of IRS1.
This study highlights that inhibition of miR-183 expression may resist HUVECs injury by upregulating expression of IRS1. PMID: 31210063 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - June 19, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Multifunctional nanoplatform based on star-shaped copolymer for liver cancer targeting therapy.
Authors: Gong X, Zheng Y, He G, Chen K, Zeng X, Chen Z Abstract With high morbidity and death rates, liver cancer has become one of the most common cancers in the world. But, most chemotherapeutic anticancer drugs have high toxicity as well as low specificity. To improve the treatment modalities and enhance the therapeutic effect of liver cancer, a brand new liver-targeting nanoparticle (NP), Ent-11α-hydroxy-15-oxo-kaur-16-en-19-oic acid (5 F)-loaded cholic acid (CA)-functionalized star-shaped poly (lactic-co-glycolic acid) (PLGA)-polyethylene glycol (PEG)-lactobionic acid (LA) (5 F-loaded CA-PL...
Source: Drug Delivery - June 16, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Development of an intravaginal ring delivering simultaneously anastrozole and levonorgestrel: a pharmacokinetic perspective.
This article describes the developmental pharmacokinetic (PK) aspects covering the characterization of in vitro release, preclinical IVR PK investigations in monkeys, and clinical PK considerations. An IVR for ATZ has been developed and investigated in healthy menstruating female cynomolgus monkeys showing effective in vivo release. PK data from the size-adapted IVR used in these animals can be translated into a human context as confirmed in human studies where predefined exposure levels of ATZ were reached. As ATZ may cause harm to the fetus, use of effective contraception has to be assured in women of childbearing potent...
Source: Drug Delivery - June 10, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

New micelle myricetin formulation for ocular delivery: improved stability, solubility, and ocular anti-inflammatory treatment.
Authors: Sun F, Zheng Z, Lan J, Li X, Li M, Song K, Wu X Abstract Myricetin (Myr) is a naturally occurring flavonoid exhibiting diverse biological and pharmacological properties, but its characteristics such as water insolubility, poor aqueous stability, and poor bioavailability limit its clinical application, including in ophthalmology. To increase its clinical application in ophthalmology, Myr was designed to be encapsulated in a polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (PVCL-PVA-PEG) polymeric micelles to increases its aqueous solubility, stability, and corneal permeability to ...
Source: Drug Delivery - June 9, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Use of magnoflorine-phospholipid complex to permeate blood-brain barrier and treat depression in the CUMS animal model.
Authors: Li B, Han L, Cao B, Yang X, Zhu X, Yang B, Zhao H, Qiao W Abstract To improve the liposolubility and blood-brain barrier permeability of magnoflorine, a new formulation of magnoflorine-phospholipid complex was prepared, characterized, and pharmacologically evaluated in the chronic unpredictable mild stress animal model. In this paper, the magnoflorine-phospholipid complex was synthesized and its characterization was determined. The antidepressant-like and antioxidant activity of magnoflorine-phospholipid complex was investigated by behavioral tests and western blotting analysis. As a result, the magnoflori...
Source: Drug Delivery - May 22, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Proniosomal gel-derived niosomes: an approach to sustain and improve the ocular delivery of brimonidine tartrate; formulation, in-vitro characterization, and in-vivo pharmacodynamic study.
Authors: Emad Eldeeb A, Salah S, Ghorab M Abstract Brimonidine tartrate (BRT) is a hydrophilic α2 adrenergic agonist used for the treatment of glaucoma. Glaucoma is an ocular disease affecting the anterior segment of the eye requiring lifetime treatment. Owing to the obstacles facing ocular delivery systems and hydrophilicity of BRT, frequent administration of the eye drops is required. Niosomes have been widely used to improve the ocular bioavailability of the topically applied drugs and to enhance the ocular residence time. However, they have drawbacks as physical instability, aggregation, and loss of the e...
Source: Drug Delivery - May 17, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Co-encapsulation of docetaxel and cyclosporin A into SNEDDS to promote oral cancer chemotherapy.
Authors: Cui W, Zhao H, Wang C, Chen Y, Luo C, Zhang S, Sun B, He Z Abstract Self-nanoemulsifying drug delivery system (SNEDDS) have been considered as a promising platform for oral delivery of many BCS (biopharmaceutics classification system) class IV drugs, such as docetaxel (DTX). However, oral chemotherapy with DTX is also restricted by its active P-glycoprotein (P-gp) efflux and hepatic first-pass metabolism. To address these challenges, we developed a novel SNEDDS co-loaded with DTX and cyclosporine A (CsA) to achieve effective inhibition of P-gp efflux and P450 enzyme metabolization, improving oral bioavaila...
Source: Drug Delivery - May 17, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Exploring the mucoadhesive behavior of sucrose acetate isobutyrate: a novel excipient for oral delivery of biopharmaceuticals.
In conclusion, SAIB is an interesting and safe biomaterial to promote high mucoadhesion in the GIT after oral administration. PMID: 31090468 [PubMed - in process] (Source: Drug Delivery)
Source: Drug Delivery - May 17, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Co-delivery of metformin and levofloxacin hydrochloride using biodegradable thermosensitive hydrogel for the treatment of corneal neovascularization.
Authors: Liu D, Wu Q, Zhu Y, Liu Y, Xie X, Li S, Lin H, Chen W, Zhu F Abstract Corneal neovascularization (CNV) is one of the major causes of severe disorders in ocular surface. Subconjunctival administration provides a localized and effective delivery of anti-angiogenic agents to inhibit neovascularization. In the present study, the ABA triblock copolymer of poly(D,L-lactic-co-glycolic acid)-block-poly(ethylene glycol)-block-poly(D,L-lactic-co-glycolic acid) (PLGA-PEG-PLGA) was used as a sustained drug delivery carrier for metformin (MET) and levofloxacin hydrochloride (LFH). Both drugs and PLGA-PEG-PLGA copolymer...
Source: Drug Delivery - May 17, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research

Cubic and hexagonal liquid crystals as drug carriers for the transdermal delivery of triptolide.
Authors: Shan QQ, Jiang XJ, Wang FY, Shu ZX, Gui SY Abstract The purpose of this study was to develop and evaluate triptolide-loaded cubic and hexagonal liquid crystals for transdermal drug delivery systems (TDDSs). We prepared and characterized triptolide-loaded lyotropic liquid crystals and evaluated for their percutaneous permeation properties in vitro and in vivo. We then used the adjuvant arthritic rat model and HaCaT cells to analyze the pharmacodynamics and conduct cell-stimulating studies of these liquid crystals. The optimized preparations were identified as cubic and hexagonal phase structures, respective...
Source: Drug Delivery - May 14, 2019 Category: Drugs & Pharmacology Tags: Drug Deliv Source Type: research